A pharmaceutical product for administration of an antibody-drug conjugate in combination with a bispecific checkpoint inhibitor is provided. The antibody-drug conjugate is an antibody-drug conjugate in which a drug linker represented by the following formula (wherein A represents the connecting position to an antibody) is con jugated to an antibody, preferably an anti-TROP2 or anti-HER2 antibody, via a thioether bond. Also provided is a therapeutic use and method wherein the antibody-drug con jugate and the bispecific checkpoint inhibitor are administered in combination to a subject (Formula I).
A61K 47/68 - 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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
The present invention relates to a CD47 inhibitor for use in the treatment or prevention of cancer by simultaneous or sequential administration with an antibody specific for a tumor antigen. The invention also relates to a pharmaceutical composition comprising : a CD47 inhibitor; and an antibody specific for a tumor antigen.
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
C07K 16/30 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants from tumour cells
C07K 16/32 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against translation products from oncogenes
A61K 39/395 - Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
A61K 47/68 - 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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
A pharmaceutical product, wherein an antibody-drug conjugate in which a drug-linker represented by the following formula (I) (wherein A represents a connecting position to an antibody) is conjugated to the antibody via a thioether bond, and an inhibitor selected from the group consisting of an EZH1 inhibitor, an EZH2 inhibitor and an EZH1/2 dual inhibitor are administered in combination, and/or a method of treatment, wherein the antibody-drug conjugate and the inhibitor are administrated in combination to a subject.
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61K 47/68 - 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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
The present disclosure provides antibodies and antigen-binding fragments thereof that specifically bind to the spike protein of SARS-CoV-2 and methods of making and using the same. The antibodies can be used, for example, in prophylaxis, post-exposure prophylaxis, or treatment of SARS-CoV-2 infection. The antibodies can also be used to detect SARS-CoV-2, e.g., an infection in subject.
A method for predicting how a cancer patient will respond to an antibody drug conjugate (ADC) therapy involves computing a predictive response score by performing statistical operations on the staining of each cancer cell in a tissue sample. The ADC includes an ADC payload and an ADC antibody that targets the trophoblast antigen 2 (TROP2) protein in the cancer cells. The tissue sample is stained using a dye linked to a diagnostic antibody that binds to the protein. Cancer cells in digital images of tissue are detected. The statistical operations are performed for each cancer cell based on the staining intensities of the dye in the membrane and/or cytoplasm of each cancer cell and/or in the membranes of neighboring cancer cells. The response of the cancer patient to the ADC therapy is predicted based on whether the results of the statistical operations exceed various clinically derived thresholds.
A pharmaceutical product for administration of an anti HER2 antibody-drug conjugate in combination with a RASG12C inhibitor is provided. Also provided is a therapeutic use and method wherein the antibody-drug conjugate and the RASG12C inhibitor are administered in combination to a subject.
A61K 31/519 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic 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
A61K 39/00 - Medicinal preparations containing antigens or antibodies
A pharmaceutical product for administration of an anti TROP2 antibody-drug conjugate in combination with an ATR inhibitor is provided. The anti-TROP2 antibody-drug conjugate is an antibody-drug conjugate in which a drug linker represented by the following formula (wherein A represents the connecting position to an anti-TROP2 antibody) is conjugated to an anti-TROP2 antibody via a thioether bond. Also provided is a therapeutic use and method wherein the anti-TROP2 antibody-drug conjugate and the ATR inhibitor are administered in combination to a subject : Formula (I).
A61K 47/68 - 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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
Compounds, e.g., radioimmunoconjugates, including a chelating moiety or a metal complex thereof, a linker, and an antibody or antigen-binding fragment thereof targeting both EGFR and cMET. Pharmaceutical compositions of such compounds and methods of treatment for conditions, e.g., cancer, using such compounds or pharmaceutical compositions.
A pharmaceutical product for administration of an anti-TROP2 antibody-drug conjugate in combination with a PARP1 selective inhibitor is provided. The anti-TROP2 antibody-drug conjugate is an antibody-drug conjugate in which a drug-linker represented by the following formula (wherein A represents the connecting position to an anti-TROP2 antibody) is conjugated to an anti-TROP2 antibody via a thioether bond. Also provided is a therapeutic use and method wherein the anti-TROP2 antibody-drug conjugate and the PARP1 selective inhibitor are administered in combination to a subject : Formula (II)
The present disclosure provides pharmaceutical compositions comprising antibodies and antigen-binding fragments thereof that specifically bind to the spike protein of SARS-CoV-2 the prevention and treatment of Coronavirus Disease 2019 (COVID-19) in a subject.
OXFORD UNIVERSITY INNOVATION LIMITED (United Kingdom)
Inventor
Tabor, David
Bright, Helen
Abram, Michael
Abstract
The invention relates to A composition comprising a viral vector, wherein the viral vector is an adenovirus based vector, the viral vector comprising nucleic acid having a polynucleotide sequence encoding a polypeptide, said polypeptide having an amino acid sequence having at least 90% sequence identity to SEQ ID NO: 1, characterised in that said polypeptide comprises the following substitutions relative to SEQ ID NO: 1: L18F, D80A, G215D, L242 Δ, A243 Δ, L244 Δ, K417N, E484K, N501Y, D614G; and A701V. The invention also related to uses and methods.
A method is provided for lowering blood sugar in a subject in need thereof by administering a gliflozin Sodium-Glucose Cotransport 2 inhibitor pharmaceutical composition to a subject qualified for over-the-counter access to the gliflozin Sodium- Glucose Cotransport 2 inhibitor pharmaceutical composition. In some embodiments, the gliflozin Sodium-Glucose Cotransport 2 inhibitor pharmaceutical composition includes empagliflozin, canagliflozin, and ertugliflozin. In some embodiments, the gliflozin Sodium- Glucose Cotransport 2 inhibitor pharmaceutical composition includes (2S,3R,4R,5S,6R)-2- [4-chloro-3-[(4-ethoxyphenyl)methyl]phenyl]-6-(hydroxymethyl)oxane-3,4,5-triol or a pharmaceutically acceptable salt thereof.
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
Methods of purifying adenovirus that can be performed on a large scale. The methods purify adenovirus from an adenovirus-containing sample comprising or derived from a host cell population by clarifying the sample, wherein clarification comprises depth filtration followed by microfiltration; processing the clarified sample by anion exchange chromatography; and processing the anion exchange product by tangential flow filtration (TFF) to provide a TFF product.
Methods for the production of adenoviruses which are suitable for use in a vaccine, and methods for increasing the yield of adenoviruses during production. These methods include adding an adenovirus to a cell population in culture; culturing the cell population under conditions which are permissive for infection of the cell population with the adenovirus to provide a cell population comprising adenovirus-infected cells; culturing the cell population comprising adenovirus-infected cells under conditions which are permissive for replication of the adenovirus; and harvesting the adenovirus from the culture.
