This invention is in the field of medicinal pharmacology. In particular, the present invention relates to pharmaceutical agents which function as inhibitors of sodium-glucose cotransporter 1 (SGLT-1) activity. The invention further relates to methods of treating and/or ameliorating symptoms related to cystic fibrosis-related liver disease and diseases characterized with increased SGLT-1 activity, increased endoplasmic reticulum (ER) stress response, and/or increased hepatic inflammation.
A61K 31/351 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom not condensed with another ring
A61K 31/357 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having two or more oxygen atoms in the same ring, e.g. crown ethers, guanadrel
The disclosure is directed compositions comprising antigen-specific IgA immune complexes and methods of using the compositions to induce immune tolerance against allergens in a subject who has an established Th2 polarized immune response at one or more mucosal sites prior to administering the composition.
This disclosure provides compositions and methods for stimulating the innate immune response in a subject with agents capable of stimulating an innate immune response in a subject upon administration to the subject (e.g., damage-associated molecular patterns (DAMPs) and pathogen-associated molecular patterns (PAMPs)). In particular, the present invention is directed to compositions of DAMPs/PAMPs and metals ions, as well as systems and methods utilizing such nanoparticles (e.g., in diagnostic and/or therapeutic settings).
A61K 47/69 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit
Provided herein are compositions and methods to prevent and to treat thrombosis, to reverse the anticoagulant action of heparin, and to prevent and to treat the thrombotic and antifibrinolytic effect of nucleic acids. In particular, provided herein are compositions, methods, kits, systems and uses for switchable charge state multivalent biocompatible polycations for polyanion inhibition in blood.
A61K 39/395 - Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
G16H 50/20 - ICT specially adapted for medical diagnosis, medical simulation or medical data mining; ICT specially adapted for detecting, monitoring or modelling epidemics or pandemics for computer-aided diagnosis, e.g. based on medical expert systems
A61B 5/02 - Measuring pulse, heart rate, blood pressure or blood flow; Combined pulse/heart-rate/blood pressure determination; Evaluating a cardiovascular condition not otherwise provided for, e.g. using combinations of techniques provided for in this group with electrocardiography; Heart catheters for measuring blood pressure
Disclosed herein are solvent-free vapor deposition methods comprising: vaporizing a bulk cocrystalline material to form a vapor, entraining the vapor into a carrier gas, and depositing a film comprising the cocrystalline material on one or more discrete regions of a substrate. Also provided are solid films and articles comprising a surface of a solid substrate having one or more discrete regions patterned with a deposited solid film of a cocrystalline material, produced by the solvent-free vapor deposition methods disclosed herein.
A near-infrared (NIR) light therapy device having at least one NIR light source and a waveguide having i) a NIR light input surface and ii) a NIR light emitting surface. The waveguide includes a lens feature forming the NIR light input surface. The lens feature is configured to at least substantially collimate treatment NIR light from the at least one NIR light source and convey substantially collimated light in a first direction through the waveguide. The waveguide also includes a plurality of extractive surfaces on a surface of the waveguide that is configured to reflect the substantially collimated light through the light emitting surface to a subject. The plurality of extractive surfaces is also configured to create a substantially uniform NIR light output across the light emitting surface.
F21V 8/00 - Use of light guides, e.g. fibre optic devices, in lighting devices or systems
G02B 1/04 - Optical elements characterised by the material of which they are made; Optical coatings for optical elements made of organic materials, e.g. plastics
The present disclosure relates to materials and methods for measuring human papillomavirus (HPV) circulating tumor DNA (ctDNA). In particular, the disclosure provides a droplet digital PCR-based assay for HPV16 ctDNA, and the use thereof for predicting response to treatment in patients having HPV positive head and neck squamous cell carcinoma (HNSCC), such as oropharyngeal squamous cell carcinoma (OPSSC).
A power conversion device may perform model-referenced power processing for multiple diverse power nodes. The power conversion device includes interconnects that couple power nodes connection ports to power converters. The power converters include a dense tier of power converters sized to correct from varied power flow levels of a defined portion of a population of power nodes to interim power flows in accord with center values for that portion of power nodes. The center values are provided by a model of the power node diversity. The power converters also include a sparse tier. The sparse tier performs power processing to convert from the interim power flows generated by the dense tier to a uniform model-corrected target flow.
Provided herein are methods of treating a cancer comprising administering an EGFR degrader to a patient suffering therefrom and subjecting the patient to radiation. The cancer can express mutant, overexpressed or overly activated EGFR, mutant KRAS, or mutant BRAF.
The present disclosure provides means such as uses, nanoparticles, solutions, methods, kits and systems for screening target proteins for self-association properties (viscosity and opalescence) in ultra-dilute solutions. They provide means for screening a large number of target proteins at orders of magnitude lower concentrations than end-use formulations.
A dynamic standing desk having a work surface configured to move with planar motion parallel with the ground and with a range of movement that adjusts as a function of the size of a user of the desk. The desk may include a base, a tabletop that includes the work surface, a frame that movably couples the tabletop to the base, and at least one actuator configured to provide the planar motion. The desk may be used to reduce lower musculoskeletal discomfort of a user of the desk by oscillating the work surface of the desk with a range of movement based on a length of a limb of the user.
The invention provides a method for treating biliary tract cancer in a patient in need thereof, comprising the step of intravenously administering to the patient a therapeutically effective amount of (i) devimistat, (ii) gemcitabine, and (iii) cisplatin, in order to treat the biliary tract cancer.
A61K 31/20 - Carboxylic acids, e.g. valproic acid having a carboxyl group bound to an acyclic chain of seven or more carbon atoms, e.g. stearic, palmitic or arachidic acid
A61K 31/7068 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
Protein-based nanoparticles and methods of forming such protein-based nanoparticles via electrohydrodynamic jetting methods are provided. The nanoparticle may comprise a water- soluble protein having an average molecular weight of > about 8 kDa and < about 700 kDa. In certain variations, the water-soluble protein is cross-linked (e.g., with an optional crosslinking agent) and defines a mesh structure having an average linear mesh size of > about 1 nm to < about 4 nm. Methods of making such nanoparticles may include jetting a liquid comprising the water-soluble protein through a nozzle, followed by exposing the liquid to an electric field sufficient to solidify the liquid and form the protein-based nanoparticles described above.
A61K 47/42 - Proteins; Polypeptides; Degradation products thereof; Derivatives thereof, e.g. albumin, gelatin or zein
C12N 15/113 - Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides
A61K 47/69 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit
A device receiving an unsterile supply of air, subjects the airflow to one or more sterilizing agents or sterilizing conditions, and then exhausts the treated airflow through a nozzle or array of nozzles, forming a jet of air or array of air jets directed at or along the surface of the head of a living being such that the sterilized airflow envelopes the head. The result is a) the living being breathes air that is free of one or more infectious agents and b) the jet of air forms an air curtain such that the living being is protected from inhaling infectious agents that may surround them.
Disclosed herein are systems for tracking patient medication protocol adherence, the system comprising a computing device for tracking the amount of an active pharmaceutical ingredient (Al) to be administered to the subject using an augmented utensil comprising a layered Al delivery structure formed. Also disclosed are methods of customizing drug delivery, and augmented utensils and methods of making the same.
G16H 20/10 - ICT specially adapted for therapies or health-improving plans, e.g. for handling prescriptions, for steering therapy or for monitoring patient compliance relating to drugs or medications, e.g. for ensuring correct administration to patients
G16C 20/00 - Chemoinformatics, i.e. ICT specially adapted for the handling of physicochemical or structural data of chemical particles, elements, compounds or mixtures
16.
