This disclosure provides a method for treating a subject afflicted with a renal cancer, which method comprises administering to the subject therapeutically effective amounts of: (a) an anti-cancer agent which is an antibody or an antigen-binding portion thereof that specifically binds to a Programmed Death-1 (PD-1) receptor and inhibits PD-1 activity; and (b) another anti-cancer agent. The other anti-cancer agent may be an anti-angiogenic tyrosine kinase inhibitor or an anti-Cytotoxic T-Lymphocyte Antigen-4 (CTLA-4) antibody. The disclosure also provides a kit for treating a subject afflicted with a renal cancer, the kit comprising a dosage of an anti-PD-1 antibody, a dosage of another anti-cancer agent which is an anti-angiogenic tyrosine kinase inhibitor or an anti-CTLA-4 antibody, and instructions for using the anti-PD-1 antibody and the other anti-cancer agent in any of the disclosed methods for treating a renal cancer.
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
In one aspect, a system is provided of verifying the accuracy of a plurality of serially-connected drug modules of a combinatorial drug delivery device, each of the drug modules including a drug reservoir, the system including: a machine-readable code located on each of the drug modules; application software configured to generate an activation code based on the machine-readable codes and the sequence of the machine-readable codes; a flow controller on the drug delivery device which is selectively actuatable to a use state to permit flow of drug from the drug delivery device; and, a control unit on the drug delivery device having a computing processing unit configured to compare the activation code with an authentication code, and, wherein, if the authentication code matches the activation code, the computing processing unit causes actuation of the flow controller to permit flow of the drug from the drug delivery device.
The present invention provides a newly identified B7 receptor, zB7R1 that functions as lymphocyte inhibitory receptor, which is a PD-1-like molecule and is expressed on T cells. The present invention also provides the discovery of zB7R1's ability to bind to CD155. Methods and compositions for modulating zB7R1-mediated negative signaling and interfering with the interaction of its counter-receptor for therapeutic, diagnostic and research purposes are also provided.
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
A61K 39/00 - Medicinal preparations containing antigens or antibodies
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
C07K 14/47 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans from vertebrates from mammals
C12Q 1/66 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving luciferase
G01N 33/50 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing
G01N 33/569 - ImmunoassayBiospecific binding assayMaterials therefor for microorganisms, e.g. protozoa, bacteria, viruses
Provided herein are compounds and compositions thereof that reduce FAK protein levels. In some embodiments, the compounds have structures of Formula I: In some embodiments, the compounds and compositions are provided for treatment of FAK associated diseases 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 31/437 - 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 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
In accordance with the present disclosure, macrocyclic compounds have been discovered which inhibit the LAG-3/MHC Class II protein/protein interaction, and may be useful for the amelioration of various diseases, including cancer and infectious diseases.
C07K 7/56 - Cyclic peptides containing at least one abnormal peptide link with at least one abnormal peptide link in the ring the cyclisation not occurring through 2,4-diamino-butanoic acid
In accordance with the present disclosure, macrocyclic compounds have been discovered which inhibit the LAG-3/MHC Class II protein/protein interaction, and may be useful for the amelioration of various diseases, including cancer and infectious 5 diseases.
C07K 7/08 - Linear peptides containing only normal peptide links having 12 to 20 amino acids
C07K 7/56 - Cyclic peptides containing at least one abnormal peptide link with at least one abnormal peptide link in the ring the cyclisation not occurring through 2,4-diamino-butanoic acid
In accordance with the present disclosure, macrocyclic compounds have been discovered which inhibit the LAG-3/MHC Class II protein/protein interaction, and may be useful for the amelioration of various diseases, including cancer and infectious diseases.
C07K 7/08 - Linear peptides containing only normal peptide links having 12 to 20 amino acids
C07K 7/56 - Cyclic peptides containing at least one abnormal peptide link with at least one abnormal peptide link in the ring the cyclisation not occurring through 2,4-diamino-butanoic acid
In accordance with the present disclosure, macrocyclic compounds have been discovered which inhibit the LAG-3/MHC Class II protein/protein interaction, and may be useful for the amelioration of various diseases, including cancer and infectious 5 diseases.
In accordance with the present disclosure, macrocyclic compounds have been discovered which inhibit the LAG-3/MHC Class II protein/protein interaction and may be useful for the amelioration of various diseases, including cancer and infectious diseases.
C07K 7/56 - Cyclic peptides containing at least one abnormal peptide link with at least one abnormal peptide link in the ring the cyclisation not occurring through 2,4-diamino-butanoic acid
In accordance with the present disclosure, macrocyclic compounds have been discovered which inhibit the LAG-3/MHC Class II protein/protein interaction, and may be useful for the amelioration of various diseases, including cancer and infectious diseases.
C07K 7/56 - Cyclic peptides containing at least one abnormal peptide link with at least one abnormal peptide link in the ring the cyclisation not occurring through 2,4-diamino-butanoic acid
In accordance with the present disclosure, macrocyclic compounds have been discovered which inhibit the mouse LAG-3/MHC Class II protein/protein interaction, and may be useful for the amelioration of various diseases, including cancer and infectious diseases.
Compounds according to Formula (I) are useful as agonists of Toll-like receptor 7 (TLR7). Such compounds can be used alone or as part of an antibody-drug conjugate in cancer treatment, for example in combination with an anti-cancer immunotherapy agent. Such compounds may also be used as vaccine adjuvants.