Described herein are stable pharmaceutical formulations for bioactive agents, including macromolecular bioactive agents such as polynucleotides and polypeptides. Also provided are medicaments and treatments using the pharmaceutical formulations described herein, as well as kits and methods of treating, preventing or managing a disease or disorder using the pharmaceutical formulations described herein.
A pharmaceutical product for administration of an anti-HER2 antibody-drug conjugate in combination with a PARP1 selective inhibitor is provided. The anti-HER2 antibody drug conjugate is an antibody-drug conjugate in which a drug-linker represented by the following formula (wherein A represents the connecting position to an antibody) is conjugated to an anti-HER2 antibody via a thioether bond. Also provided is a therapeutic use and method wherein the antibody-drug conjugate and the PARP1 selective inhibitor are administered in combination to a subject: Formula (I).
A61P 35/02 - Antineoplastic agents specific for leukemia
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
A method for predicting how a cancer patient will respond to an antibody drug conjugate (ADC) therapy involves computing a predictive response score based on single-cell ADC scores for each cancer cell. The ADC includes an ADC payload and an ADC antibody that targets a protein on each cancer cell, wherein the protein is human epidermal growth factor receptor 2 (HER2). A tissue sample is immunohistochemically stained using a dye linked to a diagnostic antibody that binds to the protein on cancer cells in the tissue sample. Cancer cells in a digital image of the tissue are detected. For each cancer cell, a single-cell ADC score is computed based on the staining intensities of the dye in the membrane and/or cytoplasm of the cancer cell and/or in the membranes and cytoplasms of neighboring cancer cells. The response of the cancer patient to the ADC therapy is predicted by aggregating all single-cell ADC scores of the tissue sample using a statistical operation.
The present disclosure provides antibodies and antigen-binding fragments thereof that specifically bind to the spike protein of SARS-CoV-2 and methods of using such antibodies and antigen-binding fragments thereof for the prevention and treatment of Coronavirus Disease 2019 (COVID-19) in a subject.
The present disclosure provides SARS-CoV-2 spike proteins and trimers containing such spike proteins. The present disclosure also provides antibodies and antigen-binding fragments thereof that specifically bind to the spike protein of SARS-CoV-2. The proteins, trimers, and antibodies can be used, for example, to detect anti-SARS-CoV-2 antibodies in sample obtained from a subject.
A pharmaceutical product for administration of an anti HER2 antibody-drug conjugate in combination with an ATM inhibitor is provided. The anti-HER2 antibody-drug conjugate is an antibody-drug conjugate in which a drug linker represented by the following formula (wherein A represents the connecting position to an antibody) is conjugated to an anti-HER2 antibody via a thioether bond. Also provided is a therapeutic use and method wherein the antibody-drug conjugate and the ATM inhibitor are administered in combination to a subject: Formula (I).
A61K 47/68 - 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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
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 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A pharmaceutical product for administration of an anti HER2 antibody-drug conjugate in combination with a CDK9 inhibitor is provided. The anti-HER2 antibody-drug conjugate is an antibody-drug conjugate in which a drug linker represented by the following formula (wherein A represents the connecting position to an antibody) is conjugated to an anti-HER2 antibody via a thioether bond. Also provided is a therapeutic use and method wherein the antibody-drug conjugate and the CDK9 inhibitor are administered in combination to a subject: Formula (I):
A61K 47/68 - 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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
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 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A pharmaceutical product for administration of an anti HER2 antibody-drug conjugate in combination with an ATR inhibitor is provided. The anti-HER2 antibody-drug conjugate is an antibody-drug conjugate in which a drug linker represented by the following formula (wherein A represents the connecting position to an antibody) is conjugated to an anti-HER2 antibody via a thioether bond. Also provided is a therapeutic use and method wherein the antibody-drug conjugate and the ATR inhibitor are administered in combination to a subject: Formula (I):
A61K 47/68 - 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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A pharmaceutical product for administration of an anti HER2 antibody-drug conjugate in combination with an Aurora B inhibitor is provided. The anti-HER2 antibody drug conjugate is an antibody-drug conjugate in which a drug-linker represented by the following formula (wherein A represents the connecting position to an antibody) is conjugated to an anti-HER2 antibody via a thioether bond. Also provided is a therapeutic use and method wherein the antibody-drug conjugate and the Aurora B inhibitor are administered in combination to a subject: Formula (I):
A61K 47/68 - 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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
A61K 31/517 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A pharmaceutical product for administration of an anti HER2 antibody-drug conjugate in combination with a DNA-PK inhibitor is provided. The ant1-HER2 antibody-drug conjugate is an antibody-drug conjugate in which a drug linker represented by the following formula (wherein A represents the connecting position to an antibody) is conjugated to an ant1-HER2 antibody via a thioether bond. Also provided is a therapeutic use and method wherein the antibody-drug conjugate and the DNA-PK inhibitor are administered in combination to a subject:
A61K 47/68 - 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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
A61K 31/522 - Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
The present disclosure provides antibodies and antigen-binding fragments thereof that specifically bind to the spike protein of SARS-CoV-2 and methods of making and selecting the same. The antibodies can be used, for example, in prophylaxis, post-exposure prophylaxis, or treatment of SARS-CoV-2 infection. The antibodies can also be used to detect SARS-CoV-2 infection in subject.
A method is provided for lowering blood pressure in a subject in need thereof by administering a dihydropyridine-type calcium channel blocker pharmaceutical composition to a subject qualified for over-the-counter access to the dihydropyridine-type calcium channel blocker pharmaceutical composition. In some embodiments, the dihydropyridine-type calcium channel blocker pharmaceutical composition includes isradipine, nifedipine, or nisoldipine. In some embodiments, the dihydropyridine-type calcium channel blocker pharmaceutical composition includes 3-O-ethyl 5-O-methyl 2-(2-aminoethoxymethyl)-4-(2- chlorophenyl)-6-methyl-l,4-dihydropyridine-3,5-dicarboxylate or a pharmaceutically acceptable salt thereof.
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
G16H 10/20 - ICT specially adapted for the handling or processing of patient-related medical or healthcare data for electronic clinical trials or questionnaires
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 31/4422 - 1,4-Dihydropyridines, e.g. nifedipine, nicardipine
A method is provided for lowering triglyceride levels in a subject in need thereof by administering a concentrated fish oil-based pharmaceutical composition to a subject qualified for over-the-counter access to the concentrated fish oil-based pharmaceutical composition. In some embodiments, the concentrated fish oil-based pharmaceutical composition includes an omega-3-carboxylic acid pharmaceutical composition. In some embodiments, the concentrated fish oil-based pharmaceutical composition includes an omega-3 acid ethyl ester pharmaceutical composition, an ethyl eicosapentaenoic acid pharmaceutical composition, or a krill oil pharmaceutical composition.