CRYSTALLINE POLYMORPHIC FORMS OF STING AGONISTS ASSOCIATED WITH METAL IONS CAPABLE OF MODULATING AN IMMUNE RESPONSE
This disclosure provides compositions and methods for stimulating the innate immune response in a subject with agents capable of stimulating an innate immune response in a subject upon administration to the subject. In particular, the present invention is directed to crystalline polymorphic forms (e.g., coordinate polymeric forms) of STING agonists associated (e.g., mixed) with one or more metal ions (e.g., Zn2+, Mn2+, Al3+, Fe3+, Cu2+), as well as systems and methods utilizing such compositions (e.g., in therapeutic settings).
A61K 31/7084 - Compounds having two nucleosides or nucleotides, e.g. nicotinamide-adenine dinucleotide, flavine-adenine dinucleotide
A61K 47/64 - Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
A61K 47/14 - Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
17.
COMPOSITIONS AND METHODS FOR TREATING AND/OR PREVENTING AUTOIMMUNE DISORDERS
This invention relates generally to compositions comprising a gel-based inulin formulation associated with (e.g., complexed, conjugated, encapsulated, absorbed, adsorbed, admixed) one or more therapeutic agents (e.g., immunomodulatory agent, immunosuppressant, allergen) and related methods for the treatment of autoimmune disorders (e.g., colitis) (e.g, allergy, such as food allergy). Also provided herein are compositions and methods for modulating an immune response associated with an autoimmune disorder (e.g., allergy) and/or inducing immune tolerance or desensitization to an autoimmune disorder (e.g., allergy, such as a food allergy).
A transcranial magnetic resonance (MR)-guided histotripsy (tcMRgHt) system is provided. Using electronic steering only, the tcMRgHt system is configured to create lesions of 25.5 mm in the transverse plane and 50 mm in the axial plane through the skull of a patient. This disclosure provides the design, fabrication, acoustic characterization, and MR compatibility assessment of tcMRgHt systems for histotripsy.
A histotripsy therapy system configured for the treatment of tissue is provided, which may include any number of features. Provided herein are systems and methods that provide efficacious non-invasive and minimally invasive therapeutic, diagnostic and research procedures. In particular, provided herein are optimized systems and methods that provide targeted, efficacious histotripsy in a variety of different regions and under a variety of different conditions without causing undesired tissue damage to intervening/non-target tissues or structures.
A61B 17/225 - Surgical instruments, devices or methods, e.g. tourniquets for extracorporeal shock wave lithotripsy [ESWL], e.g. by using ultrasonic waves
A compact, three-dimensional (3D) photovoltaic charging system comprising a photovoltaic unit encased in a transparent housing, a power management unit, and a support base. The photovoltaic unit having non-coplanar photovoltaic surfaces that are positioned at a relative distance and a relative orientation. Compared to conventional flat solar panels, the 3D photovoltaic charging system can collect light vertically, therefore amplifying solar module power density, defined as power output per installation footprint area. A photo-tracking, 3D photovoltaic charging system is also described, having a photovoltaic unit encased in a transparent housing, a power management unit, and means to track a source of electromagnetic radiation. The photo-tracking, 3D photovoltaic charging system tracks a moving light source, resulting in improved light flux intake, and therefore, enhanced electric power output.
Provided herein is technology relating to molecular biological manipulation of genes and genomes and particularly, but not exclusively, to CRISPR (Clustered Regularly Interspaced Short Palindromic Repeats) methods, compositions, systems, and kits for improved genetic editing.
A61K 8/44 - Aminocarboxylic acids or derivatives thereof, e.g. aminocarboxylic acids containing sulfur; Salts, esters or N-acylated derivatives thereof
A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
A61P 9/00 - Drugs for disorders of the cardiovascular system
A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
Provided herein are compositions and methods for activating pyruvate kinase (e.g., in a subject). In particular, provided herein are compositions and methods for treating a disease or condition (e.g., eye disease, blood disorders, or cancer) using pyruvate kinase activators.
A61K 31/5025 - Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
A61K 31/519 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/551 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogens as ring hetero atoms, e.g. clozapine, dilazep
A61P 7/00 - Drugs for disorders of the blood or the extracellular fluid
UNIVERSITY OF PITTSBURGH - OF THE COMMONWEALTH SYSTEM OF HIGHER EDUCATION (USA)
THE REGENTS OF THE UNIVERSITY OF MICHIGAN (USA)
Inventor
Schopfer, Francisco J.
Freeman, Bruce A.
Zhao, Yang
Chen, Yuqing E.
Zhang, Jifeng
Abstract
A method comprising administering to a subject having an aneurysm, suspected of having an aneurysm, or at risk of developing an aneurysm, a therapeutically effective amount of a compound selected from (i) a nitroalkene fatty acid, (ii) an unsaturated fatty acid having an electron withdrawing group, a leaving group, and a carbon-carbon double bond disposed between the electron withdrawing group and the leaving group, (iii) a thiolated nitro fatty acid, (iv) a dicarboxylic acid compound containing an electron withdrawing group, or a mixture of at least two of (i)-(iv).
A61K 31/194 - Carboxylic acids, e.g. valproic acid having two or more carboxyl groups, e.g. succinic, maleic or phthalic acid
A61K 31/197 - Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid (GABA), beta-alanine, epsilon-aminocaproic acid, pantothenic acid
A61K 31/201 - Carboxylic acids, e.g. valproic acid having a carboxyl group bound to an acyclic chain of seven or more carbon atoms, e.g. stearic, palmitic or arachidic acid having one or two double bonds, e.g. oleic or linoleic acid
A61P 43/00 - Drugs for specific purposes, not provided for in groups
25.
CYSTEAMINE FOR THE TREATMENT OF SARS-COV-2 INFECTION
Provided herein are methods for the treatment and prevention of viral infections (e.g., coronavirus infections (e.g., severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), etc.), etc.) and diseases (e.g., Coronavirus disease 2019 (COVID-19)) associated therewith by the administration of cysteamine or derivatives thereof to a subject.
A61K 31/145 - Amines, e.g. amantadine having sulfur atoms, e.g. thiurams (N—C(S)—S—C(S)—N or N—C(S)—S—S—C(S)—N); Sulfinylamines (—N=SO); Sulfonylamines (—N=SO2)
A personal respiratory isolation system (PRIS) provides a personal, negative pressure environment for a patient or user that reduces contamination and spread of pathogens exhaled by the patient into the environment. The PRIS includes an enclosure to receive the patient's head (such as a hood and a drape) and a negative pressure source which draws ambient air into the interior of the enclosure and draws air within the enclosure's interior (including the exhalations of the patient, including any contaminants and/or pathogens) out of the enclosure via a fluid port into a container for biohazard processing or disposal. The PRIS may allow positive air pressure therapeutic treatments to be delivered to the patient within the negative pressure environment, and the PRIS may maintain a constant pressure within the interior of the enclosure. The PRIS may include a transparent, hinged face shield for ease of patient observation and/or access.
A61B 90/00 - Instruments, implements or accessories specially adapted for surgery or diagnosis and not covered by any of the groups , e.g. for luxation treatment or for protecting wound edges
A61B 90/40 - Apparatus fixed or close to patients specially adapted for providing an aseptic surgical environment
THE UNITED STATES OF AMERICA AS REPRESENTED BY THE DEPARTMENT OF VETERAN AFFAIRS (USA)
Inventor
Xu, Zhen
Cho, Clifford Suhyun
Abstract
Systems and methods for histotripsy and immunotherapy are provided. In some embodiments, histotripsy can be applied to a target tissue volume to lyse and solubilize the target tissue volume to release tumor antigens. In some embodiments, an immune response of the treatment can be evaluated. In other embodiments, an immune therapy can be applied after applying the histotripsy. In one embodiment, the lysed and solubilized cells can be extracted from the tissue. The extracted cells can be used to create immune therapies, including vaccines.