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
Compounds according to Formula (I) are useful as agonists of Toll-like receptor 7 (TLR7). Such compounds can be used in cancer treatment, especially in combination with an anti-cancer immunotherapy agent, or as a vaccine adjuvant.
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
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
The present disclosure provides compositions and methods of inactivating a virus in a product feedstream in a manufacturing process of a therapeutic agent using an antifoam reagent. In some aspects, the therapeutic agent comprises a therapeutic protein, a viral particle, a nucleic acid molecule, or any combination thereof. Other aspects of the present disclosure are directed to methods of inactivating a virus in a eukaryotic cell culture of a product feedstream, comprising contacting the cell culture with an antifoam reagent. In some aspects, the antifoam reagent comprises an emulsifier, e.g., a nonionic emulsifier, and optionally a silicone polymer.
A01N 25/30 - Biocides, pest repellants or attractants, or plant growth regulators, characterised by their forms, or by their non-active ingredients or by their methods of applicationSubstances for reducing the noxious effect of the active ingredients to organisms other than pests characterised by the surfactants
A01P 1/00 - DisinfectantsAntimicrobial compounds or mixtures thereof
C12N 7/00 - Viruses, e.g. bacteriophagesCompositions thereofPreparation or purification thereof
Compounds according to Formula (I) are useful as agonists of Toll-like receptor 7 (TLR7).
Compounds according to Formula (I) are useful as agonists of Toll-like receptor 7 (TLR7).
Compounds according to Formula (I) are useful as agonists of Toll-like receptor 7 (TLR7).
Such compounds can be used in cancer treatment, especially in combination with an anti-cancer immunotherapy agent, or as a vaccine adjuvant.
A61K 31/519 - PyrimidinesHydrogenated 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 31/541 - Non-condensed thiazines containing further heterocyclic rings
A61K 31/675 - Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting 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
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
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
The subject invention is for use with various drug delivery devices, including medical injectors, medical pill bottles, and medical pill blister packs. The subject invention utilizes one or more optically readable codes which are initially concealed and, later revealed during or after use. The encoded data of the optically readable codes may be obtained to provide information for various purposes, including, but not limited to, verification of proper drug and dose for a given patient, dosing duration, and successful completion of dosing.
G16H 20/17 - 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 delivered via infusion or injection
A61M 5/20 - Automatic syringes, e.g. with automatically actuated piston rod, with automatic needle injection, filling automatically
A61M 5/24 - Ampoule syringes, i.e. syringes with needle for use in combination with replaceable ampoules or cartridges, e.g. automatic
G06K 7/10 - Methods or arrangements for sensing record carriers by electromagnetic radiation, e.g. optical sensingMethods or arrangements for sensing record carriers by corpuscular radiation
Compounds according to Formula (I) are useful as agonists of Toll-like receptor 7 (TLR7).
Compounds according to Formula (I) are useful as agonists of Toll-like receptor 7 (TLR7).
Compounds according to Formula (I) are useful as agonists of Toll-like receptor 7 (TLR7).
Such compounds can be used alone or as part of an antibody-drug conjugate in cancer treatment, for example in combination with an anti-cancer immunotherapy agent. Such compounds may also be used as vaccine adjuvants.
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting 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
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
Provided herein are isolated anti-CEACAM5 antibodies, antigen binding portions thereof, bispecific antibodies, and conjugates (e.g., antibody-drug conjugates), which specifically bind to CEACAM5 and are internalized by CEACAM5 expressing cells. Also provided are nucleic acids encoding the anti-CEACAM5 antibodies and antigen binding portions, methods for treating cancer comprising administration of CEACAM5-targeted antibodies, antigen binding portions thereof, bispecific antibodies, and conjugates and/or associated therapies, as well as methods of diagnosis, and kits.
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
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
Provided herein are antibody drug conjugates of the formula (I) comprising an anti-CEACAM5 antibodies, antigen binding portions thereof that is conjugated with a linker and exatecan. The disclosure also provides a method of treating cancer in a subject in need thereof comprising administering to the subject an antibody drug conjugate disclosed herein.
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting 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
Provided herein are antibody drug conjugates of the formula (I) comprising an anti-CEACAM5 antibodies, antigen binding portions thereof that is conjugated with a linker and exatecan. The disclosure also provides a method of treating cancer in a subject in need thereof comprising administering to the subject an antibody drug conjugate disclosed herein.
A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting 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 disclosure relates to compounds of Formula (I), which are RXFP1 receptor agonists, compositions containing them, and methods of using them, for example, in the treatment of heart failure, fibrotic diseases, and related diseases such as lung disease (e.g., idiopathic pulmonary fibrosis), kidney disease (e.g., chronic kidney disease), or hepatic disease (e.g., non-alcoholic steatohepatitis and portal hypertension).
The disclosure relates to compounds of Formula (I), which are RXFP1 receptor agonists, compositions containing them, and methods of using them, for example, in the treatment of heart failure, fibrotic diseases, and related diseases such as lung disease (e.g., idiopathic pulmonary fibrosis), kidney disease (e.g., chronic kidney disease), or hepatic disease (e.g., non-alcoholic steatohepatitis and portal hypertension).