G16H 10/20 - ICT specially adapted for the handling or processing of patient-related medical or healthcare data for electronic clinical trials or questionnaires
A61K 31/202 - 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 three or more double bonds, e.g. linolenic acid
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
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
28.
METHODS FOR LOWERING BLOOD SUGAR WITH A DIPEPTIDYL PEPTIDASE-4 INHIBITOR PHARMACEUTICAL COMPOSITION
A method is provided for lowering blood sugar in a subject in need thereof by administering a dipeptidyl peptidase-4 inhibitor pharmaceutical composition to a subject qualified for over-the-counter access to the dipeptidyl peptidase-4 inhibitor pharmaceutical composition. In some embodiments, the dipeptidyl peptidase-4 inhibitor pharmaceutical composition includes saxagliptin, sitagliptin, linagliptin, alogliptin, or a pharmaceutically acceptable salt thereof. In some embodiments, the dipeptidyl peptidase-4 inhibitor pharmaceutical composition includes (1S,3S,5S)-2-[(2S)-2-amino-2-(3-hydroxy-1- adamantyl)acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile or a pharmaceutically acceptable salt thereof.
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
G16H 10/20 - ICT specially adapted for the handling or processing of patient-related medical or healthcare data for electronic clinical trials or questionnaires
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 31/403 - 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 condensed with carbocyclic rings, e.g. carbazole
A61K 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
A61K 31/513 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
A61K 31/522 - Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
29.
METHODS FOR TREATING ERECTILE DYSFUNCTION WITH A CGMP-SPECIFIC PHOSPHODIESTERASE 5 INHIBITOR PHARMACEUTICAL COMPOSITION
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
G16H 10/20 - ICT specially adapted for the handling or processing of patient-related medical or healthcare data for electronic clinical trials or questionnaires
30.
METHODS FOR TREATING ERECTILE DYSFUNCTION WITH A CGMP-SPECIFIC PHOSPHODIESTERASE 5 INHIBITOR PHARMACEUTICAL COMPOSITION
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
G16H 10/20 - ICT specially adapted for the handling or processing of patient-related medical or healthcare data for electronic clinical trials or questionnaires
31.
METHODS FOR TREATMENT OF HYPERTENSION WITH AN ANGIOTENSIN II RECEPTOR BLOCKER PHARMACEUTICAL COMPOSITION
A method is provided for lowering blood pressure in a subject in need thereof by administering an angiotensin II receptor blocker pharmaceutical composition to a subject qualified for over-the-counter access to the angiotensin II receptor blocker pharmaceutical composition. In some embodiments, the angiotensin II receptor blocker pharmaceutical composition includes azilsartan medoxomil, candesartan, eprosartan, irbesartan, losartan, olmesartan, telmisartan, or valsartan. In some embodiments, the angiotensin II receptor blocker pharmaceutical composition comprises an active ingredient that is (5-methyl-2-oxo- 1,3-dioxol-4-yl)methyl 2-ethoxy-1-{[2'-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)biphenyl-4- yl]methyl}-1H-benzimidazole-7-carboxylate or a pharmaceutically acceptable salt thereof.
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
G16H 10/20 - ICT specially adapted for the handling or processing of patient-related medical or healthcare data for electronic clinical trials or questionnaires
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 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 31/4178 - 1,3-Diazoles not condensed and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
A61K 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
A method is provided for lowering blood sugar in a subject in need thereof by administering a gliflozin Sodium-Glucose Cotransport 2 inhibitor pharmaceutical composition to a subject qualified for over-the-counter access to the gliflozin Sodium- Glucose Cotransport 2 inhibitor pharmaceutical composition. In some embodiments, the gliflozin Sodium-Glucose Cotransport 2 inhibitor pharmaceutical composition includes empagliflozin, canagliflozin, and ertugliflozin. In some embodiments, the gliflozin Sodium- Glucose Cotransport 2 inhibitor pharmaceutical composition includes (2S,3R,4R,5S,6R)-2- [4-chloro-3-[(4-ethoxyphenyl)methyl]phenyl]-6-(hydroxymethyl)oxane-3,4,5-triol or a pharmaceutically acceptable salt thereof.
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
G16H 10/20 - ICT specially adapted for the handling or processing of patient-related medical or healthcare data for electronic clinical trials or questionnaires
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 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 31/381 - Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
33.
METHODS FOR LOWERING BLOOD SUGAR WITH A METFORMIN PHARMACEUTICAL COMPOSITION
A method is provided for lowering blood sugar in a subject in need thereof by administering a biguanide anti -hyperglycemic pharmaceutical composition to a subject qualified for over-the-counter access to the biguanide anti-hyperglycemic pharmaceutical composition. In some embodiments, the biguanide anti-hyperglycemic pharmaceutical composition includes Ν,Ν-dimethylimidodicarbonimidic diamide, or a pharmaceutically acceptable salt thereof. In some embodiments, the biguanide anti-hyperglycemic pharmaceutical composition includes metformin hydrochloride.
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
G16H 10/20 - ICT specially adapted for the handling or processing of patient-related medical or healthcare data for electronic clinical trials or questionnaires
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
A method is provided for treating or preventing symptoms of asthma in a subject in need thereof by administering a corticosteroid pharmaceutical composition to a subject qualified for over-the-counter access to the corticosteroid pharmaceutical composition. In some embodiments, the corticosteroid pharmaceutical composition includes a class B corticosteroid, a glucocorticosteroid, budesonide, ciclesonide, fluticasone furoate, mometasone furoate, fluticasone propionate, or beclomethasone dipropionate.
G16H 10/20 - ICT specially adapted for the handling or processing of patient-related medical or healthcare data for electronic clinical trials or questionnaires
A61K 31/573 - Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
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
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
35.
METHODS BASED ON THE DETECTION OF RAD51 FOCI IN TUMOR CELLS
FUNDACIÓ PRIVADA INSTITUT D'INVESTIGACIÓ ONCOLÒGICA DE VALL HEBRON (Spain)
ASTRAZENECA UK LIMITED (United Kingdom)
XENTECH SAS (France)
Inventor
Serra Elizalde, Violeta
Balmaña Gelpi, Judith
Cruz Zambrano, Cristina
Llop Guevara, Alba
Castroviejo Bermejo, Marta
O'Connor, Mark J.
Jones, Gemma Nicole
Abstract
The invention provides a method allowing to determine whether a subject diagnosed with cancer is sensitive or resistant to an anti-cancer treatment, based on the level of cells with RAD51 foci in a sample containing tumor cells isolated from said subject, wherein the subject has not received at 24 hours prior to the isolation of the sample, a chemotherapy selected from the group consisting of AC, FEC, ECF and navelbine/epirubicin, and wherein the sample has not been treated with a method that induces DNA damage before determining the level of cells with RAD51 foci.