Methods and devices for producing cavitation in tissue are provided. Methods and devices are also provided for surgical navigation, including defining a target treatment zone and navigating a focus of a therapy transducer to the target treatment zone. Embodiments are provided for co-registering a plurality of surgical imaging and navigation systems. Systems for performing Histotripsy therapy are also discussed.
A gas chromatography device for peak focusing of one or more target analytes is provided that include a chromatographic column with an inlet and an outlet. A stationary phase is deposited inside the chromatographic column and has a positive thickness gradient. The stationary phase extends from the inlet to the outlet and has a first thickness at the inlet of the chromatographic column and a second thickness at the outlet of the chromatographic column. The second thickness is at least about 10% greater than the first thickness. Methods of peak focusing in a gas chromatography device, method of verifying peak focusing in a gas chromatography device and creating a gas chromatography device having a chromatographic column with a positive thickness gradient are also provided.
The invention features polypeptides that include variants of plasminogen activator inhibitor 1 (PAI-1) having a reduced ability to bind with vitronectin, having a reduced ability to interact with the PAI-1 clearance receptor LDL receptor-related protein 1 (LRP1), and having the ability to efficiently inhibit neutrophil elastase in the presence of neutrophil extracellular traps (NETs). In some embodiments, a polypeptide of the invention includes PAI-1 variants optionally fused to an Fc domain monomer or moiety. The invention also features pharmaceutical compositions and methods of using the polypeptides to treat diseases and conditions characterized with aberrant neutrophil elastase activity (e.g., Idiopathic Pulmonary Fibrosis).
A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
C07H 21/04 - Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids with deoxyribosyl as saccharide radical
C07K 1/00 - General processes for the preparation of peptides
C07K 14/00 - Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
A non-thermal plasma reactor system having an outer member; a non-thermal plasma inner member sleeve disposed within the outer member, the non-thermal plasma inner member sleeve having an central core volume, the non-thermal plasma inner member sleeve being smaller than the outer member to define an annular volume there between, the non-thermal plasma inner member sleeve having an inner surface boundary and an outer surface boundary to define a sleeve volume there between, the inner surface boundary and the outer surface boundary being permeable and configured to permit airflow between the annular volume and the central core volume; dielectric material being disposed within the sleeve volume; and at least one electrode extending within the sleeve volume and another electrode coupled to the inner sleeve member generating the non-thermal plasma contacting the airflow as it flows between the annular volume and the central core volume.
B01J 19/08 - Processes employing the direct application of electric or wave energy, or particle radiation; Apparatus therefor
B01D 53/32 - Separation of gases or vapours; Recovering vapours of volatile solvents from gases; Chemical or biological purification of waste gases, e.g. engine exhaust gases, smoke, fumes, flue gases or aerosols by electrical effects other than those provided for in group
C02F 1/46 - Treatment of water, waste water, or sewage by electrochemical methods
The disclosure relates to the development of methods for predicting effectiveness of an anti-TNF agent in the treatment of psoriasis. More particularly, the disclosure provides new biomarkers and combinations of biomarkers for predicting effectiveness of an anti-TNF agent in the treatment of psoriasis and subsequently treating with an anti-TNF agent if the biomarker level is indicative of effectiveness in the anti-TNF treatment of the subject.
C12Q 1/6883 - Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes for diseases caused by alterations of genetic material
35.
COMPOSITIONS AND METHODS FOR INCREASING THE EFFICACY OF IMMUNOTHERAPIES AND VACCINES
This invention relates generally to compositions and methods for increasing the efficacy of immunotherapies and vaccines. In particular, the present invention relates to elevating the richness and diversity of a subject's gut microbiome through administration of an agent (e.g., fiber containing prebiotic agent (e.g., epigallocatechin gallate (EGCG), fucoidan, potato starch, oligofructose and inulin)) (e.g., melatonin) with an immunotherapy or vaccine. Such compositions and methods are useful for treating cancer, infectious pathogens, autoimmune diseases, neurological disorders, and/or obesity.
The present disclosure provides compounds represented by Formula( I ) and the salts or solvates thereof, wherein R3a, E, L, A1, B1, X1, X2, Z1, and Z2 are as defined in the specification. Compounds having Formula (I) are androgen receptor degraders useful for the treatment of cancer and other diseases.
A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
A61K 31/501 - Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
This invention is in the field of medicinal pharmacology. In particular, the present invention relates to pharmaceutical agents which function as inhibitors of sodium-glucose cotransporter (SGLT) activity. The invention further relates to methods of treating and/or ameliorating symptoms related to cystic fibrosis (CF), comprising administering to a subject (e.g., a human patient) a composition comprising one or more pharmaceutical agents which function as inhibitors of SGLT activity.
A61K 31/341 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide not condensed with another ring, e.g. ranitidine, furosemide, bufetolol, muscarine
A61K 31/7034 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
A61K 38/02 - Peptides of undefined number of amino acids; Derivatives thereof
A61K 39/395 - Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
A61P 11/00 - Drugs for disorders of the respiratory system
The present disclosure provides compounds represented by Formula I: wherein R2a, R2b, R2c, R2d, R3, R13, and Z are as defined in the specification, and the salts and solvates thereof. Compounds of Formula I are cereblon (CRBN) ubiquitination inhibitors or monofunctional synthetic intermediates that can be used to prepare PROTAC molecules. CRBN ubiquitination inhibitors and PROTAC molecules are useful for the treatment of cancer and other diseases.
A61K 31/395 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
A61K 31/4745 - Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenanthrolines
A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
Disclosed are methods of treating cancer characterized by expression of at least one KRAS mutation, using a compound of Formula I, below, or a pharmaceutically acceptable salt thereof, or a prodrug thereof: (I) Also disclosed are methods of altering the level of KRAS or cMet in a cell characterized by expression of at least a KRAS mutation with the compound of Formula I.
The present invention relates to compositions comprising nanoparticles associated with a plurality of tolerogenic antigens (e.g., between 1 - 30 tolerogenic 5 antigens per nanoparticle) in such a manner that facilitates strong immune tolerance upon administration to a subject (e.g., a human subject suffering from or at risk of suffering from an autoimmune disorder e.g., MS or celiac disease). The present invention further relates to methods for utilizing such nanoparticles to treat autoimmune disorders (e.g., MS or celiac disease).
A61K 39/385 - Haptens or antigens, bound to carriers
A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
A61K 47/69 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit
A61P 37/00 - Drugs for immunological or allergic disorders
A61K 31/381 - Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
A61K 31/4025 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
C07D 333/06 - Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulfur atom with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to the ring carbon atoms
C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 409/06 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
42.
IMIDAZOPYRIMIDINES AS EED INHIBITORS AND THE USE THEREOF
The present disclosure provides compounds represented by Formula (I) wherein R1, R2, R3, and R4 are as defined in the specification, and the salts and solvates thereof. Compounds of Formula (I) are FED inhibitors. FED inhibitors are useful for the treatment of cancer and other diseases.
C07D 471/22 - Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups in which the condensed systems contains four or more hetero rings
A61K 31/5383 - 1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
C07D 491/22 - Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups , , or in which the condensed system contains four or more hetero rings
C07D 495/22 - Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
C07D 498/22 - Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
43.
