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
(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; Radiopharmaceutical preparations for the treatment of cancer and solid tumors; Diagnostic radiopharmaceutical preparations; Diagnostic preparations for medical purposes.
(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; Radiopharmaceutical preparations for the treatment of cancer and solid tumors; Diagnostic radiopharmaceutical preparations; Diagnostic preparations for medical purposes.
(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; Radiopharmaceutical preparations for the treatment of cancer and solid tumors; Diagnostic radiopharmaceutical preparations; Diagnostic preparations for medical purposes.
(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; Radiopharmaceutical preparations for the treatment of cancer and solid tumors; Diagnostic radiopharmaceutical preparations; Diagnostic preparations for medical purposes.
(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; Radiopharmaceutical preparations for the treatment of cancer and solid tumors; Diagnostic radiopharmaceutical preparations; Diagnostic preparations for medical purposes.
(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; Radiopharmaceutical preparations for the treatment of cancer and solid tumors; Diagnostic radiopharmaceutical preparations; Diagnostic preparations for medical purposes.
8.
2,3-DIHYDROBENZO[B][1,4]DIOXIN-6-YL CONTAINING COMPOUNDS USEFUL AS IMMUNOMODULATORS
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
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
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
11.
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
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
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
The present disclosure is directed methods of isolating and/or purifying a species of a protein, comprising contacting a mixture comprising the species and one or more impurities with two or more chromatography columns in a continuous operation mode. In some aspects, the species of the protein is a charge variant.
Provided herein are compounds and compositions thereof that reduce WEE1 kinase protein levels. In some embodiments, the compounds and compositions are provided for treatment WEE1 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
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 31/4709 - Non-condensed quinolines containing further heterocyclic rings
A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
A61K 31/4725 - Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
A61K 31/5386 - 1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
A61K 31/499 - Spiro-condensed pyrazines or piperazines
A61K 31/4375 - 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 six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 31/498 - Pyrazines or piperazines ortho- or peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
39.
LEVERAGING LARGE LANGUAGE MODELS FOR AUTOMATING LINES OF THERAPY ADJUDICATION IN CANCER PATIENTS
A method (500) includes receiving natural language input text (116) characterizing clinical data (102) for a patient. The method also includes receiving a prompt composition (300) that includes adjudication rules (300a) for performing lines of therapy adjudication and an instruction parameter (300b) that specifies a task for a LLM (160) to synthesize a group of multiple synthetic experts (400) that each use the adjudication rules to perform chain-of-thought reasoning for making lines of therapy (LoT) adjudication decisions. The method also includes structuring an adjudication prompt (155) by concatenating the prompt composition to the natural language input text, processing, using the LLM, the adjudication prompt to cause the LLM to synthesize the group of multiple synthetic experts and generate a respective group answer (480). The method also includes determining a final answer (180) based on the respective group answer generated from the group of multiple synthetic experts.
G16H 15/00 - ICT specially adapted for medical reports, e.g. generation or transmission thereof
G16H 10/60 - ICT specially adapted for the handling or processing of patient-related medical or healthcare data for patient-specific data, e.g. for electronic patient records
G16H 50/70 - ICT specially adapted for medical diagnosis, medical simulation or medical data miningICT specially adapted for detecting, monitoring or modelling epidemics or pandemics for mining of medical data, e.g. analysing previous cases of other patients
Provided are novel antibodies and antigen-binding fragments thereof that bind interleukin-18 receptor beta (IL-18RP), 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
A61P 1/00 - Drugs for disorders of the alimentary tract or the digestive system
A61K 39/00 - Medicinal preparations containing antigens or antibodies
41.
ANTI-LAG-3 ANTIBODIES TO TREAT HEMATOLOGICAL MALIGNANCIES
Provided are methods for clinical treatment of hematological malignancies, such as relapsed or refractory chronic lymphocytic leukemia or lymphoma using an anti-LAG-3 antibody. Particular malignancies include, e.g., chronic lymphocytic leukemia (CLL), Hodgkin lymphoma (HL), or non-Hodgkin lymphoma (NHL).