Systems and methods are provided for over the counter statin delivery to a subject. 5 Survey results from the subject are run against a first plurality of filters. When a filter in the first plurality of filters is fired, the subject is deemed not qualified. The survey results are also run against a second plurality of filters. When a respective filter in the second plurality is fired, the subject is provided with a corresponding warning. The method proceeds to a fulfillment process when no filter in the first plurality fires and the subject has acknowledged each warning associated with each fired filter in the second plurality. The fulfillment stores the composition order, communicates a drug facts label for the statin to the subject, and authorizes, upon subject confirmation that the label has been read, provision of the statin to the subject, the authorization including a destination associated with the subject.
G16H 10/20 - ICT specially adapted for the handling or processing of patient-related medical or healthcare data for electronic clinical trials or questionnaires
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
G06Q 50/00 - Systems or methods specially adapted for specific business sectors, e.g. utilities or tourism
37.
1-[2-(AMINOMETHYL)BENZYL]-2-THIOXO-1,2,3,5-TETRAHYDRO-4H-PYRROLO[3,2-D]PYRIMIDIN-4-ONES AS INHIBITORS OF MYELOPEROXIDASE
There are disclosed certain 1-[2-(aminomethyl)benzyl]-2-thioxo-1,2,3,5-tetrahydro-4H- pyrrolo[3,2-d]pyrimidin-4-one compounds of formula (I), and pharmaceutically acceptable salts thereof, together with compositions containing them and their use in therapy. The compounds are inhibitors of the enzyme MPO and are thereby particularly useful in the treatment or prophylaxis of cardiovascular disorders such as heart failure and coronary artery disease related conditions.
A61K 31/519 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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
38.
PARTICULATE PHARMACEUTICAL COMPOSITIONS AND DOSAGE FORMS OF SAXAGLIPTIN AND METHODS FOR MAKING THE SAME
The present disclosure relates generally to formulations of saxagliptin. One aspect of the invention is a particulate pharmaceutical composition including (or consisting essentially of) a plurality of particles, each particle including saxagliptin in a crystalline HCl salt form and one or more polymers. Another aspect of the invention is a method for making such particulate pharmaceutical compositions. Advantageously, formulations including such particulate pharmaceutical compositions in compressed form can exhibit increased storage stability.
A61K 31/403 - 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 condensed with carbocyclic rings, e.g. carbazole
39.
[1,2,4]TRIAZOLO[4,3-B]PYRIDAZINES FOR USE IN THE TREATMENT OF PROLIFERATIVE DISEASES
The invention concerns compounds of Formula (I) (Formula (I)) or pharmaceutically-acceptable salts thereof, wherein R1, R2 and n have any of the meanings defined herein before in the description; processes for their preparation, pharmaceutical compositions containing them and their use as anti-proliferative and/or cell-killing agents.
Disclosed arecertain derivatives of benzoxazinone amidesof formula (I),or pharmaceutically acceptable salts thereof, (Formula (I)) that act as mineralocorticoid (MR) receptor modulatorsthat may reduce oxidative stress in endothelium and hence improve vascular function, to methods for their potential therapeutic use, to pharmaceutical compositions containing them and to processes for preparing such compounds.
There is provided a process for the preparation of AZD5363, or a salt of AZD5363, comprising: (a) the reaction of 8-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-3-oxa-l,8- diazaspiro[4.5]decane-2,4-dione: or a salt thereof, with (S)-3-amino-3-(4-chlorophenyl)propan-1-ol, or a salt thereof, in the presence of base; and (b) either isolating AZD5363 or isolating AZD5363 as a salt. 8-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-3-oxa-1,8-diazaspiro[4.5]decane-2,4-dione is provided and is prepared by reacting 4-(alkyloxycarbonylamino)-1-(7H-pyrrolo[2,3-d]pyrimidin-4- yl)piperidine-4-carboxylic acid, or a salt thereof, with a cyclising agent
Methods are provided for avoiding an increase in glucagon secretion associated with the administration of a sodium glucose co-transporter 2 (SGLT2) inhibitor via the co-administration of a dipeptidyl peptidase IV (DPP IV) inhibitor. Additionally, methods are provided for normalizing the glucagon secretion associated with the administration of a sodium glucose co-transporter 2 (SGLT2) inhibitor via the co-administration of a dipeptidyl peptidase IV (DPP IV) inhibitor. The present invention also relates to methods for treating diabetes, especially Type 2 diabetes, as well as hyperglycemia, hyperinsulinemia, obesity, hypertriglyceridemia, Syndrome X, diabetic complications, atherosclerosis and related diseases, comprising administering an SGLT2 inhibitor and a dipeptidyl peptidase IV (DPP IV) inhibitor.
A61K 31/40 - 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
A61K 31/403 - 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 condensed with carbocyclic rings, e.g. carbazole
A61K 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
A61K 31/522 - Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
The specification generally relates to compounds of Formula (I) and pharmaceutically acceptable salts thereof, where Q, R1, R2, R3, R4 and R5 have any of the meanings defined herein. The specification also relates to the use of such compounds and salts thereof to treat or prevent ATM kinase mediated disease, including cancer. The specification further relates to crystalline forms of compounds of imidazo[4,5- c]quinolin-2-one compounds and pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising such compounds and salts; kits comprising such compounds and salts; methods of manufacture of such compounds and salts; intermediates useful in the manufacture of such compounds and salts; and to methods of treating ATM kinase mediated disease, including cancer, using such compounds and salts.
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
The invention relates to the methods for identifying resistance to cancer therapy, by identification of an E63K NRAS mutation, a G12V NRAS mutation or a gain of copy number of NRAS gene. A further aspect of the invention relates to methods of treatment that may overcome such resistance mechanisms, involving the use of an EGFR inhibitor in combination with a MEK inhibitor for the treatment of cancers involving an NRAS mutation selected from E63K, G12V, G12R, G12A, G12D, G12S and G12C, and/or cancel- involving a gain of copy number of NRAS gene.
The present invention provides a compound of a formula (I): or a pharmaceutically acceptable salt thereof; a process for preparing such a compound; and to the use of such a compound in the treatment of an ENaC mediated disease state (such as asthma, CF or COPD).
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 241/28 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with nitrogen atoms directly attached to ring carbon atoms in which said hetero-bound carbon atoms have double bonds to oxygen, sulfur or nitrogen atoms
A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
A61P 11/00 - Drugs for disorders of the respiratory system
Disclosed are methods of treating disorders associated with sebaceous glands, inducing sebaceous gland atrophy and reducing sebum production by administering 2- ((1R,4R)-4-(4-(6-carbamoyl-3,5-dimethylpyrazin-2-yl)phenyl)cyclohexyl)acetic acid, or a pharmaceutically acceptable salt thereof, to a subject.