CATHETER INSERT DEVICE WITH POWDER COMPRISING S-NITROSOTHINIOL
A catheter insert device includes a powder composition, and a housing. The powder composition includes a solid phase S-nitrosothiol (RSNO). The housing includes a polymeric wall that is i) permeable to nitric oxide, ii) non-porous, and iii) permeable to water vapor, and an inner lumen defined at least in part by the polymeric wall. The powder composition is completely sealed within the inner lumen of the housing.
A01N 41/12 - Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a sulfur atom bound to a hetero atom not containing sulfur-to-oxygen bonds, e.g. polysulfides
A01P 1/00 - Disinfectants; Antimicrobial compounds or mixtures thereof
A61L 29/14 - Materials characterised by their function or physical properties
A61M 25/01 - Introducing, guiding, advancing, emplacing or holding catheters
A grip assessment device includes a support structure having a periphery, a cover positioned around the support structure and configured to define a grip surface, and a plurality of sensor elements disposed along the periphery of the support structure, each respective sensor element of the plurality of sensor elements being configured to generate an output signal indicative of force applied to the grip surface at the respective sensor element. The plurality of sensor elements are distributed across the grip surface such that the output signals from the plurality of sensor elements are collectively indicative of a grip profile along the grip surface, the grip profile providing grip position data and grip magnitude data correlated with the grip position data.
Provided herein are devices, systems, and methods for biological sample collection. In particular, provided herein are devices, systems, and methods that employ small, hand-held devices that collect small volumes of biological samples, such as vitreous from the eye, for diagnostic and other purposes.
A61B 10/00 - Other methods or instruments for diagnosis, e.g. for vaccination diagnosis; Sex determination; Ovulation-period determination; Throat striking implements
A61F 9/00 - Methods or devices for treatment of the eyes; Devices for putting in contact-lenses; Devices to correct squinting; Apparatus to guide the blind; Protective devices for the eyes, carried on the body or in the hand
Disclosed herein is are methods and apparatuses for synthesizing deposited films of compounds (e.g., organic compounds such as a pharmaceutical active ingredient or a new chemical entity) on or in a variety of substrates, where such deposited compounds have the desired stability under storage conditions, ease of handling, and yet enhanced dissolution properties when used in various assays. The disclosure further relates to methods of coating substrates, such as medical or diagnostic devices, with deposited films of organic compounds, as well as film-coated substrates.
The present disclosure provides compounds represented by Formula I or Formula VIII: wherein R1a, R1b, M, A, E, QA, and QB are as defined in the specification, and the salts and solvates thereof. Compounds of Formula I are degraders of STAT3 or dedraders of STAT3 and STAT1. Compounds of Formula VIII are inhibitors of STAT3. STAT3 degraders and inhibitors are useful for the treatment of cancer and other diseases.
C07F 9/6561 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
A61K 31/675 - Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
This invention is in the field of medicinal chemistry. In particular, the invention relates to small molecule compounds having bicyclic and tetracyclic quinone scaffolds which have antiproliferative activities through, for example, induction of reactive oxygen species. The invention further processes for preparing, and methods for using these compounds to treat cancer (e.g., pancreatic cancer, leukemia, non-small cell lung cancer, colon cancer, CNS cancer, melanoma, ovarian cancer, breast cancer, renal cancer, and prostate cancer).
A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
A61K 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/551 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogens as ring hetero atoms, e.g. clozapine, dilazep
C07D 241/38 - Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems with only hydrogen or carbon atoms directly attached to the ring nitrogen atoms
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
49.
METHODS AND SYSTEM FOR THE RECONSTRUCTION OF DRUG RESPONSE AND DISEASE NETWORKS AND USES THEREOF
Methods comprising an integrated, multiscale artificial intelligence-based system that reconstructs drug- specific pharmacogenomic networks and their constituent functional sub-networks are described. The system uses features of the functional topology of the three-dimensional architecture of drug-modulated spatial contacts in chromatin space. Discovery of a drug pharmacogenomic network is made through the selection of candidate SNPs by imputation, determination of the predicted causality of the SNPs using machine learning and deep learning, use of the causal SNPs to probe the spatial genome as determined by chromosome conformation capture analysis, combining targeted genes controlled by the same cell and tissue- specific enhancers, and reconstruction of the pharmacogenomic network using diverse data sources and metrics based on the results of genome-wide association studies. Knowledge-based segmentation methods are used to deconstruct the pharmacogenomic network into its constituent efficacy and adverse event sub-networks for applications in clinical decision support, drug repurposing, and in silico drug discovery.
G16H 20/10 - ICT specially adapted for therapies or health-improving plans, e.g. for handling prescriptions, for steering therapy or for monitoring patient compliance relating to drugs or medications, e.g. for ensuring correct administration to patients
50.
PHARMACOGENOMIC DECISION SUPPORT FOR MODULATORS OF THE NMDA, GLYCINE, AND AMPA RECEPTORS
Methods for identifying patients diagnosed with treatment resistant or refractory depression, pain or other clinical indications who are eligible to receive N-methyl-D-aspartate receptor antagonist, glycine receptor beta (GLRB) modulator, or a- amino-3 -hydroxy- 5 -methyl- 4-isoxazolepropionic acid receptor (AMPAR)-based therapies to include determining the appropriate medication, an optimal dose for each patient, and determining which patients are not eligible to receive the therapy. The pharmacogenomic clinical decision support assays include targeted single nucleotide polymorphisms and clinical values or a combination of targeted single nucleotide polymorphisms, targeted ketamine- specific expansion and contraction of topologically associated domains, and clinical values. The methods described herein allow for a more effective determination of which patients will experience drug efficacy and which patients will experience adverse drug events. The methods provide personalized patient recommendations for dose, the frequency of medication administration, and recommendations on drug choice.
G16H 20/10 - ICT specially adapted for therapies or health-improving plans, e.g. for handling prescriptions, for steering therapy or for monitoring patient compliance relating to drugs or medications, e.g. for ensuring correct administration to patients
Provided herein is technology relating to materials having microscale and/or nanoscale features and particularly, but not exclusively, to porous materials comprising microscale features, methods for producing porous materials comprising microscale features, drug delivery vehicles, and related kits, systems, and uses.
B32B 3/10 - Layered products essentially comprising a layer with external or internal discontinuities or unevennesses, or a layer of non-planar form; Layered products essentially having particular features of form characterised by a discontinuous layer, i.e. apertured or formed of separate pieces of material
B29C 59/02 - Surface shaping, e.g. embossing; Apparatus therefor by mechanical means, e.g. pressing
A composite structure includes a concrete matrix and a fiber embedded in the concrete matrix. The fiber includes steel. A surface of the fiber has a series of striations. The series of striations are arranged in a striation pattern.
The present disclosure provides compounds represented by Formula (I): A-L-B and the salts or solvates thereof, wherein A, L, and B are as defined in the specification. Compounds having Formula I are estrogen receptor degraders useful for the treatment of cancer.
C07D 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
A61K 31/41 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
54.
CO-CRYSTALS, METHOD AND APPARATUS FOR FORMING THE SAME
Disclosed herein is a method and apparatus for synthesizing co-crystals from the vapor phase without the need for liquid solvent. Also disclosed herein are co-crystals formed from the vapor phase, substrates coated with said co-crystals, pharmaceutical compositions thereof and apparatuses for producing said co-crystals.