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 31/27 - Esters, e.g. nitroglycerine, selenocyanates of carbamic or thiocarbamic acids, e.g. meprobamate, carbachol, neostigmine
A61K 31/337 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
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 31/351 - 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 31/41 - 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 31/4174 - Arylalkylimidazoles, e.g. oxymetazolin, naphazoline, miconazole
A61K 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
A61K 31/445 - Non-condensed piperidines, e.g. piperocaine
C07C 237/24 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a ring other than a six-membered aromatic ring of the carbon skeleton
C07C 271/54 - Esters of carbamic acids having oxygen atoms of carbamate groups bound to carbon atoms of six-membered aromatic rings with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by carboxyl groups
C07C 317/50 - SulfonesSulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton the carbon skeleton being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups at least one of the nitrogen atoms being part of any of the groups X being a hetero atom, Y being any atom
C07D 257/06 - Five-membered rings with nitrogen atoms directly attached to the ring carbon atom
C07D 295/155 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
C07D 305/06 - Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to the ring atoms
C07D 309/08 - Heterocyclic compounds containing six-membered rings having one oxygen 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 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
23.
COMBINATION THERAPY USING A SUBSTITUTED PYRIMIDIN-4(3H)-ONE AND NIVOLUMAB AS WELL AS ITS USE IN THE TREATMENT OF CANCER
The present disclosure provides a method of treating cancer in a subject. The method including administering to the subject: a) a therapeutically effective amount of a compound of formula (I); and b) a therapeutically effective amount of nivolumab, wherein the compound of formula (I) is represented by formula (I) or a pharmaceutically acceptable salt, hydrate, solvate, stereoisomer, conformational isomer, tautomer, or a combination thereof. In particular, the present disclosure provides a method of treating a solid tumor (e.g., an advanced non-small cell lung cancer) with a therapeutically effective amount of a compound of formula (10b) (i.e., 6-((3S,4S)-4-amino-3-methyl-2-oxa-8-azaspiro[4.5]decan-8-yl)-3-(Ra)-(2,3-dichlorophenyl)-2,5-dimethyl-4(3/7)-pyrimidinone) in combination with nivolumab in a subject, wherein the subject has one or more mutations in KRAS.
The present disclosure provides a method of treating cancer in a subject. The method including administering to the subject: a) a therapeutically effective amount of a compound of formula (I); and b) a therapeutically effective amount of nivolumab, wherein the compound of formula (I) is represented by formula (I) or a pharmaceutically acceptable salt, hydrate, solvate, stereoisomer, conformational isomer, tautomer, or a combination thereof. In particular, the present disclosure provides a method of treating a solid tumor (e.g., an advanced non-small cell lung cancer) with a therapeutically effective amount of a compound of formula (10b) (i.e., 6-((3S,4S)-4-amino-3-methyl-2-oxa-8-azaspiro[4.5]decan-8-yl)-3-(Ra)-(2,3-dichlorophenyl)-2,5-dimethyl-4(3/7)-pyrimidinone) in combination with nivolumab in a subject, wherein the subject has one or more mutations in KRAS.
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
24.
CANCER IMMUNOTHERAPY BY DISRUPTING PD-1/PD-L1 SIGNALING
The disclosure provides a method for immunotherapy of a subject afflicted with cancer, comprises administering to the subject a composition comprising a therapeutically effective amount of an antibody that inhibits signaling from the PD-1/PD-L1 signaling pathway. This disclosure also provides a method for immunotherapy of a subject afflicted with cancer comprising selecting a subject that is a suitable candidate for immunotherapy based on an assessment that the proportion of cells in a test tissue sample from the subject that express PD-L1 on the cell surface exceeds a predetermined threshold level, and administering a therapeutically effective amount of an anti-PD-1 antibody to the selected subject. The invention additionally provides rabbit mAbs that bind specifically to a cell surface-expressed PD-L1 antigen in a FFPE tissue sample, and an automated IHC method for assessing cell surface expression in FFPE tissues using the provided anti-PD-L1 Abs.
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
A61K 39/00 - Medicinal preparations containing antigens or antibodies
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
C07K 16/18 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans
G01N 33/574 - ImmunoassayBiospecific binding assayMaterials therefor for cancer
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
(1) Pharmaceutical preparations for the treatment and prevention of oncological, hematological, metabolic, endocrine, musculoskeletal, cardiovascular, cardiopulmonary, genitourinary, hepatological, respiratory, neurological, gastrointestinal, dermatological, psychiatric, and immune system related diseases and disorders; stem cells for medical purposes; diagnostic radiopharmaceutical preparations; diagnostic preparations for medical purposes; radiopharmaceutical preparations for the treatment of cancer and immune system related diseases and disorders.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations for the treatment and prevention of oncological, hematological, metabolic, endocrine, musculoskeletal, cardiovascular, cardiopulmonary, genitourinary, hepatological, respiratory, neurological, gastrointestinal, dermatological, psychiatric, and immune system related diseases and disorders; stem cells for medical purposes; diagnostic radiopharmaceutical preparations; diagnostic preparations for medical purposes; radiopharmaceutical preparations for the treatment of cancer and immune system related diseases and disorders.
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
A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
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 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 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
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
The present application relates to particular anti-CD33 antibodies, nucleic acids encoding the antibodies, vectors and host cells comprising the nucleic acids, and methods of making and using the antibodies, as well as immunoconjugates comprising the anti-CD33 antibodies.