The present disclosure relates to certain (2S)-N-[(1S)-1-cyano-2-phenylethyl]-1,4- oxazepane-2-carboxamide compounds (including pharmaceutically acceptable salts thereof), (Formula (I)) that inhibit dipeptidyl peptidase 1(DPP1) activity, to their utility in treating and/or preventing clinical conditions including respiratory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), to their use in therapy, to pharmaceutical compositions containing them and to processes for preparing such compounds.
C07D 267/10 - Seven-membered rings having the hetero atoms in positions 1 and 4 not condensed with other rings
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
C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms 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
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
A61P 11/00 - Drugs for disorders of the respiratory system
The present invention relates to pharmaceutical compositions suitable for oral administration, and more particularly to pharmaceutical compositions, including pharmaceutical tablet compositions, containing N-(2-{2-dimethylaminoethyl- methylamino}-4-methoxy-5-{[4-(1-methylindol-3-yl)pyrimidin-2-yl]amino}phenyl)prop- 2-enamide ("AZD9291") or a pharmaceutically acceptable salt thereof, wherein such compositions comprise a certain amount of microcrystalline cellulose and at least one other pharmaceutical diluent.
The present invention is directed to, inter alia, the predictive potential of serum protein and tumour gene expression in patients with metastatic colorectal cancer (mCRC) receiving either chemotherapy plus placebo or chemotherapy plus the VEGF signalling inhibitor cediranib, sunitinib, sorafenib, pazopanib, tivozanib, vandetanib, soraninib, axitinib, cabozantinib, bevacizumab, aflibercept or ramucirumab. The present invention, in addition, provides for patient selection methods, as well as kits, that may be used in determining suitable cancer treatment regimens in subjects with cancer, with particular reference to whether the subject will gain benefit from treatment with VEGF signalling inhibitors.
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 31/4725 - Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
A61K 31/506 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 31/513 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
A61K 31/517 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
A61K 31/519 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
Prodrugs of an NMDA antagonist, (S)-1-phenyl-2-(pyridin-2-yl)ethanamine, useful for the treatment of depression (particularly major depressive disorder) or pain; compositions comprising them, and methods of making them.
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 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 31/4402 - Non-condensed pyridines; Hydrogenated derivatives thereof only substituted in position 2, e.g. pheniramine, bisacodyl
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
Described herein are polymeric nanoparticles that include a therapeutic agent which is 2-(3-((7-(3-(ethyl(2-hydroxyethyl)amino)propoxy)quinazolin-4-yl)amino)-1H-pyrazol- -yl)-N-(3-fluorophenyl)acetamide (also known as AZD1152 hqpa) or a pharmaceutically acceptable salt thereof, and methods of making and using such therapeutic nanoparticles.
The invention concerns compounds of Formula (I) or pharmaceutically-acceptable salts thereof, wherein R1 to R5 have any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of cell proliferative disorders.
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
A61P 5/24 - Drugs for disorders of the endocrine system of the sex hormones
A61P 15/08 - Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
A61K 9/00 - Medicinal preparations characterised by special physical form
54.
COUNTER MECHANISM FOR A DRUG ADMINISTRATION DEVICE
There is provided a dose-counting mechanism capable of accurately displaying a dose count while at the same time fitting in the limited space inside a drug administration device. Within the dose-counting mechanism (C) used in a drug administration device (S), there is provided: a count display tape member (11) with multiple locking holes set at equal intervals; a drive shaft (17) that rotates by a specified angle in conjunction with a rotating shaft of the aforementioned drug administration device, which rotates by a given angle each time dosing is performed; a winding drum (15) for winding the aforementioned count display tape member, which rotates in conjunction with the rotation of the aforementioned drive shaft; a sprocket (19) that is mounted onto a sprocket shaft, which rotates in conjunction with the aforementioned drive shaft and features one or more locking claws that engage the locking hole of the aforementioned count display tape member and regulate the display position of the count display unit, which represents the number of doses; and an unwinding drum (13) that unwinds the aforementioned count display tape member, which is wound up by the aforementioned winding drum and is attached to the aforementioned drive shaft.
The invention relates to compounds of formula(I), or a pharmaceutically acceptable salt thereof: Formula (I) which possess inhibitory activity against activating mutant forms of EGFR,and are accordingly useful for their anti-cancer activity and in methods of treatment of the human or animal body. The invention also relates pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti- cancer effect in a warm-blooded animal such as man.
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
A61K 31/495 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
A61K 31/505 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
The present invention relates to the use of combinations comprising 8-[(1R)-1-(3,5- difluorophenylamino)ethyl]-N,N-dimethyl-2-morpholino-4-oxo-4H-chromene-6- carboxamide or a pharmaceutically acceptable salt thereof and a taxane in the treatment or prophylaxis of cancer; pharmaceutical compositions comprising Compound [I] (or a pharmaceutically acceptable salt thereof) and a taxane; kits comprising Compound [I] or a pharmaceutically acceptable salt thereof and a taxane, optionally with instructions for use; and methods of treatment comprising the simultaneous, sequential or separate administration of Compound [I] or a pharmaceutically acceptable salt thereof and a taxane to warm-blooded animal, such as man.
The present invention relates to a method of treatment of nosocomial pneumonia using a combination of ceftazidime (a third generation cephalosporin) and avibactam (a novel β-lactamase inhibitor), optionally with one or more additional therapeutic agents.
A61K 31/546 - Compounds containing 5-thia-1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula , e.g. cephalosporins, cefaclor, cephalexine containing further heterocyclic rings, e.g. cephalothin
A61K 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
A61P 11/00 - Drugs for disorders of the respiratory system
58.
COMPOUNDS AND METHODS FOR TREATING BACTERIAL INFECTIONS
Compounds of formula (I), pharmaceutically acceptable salts thereof, and uses of the compounds of formula (I) for treating bacterial infections are disclosed.
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
A61K 31/535 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
The invention concerns compounds of Formula (I) (Formula (I)) or pharmaceutically-acceptable salts thereof, wherein R1 and R2 have any of the meanings defined herein before in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of cell proliferative disorders.
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
There are provided pharmaceutical compositions comprising a compound of Formula (I) as defined herein and an amount of an alkaline effervescent agent that is sufficient to provide satisfactory in vitro dissolution; and further comprising one or more pharmaceutically acceptable ingredients; and to processes for obtaining them.
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
61.
COMPOUNDS AND METHODS FOR INHIBITING NHE-MEDIATED ANTIPORT IN THE TREATMENT OF DISORDERS ASSOCIATED WITH FLUID RETENTION OR SALT OVERLOAD AND GASTROINTESTINAL TRACT DISORDERS
The present disclosure is directed to compounds and methods for the treatment of disorders associated with fluid retention or salt overload, such as heart failure (in particular, congestive heart failure), chronic kidney disease, end-stage renal disease, liver disease, and peroxisome proliferator-activated receptor (PPAR) gamma agonist-induced fluid retention. The present disclosure is also directed to compounds and methods for the treatment of hypertension. The present disclosure is also directed to compounds and methods for the treatment of gastrointestinal tract disorders, including the treatment or reduction of pain associated with gastrointestinal tract disorders.