C07D 473/12 - Heterocyclic compounds containing purine ring systems with oxygen, sulfur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms with radicals containing only hydrogen and carbon atoms, attached in position 1 or 3 with methyl radicals in positions 1, 3, and 7, e.g. caffeine
A61K 31/194 - Carboxylic acids, e.g. valproic acid having two or more carboxyl groups, e.g. succinic, maleic or phthalic acid
A61K 31/522 - Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
The present disclosure provides compounds represented by Formula (I): wherein Rla, Rlb, R2a, R2b, R3a, R3b, R4, A, L, X, Y, and Z are as defined as set forth in the specification. The present disclosure also provides compounds of Formula (I) for use to treat cancer or any other disease, condition, or disorder that is responsive to degradation of MDM2 protein.
A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
The disclosure relates to bioreactors, for example for biological treatment and, more specifically to bioreactor insert apparatus including biofilms and related methods. The bioreactor insert apparatus provides a means for circulation of reaction medium within the bioreactor, a biofilm support, and biological treatment of an inlet feed to the reactor/insert apparatus. The bioreactor insert apparatus has a high relative surface area for biofilm attachment and is capable of generating complex flow patterns and increasing treatment efficiency/biological conversion activity in a biologically-active reactor. The high surface area structure incorporates multiple biofilm support structures such as meshes at inlet and outlet portions of the structure. The biofilm support structures and biofilms thereon can increase overall reaction rate of the bioreactor and/or perform some solid/liquid separation in the treatment of the wastewater or other influent.
An integrated microfluidic photoionization detector (PID) is provided including a microfluidic ionization chamber a microfluidic ultraviolet radiation chamber that is configured to generate ultraviolet photons. An ultrathin transmissive window is disposed between the microfluidic ionization chamber and the microfluidic ultraviolet radiation chamber that permits the ultraviolet photons to pass from the microfluidic ultraviolet radiation chamber into the microfluidic ionization chamber. Detection systems for one or more VOC analytes are also provided that include a gas chromatography (GC) unit including at least one gas chromatography column and an integrated microfluidic photoionization detector (PID) disposed downstream of the gas chromatography (GC) unit.
G01N 27/62 - Investigating or analysing materials by the use of electric, electrochemical, or magnetic means by investigating electric discharges, e.g. emission of cathode
G01N 27/64 - Investigating or analysing materials by the use of electric, electrochemical, or magnetic means by investigating electric discharges, e.g. emission of cathode using wave or particle radiation to ionise a gas, e.g. in an ionisation chamber
G01N 27/66 - Investigating or analysing materials by the use of electric, electrochemical, or magnetic means by investigating electric discharges, e.g. emission of cathode using wave or particle radiation to ionise a gas, e.g. in an ionisation chamber and measuring current or voltage
G01N 27/68 - Investigating or analysing materials by the use of electric, electrochemical, or magnetic means by investigating electric discharges, e.g. emission of cathode using electric discharge to ionise a gas
The present disclosure provides compounds represented by Formula I: and the pharmaceutically acceptable salts and solvates thereof, wherein R1a, R1b, R1c, E, G, and Q are as defined as set forth in the specification. The present disclosure also provides compounds of Formula I for use to treat cancer or any other disease, condition, or disorder that is responsive to inhibition of menin.
C07D 211/34 - Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
A61K 31/445 - Non-condensed piperidines, e.g. piperocaine
A61K 31/4523 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
59.
SMALL HIGHLY UNIFORM NANOMEDICINE COMPOSITIONS FOR THERAPEUTIC, IMAGING AND THERANOSTIC APPLICATIONS
A targetable nanoconstruct capable of simultaneously serving as a therapeutic platform for photodynamic therapy as well as an MR molecular imaging agent, free of heavy metal atoms. F3-cys targeting agent nanoconstructs, including 8PEGA-Ce6 NCs. A label-free 8PEGA nanoconstruct that can be directly and selectively imaged by MRI, using standard spin-echo imaging sequences with large diffusion magnetic field gradients to suppress the water signal.
B82Y 5/00 - Nanobiotechnology or nanomedicine, e.g. protein engineering or drug delivery
A61K 47/60 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
A61K 47/69 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit
A61B 5/055 - Detecting, measuring or recording for diagnosis by means of electric currents or magnetic fields; Measuring using microwaves or radio waves involving electronic [EMR] or nuclear [NMR] magnetic resonance, e.g. magnetic resonance imaging
A61K 41/00 - Medicinal preparations obtained by treating materials with wave energy or particle radiation
A61K 49/18 - Nuclear magnetic resonance (NMR) contrast preparations; Magnetic resonance imaging (MRI) contrast preparations characterised by a special physical form, e.g. emulsions, microcapsules, liposomes
Provided herein are methods for treating, delaying progression of, or reducing the severity of amyotrophic lateral sclerosis (ALS) in a subject through administration of therapeutically effective amounts of agents (e.g., JAK kinase inhibitors (e.g., tofacitinib)) capable of interfering with central nervous system related natural killer cell (NK) levels and function.
A61K 31/519 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61P 21/00 - Drugs for disorders of the muscular or neuromuscular system
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
C12N 5/0783 - T cells; NK cells; Progenitors of T or NK cells
The present disclosure provides a method of treating NAFLD, NASH, and atherosclerosis, comprising administering glycine-containing tripeptide molecule, or a pharmaceutically acceptable salt thereof to a subject.
Provided herein is technology relating to detecting analytes and particularly, but not exclusively, to methods, compositions, and systems for detecting, characterizing, identifying, and/or quantifying analytes.
C07H 21/04 - Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids with deoxyribosyl as saccharide radical
C12N 15/115 - Aptamers, i.e. nucleic acids binding a target molecule specifically and with high affinity without hybridising therewith
C07K 16/00 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies
This disclosure provides compositions and methods for stimulating the innate immune response in a subject with agents capable of stimulating an innate immune response in a subject upon administration to the subject (e.g., damage-associated molecular patterns (DAMPs) and pathogen-associated molecular patterns (PAMPs)). In particular, the present invention is directed to compositions of DAMPs/PAMPs and metals ions, as well as systems and methods utilizing such nanoparticles (e.g., in diagnostic and/or therapeutic settings).
Provided are prodrugs of various therapeutic agents that provide enhanced bioavilabilty of the therapeutic agent, and methods of treatment conditions in a subject by administration of the one or prodrugs. As provided herein a prodrug includes a therapeutic agent covalently attached to a cap, the cap having a structure according to formula (I) where: R1 is a branched or linear substituted or unsubstituted C2-C6 alkyl, alkenyl, or alkynl; X is -S(0)2-; R2 is a branched or linear substituted or unsubstituted C4-C20 alkyl, alkenyl, or alkynyl; and R3 is -H, C3-C5 cycloalkyl, C3-C5 cycloheteroalkyl, -C(CH3)3, -CF3, -C(CF3)3, or a substituted or unsubstituted phenyl.
C07F 9/6512 - Six-membered rings having the nitrogen atoms in positions 1 and 3
A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
A61P 31/22 - Antivirals for DNA viruses for herpes viruses
C07F 9/655 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having oxygen atoms, with or without sulfur, selenium, or tellurium atoms, as the only ring hetero atoms
C07F 9/6558 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
Provided herein are small molecule inhibitors of Polycomb Repressive Complex 1 (PRC1) activity, and methods of use thereof for the treatment of disease, including leukemia and other cancers, as well as other diseases dependent on the activity of PRC1.
C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
A61K 31/395 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
A61K 31/4155 - 1,2-Diazoles not condensed and containing further heterocyclic rings
A61K 31/416 - 1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
A61K 31/427 - Thiazoles not condensed and containing further heterocyclic rings
A61K 31/428 - Thiazoles condensed with carbocyclic rings
A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
A61K 31/4439 - Non-condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
C07D 207/34 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 405/04 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
A vehicle-to-vehicle power transfer system for use between a first vehicle and at least a second vehicle. The system includes an electric power system disposed in each of the first and second vehicles configured to provide electrical drive power to a vehicle drive system for propulsion of the associated vehicle and a power transfer system configured to transfer electric power from at least the electric power system of the first vehicle to the electric power system of the second vehicle while the vehicles are in motion or stationary.