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
Provided herein are compounds and compositions thereof that reduce WEE1 kinase protein levels. In some embodiments, the compounds and compositions are provided for treatment WEE1 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 31/4709 - Non-condensed quinolines containing further heterocyclic rings
A61K 31/4725 - Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
A61K 31/498 - Pyrazines or piperazines ortho- or peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
A61K 31/499 - Spiro-condensed pyrazines or piperazines
A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
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 31/5386 - 1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
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 491/048 - Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
A method includes receiving natural language input text characterizing clinical data for a patient. The method also includes receiving a prompt composition that includes adjudication rules for performing lines of therapy adjudication and an instruction parameter that specifies a task for a LLM to synthesize a group of multiple synthetic experts that each use the adjudication rules to perform chain-of-thought reasoning for making lines of therapy (LoT) adjudication decisions. The method also includes structuring an adjudication prompt by concatenating the prompt composition to the natural language input text, processing, using the LLM, the adjudication prompt to cause the LLM to synthesize the group of multiple synthetic experts and generate a respective group answer. The method also includes determining a final answer based on the respective group answer generated from the group of multiple synthetic experts.
G16H 20/10 - ICT specially adapted for therapies or health-improving plans, e.g. for handling prescriptions, for steering therapy or for monitoring patient compliance relating to drugs or medications, e.g. for ensuring correct administration to patients
G16H 10/60 - ICT specially adapted for the handling or processing of patient-related medical or healthcare data for patient-specific data, e.g. for electronic patient records
G16H 15/00 - ICT specially adapted for medical reports, e.g. generation or transmission thereof
44.
METHODS OF TREATING CANCER WITH ANTIBODIES AGAINST TIM3
This disclosure provides a method for treating a subject afflicted with a tumor or a cancer, wherein the method comprises administering to the subject therapeutically effective amounts of an anti-TIM3 antibody, alone or in combination with an inhibitor of the PD-1 signaling pathway (e.g., anti-PD-1 antibody). In some embodiments, the antibody is administered as a flat dose or a weight-based dose.
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
C07H 21/00 - Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids
C07H 1/00 - Processes for the preparation of sugar derivatives
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
The present disclosure provide novel methods of large-scale production of recombinant proteins, e.g., therapeutic proteins such as antibodies, comprising concentrating an eukaryotic cell culture to a high density and transiently transfecting the eukaryotic cells with a polynucleotide encoding the recombinant protein using electroporation, e.g., flow electroporation. In some aspects, the culture is performed under perfusion conditions using, e.g., a tangential flow filtration method such as alternating tangential flow filtration. The proteins obtained using the disclosed methods are comparable to those produced using stable transfection. The methods disclosed herein can be used, for example, to accelerate therapeutic agent development, to reduce host cell toxicity, or for individualized therapeutics such as small scale manufacturing of treatments for rare or orphan diseases.
The present disclosure relates to antisense oligonucleotides, which target SNCA mRNA (e.g., at an intron exon junction) in a cell, leading to reduced expression of SNCA protein. Reduction of SNCA protein expression is beneficial for the treatment of certain medical disorders, e.g., a neurological disorder.
Disclosed are compounds of Formulas (I): (Formulas (I)) or a salt thereof, wherein X, Y, Q, G, R1, and R5a are defined herein. Also disclosed are methods of using such compounds as inhibitors of TLR9, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing fibrotic diseases.
Disclosed are compounds of Formulas (I): (Formulas (I)) or a salt thereof, wherein X, Y, Q, G, R1, and R5a are defined herein. Also disclosed are methods of using such compounds as inhibitors of TLR9, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing fibrotic diseases.
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 31/4545 - 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 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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
The invention provides a method of treating a colorectal carcinoma with a combination of an anti-LAG-3 antibody and an anti-PD-1 or anti-PD-L1 antibody. In some aspects, the combination comprises 480 mg of each antibody such as, for example, 480 mg of an anti-LAG-3 antibody (e.g, relatlimab) and 480 mg of an anti-PD-1 antibody (e.g, nivolumab). In some aspects, the colorectal carcinoma is unresectable, advanced, or metastatic, including, for example, microsatellite stable or high microsatellite instable colorectal carcinoma.
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 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
51.