A61K 47/48 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates
A61P 1/00 - Drugs for disorders of the alimentary tract or the digestive system
A61P 9/04 - Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
A61P 13/12 - Drugs for disorders of the urinary system of the kidneys
62.
COMPOUNDS AND METHODS FOR INHIBITING NHE-MEDIATED ANTIPORT IN THE TREATMENT OF DISORDERS ASSOCIATED WITH FLUID RETENTION OR SALT OVERLOAD AND GASTROINTESTINAL TRACT DISORDERS
The present disclosure is directed to compounds and methods for the treatment of disorders associated with fluid retention or salt overload, such as heart failure (in particular, congestive heart failure), chronic kidney disease, end-stage renal disease, liver disease, and peroxisome proliferator-activated receptor (PPAR) gamma agonist- induced fluid retention. The present disclosure is also directed to compounds and methods for the treatment of hypertension. The present disclosure is also directed to compounds and methods for the treatment of gastrointestinal tract disorders, including the treatment or reduction of pain associated with gastrointestinal tract disorders.
A61K 47/48 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates
C07D 217/04 - Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ring; Alkylene-bis-isoquinolines with hydrocarbon or substituted hydrocarbon radicals attached to the ring nitrogen atom
A61P 1/00 - Drugs for disorders of the alimentary tract or the digestive system
A61P 9/04 - Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
The invention described herein provides methods for treating microorganism infection based on the relationship among a given set of parameters pertinent to microorganism infection.
Cycloalkyl ether compounds, therapeutically acceptable salts thereof, processes for preparation thereof, therapeutic uses of such compounds for treating Αβ-related pathologies such as Down's syndrome, β-amyloid angiopathy, Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration and pharmaceutical compositions containing such compounds. Formula (I) wherein A is -O-, or -CH2-, n is 0 or 1.
C07D 235/02 - Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
A61K 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
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
65.
2H-IMIDAZOL-4-AMINE COMPOUNDS AND THEIR USE AS BACE INHIBITORS
2H-imidazol-4-amine compounds, therapeutically acceptable salts thereof, processes for preparation thereof, therapeutic uses of such compounds for treating Αβ-related pathologies such as Down's syndrome, β-amyloid angiopathy, Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration methods of therapy, and pharmaceutical compositions containing such compounds. Formula (I) wherein A is -O- or -CH2-, n is 1 or 1.
C07D 235/02 - Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
A61K 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
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
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
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
66.
CYCLOHEXANE-1,2'-INDENE-1',2"-IMIDAZOL COMPOUNDS AND THEIR USE AS BACE INHIBITORS
Cyclohexane-1,2'-indene-1',2''-imidazole compounds, therapeutically acceptable salts thereof, processes for preparation thereof, therapeutic uses of such compounds for treating Aβ-related pathologies such as Down's syndrome, β-amyloid angiopathy, Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration, methods of therapy using such compounds, and pharmaceutical compositions containing such compounds.
C07D 235/02 - Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
A61K 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
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
67.
CYCLOHEXANE-1,2'-NAPHTHALENE-1',2"-IMIDAZOLE COMPOUNDS AND THEIR USE AS BACE INHIBITORS
Cyclohexane-1,2'-naphthalene-1',2''-imidazole compounds, therapeutically acceptable salts thereof, processes for preparation thereof, therapeutic uses of such compounds for treating Aβ-related pathologies such as Down's syndrome, β-amyloid angiopathy, Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration, methods of therapy using such compounds, and pharmaceutical compositions containing such compounds.
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
A61K 31/4188 - 1,3-Diazoles condensed with heterocyclic ring systems, e.g. biotin, sorbinil
C07D 491/107 - Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
A camsylate salt of (1r,1 'R,4R)- 4-methoxy-5"-methyl-6'-[5-(prop-1-yn-1-yl)pyridin-3-yl]-3'H-dispiro[cyclohexane-1,2'-inden-1'2'-imidazole]-4"-amine, pharmaceutical compositions containing the salt and therapeutic uses of the salt for treating Αβ-related pathologies such as Alzheimer's Disease, Down's syndrome, β-amyloid angiopathy and conditions such as dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration.
C07D 401/10 - 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 aromatic rings
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
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
69.
CRYSTALLINE FORMS OF (S) -4-AMINO-N- (1- (4 - CHLOROPHENYL) - 3 - HYDROXYPROPYL) -1- (7H - PYRROLO [2, 3-D] PYRIMIDI N-4-YL) PIPERIDINE-4-CARBOXAMIDE
The present invention discloses certain new solid state forms of (S)-4-amino-N-(1- (4-chlorophenyl)-3-hydroxypropyl)-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4- carboxamide, processes for preparing such forms, pharmaceutical compositions comprising them, and the use of such forms in therapy.
The present invention is directed to compounds which are beta-lactamase inhibitors. The compounds and their pharmaceutically acceptable salts, are useful in combination with beta-lactam antibiotics, or alone, for the treatment of bacterial infections, including infections caused by drug resistant organisms, including multi-drug resistant organisms. The present invention includes compounds according to formula (Ia): or a pharmaceutically acceptable salt thereof, wherein the values of R1, R 2, R 3 and R 4 are described herein.
A61K 31/439 - 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 forming part of a bridged ring system, e.g. quinuclidine
The invention relates to chemical compounds of Formula (I): or a salt thereof. In some embodiments, the invention relates to inhibitors of CK2. In still further embodiments, the invention relates to pharmaceutical compositions comprising compounds disclosed herein and their use in the prevention and treatment of CK2-related conditions and diseases, e.g., cancer.
An isolated si RNA comprising a sense sequence and an antisense sequence, wherein the sense and the antisense sequence are substantially complementary to each other to form a double-stranded structure that is 17-25 base pairs in length, and wherein the antisense sequence comprises a nucleotide sequence sufficiently complementary to a target human ICAM-1 nucleotide sequence selected from the group of sequences shown in Table 1.
A61P 11/00 - Drugs for disorders of the respiratory system
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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
The present invention provides a method of selection of a patient, who is a candidate for treatment with an NMDA antagonist drug, such as (S)-1-phenyl-2-(pyridin-2- yl)ethanamine or ketamine, whereby to predict an increased or decreased likelihood of response to the NMDA antagonist. The invention provides a method for determining the sequence of GABR-A2 at any of four single nucleotide polymorphism (SNP) sitesknown as rs3756007, rs11503016, rs17537359 or rs1372472. The method also provides ARMS primers optimised for determining the sequence atthese GABR-A2SNPs and diagnostic kits comprising suitable primers or probes for determining the particular SNPs.