B60L 53/10 - Methods of charging batteries, specially adapted for electric vehicles; Charging stations or on-board charging equipment therefor; Exchange of energy storage elements in electric vehicles characterised by the energy transfer between the charging station and the vehicle
B60L 50/40 - Electric propulsion with power supplied within the vehicle using propulsion power supplied by capacitors
B60L 50/53 - Electric propulsion with power supplied within the vehicle using propulsion power supplied by batteries or fuel cells in combination with an external power supply, e.g. from overhead contact lines
67.
INHIBITORS OF PLATELET FUNCTION AND METHODS FOR USE OF THE SAME
Disclosed herein are small molecule inhibitors of platelet function, and methods of using the small molecules to treat diseases, such as platelet hemostasis and thrombosis. In particular, disclosed herein are compounds of Formula (I) and pharmaceutically acceptable salts thereof: wherein the substituents are as described.
C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
The present disclosure provides compounds represented by Formula I: and the pharmaceutically acceptable salts and solvates thereof, wherein R1a, R1b, R1c, R1d, R1e, R2, R3, R8a, R8b, L, X, Z1, and Z2 are as defined as set forth in the specification. The present disclosure also provides compounds of Formula I for use to treat a condition or disorder responsive to menin inhibition such as cancer.
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
A61K 31/395 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
A61K 31/551 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogens as ring hetero atoms, e.g. clozapine, dilazep
A61K 31/553 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and at least one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
69.
METHOD AND APPARATUS FOR ANALYSIS OF CHROMATIN INTERACTION DATA
To analyze spatial organization of chromatin a computing device may compile genomic element contacts or reads into variable size bins using a binary search tree. The bins may be selected to each represent a different cutsite increment or functional element within a genome, such as a gene, TAD, chromatin state segment, loop domain, chromatin domain, etc. Two sets of bins are selected to generate a squared genome matrix of bin pairs, where each set represent an axis of the matrix. Then a normalization method is applied to the interaction frequencies for the bin pairs having variable size and/or shape to generate normalized interaction frequencies for each bin pair. The normalized interaction frequencies may be used to identify bin pairs having enriched and depleted contacts for a variety of analyses, including the detection of target genes of genomic variants, as well as genome wide analysis of contacts.
A61K 31/4166 - 1,3-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. phenytoin
A61K 31/438 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring being spiro-condensed with carbocyclic or heterocyclic ring systems
A61K 31/444 - Non-condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
The ability to automate the processes of specimen collection, image acquisition, data pre-processing, computation of derived biomarkers, modeling, classification and analysis can significantly impact clinical decision-making and fundamental investigation of cell deformation. This disclosure combine 3D cell nuclear shape modeling by robust smooth surface reconstruction and extraction of shape morphometry measure into a highly parallel pipeline workflow protocol for end-to-end morphological analysis of thousands of nuclei and nucleoli in 3D. This approach allows efficient and informative evaluation of cell shapes in the imaging data and represents a reproducible technique that can be validated, modified, and repurposed by the biomedical community. This facilitates result reproducibility, collaborative method validation, and broad knowledge dissemination.
A system is presented for analyzing and interpreting histologic images. The system includes an imaging device and a diagnostic module. The imaging device captures an image of a tissue sample at an optical section of the tissue sample, where the tissue sample has a thickness larger than the optical section. The system may further include an image interpretation subsystem located remotely from the imaging device and configured to receive the images from the imaging device. The diagnostic module is configured to receive the images for the tissue sample from the imaging device and generates a diagnosis for the tissue sample by applying a machine learning algorithm to the images. The diagnostic module may be interface directly with the imaging device or located remotely at the image interpretation subsystem.
G01N 33/574 - Immunoassay; Biospecific binding assay; Materials therefor for cancer
G01N 35/00 - Automatic analysis not limited to methods or materials provided for in any single one of groups ; Handling materials therefor
G01N 35/02 - Automatic analysis not limited to methods or materials provided for in any single one of groups ; Handling materials therefor using a plurality of sample containers moved by a conveyor system past one or more treatment or analysis stations
73.
BIOCATALYST AND METHODS FOR SYNTHESIZING MIXED DISULFIDE CONJUGATES OF THIENOPYRIDINE COMPOUNDS
The present invention relates to methods for synthesizing mixed disulfide conjugates of thienopyridine compounds with a genetically engineered variant of cytochrome P450 BM3 or CYP102A1 as a catalyst, and belongs to the field of chemical synthesis.
Provided herein are small molecule inhibitors of NSD1, NSD2 and/or NSD3 activity, and methods of use thereof for the treatment of disease, including leukemia, breast cancer, osteosarcoma, lung and prostate cancers and other solid tumors as well as other diseases dependent on the activity of NSD1, NSD2 and/or NSD3.
A61K 31/4439 - Non-condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
A61K 31/4725 - Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
Provided herein are compositions and methods for treating cancer. In particular, provided herein are compositions, methods, and uses of inhibitors of THOR for treating cancer.
Provided are materials, methods and uses for treating an ophthalmological condition such as Leber Congenital Amaurosis by administering an effective amount of an adeno-associated virus AAV2, serotype 5 (AAV 2/5) or AAV-5 comprising an expressible coding region for human RDH12.
C12N 15/63 - Introduction of foreign genetic material using vectors; Vectors; Use of hosts therefor; Regulation of expression
A61K 48/00 - Medicinal preparations containing genetic material which is inserted into cells of the living body to treat genetic diseases; Gene therapy
This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having a triazole-methyl-piperidinyl-pyrolyl-propenone structure which function as modulators of shared epitope (SE) - calreticulin (CRT) binding and/or interaction, and their use as therapeutics for the treatment of immunoregulatory abnormalities (e.g., autoimmune diseases, inflammatory diseases (e.g., chronic inflammatory disease), and bone erosive diseases) by selectively inhibiting SE-CRT interactions and/or signal transduction pathways commonly overactive or dysregulated in arthritic and/or other diseases or conditions.
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
A61P 19/02 - Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
A61P 19/08 - Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
A61P 37/06 - Immunosuppressants, e.g. drugs for graft rejection
C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
78.
ASH1L DEGRADERS AND METHODS OF TREATMENT THEREWITH
Provided herein are small molecules comprising a first domain that binds to ASHIL and a second domain that facilitates ASHIL degradation, including compounds of formulae la and Ic: In particular, ASHIL-targeting proteolysis targeting chimeras (PROTACs) and methods of use thereof for the treatment of disease (e.g., acute leukemia, solid cancers and other diseases dependent on activity of ASH1L) are provided.
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
A61P 35/02 - Antineoplastic agents specific for leukemia
C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
79.
ASH1L INHIBITORS AND METHODS OF TREATMENT THEREWITH
Provided herein are small molecules that bind to ASH1L and inhibit ASH1L activity, and methods of use thereof for the treatment of disease, including acute leukemia, solid cancers and other diseases dependent on activity of ASH1L.
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
A61K 31/395 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
A61P 35/02 - Antineoplastic agents specific for leukemia
C07D 209/18 - Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
C07D 417/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
A monolithic thermocasting system for thermocasting polymer and solid material and method of use having an internal frame system; an external frame system disposed external to the internal frame system; a mold cavity formed between the internal frame system and the external frame system, the mold cavity sized to receive the polymer and solid material and shaped to form an architectural member; a duct; and a heater element disposed in the duct for outputting thermal energy to the mold cavity to heat the polymer and solid material, the thermal energy being sufficient to thermocast the polymer and solid material to a combined building material.