INTERLEUKIN-2/INTERLEUKIN-2 RECEPTOR ALPHA FUSION PROTEINS AND METHODS OF USE
Disclosed herein are fusion proteins comprising: (a) a first polypeptide comprising Interleukin-2 (IL2); and (b) a second polypeptide, fused in frame to the first polypeptide, wherein the second polypeptide comprises an extracellular domain of Interleukin-2 Receptor alpha (IL2Rα), wherein IL2 or IL2Rα comprises at least one fewer glycosylation site compared to native IL2 or native IL2Rα. Methods of production and methods of therapeutic use of the fusion proteins are also disclosed.
A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
C07K 14/715 - ReceptorsCell surface antigensCell surface determinants for cytokinesReceptorsCell surface antigensCell surface determinants for lymphokinesReceptorsCell surface antigensCell surface determinants for 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
C12N 15/62 - DNA sequences coding for fusion proteins
A computer-implemented method includes receiving multidimensional medical data (110) for a patient (10), extracting features from the multidimensional medical data, and processing, using one or more ML medical prognosis models (200), the features to predict a probability of experiencing a progression of HCM by a threshold date. The one or more models trained using a training process including, for each of a plurality of patients, obtaining corresponding baseline training data (810) comprising baseline multidimensional medical data spanning multiple different modalities, and obtaining corresponding follow-up training data (810) including follow-up multidimensional medical data (110) spanning multiple different modalities and collected after the baseline training data and a corresponding ground-truth clinical outcome (818). The training process including training the one or more models on the baseline training data and the follow-up training data to teach the one or more models to learn how to predict the corresponding ground-truth clinical outcomes.
G16H 50/20 - ICT specially adapted for medical diagnosis, medical simulation or medical data miningICT specially adapted for detecting, monitoring or modelling epidemics or pandemics for computer-aided diagnosis, e.g. based on medical expert systems
G16H 50/30 - ICT specially adapted for medical diagnosis, medical simulation or medical data miningICT specially adapted for detecting, monitoring or modelling epidemics or pandemics for calculating health indicesICT specially adapted for medical diagnosis, medical simulation or medical data miningICT specially adapted for detecting, monitoring or modelling epidemics or pandemics for individual health risk assessment
G16H 50/70 - ICT specially adapted for medical diagnosis, medical simulation or medical data miningICT specially adapted for detecting, monitoring or modelling epidemics or pandemics for mining of medical data, e.g. analysing previous cases of other patients
61.
TIM-3 ANTAGONISTS FOR THE TREATMENT AND DIAGNOSIS OF CANCERS
Provided herein are methods for treating a subject afflicted with a cancer, comprising administering to the subject a TIM3 agonist (e.g., an anti-TIM3 antibody), alone or in conjunction with another immune checkpoint inhibitor (e.g., a PD-1 antagonist), wherein the subject is identified as having a high frequency of TIM3 positive cells (e.g., on the tumor infiltrating inflammatory cells) or soluble TIM3 in peripheral blood. Also provided are methods for assessing the efficacy of a treatment comprising a TIM3 antagonist in a subject afflicted with a cancer, comprising measuring the frequency of TIM3 (and optionally PD-1) positive cells in certain populations of cells and/or the soluble TIM3 in peripheral blood of the subject, wherein a high frequency of TIM3 (and optionally PD-1) positive cells and/or the subject's peripheral blood titer of soluble TIM3 is indicative of the response to the treatment.
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
G01N 33/50 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing
G01N 33/68 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing involving proteins, peptides or amino acids
62.
Machine-Learning Models for Prognosing Outcomes For Hypertrophic Cardiomyopathy (HCM)
A computer-implemented method includes receiving, from one or more sources, multidimensional medical data for a patient, extracting features from the multidimensional medical data, and processing, using one or more ML medical prognosis models, the features to predict a probability of experiencing a progression of HCM by a threshold date. The one or more models trained using a training process including, for each of a plurality of patients, obtaining corresponding baseline training data comprising baseline multidimensional medical data spanning multiple different modalities, and obtaining corresponding follow-up training data including follow-up multidimensional medical data spanning multiple different modalities and collected after the baseline training data and a corresponding ground-truth clinical outcome. The training process including training the one or more models on the baseline training data and the follow-up training data to teach the one or more models to learn how to predict the corresponding ground-truth clinical outcomes.
