Disclosed are compounds of Formula (I):
Disclosed are compounds of Formula (I):
Disclosed are compounds of Formula (I):
or stereoisomers, tautomers, or salts thereof, wherein each R is independently H or D. Also disclosed are methods of using such compounds to decrease the levels of IKZF1-4 proteins, and pharmaceutical compositions comprising the compound. The compounds are useful in the treatment of viral infections and proliferative disorders, such as cancer.
C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
A61K 31/4545 - 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 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
C07B 59/00 - Introduction of isotopes of elements into organic compounds
The present application relates to antibodies specifically binding to the V-domain immunoglobulin-containing suppressor of T-cell activation (VISTA) at acidic pH and their use in cancer treatment. In some embodiments, the antibodies bind specifically to human VISTA at acidic pH, but do not significantly bind to human VISTA at neutral or physiological pH.
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 38/16 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof
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. The present application also relates to antibody-drug conjugates comprising an anti-CD33 antibody and a GSPT1 degrader. The present application also relates to linker-drug moieties comprising GSPT1 degraders useful in antibody-drug conjugates.
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
A61K 31/4995 - Pyrazines or piperazines forming part of bridged ring systems
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
4.
GSPT1 COMPOUNDS AND METHODS OF USE OF THE COMPOUNDS
Provided herein are compounds of Formula I:, and pharmaceutically acceptable salts thereof for treating, preventing or managing cancer. Also provided are pharmaceutical compositions comprising the compounds and their pharmaceutically acceptable salts, and methods of use of the compounds, salts, and compositions. In certain embodiments, the methods encompass treating, preventing or managing cancer, including solid tumors and blood borne tumors.
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
The present disclosure provides novel macrocyclic peptides which inhibit the PD-1/PDL1 and PD-L1/CD80 protein/protein interaction, and thus are useful for the amelioration of various diseases, including cancer and infectious diseases.
Provided herein are methods of predicting the responsiveness of a lymphoma patient to a cancer treatment. Also provided herein are methods of treating a lymphoma patient based on predicting the responsiveness of the lymphoma patient to a cancer treatment.
C12Q 1/6886 - Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes for diseases caused by alterations of genetic material for cancer
G16B 25/10 - Gene or protein expression profilingExpression-ratio estimation or normalisation
A61P 35/02 - Antineoplastic agents specific for leukemia
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; Radiopharmaceutical preparations for the treatment of cancer and solid tumors; Diagnostic radiopharmaceutical 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; Radiopharmaceutical preparations for the treatment of cancer and solid tumors; Diagnostic radiopharmaceutical 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; Radiopharmaceutical preparations for the treatment of cancer and solid tumors; Diagnostic radiopharmaceutical 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; Radiopharmaceutical preparations for the treatment of cancer and solid tumors; Diagnostic radiopharmaceutical preparations; Diagnostic preparations for medical purposes
Provided herein are antibodies, or antigen binding portions thereof, that bind to T-cell immunoglobulin and mucin-domain containing-3 (TIM3) protein. Also provided are uses of these antibodies, or antigen binding portions thereof, in therapeutic applications, such as treatment of cancer. Further provided are cells that produce the antibodies, or antigen binding portions thereof, polynucleotides encoding the heavy and/or light chain regions of the antibodies, or antigen binding portions thereof, and vectors comprising the polynucleotides encoding the heavy and/or light chain regions of the antibodies, or antigen binding portions thereof.
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
Disclosed is a method of treating a disease, comprising administering to a human patient in need thereof, a dose of 30 mg daily of 2-(4-(2-(7,8-dimethyl-[1,2,4]triazolo[1,5-a]pyridin-6-yl)-3-isopropyl-1H-indol-5-yl)piperidin-1-yl)acetamide or a pharmaceutically acceptable salt thereof, wherein said disease is lupus.