B29C 39/10 - Shaping by casting, i.e. introducing the moulding material into a mould or between confining surfaces without significant moulding pressure; Apparatus therefor for making articles of definite length, i.e. discrete articles incorporating preformed parts or layers, e.g. casting around inserts or for coating articles
B29C 33/00 - SHAPING OR JOINING OF PLASTICS; SHAPING OF MATERIAL IN A PLASTIC STATE, NOT OTHERWISE PROVIDED FOR; AFTER-TREATMENT OF THE SHAPED PRODUCTS, e.g. REPAIRING - Details thereof or accessories therefor
B29C 35/00 - Heating, cooling or curing, e.g. crosslinking or vulcanising; Apparatus therefor
A solid film structure formed of multiple solid film insert layers each having different functionality is provided. The solid film structure forms a bio-chemotronic structure having an actuator thin film layer with one or more low molecular weight organic active agents that may be activated, a sensor thin film layer that includes one or more sensors for measuring a direct or indirect response from a target to the one or more active agents, and a control thin film layer configured to individually control activation of the active agents in the actuator layer, e.g., according to a protocol.
A61B 5/157 - Devices for taking samples of blood characterised by integrated means for measuring characteristics of blood
A61B 5/1473 - Measuring characteristics of blood in vivo, e.g. gas concentration, pH-value using chemical or electrochemical methods, e.g. by polarographic means invasive, e.g. introduced into the body by a catheter
82.
INHIBITORS OF MEK/PI3K, JAK/MEK, JAK/PI3K/MTOR AND MEK/PI3K/MTOR BIOLOGICAL PATHWAYS AND METHODS FOR IMPROVING LYMPHATIC UPTAKE, BIOAVAILABILITY, AND SOLUBILITY OF THERAPEUTIC COMPOUNDS
Inhibitors of mTOR, MEK, JAK and PI3K and compositions containing the same are disclosed. Methods of using the inhibitors in the treatment of a variety of diseases and conditions wherein inhibition of one or more of mTOR, MEK, JAK and PI3K provides a benefit also are disclosed. Methods of using chemical attachment moieties and linkers for the purposes of modifying compound solubility and/or lymphatic absorption are also disclosed.
A61K 31/167 - Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen atom of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
A61K 31/192 - Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid
A61K 31/498 - Pyrazines or piperazines ortho- or peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
A61K 31/513 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
A61K 31/519 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 31/53 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
A61K 31/555 - Heterocyclic compounds containing heavy metals, e.g. hemin, hematin, melarsoprol
A61K 31/616 - Salicylic acid; Derivatives thereof having the hydroxy group in position 2 esterified, e.g. salicylsulfuric acid by carboxylic acids, e.g. acetylsalicylic acid
A61K 31/704 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin, digitoxin
A61P 11/00 - Drugs for disorders of the respiratory system
A61P 25/00 - Drugs for disorders of the nervous system
C07C 57/30 - Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms containing six-membered aromatic rings
C07C 235/34 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton containing six-membered aromatic rings having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
C07C 259/10 - Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups without replacement of the other oxygen atom of the carboxyl group, e.g. hydroxamic acids having carbon atoms of hydroxamic groups bound to carbon atoms of six-membered aromatic rings
C07C 323/58 - Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being further substituted by nitrogen atoms, not being part of nitro or nitroso groups with amino groups bound to the carbon skeleton
C07D 239/553 - Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals with other hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms with halogen atoms or nitro radicals directly attached to ring carbon atoms, e.g. fluorouracil
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
Methods, systems, and kits for the diagnosis, prognosis and the determination of cancer progression of prostate cancer in a subject are disclosed. In particular, the disclosure relates to the use of immune cell-specific gene expression in determining prognosis and identifying individuals in need of treatment for prostate cancer who will be responsive to radiation therapy.
C12Q 1/6886 - Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes for diseases caused by alterations of genetic material for cancer
G16H 50/20 - ICT specially adapted for medical diagnosis, medical simulation or medical data mining; ICT specially adapted for detecting, monitoring or modelling epidemics or pandemics for computer-aided diagnosis, e.g. based on medical expert systems
A61K 39/395 - Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
G01N 33/574 - Immunoassay; Biospecific binding assay; Materials therefor for cancer
84.
PLASMINOGEN ACTIVATOR INHIBITOR-1 (PAI-1) INHIBITOR AND METHOD OF USE
Provided herein are plasminogen activator-1 (PAI-1 ) inhibitor compounds and uses thereof in the treatment of any disease or disorder associated with elevated PAI-1. The disclosure includes, but is not limited to, the use of such compounds to prevent or reduce thrombosis and fibrosis, to promote thrombolysis, and to modulate lipid metabolism and treat diseases or disorders associated with elevated PAI-1, cholesterol, or lipid levels.
A01N 43/42 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one nitrogen atom as the only ring hetero atom six-membered rings condensed with carbocyclic rings
A sensor for detecting heavy metals in water is provided. The sensor includes a first electrode and a second electrode, the first electrode and the second electrode having complimentary interdigitated surfaces that are separated from each other by a first gap having a distance of greater than or equal to about 500 nm to less than or equal to about 10 µm. The sensor also includes a power source connectable to the first electrode and the second electrode. The sensor is configured to continuously monitor water for the presence of heavy metals. Methods of making and using the sensor are also provided.
Cerenkov Emission (CE) during external beam radiation therapy (EBRT) from a linear accelerator (Linac) has been demonstrated as a useful tool for radiotherapy quality assurance and potentially other applications for online tracking of tumors during treatment. However, an overlooked area is the molecular probing of the cancer status during delivery mainly due to the limited detection sensitivity of CE and lack of flexible tools to fit into an already complex treatment delivery environment. Silicon photomultiplier (SiPM) can be used for low light detection due to their extreme sensitivity that mirrors photomultiplier tubes and yet has a form factor that is similar to silicon photodiodes, allowing for improved flexibility in device design. This work assesses the feasibility of using SiPMs to detect CE, interrogate the tumor molecular status during EBRT, and contrast its performance with silicon photodiodes (PDs) available commercially.
For patients who exhibit or may exhibit primary or comorbid disease, pharmacological phenotypes may be predicted through the collection of panomic, physiomic, environmental, sociomic, demographic, and outcome phenotype data over a period of time. A machine learning engine may generate a statistical model based on training data from training patients to predict pharmacological phenotypes, including drug response and dosing, drug adverse events, disease and comorbid disease risk, drug-gene, drug-drug, and polypharmacy interactions. Then the model may be applied to data for new patients to predict their pharmacological phenotypes, and enable decision making in clinical and research contexts, including drug selection and dosage, changes in drug regimens, polypharmacy optimization, monitoring, etc., to benefit from additional predictive power, resulting in adverse event and substance abuse avoidance, improved drug response, better patient outcomes, lower treatment costs, public health benefits, and increases in the effectiveness of research in pharmacology and other biomedical fields.