A61P 35/02 - Antineoplastic agents specific for leukemia
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
29.
CANCER IMMUNOTHERAPY BY DISRUPTING PD-1/PD-L1 SIGNALING
The disclosure provides a method for immunotherapy of a subject afflicted with cancer, comprises administering to the subject a composition comprising a therapeutically effective amount of an antibody that inhibits signaling from the PD-1/PD-L1 signaling pathway. This disclosure also provides a method for immunotherapy of a subject afflicted with cancer comprising selecting a subject that is a suitable candidate for immunotherapy based on an assessment that the proportion of cells in a test tissue sample from the subject that express PD-L1 on the cell surface exceeds a predetermined threshold level, and administering a therapeutically effective amount of an anti-PD-1 antibody to the selected subject. The invention additionally provides rabbit mAbs that bind specifically to a cell surface-expressed PD-L1 antigen in a FFPE tissue sample, and an automated IHC method for assessing cell surface expression in FFPE tissues using the provided anti-PD-L1 Abs.
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
A61K 39/00 - Medicinal preparations containing antigens or antibodies
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
C07K 16/18 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans
G01N 33/574 - ImmunoassayBiospecific binding assayMaterials therefor for cancer
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
(1) Pharmaceutical preparations for the treatment and prevention of obesity, cardiovascular diseases, central nervous system diseases, metabolic disorders, stroke, cancer, inflammatory diseases, respiratory diseases, infectious diseases, auto-immune diseases, solid organ transplant rejection, autoinflammatory disease, blood disease, multiple sclerosis, ulcerative colitis, cystic fibrosis, arthritis, and musculoskeletal and skin disease; antivirals; antibodies for medical purposes; biological preparations for the treatment of cancer; anticoagulants; stem cells for medical purposes; radio-pharmaceutical preparations for the treatment of cancer and solid tumors; diagnostic radio-pharmaceutical preparations; diagnostic preparations for medical purposes
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations for the treatment and prevention of obesity, cardiovascular diseases, central nervous system diseases, metabolic disorders, stroke, cancer, inflammatory diseases, respiratory diseases, infectious diseases, auto-immune diseases, solid organ transplant rejection, autoinflammatory disease, blood disease, multiple sclerosis, ulcerative colitis, cystic fibrosis, arthritis, and musculoskeletal and skin disease; antivirals; antibodies for medical purposes; biological preparations for the treatment of cancer; anticoagulants; stem cells for medical purposes; radio-pharmaceutical preparations for the treatment of cancer and solid tumors; diagnostic radio-pharmaceutical preparations; diagnostic preparations for medical purposes.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceutical preparations for the treatment and prevention of obesity, cardiovascular diseases, central nervous system diseases, metabolic disorders, stroke, cancer, inflammatory diseases, respiratory diseases, infectious diseases, auto-immune diseases, solid organ transplant rejection, autoinflammatory disease, blood disease, multiple sclerosis, ulcerative colitis, cystic fibrosis, arthritis, and musculoskeletal and skin disease; antivirals; antibodies for medical purposes; biological preparations for the treatment of cancer; anticoagulants; stem cells for medical purposes; radio-pharmaceutical preparations for the treatment of cancer and solid tumors; diagnostic radio-pharmaceutical preparations; diagnostic preparations for medical purposes.
33.
PROCESSES FOR PREPARATION OF 3-D PRINTED PHARMACEUTICAL PRODUCTS
The disclosure provides a method for immunotherapy of a subject afflicted with cancer, comprises administering to the subject a composition comprising a therapeutically effective amount of an antibody that inhibits signaling from the PD-1/PD-L1 signaling pathway. This disclosure also provides a method for immunotherapy of a subject afflicted with cancer comprising selecting a subject that is a suitable candidate for immunotherapy based on an assessment that the proportion of cells in a test tissue sample from the subject that express PD-L1 on the cell surface exceeds a predetermined threshold level, and administering a therapeutically effective amount of an anti-PD-1 antibody to the selected subject. The invention additionally provides rabbit mAbs that bind specifically to a cell surface-expressed PD-L1 antigen in a FFPE tissue sample, and an automated IHC method for assessing cell surface expression in FFPE tissues using the provided anti-PD-L1 Abs.