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 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61P 37/00 - Drugs for immunological or allergic disorders
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
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; Radiopharmaceutical preparations for the treatment of cancer and solid tumors; Diagnostic radiopharmaceutical 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; Radiopharmaceutical preparations for the treatment of cancer and solid tumors; Diagnostic radiopharmaceutical 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; Radiopharmaceutical preparations for the treatment of cancer and solid tumors; Diagnostic radiopharmaceutical 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; Radiopharmaceutical preparations for the treatment of cancer and solid tumors; Diagnostic radiopharmaceutical 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; Radiopharmaceutical preparations for the treatment of cancer and solid tumors; Diagnostic radiopharmaceutical 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; Radiopharmaceutical preparations for the treatment of cancer and solid tumors; Diagnostic radiopharmaceutical 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; Radiopharmaceutical preparations for the treatment of cancer and solid tumors; Diagnostic radiopharmaceutical 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; Radiopharmaceutical preparations for the treatment of cancer and solid tumors; Diagnostic radiopharmaceutical 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; Radiopharmaceutical preparations for the treatment of cancer and solid tumors; Diagnostic radiopharmaceutical 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; Radiopharmaceutical preparations for the treatment of cancer and solid tumors; Diagnostic radiopharmaceutical 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; Radiopharmaceutical preparations for the treatment of cancer and solid tumors; Diagnostic radiopharmaceutical 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; Radiopharmaceutical preparations for the treatment of cancer and solid tumors; Diagnostic radiopharmaceutical 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; Radiopharmaceutical preparations for the treatment of cancer and solid tumors; Diagnostic radiopharmaceutical 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; Radiopharmaceutical preparations for the treatment of cancer and solid tumors; Diagnostic radiopharmaceutical 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; Radiopharmaceutical preparations for the treatment of cancer and solid tumors; Diagnostic radiopharmaceutical 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; Radiopharmaceutical preparations for the treatment of cancer and solid tumors; Diagnostic radiopharmaceutical 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; Radiopharmaceutical preparations for the treatment of cancer and solid tumors; Diagnostic radiopharmaceutical preparations; Diagnostic preparations for medical purposes
31.
TRIAZOLOPYRIDINYL ETHER LINKED COMPOUNDS AS KINASE INHIBITORS
Compounds having formula (I), and enantiomers, and diastereomers, stereoisomers, pharmaceutically˗acceptable salts thereof, are useful as kinase modulators, including RIPK1 modulation. All the variables are as defined herein.
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
32.
PIPERIDINE SUBSTITUTED PYRAZOLOPYRIMIDINE DERIVATIVES AS INHIBITORS OF SGK1
The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective SGK1 inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating disorders associated with serum- and glucocorticoid-regulated kinase 1 (SGK1) activity, such as cardiovascular disorders, fibrotic diseases, metabolic diseases, immune and inflammatory diseases, neurological disorders, and cancer, by using the compounds and pharmaceutical compositions.
A61P 9/00 - Drugs for disorders of the cardiovascular 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
Compounds having formula (I), and enantiomers, and diastereomers, stereoisomers, pharmaceutically acceptable salts thereof, (I) are useful as kinase modulators, including RIPK1 modulation. All the variables are as defined herein.
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
A61K 31/395 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
The present disclosure provides isolated monoclonal antibodies (e.g., humanized and human monoclonal antibodies), or antigen-binding fragments thereof, that specifically bind to human natural killer cell inhibitory receptor group 2A (NKG2A) protein with high affinity and exhibit therapeutically desirable functional properties, such as for the treatment of, for example, cancer. Immunoconjugates, bispecific molecules, and pharmaceutical compositions comprising the anti-NKG2A antibodies of the invention are also provided. Nucleic acid molecules encoding the antibodies, expression vectors, host cells, and methods of treatment of, for example, cancer using the antibodies are further provided. Combination therapy, in which an anti-NKG2A antibody in the present disclosure is co-administered with at least one additional agent such as another antibody (e.g., anti-PD-1, anti-PD-L1, and/or anti-CTLA-4 antibodies), is 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
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
Disclosed are compounds of Formula (I): (I) or stereoisomers, tautomers, or salts thereof, wherein R is defined herein. Also disclosed are methods of using such compounds to decrease the levels of Ikaros protein, Helios protein, Aiolos protein, and Eos protein; and pharmaceutical compositions comprising such compounds. These compounds are useful in the treatment of viral infections and proliferative disorders, 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 31/4545 - 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
37.
NAPHTHALENE AND QUINOLINE ANALOGS AS RXFP1 AGONISTS
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).
C07C 235/56 - Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings and singly-bound oxygen atoms bound to the same carbon skeleton with carbon atoms of carboxamide groups and singly-bound oxygen atoms bound to carbon atoms of the same non-condensed six-membered aromatic ring having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a six-membered aromatic ring
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 31/351 - 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 31/423 - Oxazoles condensed with carbocyclic rings
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
C07C 317/22 - SulfonesSulfoxides having sulfone or sulfoxide groups and singly-bound oxygen atoms bound to the same carbon skeleton with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
C07D 261/20 - Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings condensed with carbocyclic rings or ring systems
C07D 275/02 - Heterocyclic compounds containing 1, 2-thiazole or hydrogenated 1,2-thiazole rings not condensed with other rings
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
38.