G16H 50/20 - ICT specially adapted for medical diagnosis, medical simulation or medical data miningICT specially adapted for detecting, monitoring or modelling epidemics or pandemics for computer-aided diagnosis, e.g. based on medical expert systems
G16H 10/60 - ICT specially adapted for the handling or processing of patient-related medical or healthcare data for patient-specific data, e.g. for electronic patient records
In certain embodiments, this disclosure provides novel methods of increasing the viable cell density of an N-1 large-scale bioreactor cell culture, comprising culturing a host cell expressing a recombinant poly peptide of interest in a non-perfusion-based culture system, and wherein the viable cell density is increased to at least 5×106 cells/mL. In certain embodiments, the disclosure provides novel methods for large-scale production of a recombinant polypeptide of interest, comprising: (1) culturing a host cell expressing a recombinant polypeptide of interest in an N-1 stage in a non-perfusion-based culture system, wherein the viable cell density is increased to at least 5×106 cells/mL: and (2) culturing N fed-batch production cells in an enriched media with high-seed density at least 1.5×106 cells/mL, wherein the N fed-batch production cells are inoculated from the N-1 stage in a non-perfusion-based culture system.
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 31/538 - 1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring systems
A61K 31/5386 - 1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
A61K 31/553 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and at least one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
A61K 31/554 - 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 sulfur as ring hetero atoms, e.g. clothiapine, diltiazem
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
65.
SUBSTITUTED BICYCLIC HETEROARYL COMPOUNDS USEFUL AS INHIBITORS OF TLR9
Disclosed are compounds of Formulas (I) or a salt thereof, wherein Q, G, R1, R5,a, and R5b are defined herein. Also disclosed are methods of using such compounds as inhibitors of TLR9, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing fibrotic diseases.
Disclosed are compounds of Formulas (I) or a salt thereof, wherein Q, G, R1, R5,a, and R5b are defined herein. Also disclosed are methods of using such compounds as inhibitors of TLR9, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing fibrotic diseases.
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 31/4545 - 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
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
66.
2-(4-(2-(7,8-DIMETHYL-[L,2,4JTRIAZOLO[L,5-A]PYRIDIN-6-YL)-3-ISOPROPYL- LH-INDOL-5-YL)PIPERID!N-L-YL)ACETAMIDE AND CRYSTALLINE FORMS THEREOF
Disclosed are a free base hemihydrate and free base anhydrates 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, and crystalline forms thereof.
In accordance with the present disclosure, macrocyclic compounds have been discovered that bind to PD-I and are capable of inhibiting the interaction of PD-I with PD-LI. These macrocyclic compounds exhibit in vitro immunomodulatory efficacy thus making them therapeutic candidates for the treatment 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
There are disclosed compounds of the following formula I:
There are disclosed compounds of the following formula I:
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.
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
69.
COMPOSITIONS COMPRISING A COMBINATION OF AN ANTI-LAG-3 ANTIBODY, A PD-1 PATHWAY INHIBITOR, AND AN IMMUNOTHERAPEUTIC AGENT
Provided are methods for clinical treatment of malignant tumors (e.g., advanced solid tumors) using a combination of an anti-LAG-3 antibody, an anti-PD-1 antibody, and an immunotherapeutic 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 39/00 - Medicinal preparations containing antigens or antibodies
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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
70.
Compounds and Their Use for Treatment of Hemoglobinopathies
Disclosed herein are compounds and methods for the prevention and/or treatment of hemoglobinopathies. Also provided herein are such compounds for use in such methods. Also disclosed herein are pharmaceutical compositions comprising such compounds for use in such methods of preventing or treating hemoglobinopathies.
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
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 31/4709 - Non-condensed quinolines containing further heterocyclic rings
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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 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 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
C07D 417/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
71.
COMBINATION OF ANTI-LAG-3 ANTIBODIES AND ANTI-PD-1 ANTIBODIES TO TREAT TUMORS
Provided are methods for clinical treatment of tumors (e.g., advanced solid tumors) using an anti-LAG-3 antibody in combination with an anti-PD-1 antibody.
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 are salts 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 and crystalline forms thereof.