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
A61K 39/00 - Medicinal preparations containing antigens or antibodies
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
C07K 16/18 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans
G01N 33/574 - ImmunoassayBiospecific binding assayMaterials therefor for cancer
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
(1) Pharmaceutical preparations for the treatment and prevention of obesity, cardiovascular diseases, central nervous system diseases, metabolic disorders, stroke, cancer, inflammatory diseases, respiratory diseases, infectious diseases, auto-immune diseases, solid organ transplant rejection, autoinflammatory disease, blood disease, multiple sclerosis, ulcerative colitis, cystic fibrosis, arthritis, and musculoskeletal and skin disease; antivirals; antibodies for medical purposes; biological preparations for the treatment of cancer; anticoagulants; stem cells for medical purposes; radio-pharmaceutical preparations for the treatment of cancer and solid tumors; diagnostic radio-pharmaceutical preparations; diagnostic preparations for medical purposes
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
(1) Pharmaceutical preparations for the treatment and prevention of obesity, cardiovascular diseases, central nervous system diseases, metabolic disorders, stroke, cancer, inflammatory diseases, respiratory diseases, infectious diseases, auto-immune diseases, solid organ transplant rejection, autoinflammatory disease, blood disease, multiple sclerosis, ulcerative colitis, cystic fibrosis, arthritis, and musculoskeletal and skin disease; antivirals; antibodies for medical purposes; biological preparations for the treatment of cancer; anticoagulants; stem cells for medical purposes; radio-pharmaceutical preparations for the treatment of cancer and solid tumors; diagnostic radio-pharmaceutical preparations; diagnostic preparations for medical purposes
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
(1) Pharmaceutical preparations for the treatment and prevention of obesity, cardiovascular diseases, central nervous system diseases, metabolic disorders, stroke, cancer, inflammatory diseases, respiratory diseases, infectious diseases, auto-immune diseases, solid organ transplant rejection, autoinflammatory disease, blood disease, multiple sclerosis, ulcerative colitis, cystic fibrosis, arthritis, and musculoskeletal and skin disease; antivirals; antibodies for medical purposes; biological preparations for the treatment of cancer; anticoagulants; stem cells for medical purposes; radio-pharmaceutical preparations for the treatment of cancer and solid tumors; diagnostic radio-pharmaceutical preparations; diagnostic preparations for medical purposes
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
(1) Pharmaceutical preparations for the treatment and prevention of obesity, cardiovascular diseases, central nervous system diseases, metabolic disorders, stroke, cancer, inflammatory diseases, respiratory diseases, infectious diseases, auto-immune diseases, solid organ transplant rejection, autoinflammatory disease, blood disease, multiple sclerosis, ulcerative colitis, cystic fibrosis, arthritis, and musculoskeletal and skin disease; antivirals; antibodies for medical purposes; biological preparations for the treatment of cancer; anticoagulants; stem cells for medical purposes; radio-pharmaceutical preparations for the treatment of cancer and solid tumors; diagnostic radio-pharmaceutical preparations; diagnostic preparations for medical purposes
05 - Pharmaceutical, veterinary and sanitary products
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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
In accordance with the present disclosure, macrocyclic compounds have been discovered that bind to PD-1 and are capable of inhibiting the interaction of PD-1 with PD-L1. These macrocyclic compounds exhibit in vitro immunomodulatory efficacy thus making them therapeutic candidates for the treatment of various diseases including cancer and infectious diseases.
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50.
AMIDE-SUBSTITUTED HETEROCYCLIC COMPOUNDS USEFUL AS MODULATORS OF IL-12, IL-23 AND/OR IFN ALPHA RESPONSES
Compounds having the following formula I:
Compounds having the following formula I:
or a stereoisomer or pharmaceutically-acceptable salt thereof, where R1, R2, R3, R4, and R5 are as defined herein, are useful in the modulation of IL-12, IL-23 and/or IFNα, by acting on Tyk-2 to cause signal transduction inhibition.
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
C07B 59/00 - Introduction of isotopes of elements into organic compounds
C07D 237/24 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
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 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 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 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
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 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 417/12 - 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
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57.
ENHANCING ANTI-CANCER ACTIVITY OF IMMUNOMODULATORY FC FUSION PROTEINS
The present disclosure provides a method for enhancing the anti-tumor efficacy of an Fc fusion protein which binds specifically to a target, e.g., a co-inhibitory or co-stimulatory receptor of ligand, on a T cell in a subject afflicted with a cancer or a disease caused by an infectious agent and alters the activity of the immunomodulatory target, thereby potentiating an endogenous immune response against cells of the cancer or the infectious agent, wherein the method comprises selecting, designing or modifying the Fc region of the Fc fusion protein so as to enhance the binding of said Fc region to an activating Fc receptor (FcR). The disclosure also provides an Fc fusion protein produced by said method and its use in treating a subject afflicted with a cancer or a disease caused by an infectious agent.
C07K 14/435 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
A61K 39/00 - Medicinal preparations containing antigens or antibodies
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
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A compound of formula I
A compound of formula I
A compound of formula I
wherein A, X, Y, Z, R1 and R24 are described herein. The compounds are useful as inhibitors of potassium channel function and in the treatment and prevention of arrhythmia, IKur-associated disorders, and other disorders mediated by ion channel function.
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 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/549 - 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 sulfur as the ring hetero atoms, e.g. sulthiame having two or more nitrogen atoms in the same ring, e.g. hydrochlorothiazide
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
C07D 239/95 - QuinazolinesHydrogenated quinazolines with hetero atoms directly attached in positions 2 and 4
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 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
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 405/12 - 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
C07D 407/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen 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 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 417/12 - 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
The present disclosure generally relates to 2,3-dihydrobenzo[b][1,4]dioxin-6-yl containing compounds useful as immunomodulators. Provided herein are compounds, compositions comprising such compounds, and methods of their use. The disclosure further pertains to pharmaceutical compositions comprising at least one compound according to the disclosure that are useful for the treatment of various diseases, including cancer and infectious diseases.
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 31/357 - 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
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
A61K 31/4155 - 1,2-Diazoles not condensed and containing further heterocyclic rings
A61K 31/427 - Thiazoles not condensed and containing further heterocyclic rings
A61K 31/4433 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with oxygen as a ring hetero atom
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
A61K 31/453 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with oxygen as a ring hetero atom
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 31/5377 - 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
C07D 319/18 - Ethylenedioxybenzenes, not substituted on the hetero ring
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
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 407/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen 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 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 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 417/12 - 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
80.