MEDICAL INJECTOR FOR ON-BODY MOUNTING WITH FLOW DETECTING
In one aspect, a medical injector is provided for mounting onto the skin of a user for administering a dose of liquid drug to the user, the medical injector including: a body containing a reservoir of the liquid drug; a cannula for insertion into the skin of the user; a conduit for fluidically connecting the body and the cannula to allow the liquid drug to be conveyed to the cannula, wherein the conduit includes a tubular metallic section; a temperature sensor for measuring the temperature of the metallic section; and, a CPU for collecting periodic temperature measurements from the temperature sensor to evaluate change in temperature of the metallic section over time. Advantageously, the subject invention allows for a non-invasive mode of detecting drug flow in an on-body medical injector.
A61M 5/168 - Means for controlling media flow to the body or for metering media to the body, e.g. drip meters, counters
A61M 5/44 - Devices for bringing media into the body in a subcutaneous, intra-vascular or intramuscular wayAccessories therefor, e.g. filling or cleaning devices, arm rests having means for cooling or heating the devices or media
39.
GSPT1 COMPOUNDS AND METHODS OF USE OF THE NOVEL COMPOUNDS
Provided herein are compounds having the formula I
Provided herein are compounds having the formula I
Provided herein are compounds having the formula I
for treating, preventing or managing cancer. Also provided are pharmaceutical compositions comprising the compounds and methods of use of the compounds and compositions. In certain embodiments, the methods encompass treating, preventing or managing cancer, including solid tumors and blood borne tumors using the compounds provided herein.
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 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 405/14 - 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
1233, m, and n are defined herein. Also disclosed are methods of using such compounds to decrease the level Cyclin E1; and pharmaceutical compositions comprising such compounds. These compounds are useful in the treatment of proliferative disorders, such as cancer.
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 405/14 - 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 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
A61P 25/00 - Drugs for disorders of the nervous system
A61K 31/45 - Non-condensed piperidines, e.g. piperocaine having oxo groups directly attached to the heterocyclic ring, e.g. cycloheximide
The disclosure provides a novel flush method using a recovery flush technique that minimizes yield losses due to inadequate flushing and prevents or reduces dilution of a target protein during a recovery flush.
C07K 1/34 - ExtractionSeparationPurification by filtration, ultrafiltration or reverse osmosis
C07K 16/24 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against cytokines, lymphokines or interferons
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
42.
MODULATORS OF BCL6 FOR USE IN A METHOD OF TREATING A CANCER OR AN AUTOIMMUNE DISEASE
Provided herein are compounds and compositions thereof for modulating BCL6. In some embodiments, the compounds and compositions are provided for treatment of cancer or an autoimmune disease. In some embodiments, the compounds are of Formula (IA):
The present invention relates to assays for monitoring and measuring the binding of a drug of interest to a receptor. In this assay, a blood sample collected from a subject dosed with the compound of interest is incubated with a lysis solution containing a quencher. The drug bound and quencher bound receptor is then isolated from the lysed blood sample. The isolated drug bound and quencher bound receptor is digested to generate surrogate drug bound and quencher bound peptides. The amount of surrogate peptides is determined. Receptor occupancy can be determined by comparing the amount of drug bound surrogate peptide to the total of drug bound and quencher bound surrogate peptide.
Disclosed are compounds of Formula (I):
Disclosed are compounds of Formula (I):
Disclosed are compounds of Formula (I):
or stereoisomers, tautomers, or salts thereof, wherein:
R is
Disclosed are compounds of Formula (I):
or stereoisomers, tautomers, or salts thereof, wherein:
R is
Disclosed are compounds of Formula (I):
or stereoisomers, tautomers, or salts thereof, wherein:
R is
and Ring A, L, R1, R2, R3, m, and n are defined herein. Also disclosed are methods of using such compounds to decrease the level Cyclin E1; and pharmaceutical compositions comprising such compounds. These compounds are useful in the treatment of proliferative disorders, such as cancer.
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 31/454 - 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 31/5377 - 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
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
C07D 405/14 - 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 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
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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
Disclosed are compounds of Formula (I): (I) or stereoisomers, tautomers, or salts thereof, wherein R is defined herein. Also disclosed are methods of using such compounds to decrease the levels of Ikaros protein, Helios protein, Aiolos protein, and Eos protein; and pharmaceutical compositions comprising such compounds. These compounds are useful in the treatment of viral infections and proliferative disorders, such as cancer.
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 491/052 - Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being six-membered
A61K 31/4355 - 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 oxygen as a ring hetero atom
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
Compounds having formula (I)-(IX), and enantiomers, and diastereomers, stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, are useful as kinase modulators, including RIPK1 modulation. All the variables are as defined herein.