The present invention relates to a combination comprising AZD5363, or a pharmaceutically acceptable salt thereof, and at least one androgen receptor signalling modulator selected from MDV-3100 (also known as enzalutamide), AZD3514, abiraterone (or an ester prodrug thereof: e.g. abiraterone acetate), and bicalutamide; or a pharmaceutically acceptable salt thereof. Each of these combinations may be useful in the treatment of cancer. The invention also relates to pharmaceutical compositions comprising such combinations, and further relates to methods of treatment comprising the simultaneous, sequential or separate administration of AZD5363, or a pharmaceutically acceptable salt thereof, with at least one androgen receptor signalling modulator as described above, to warm-blooded animal, such as a human for the treatment of cancer. The invention also relates to a kit comprising such combinations.
Beta-secretase inhibitors, of formula (I) as described in the specification, pharmaceutical compositions comprising them and therapeutic methods using them for the treatment and/or prevention of Αβ-related pathologies such as Down's syndrome, β-amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI ("mild cognitive impairment"), Alzheimer's Disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease, progressive supranuclear palsy or cortical basal degeneration.
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 401/10 - 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 aromatic rings
C07D 403/10 - 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 carbon chain containing aromatic rings
C07D 491/107 - Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
A61K 31/506 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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
A61P 25/00 - Drugs for disorders of the nervous 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
An inhaler for delivery of a medicament by inhalation is disclosed. The inhaler comprises a dose counting mechanism comprising a counter. The inhaler further comprises a dispensing mechanism, the dispensing mechanism being configured, on actuation, to dispense a dose of medicament and to adjust the counter. The inhaler further comprises a resetting member configured for movement in a first direction between a first position and a second position to reset the dispensing mechanism, and a prevention mechanism comprising a pair of first and second engaging members. If the movement of the resetting member in the first direction is reversed before it reaches the second position, the first and second engaging members prevent further actuation of the dispensing mechanism until the resetting member is again moved in the first direction. At least one of the first and second engaging members is configured to resiliently flex, under load, into abutment with a substantially rigid component of the inhaler. Preferably the dose counting mechanism counter indicates the number of remaining doses in, or the number of dispensed doses from, the inhaler.
An inhaler for delivery of a medicament by inhalation is disclosed. The inhaler comprises a dispensing mechanism, the dispensing mechanism being configured to dispense a dose of medicament on actuation. The inhaler further comprises a dose counting mechanism comprising a counter and a translating member. The translating member comprises a pawl. The counter comprises a first count wheel, a second count wheel and an intermediate wheel engaged with the second count wheel and in selective engagement with the first count wheel. When the inhaler is fired to dispense a dose of medicament, the dispensing mechanism moves the translating member in a substantially linear direction. The pawl thus rotates the first count wheel, and as the first count wheel rotates, the intermediate wheel is selectively engaged thereby selectively rotating the second count wheel to count the doses of the inhaler.
The present invention relates to certain 2-(2,4,5-substituted-anilino) pyrimidine compounds and pharmaceutically acceptable salts thereof which may be useful in the treatment or prevention of a disease or medical condition mediated through certain mutated forms of epidermal growth factor receptor (for example the L858R activating mutant, the Exonl9 deletion activating mutant and the T790M resistance mutant). Such compounds and salts thereof may be useful in the treatment or prevention of a number of different cancers. The invention also relates to pharmaceutical compositions comprising said compounds and salts thereof, especially useful polymorphic forms of these compounds and salts, intermediates useful in the manufacture of said compounds and to methods of treatment of diseases mediated by various different forms of EGFR using said compounds and salts thereof.
C07D 401/02 - 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
A61K 31/506 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic 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
There are provided pharmaceutical compositions comprising greater than 15% w/w of a compound of Formula (I) as defined herein and/or hydrate thereof and an amount of one or more effervescent agents that is sufficient to provide satisfactory in vitro dissolution; and further comprising one or more pharmaceutically acceptable ingredients; and to processes for obtaining them.
Disclosed herein are azetidinyl compounds of formula I, as described herein, pharmaceutical compositions comprising an azetidinyl compound, and a method of using an azetidinyl compound in the treatment or prophylaxis of a melanin- concentrating hormone related disease or condition.
C07D 491/044 - Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
C07D 491/048 - Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
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 31/407 - 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 condensed with heterocyclic ring systems, e.g. ketorolac, physostigmine
There is provided a compound which is (a) a pyrimidine sulfonamide of formula (I) or (b) a pharmaceutically acceptable salt thereof, crystalline forms of the compound, processes for obtaining the compound, pharmaceutical intermediates used in the manufacture of the compound, and pharmaceutical compositions containing the compound. The compound is useful in the treatment of a disease/condition in which modulation of chemokine receptor activity is beneficial.
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 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
A61K 31/506 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
C07D 317/24 - Radicals substituted by singly bound oxygen or sulfur atoms esterified
C07C 69/92 - Esters of carboxylic acids having an esterified carboxyl group bound to a carbon atom of a six-membered aromatic ring of monocyclic hydroxy carboxylic acids, the hydroxy groups and the carboxyl groups of which are bound to carbon atoms of a six-membered aromatic ring with etherified hydroxyl groups
82.
PROCESS FOR PREPARING HETEROCYCLIC COMPOUNDS INCLUDING TRANS-7-OXO-6-(SULPHOOXY)-1,6-DIAZABICYCLO[3,2,1]OCTANE-2-CARBOXAMIDE AND SALTS THEREOF
The present invention relates to compounds and processes for preparing compounds of Formula (I), including compounds such as trans-7-oxo-6-(sulphooxy)-1,6- diazabicyclo[3,2,1]octane-2-carboxamide and salts thereof (e.g., NXL-104).
The present invention relates to a novel co-crystal of the compound of formula (I): wherein the co-former molecule is acetyl salicylic acid, to processes for the preparation of the co-crystal, to pharmaceutical compositions containing the co-crystal, to the use of such a co-crystal in the manufacture of a medicament for use in the prevention of arterial thrombotic complications in patients with coronary artery, cerebrovascular or peripheral vascular disease and to methods of treating such diseases in the human or animal body by administering a therapeutically effective amount of a such a co-crystal.
C07D 277/68 - Benzothiazoles 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 in position 2
C07C 309/08 - Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing oxygen atoms bound to the carbon skeleton containing hydroxy groups bound to the carbon skeleton
86.
CHROMENONE COMPOUNDS AS PI 3 -KINASE INHIBITORS FOR THE TREATMENT OF CANCER
The invention concerns chromenone compounds of Formula I; or pharmaceutically-acceptable salts thereof, wherein each of R1, R2, R3, R4, R5, n and R6 has any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of cell proliferative disorders.