ANTIBODIES TARGETING IL-18 RECEPTOR BETA (IL-18RB) AND RELATED METHODS
Provided are novel antibodies and antigen-binding fragments thereof that bind interleukin-18 receptor beta (IL-18Rβ), along with conjugates thereof, nucleic acids encoding the same, compositions comprising the same, and methods of producing and using the same, including in the treatment of various diseases and conditions, such as inflammatory bowel disease, and other immune-mediated diseases, autoimmune diseases, inflammatory diseases, cancers, and infectious diseases.
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
A61K 39/00 - Medicinal preparations containing antigens or antibodies
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61P 1/00 - Drugs for disorders of the alimentary tract or the digestive system
A61P 37/06 - Immunosuppressants, e.g. drugs for graft rejection
81.
HETEROARYL COMPOUNDS AS LIGAND DIRECTED DEGRADERS OF IRAK4
Provided herein are compounds (I) and compositions thereof for modulating IRAK4. In some embodiments, the compounds and compositions are provided for treatment of inflammatory or autoimmune diseases.
C07D 491/107 - Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
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
A61K 31/4353 - 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
Provided herein is a compound of the following structural formula: or a pharmaceutically acceptable salt thereof, and compositions thereof. In some embodiments, the compound and compositions are provided for modulating IRAK4 and/or treating inflammatory or autoimmune diseases.
A61K 31/4353 - 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 disclosure relates to compounds of Formula (I), which are RXFP1 receptor agonists, compositions containing them, and methods of using them, for example, in the treatment of heart failure, fibrotic diseases, and related diseases such as lung disease (e.g., idiopathic pulmonary fibrosis), kidney disease (e.g., chronic kidney disease), or hepatic disease (e.g., non-alcoholic steatohepatitis and portal hypertension).
The disclosure relates to compounds of Formula (I), which are RXFP1 receptor agonists, compositions containing them, and methods of using them, for example, in the treatment of heart failure, fibrotic diseases, and related diseases such as lung disease (e.g., idiopathic pulmonary fibrosis), kidney disease (e.g., chronic kidney disease), or hepatic disease (e.g., non-alcoholic steatohepatitis and portal hypertension).
A61K 31/424 - Oxazoles condensed with heterocyclic ring systems, e.g. clavulanic acid
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 31/222 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin with compounds having aromatic groups, e.g. dipivefrine, ibopamine
A61K 31/27 - Esters, e.g. nitroglycerine, selenocyanates of carbamic or thiocarbamic acids, e.g. meprobamate, carbachol, neostigmine
A61K 31/277 - NitrilesIsonitriles having a ring, e.g. verapamil
A61K 31/337 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
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 31/351 - 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
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 31/40 - 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 31/4015 - 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 having oxo groups directly attached to the heterocyclic ring, e.g. piracetam, ethosuximide
A61K 31/4402 - Non-condensed pyridinesHydrogenated derivatives thereof only substituted in position 2, e.g. pheniramine, bisacodyl
A61K 31/4409 - Non-condensed pyridinesHydrogenated derivatives thereof only substituted in position 4, e.g. isoniazid, iproniazid
A61K 31/4418 - Non-condensed pyridinesHydrogenated derivatives thereof having a carbocyclic ring directly attached to the heterocyclic ring, e.g. cyproheptadine
A61K 31/451 - Non-condensed piperidines, e.g. piperocaine having a carbocyclic ring directly attached to the heterocyclic ring, e.g. glutethimide, meperidine, loperamide, phencyclidine, piminodine
A61K 31/505 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
C07C 233/81 - Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by carboxyl groups
C07C 255/60 - Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the carbon skeleton at least one of the singly-bound nitrogen atoms being acylated
C07C 271/24 - Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atom of at least one of the carbamate groups bound to a carbon atom of a ring other than a six-membered aromatic ring
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 207/09 - Radicals substituted by nitrogen atoms not forming part of a nitro radical
C07D 213/75 - Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
C07D 231/12 - Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 233/64 - Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
C07D 239/26 - Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 261/08 - Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 261/20 - Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings condensed with carbocyclic rings or ring systems
C07D 295/155 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
C07D 305/08 - Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms not condensed with other rings having no 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 atoms
C07D 307/28 - Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 309/22 - Radicals substituted by oxygen atoms
C07D 309/28 - Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member 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 333/24 - 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
The disclosure provides a method of treating a hepatocellular carcinoma with a combination of a LAG-3 antagonist, a PD-1 pathway inhibitor, and an anti-angiogenesis agent.
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
A61K 31/7105 - Natural ribonucleic acids, i.e. containing only riboses attached to adenine, guanine, cytosine or uracil and having 3'-5' phosphodiester links
A61K 39/00 - Medicinal preparations containing antigens or antibodies
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
In accordance with the present disclosure, pharmaceutical formulations that improve the oral bioavailability of biologically active compounds, including macrocyclic compounds, have been discovered.