Compounds having formula (I)-(IX), and enantiomers, and diastereomers, stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, are useful as kinase modulators, including RIPK1 modulation. All the variables are as defined herein.
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There are disclosed compounds of the following formula (I): or a stereoisomer or pharmaceutically acceptable salt thereof, wherein all substituents are as defined herein, which are useful in the modulation of IL-12, IL-23 and/or IFNα, by acting on Tyk-2 to cause signal transduction inhibition. The compounds of the invention may be useful for treating neurodegenerative diseases or disorders.
There are disclosed compounds of the following formula (I): or a stereoisomer or pharmaceutically acceptable salt thereof, wherein all substituents are as defined herein, which are useful in the modulation of IL-12, IL-23 and/or IFNα, by acting on Tyk-2 to cause signal transduction inhibition. The compounds of the invention may be useful for treating neurodegenerative diseases or disorders.
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
A61K 31/501 - PyridazinesHydrogenated pyridazines not condensed and containing further heterocyclic rings
67.
BENZOTHIAZOLE, BENZOISOXAZOLE, AND BENZODIOXOLE ANALOGS AS RXFP1 RECEPTOR AGONISTS
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).
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 31/357 - 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 31/397 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
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 31/422 - Oxazoles not condensed and containing further heterocyclic rings
A61K 31/423 - Oxazoles condensed with carbocyclic rings
A61K 31/424 - Oxazoles condensed with heterocyclic ring systems, e.g. clavulanic acid
A61K 31/428 - Thiazoles condensed with carbocyclic rings
A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
A61K 31/438 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring being spiro-condensed with carbocyclic or heterocyclic ring systems
A61K 31/443 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
A61K 31/4525 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
A61K 31/4725 - Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
A61K 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
A61K 31/675 - Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
C07D 261/20 - Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings condensed with carbocyclic rings or ring systems
C07D 317/48 - Methylenedioxybenzenes or hydrogenated methylenedioxybenzenes, unsubstituted 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 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
C07F 9/6558 - Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
68.
COMPOSITIONS COMPRISING ANTIBODIES THAT BIND BCMA AND CD3 AND METHODS OF TREATMENT
Provided herein are compositions comprising multispecific (e.g. bispecific) antibodies that bind to CD3 and BCMA, such as alnuctamab, and methods of using such compositions to treat a patient having a disorder associated with BCMA expression (e.g. BCMA-expressing B-cell cancers, such as multiple myeloma).
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
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
NN-hydroxysulfonamide compounds, pharmaceutical compositions and kits comprising such co-crystals, and methods of using such co-crystals or pharmaceutical compositions comprising them. In particular, the disclosed subject matter provides methods of using such co-crystals or pharmaceutical compositions for treating heart failure.
C07D 207/16 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 261/10 - 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 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
C07C 311/00 - Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
A61P 9/00 - Drugs for disorders of the cardiovascular system
A61K 31/381 - Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
A61K 31/401 - ProlineDerivatives thereof, e.g. captopril
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
The disclosure provides a method for treating a subject afflicted with a tumor, e.g., lung cancer, having a high tumor mutation burden (TMB) status comprising administering to the subject an immunotherapy, e.g., an anti-PD-I antibody or antigen-binding portion thereof. The present disclosure also provides a method for identifying a subject suitable for an immunotherapy, e.g., a treatment with an anti-PD-I antibody or antigen-binding portion thereof, comprising measuring a TMB status of a biological sample of the subject. A high TMB status identifies the patient as suitable for treatment with an anti-PD-I antibody or antigen-binding portion thereof. The TMB status can be determined by sequencing nucleic acids in the tumor and identifying a genomic alteration, e.g., a somatic nonsynonymous mutation, in the sequenced nucleic acids.
C12Q 1/6886 - Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes for diseases caused by alterations of genetic material for cancer
71.
CERAMIC HYDROXYAPATITE CHROMATOGRAPHY FLOW THROUGH METHOD
The present disclosure is directed methods of isolating and/or purifying a protein in a ceramic hydroxyapatite chromatography in a flow-through mode, comprising loading a sample comprising the protein and one or more impurities on a CHT columns in a flow-through mode.