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
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
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/541 - Non-condensed thiazines containing further heterocyclic rings
The present invention relates to a combination comprising (5)-4-amino-N-(1-(4- chlorophenyl)-3 -hydroxypropyl)-1-(7H-pyrrolo [2,3 -d]pyrimidin-4-yl)piperidine-4- carboxamide, or a pharmaceutically acceptable salt thereof, hereafter "Compound (I)", and a taxane. Taxanes include established cancer drugs such as docetaxel (TaxotereTM) and paclitaxel (TaxolTM). Such combinations may be useful in the treatment or prophylaxis of cancer. The invention also relates to a pharmaceutical composition comprising such Compound (I) and a taxane. The invention further relates to a method of treatment comprising the simultaneous, sequential or separate administration of Compound (I) and a taxane, to warm-blooded animal, such as man. The invention also relates to a kit comprising Compound (I) and a taxane, optionally with instructions for use.
A method for identifying binding agents having binding specificity for a nucleic acid modification, the binding agents comprising an antigen binding site and including for example, antibodies or fragments or derivatives thereof. Binding agents having binding specificity for a nucleic acid modification, particularly of the backbone or sugar component, the binding agents comprising an antigen binding site, and including for example, antibodies or fragments or derivatives thereof. Uses of the binding agents and associated compositions in diagnostics and therapy.
The present invention relates to solid, semisolid, or liquid formulations comprising amine compounds that prevent or reduce formic acid and/or formyl species generation in the dosage form during the manufacturing process and/or during shelf -life storage. The formulations of the present invention prevent or reduce formation of N- formyl impurities (and gelatin crosslinking) during the manufacturing process and/or during shelf -life storage.
A61K 31/40 - 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
The invention provides the compound of formula. (I) and pharmaceutically acceptable salt thereof, pharmaceutical compositions containing the compound and the use of the compound in therapy.
C07D 473/18 - Heterocyclic compounds containing purine ring systems with oxygen, sulfur, or nitrogen atoms directly attached in positions 2 and 6 one oxygen and one nitrogen atom, e.g. guanine
A61K 31/522 - Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
The invention provides the compound of formula (I) and pharmaceutically acceptable salt thereof, pharmaceutical compositions containing the compound and the use of the compound in therapy.
A61K 31/4188 - 1,3-Diazoles condensed with heterocyclic ring systems, e.g. biotin, sorbinil
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
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
92.
PHENOL COMPOUNDS ALS TOLL -LIKE RECEPTOR 7 AGONISTS
The invention concerns compounds of Formula (I): wherein R1, R2, R3 and Q are as defined in the description. The present invention also relates to processes for the preparation of such compounds, novel intermediates useful in the preparation of such compounds, pharmaceutical compositions containing them and their use as toll-like receptor 7 agonists.
The invention concerns compounds of Formula (I), and pharmaceutically acceptable salts thereof: where such compounds act as TLR7 agonists and at the same time show advantageous selectivity over TLR8 and hERG, wherein the variable groups R1, R2 and n are as defined herein. The invention also relates to methods for the preparation of such compounds and intermediates useful in the preparation thereof, to pharmaceutical compositions containing such compounds, to the use of such compounds in the preparation of medicaments, and to the use of such compounds in the treatment of conditions mediated by TLR7, such as allergic diseases, autoimmune diseases, viral diseases and, in particular, cancer.
C07D 239/49 - Two nitrogen atoms with an aralkyl radical, or substituted aralkyl radical, attached in position 5, e.g. trimethoprim
C07D 403/10 - 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 carbon chain containing aromatic rings
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
A61K 31/505 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
A61K 31/506 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
The present invention relates to a method for stratifying cancer patients according to the cellular phenotype of the tumour based and in particular, according to the presence of stroma and/or location of tumour vessels within the tumour or stromal compartments of a tumour. This patient stratification permits identification of patients whose tumours are more likely to be responsive to treatment with anti-cancer drugs, such as Vascular Endothelial Growth Factors (VEGF) signalling inhibitors. This invention therefore provides personalised healthcare opportunities in the cancer arena.
The invention is directed at a method for predicting a patient's responsiveness to an IAP antagonist. The method includes analysing a tumour cell containing sample from a test patient for the gene status of the TP53 gene, wherein tumours that possess a mutant TP53 gene are more likely to respond favourably to treatment with an IAP antagonist and can thus be selected for, and treated with, an IAP antagonist.
The invention provides a pharmaceutical product comprising, in combination, (1) a named glucocorticosteroid receptor agonist and (2) a β2 adrenoreceptor agonist, a dual β2 adrenoreceptor agonist/M3 receptor antagonist, a muscarinic antagonist, a p38 kinase inhibitor, a neutrophil elastase inhibitor, a phosphodiesterase PDE4 inhibitor, an IKK2 kinase inhibitor or a non-steroidal glucocorticoid receptor agonist, and the use of said product in treating respiratory diseases.
The present invention relates to solid, semisolid, or liquid formulations comprising water soluble antioxidants that prevent or reduce formic acid and/or formyl species generation in the dosage form during the manufacturing process and/or during shelf-life storage. The formulations of the present invention prevent or reduce formation of N-formyl impurities (and gelatin crosslinking) during the manufacturing process and/or during shelf-life storage.
A61K 31/403 - 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 condensed with carbocyclic rings, e.g. carbazole
The present invention relates to compounds of Formula (I) and/or Formula (Ia): and to their salts, pharmaceutical compositions, methods of use, and methods for their preparation. These compounds inhibit ALK kinase activity, and thus may be used for the treatment of 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
C07F 9/6568 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus atoms as the only ring hetero atoms
A61K 31/506 - Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
The present invention relates to compounds of Formula (I): and to their salts, pharmaceutical compositions, methods of use, and methods for their preparation. These compounds inhibit Bcl-2 and/or Bcl-XL activities and may be used for the treatment of cancer.
C07D 211/22 - 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 singly bound oxygen or sulfur atoms by oxygen atoms
A61K 31/445 - Non-condensed piperidines, e.g. piperocaine
A dry powder inhaler comprises a disc-shaped assembly (14) having cavities (16) filled with medicament powder for inhalation. The assembly is rotatably mounted in a housing (6, 8) on which is mounted a rotatable external casing (11, 12). A mouthpiece (10) is movably mounted on the housing (6, 8) allowing it to be brought into and out of engagement with the edge of the disc (14) whereby the mouthpiece acts as a brake to prevent or permit rotational movement of the disc (14). The inhaler is opened by rotating the housing with respect to the casing (11, 12) to expose the mouthpiece (10). As the inhaler is opened and closed, cam followers (105) on the mouthpiece move along cam tracks (109) in the casing (11, 12), causing the mouthpiece to move against or away from the disc (14). A gap is defined between the disc and mouthpiece to allow a flow of bypass air to enter the mouthpiece.
patents