G16B 20/00 - ICT specially adapted for functional genomics or proteomics, e.g. genotype-phenotype associations
G16B 5/00 - ICT specially adapted for modelling or simulations in systems biology, e.g. gene-regulatory networks, protein interaction networks or metabolic networks
G16B 30/00 - ICT specially adapted for sequence analysis involving nucleotides or amino acids
G16B 40/00 - ICT specially adapted for biostatistics; ICT specially adapted for bioinformatics-related machine learning or data mining, e.g. knowledge discovery or pattern finding
An aspiration catheter system for navigation within a vascular lumen and thrombectomy of a thrombus. The system includes a tubular catheter member having an open distal end defming a catheter lumen, a vacuum source, a rotational drive system, a flexible shaft having a channel coupled to the rotational drive system for rotational movement in response thereto, and an optional guidewire selectively inserted at least partially within the the flexible shaft. The flexible shaft is at least partially disposed within the tubular catheter member configured for uncoupled rotational and translational motion therein and to optionally define a corkscrew motion in response to rotational driving force by the drive system that results in formation of hydrodynamic vortices within the catheter lumen. In some embodiments, the guidewire member and the flexible shaft are collectively sufficient to navigate the vascular lumen and steer translational movement of the tubular catheter member there along.
A61M 1/00 - Suction or pumping devices for medical purposes; Devices for carrying-off, for treatment of, or for carrying-over, body-liquids; Drainage systems
A61M 25/01 - Introducing, guiding, advancing, emplacing or holding catheters
Small molecule covalent inhibitors of DCNl and compositions containing the same are disclosed. Methods of using the DCNl covalent inhibitors in the treatment of diseases and conditions wherein inhibition of DCNl provides a benefit, like oxidative stress- related diseases and conditions, neurodegenerative diseases and conditions, metabolic disorders, and muscular nerve degeneration, also are disclosed.
C07D 277/64 - Benzothiazoles with only hydrocarbon or substituted hydrocarbon radicals attached in position 2
A61K 31/428 - Thiazoles condensed with carbocyclic rings
A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
The present disclosure provides compounds represented by Formula (I): and the pharmaceutically acceptable salts and solvates thereof, wherein A, R1a, R1b, R1c, R1d, R2, R3, R8a, R8b, R10, X, Z2, m, and n are as defined as set forth in the specification. The present disclosure also provides compounds of Formula (I) for use to treat a condition or disorder responsive to menin inhibition such as cancer.
C07D 401/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
A61K 31/397 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
A61K 31/4725 - Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
C07D 205/04 - Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
Provided herein is technology relating to the detection of analytes and particularly, but not exclusively, to methods, systems, compositions, and kits for detecting analytes such as nucleic acids, proteins, small molecules, and other molecules using a technology based on the transient binding of detection probes.
C07K 16/00 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies
C12N 15/115 - Aptamers, i.e. nucleic acids binding a target molecule specifically and with high affinity without hybridising therewith
C12Q 1/6816 - Hybridisation assays characterised by the detection means
C12Q 1/68 - Measuring or testing processes involving enzymes, nucleic acids or microorganisms; Compositions therefor; Processes of preparing such compositions involving nucleic acids
G01N 21/29 - Colour; Spectral properties, i.e. comparison of effect of material on the light at two or more different wavelengths or wavelength bands using visual detection
The present disclosure provides compounds represented by Formula( I), and the pharmaceutically acceptable salts and solvates thereof, wherein R1a, R1b, R2a, R2b, R3, R4, R5, R6, R7, E and (B) are as defined as set forth in the specification. The present disclosure also provides compounds of Formula ( I) for use to treat a condition or disorder responsive to inhibition of ALK such as cancer.
A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
A cold spray apparatus for applying a coating of particles to a substrate includes a nozzle assembly having a plurality of inner passages terminating at a common exit. The nozzle assembly includes a particle supply members in communication with the inner passages. The particle supply members supply the particles to flow and accelerate through the inner passages and out of the nozzle assembly via the common exit toward the substrate to be coated thereon. Furthermore, each inner passage includes a laser that emits a laser beam that is transmitted through the inner passage. The laser heats at least one of the particles and the substrate to promote coating of the substrate with the particles.
C23C 24/08 - Coating starting from inorganic powder by application of heat or pressure and heat
B05B 7/14 - Spraying apparatus for discharge of liquids or other fluent materials from two or more sources, e.g. of liquid and air, of powder and gas designed for spraying particulate materials
B05B 7/22 - Spraying apparatus for discharge of liquids or other fluent materials from two or more sources, e.g. of liquid and air, of powder and gas incorporating means for heating the material to be sprayed electrically, e.g. by arc
The present disclosure provides compounds represented by Formula I: I, and the pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein R1, R2a, R2b, R3, R4, Ar, L, X, Y, and B are as defined as set forth in the specification. The present disclosure also provides compounds of Formula I for use to treat a condition or disorder responsive to degradation of BET bromodomains such as cancer.
A61K 31/5517 - 1,4-Benzodiazepines, e.g. diazepam condensed with five-membered rings having nitrogen as a ring hetero atom, e.g. imidazobenzodiazepines, triazolam
The present disclosure provides compounds represented by Formula I and the pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein R1, R2a, R2b, R3a, R3b, R4, Ar, L, X, Y, and B are as defined as set forth in the specification. The present disclosure also provids compounds of Formula I for use to treat a condition or disorder responsive to degradation of BET bromodomains such as cancer.
A61K 31/553 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and at least one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
The present disclosure provides compounds represented by Formula (I): and the pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein R1a, R1b, R2a, R2b, R3, R4, R5, R6, and R7 are as defined as set forth in the specification. The present disclosure also provides compounds of Formula (I) for use to treat a condition or disorder responsive to inhibition of ALK such as cancer.
C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
A61K 31/506 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
A61P 37/00 - Drugs for immunological or allergic disorders
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
98.
N-(PHENYLSULFONYL)BENZAMIDES AND RELATED COMPOUNDS AS BCL-2 INHIBITORS
The present disclosure provides compounds having Formula I-A: and the pharmaceutically acceptable salts and solvates thereof, wherein A, X1 , X2, X3 R1a, R1b E, and = are as defined as set forth in the specification. The present disclosure also provides compounds of Formula I-A for use to treat a disease, disorder, or condition responsive to Bc1-2 protein inhibition such as cancer.
A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
Multifunctional inhibitors of mTOR, MEK, and PI3K and compositions containing the same are disclosed. The multifunctional inhibitors may have, for example, the following structural formula: Methods of using the multifunctional inhibitors in the treatment of diseases and conditions wherein inhibition of one or more of mTOR, MEK, and PI3K provides a benefit, like cancers, also are disclosed.
C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
A61K 31/553 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and at least one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
100.
COMPOSITIONS AND METHODS FOR DELIVERY OF BIOMACROMOLECULE AGENTS
The present invention relates to nanoparticles associated with (e.g., complexed, conjugated, encapsulated, absorbed, adsorbed, admixed) biomacromolecule agents configured for treating, preventing or ameliorating various types of disorders, and methods of synthesizing the same. In particular, the present invention is directed to compositions comprising nanoparticles (e.g., synthetic high density lipoprotein (sHDL)) associated with (e.g., complexed, conjugated, encapsulated, absorbed, adsorbed, admixed) biomacromolecule agents (e.g., nucleic acid, peptides, glycolipids, etc.), methods for synthesizing such nanoparticles, as well as systems and methods utilizing such nanoparticles (e.g., in diagnostic and/or therapeutic settings).
C12N 15/113 - Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides
B82Y 5/00 - Nanobiotechnology or nanomedicine, e.g. protein engineering or drug delivery
A61K 47/69 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit
A61K 31/713 - Double-stranded nucleic acids or oligonucleotides
A61K 39/00 - Medicinal preparations containing antigens or antibodies
A61K 47/24 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
A61K 47/42 - Proteins; Polypeptides; Degradation products thereof; Derivatives thereof, e.g. albumin, gelatin or zein
patents