A61K 31/455 - Nicotinic acid, i.e. niacinDerivatives thereof, e.g. esters, amides
A61K 9/00 - Medicinal preparations characterised by special physical form
A61K 31/24 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids having an aromatic ring attached to a carboxyl group having an amino or nitro group
In some aspects, the present disclosure is directed to a method of treating a tumor in a subject in need thereof comprising administering a KRAS inhibitor and a regulatory T cell (Treg)-depleting agent to the subject. In some aspects, the present disclosure is further directed to methods of reducing the number of Treg cells (Tregs) in a tumor environment (TME) in a subject who receives a therapy with a KRAS inhibitor comprising administering a Treg-depleting agent to the subject. In some aspects, the present disclosure is further directed to methods of treating a tumor in a subject who is identified as having an increased number of Tregs in a TME, or as having a spatial cellular community comprising Tregs in a TME.
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
A61K 39/00 - Medicinal preparations containing antigens or antibodies
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
In some aspects, the present disclosure is directed to a method of treating a tumor in a subject in need thereof comprising administering a KRAS inhibitor and a regulatory T cell (Treg)-depleting agent to the subject. In some aspects, the present disclosure is further directed to methods of reducing the number of Treg cells (Tregs) in a tumor environment (TME) in a subject who receives a therapy with a KRAS inhibitor comprising administering a Treg-depleting agent to the subject. In some aspects, the present disclosure is further directed to methods of treating a tumor in a subject who is identified as having an increased number of Tregs in a TME, or as having a spatial cellular community comprising Tregs in a TME.
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Pharmaceutical preparations for the treatment and prevention of obesity, cardiovascular diseases, central nervous system diseases, metabolic disorders, stroke, cancer, inflammatory diseases, respiratory diseases, infectious diseases, auto-immune diseases, solid organ transplant rejection, autoinflammatory disease, blood disease, multiple sclerosis, ulcerative colitis, cystic fibrosis, arthritis, and musculoskeletal and skin disease; Antivirals; Antibodies for medical purposes; Biological preparations for the treatment of cancer; Anticoagulants; Stem cells for medical purposes; Radiopharmaceutical preparations for the treatment of cancer and solid tumors; Diagnostic radiopharmaceutical preparations; Diagnostic preparations for medical purposes
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Pharmaceutical preparations for the treatment and prevention of obesity, cardiovascular diseases, central nervous system diseases, metabolic disorders, stroke, cancer, inflammatory diseases, respiratory diseases, infectious diseases, auto-immune diseases, solid organ transplant rejection, autoinflammatory disease, blood disease, multiple sclerosis, ulcerative colitis, cystic fibrosis, arthritis, and musculoskeletal and skin disease; Antivirals; Antibodies for medical purposes; Biological preparations for the treatment of cancer; Anticoagulants; Stem cells for medical purposes; Radiopharmaceutical preparations for the treatment of cancer and solid tumors; Diagnostic radiopharmaceutical preparations; Diagnostic preparations for medical purposes
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Pharmaceutical preparations for the treatment and prevention of obesity, cardiovascular diseases, central nervous system diseases, metabolic disorders, stroke, cancer, inflammatory diseases, respiratory diseases, infectious diseases, auto-immune diseases, solid organ transplant rejection, autoinflammatory disease, blood disease, multiple sclerosis, ulcerative colitis, cystic fibrosis, arthritis, and musculoskeletal and skin disease; Antivirals; Antibodies for medical purposes; Biological preparations for the treatment of cancer; Anticoagulants; Stem cells for medical purposes; Radiopharmaceutical preparations for the treatment of cancer and solid tumors; Diagnostic radiopharmaceutical preparations; Diagnostic preparations for medical purposes
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Pharmaceutical preparations for the treatment and prevention of obesity, cardiovascular diseases, central nervous system diseases, metabolic disorders, stroke, cancer, inflammatory diseases, respiratory diseases, infectious diseases, auto-immune diseases, solid organ transplant rejection, autoinflammatory disease, blood disease, multiple sclerosis, ulcerative colitis, cystic fibrosis, arthritis, and musculoskeletal and skin disease; Antivirals; Antibodies for medical purposes; Biological preparations for the treatment of cancer; Anticoagulants; Stem cells for medical purposes; Radiopharmaceutical preparations for the treatment of cancer and solid tumors; Diagnostic radiopharmaceutical preparations; Diagnostic preparations for medical purposes
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Pharmaceutical preparations for the treatment and prevention of obesity, cardiovascular diseases, central nervous system diseases, metabolic disorders, stroke, cancer, inflammatory diseases, respiratory diseases, infectious diseases, auto-immune diseases, solid organ transplant rejection, autoinflammatory disease, blood disease, multiple sclerosis, ulcerative colitis, cystic fibrosis, arthritis, and musculoskeletal and skin disease; Antivirals; Antibodies for medical purposes; Biological preparations for the treatment of cancer; Anticoagulants; Stem cells for medical purposes; Radiopharmaceutical preparations for the treatment of cancer and solid tumors; Diagnostic radiopharmaceutical preparations; Diagnostic preparations for medical purposes