B01D 15/08 - Selective adsorption, e.g. chromatography
B01J 20/04 - Solid sorbent compositions or filter aid compositionsSorbents for chromatographyProcesses for preparing, regenerating or reactivating thereof comprising inorganic material comprising compounds of alkali metals, alkaline earth metals or magnesium
C07K 1/16 - ExtractionSeparationPurification by chromatography
B01D 15/32 - Bonded phase chromatography, e.g. with normal bonded phase, reversed phase or hydrophobic interaction
B01D 15/36 - Selective adsorption, e.g. chromatography characterised by the separation mechanism involving ionic interaction, e.g. ion-exchange, ion-pair, ion-suppression or ion-exclusion
B01D 15/38 - Selective adsorption, e.g. chromatography characterised by the separation mechanism involving specific interaction not covered by one or more of groups , e.g. affinity, ligand exchange or chiral chromatography
The present invention relates to radiolabeled LPA1 receptor antagonists of Formula (I):
The present invention relates to radiolabeled LPA1 receptor antagonists of Formula (I):
The present invention relates to radiolabeled LPA1 receptor antagonists of Formula (I):
or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein, which are useful for the quantitative imaging of LPA1 receptors in mammals.
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
73.
CARBAMOYLOXYMETHYL TRIAZOLE CYCLOHEXYL ACIDS AS LPA ANTAGONISTS
The present invention provides compounds of Formula (I):
The present invention provides compounds of Formula (I):
The present invention provides compounds of Formula (I):
or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein all the variables are as defined herein. These compounds are selective LPA receptor inhibitors.
A61K 31/27 - Esters, e.g. nitroglycerine, selenocyanates of carbamic or thiocarbamic acids, e.g. meprobamate, carbachol, neostigmine
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 31/454 - 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
C07C 62/10 - Saturated compounds containing ether groups, groups, groups, or groups with a six-membered ring
C07D 249/06 - 1,2,3-TriazolesHydrogenated 1,2,3-triazoles with aryl radicals directly attached to ring atoms
C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
C07D 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
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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; 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
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 31/423 - Oxazoles condensed with carbocyclic rings
A61K 31/27 - Esters, e.g. nitroglycerine, selenocyanates of carbamic or thiocarbamic acids, e.g. meprobamate, carbachol, neostigmine
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
C07D 261/04 - Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
C07D 261/20 - Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings condensed with carbocyclic rings or ring systems
91.
SYSTEMS AND METHODS OF SELECTING COMPOUNDS THAT INDUCE CONFORMATIONAL CHANGES IN MUTANT CEREBLON
Provided herein are systems and methods for screening and analyzing compounds based upon the elucidation of the interaction among cereblon, its substrates and certain compounds or agents. As an example, a system and method can include a computational model that mimics in silico the cereblon protein. Also provided herein are systems and methods for identifying a compound that induces a conformational change in Cereblon, and in particular P98A mutant cereblon.
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
The present disclosure provides compositions and methods of inactivating a lipid enveloped virus in a product feedstream in a manufacturing process of a therapeutic protein using environmentally compatible detergents. The present disclosure provides a detergent mixture comprising two environmentally sustainable detergents: n-Octyl-β-D-Glucopyranoside (OG) and n-Dodecyl-β-D-Maltopyranoside (DDM). The performance of this OG:DDM detergent combination is superior to that of Lauryldimethylamine Oxide (LDAO), ECOSURF™ EH9, or Triton X-100 in the purification of therapeutic proteins such as abatacept and belatacept. OG:DDM combinations are highly effective for viral inactivation, while having essentially no impact on protein stability, protein charge distribution (e.g., sialic acid levels), impurity clearance, protein deamination, or protein oxidation. Accordingly, combinations of OG and DDM can be used as substitutes of Triton X-100 for viral inactivation steps in the production of biologics.
A01N 43/16 - Biocides, pest repellants or attractants, or plant growth regulators containing heterocyclic compounds having rings with one or more oxygen or sulfur atoms as the only ring hetero atom with one hetero atom six-membered rings with oxygen as the ring hetero atom
A01P 1/00 - DisinfectantsAntimicrobial compounds or mixtures thereof
A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
The invention provides a method of treating a tumor in a human patient comprising (i) identifying a patient as having a LAG-3 positive tumor and (ii) administering to the patient a PD-1 pathway inhibitor, a combination of a PD1 pathway inhibitor and an immune checkpoint inhibitor, a combination of a LAG-3 inhibitor and a PD-1 pathway inhibitor, or an anti-CTLA4 antibody. In some embodiments, the method further comprises identifying the patient as having a LAG-3 positive PD-L1 positive tumor. In some embodiments, the LAG-3 inhibitor is an anti-LAG-3 antibody and the PD-1 pathway inhibitor is an anti-PD-1 antibody. The methods of the invention can improve response rates to treatment with a PD-1 pathway inhibitor, a combination of a PD1 pathway inhibitor and an immune checkpoint inhibitor, or a combination of a LAG-3 inhibitor and a PD-1 pathway inhibitor.
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
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
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
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
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
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
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