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Pharmaceutical preparations for the treatment and prevention of obesity, cardiovascular diseases, central nervous system diseases, metabolic disorders, stroke, cancer, inflammatory diseases, respiratory diseases, infectious diseases, auto-immune diseases, solid organ transplant rejection, autoinflammatory disease, blood disease, multiple sclerosis, ulcerative colitis, cystic fibrosis, arthritis, and musculoskeletal and skin disease; Antivirals; Antibodies for medical purposes; Biological preparations for the treatment of cancer; Anticoagulants; Stem cells for medical purposes; Radiopharmaceutical preparations for the treatment of cancer and solid tumors; Diagnostic radiopharmaceutical preparations; Diagnostic preparations for medical purposes
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Pharmaceutical preparations for the treatment and prevention of obesity, cardiovascular diseases, central nervous system diseases, metabolic disorders, stroke, cancer, inflammatory diseases, respiratory diseases, infectious diseases, auto-immune diseases, solid organ transplant rejection, autoinflammatory disease, blood disease, multiple sclerosis, ulcerative colitis, cystic fibrosis, arthritis, and musculoskeletal and skin disease; Antivirals; Antibodies for medical purposes; Biological preparations for the treatment of cancer; Anticoagulants; Stem cells for medical purposes; Radiopharmaceutical preparations for the treatment of cancer and solid tumors; Diagnostic radiopharmaceutical preparations; Diagnostic preparations for medical purposes
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Pharmaceutical preparations for the treatment and prevention of obesity, cardiovascular diseases, central nervous system diseases, metabolic disorders, stroke, cancer, inflammatory diseases, respiratory diseases, infectious diseases, auto-immune diseases, solid organ transplant rejection, autoinflammatory disease, blood disease, multiple sclerosis, ulcerative colitis, cystic fibrosis, arthritis, and musculoskeletal and skin disease; Antivirals; Antibodies for medical purposes; Biological preparations for the treatment of cancer; Anticoagulants; Stem cells for medical purposes; Radiopharmaceutical preparations for the treatment of cancer and solid tumors; Diagnostic radiopharmaceutical preparations; Diagnostic preparations for medical purposes
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Pharmaceutical preparations for the treatment and prevention of obesity, cardiovascular diseases, central nervous system diseases, metabolic disorders, stroke, cancer, inflammatory diseases, respiratory diseases, infectious diseases, auto-immune diseases, solid organ transplant rejection, autoinflammatory disease, blood disease, multiple sclerosis, ulcerative colitis, cystic fibrosis, arthritis, and musculoskeletal and skin disease; Antivirals; Antibodies for medical purposes; Biological preparations for the treatment of cancer; Anticoagulants; Stem cells for medical purposes; Radiopharmaceutical preparations for the treatment of cancer and solid tumors; Diagnostic radiopharmaceutical preparations; Diagnostic preparations for medical purposes
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Pharmaceutical preparations for the treatment and prevention of obesity, cardiovascular diseases, central nervous system diseases, metabolic disorders, stroke, cancer, inflammatory diseases, respiratory diseases, infectious diseases, auto-immune diseases, solid organ transplant rejection, autoinflammatory disease, blood disease, multiple sclerosis, ulcerative colitis, cystic fibrosis, arthritis, and musculoskeletal and skin disease; Antivirals; Antibodies for medical purposes; Biological preparations for the treatment of cancer; Anticoagulants; Stem cells for medical purposes; Radiopharmaceutical preparations for the treatment of cancer and solid tumors; Diagnostic radiopharmaceutical preparations; Diagnostic preparations for medical purposes
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Pharmaceutical preparations for the treatment and prevention of obesity, cardiovascular diseases, central nervous system diseases, metabolic disorders, stroke, cancer, inflammatory diseases, respiratory diseases, infectious diseases, auto-immune diseases, solid organ transplant rejection, autoinflammatory disease, blood disease, multiple sclerosis, ulcerative colitis, cystic fibrosis, arthritis, and musculoskeletal and skin disease; Antivirals; Antibodies for medical purposes; Biological preparations for the treatment of cancer; Anticoagulants; Stem cells for medical purposes; Radiopharmaceutical preparations for the treatment of cancer and solid tumors; Diagnostic radiopharmaceutical preparations; Diagnostic preparations for medical purposes
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Pharmaceutical preparations for the treatment and prevention of obesity, cardiovascular diseases, central nervous system diseases, metabolic disorders, stroke, cancer, inflammatory diseases, respiratory diseases, infectious diseases, auto-immune diseases, solid organ transplant rejection, autoinflammatory disease, blood disease, multiple sclerosis, ulcerative colitis, cystic fibrosis, arthritis, and musculoskeletal and skin disease; Antivirals; Antibodies for medical purposes; Biological preparations for the treatment of cancer; Anticoagulants; Stem cells for medical purposes; Radiopharmaceutical preparations for the treatment of cancer and solid tumors; Diagnostic radiopharmaceutical preparations; Diagnostic preparations for medical purposes
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Pharmaceutical preparations for the treatment and prevention of obesity, cardiovascular diseases, central nervous system diseases, metabolic disorders, stroke, cancer, inflammatory diseases, respiratory diseases, infectious diseases, auto-immune diseases, solid organ transplant rejection, autoinflammatory disease, blood disease, multiple sclerosis, ulcerative colitis, cystic fibrosis, arthritis, and musculoskeletal and skin disease; Antivirals; Antibodies for medical purposes; Biological preparations for the treatment of cancer; Anticoagulants; Stem cells for medical purposes; Radiopharmaceutical preparations for the treatment of cancer and solid tumors; Diagnostic radiopharmaceutical preparations; Diagnostic preparations for medical purposes