This invention provides methods for treating cancer in a subject comprising administering to the subject an anti-PD-1 antibody and an anti-CD27 antibody. In some embodiments, the cancer is colorectal cancer, rectal cancer, colon cancer, lung cancer, melanoma, ovarian cancer, head and neck cancer, or any combination 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
A61K 39/395 - AntibodiesImmunoglobulinsImmune serum, e.g. antilymphocytic serum
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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
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
This disclosure provides a method for treating a subject afflicted with a urothelial carcinoma or cancer derived therefrom, which method comprises administering to the subject an antibody or an antigen-binding portion thereof that specifically binds to a Programmed Death-1 (PD-1) receptor and inhibits PD-1 activity or the combination of (a) an antibody or an antigen-binding portion thereof that specifically binds to a PD-1 receptor and inhibits PD-1 activity; and (b) an antibody or an antigen-binding portion thereof that specifically binds to a Cytotoxic T-Lymphocyte Antigen-4 (CTLA-4) and inhibits CTLA-4 activity.
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
This provides pharmaceutical compositions that comprise (i) an anti-LAG-3 antibody or antigen binding fragment thereof or (ii) an anti-LAG-3 antibody or antigen binding fragment thereof and an anti-PD-1 antibody, anti-PD-L1 antibody, or antigen binding fragment thereof. Also provided are pharmaceutical compositions that comprise a buffering agent, stabilizing or bulking agent, and a surfactant. The disclosure also provides a vial, syringe, intravenous bag, or kit that comprises the compositions, and methods for using the compositions.
A61K 47/12 - Carboxylic acidsSalts or anhydrides thereof
A61K 47/18 - AminesAmidesUreasQuaternary ammonium compoundsAmino acidsOligopeptides having up to five amino acids
A61K 47/22 - Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
A61K 47/26 - Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharidesDerivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
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
77.
CRYSTAL FORM OF 6-(CYCLOPROPANECARBOXAMIDO)-4-((2-METHOXY-3-(1-METHYL-1H-1,2,4-TRIAZOL-3-YL)PHENYL)AMINO)-N-(METHYL-D3)PYRIDAZINE-3-CARBOXAMIDE
Disclosed is crystalline Form E of 6-(cyclopropanecarboxamido)-4-((2-methoxy-3-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl) amino)-N-(methyl-d3)pyridazine-3-carboxamide. Form E is a neat crystalline form. Characterization data for Form E are disclosed.
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
78.
METHODS TO MANIPULATE QUALITY ATTRIBUTES OF POLYPEPTIDES PRODUCED IN CHO CELLS
In accordance with the present invention, CHO cells expressing a recombinant polypeptide of interest are grown in media where the amino acids, vitamins, phosphate, lipids and/or antioxidant optimization is utilized to manipulate and/or control the protein quality attributes of the polypeptides. Polypeptides expressed in accordance with the present invention may be advantageously used in the preparation of pharmaceutical compositions.
This disclosure provides a method for treating a subject afflicted with a lung cancer, which method comprises administering to the subject therapeutically effective amounts of: (a) 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) an antibody or an antigen-binding portion thereof that specifically binds to a Cytotoxic T-Lymphocyte Antigen-4 (CTLA-4) and inhibits CTLA-4 activity.
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
This invention relates to methods for predicting a prognosis of a patient with cancer in need of an anti-cancer treatment comprising measuring a cytokine score from a sample obtained from the patient. In some embodiments, the subject is administered an anti-cancer treatment, e.g., an anti-PD-1 antibody, following the cytokine score measurement. In some embodiments, the cancer is lung cancer.
G01N 33/68 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing involving proteins, peptides or amino acids
C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
G01N 33/574 - ImmunoassayBiospecific binding assayMaterials therefor for cancer
81.
METHODS OF TREATING A TUMOR USING AN ANTI-PD-1 ANTIBODY
This disclosure provides a method for treating a subject afflicted with tumor, which method comprises administering to the subject an antibody or an antigen-binding portion thereof that specifically binds to a Programmed Death-1 (PD-1) receptor and inhibits PD-1 activity. In some embodiments, the tumor is derived from a non-small cell lung cancer (NSCLC). In some embodiments, the tumor expresses Programmed Death Ligand 1. In some embodiments, the subject carries a wild-type STK11 gene.
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
Compounds having the following formula (I) or a stereoisomer or pharmaceutically-acceptable salt thereof, where all substituents are as defined herein, are inhibitors of USP1 useful for treating diseases including, among others, treating proliferative, metabolic, allergic, autoimmune and inflammatory diseases. (Formula (I))
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
83.
UBIQUITIN SPECIFIC PROCESSING PROTEASE 1 (USP1) COMPOUNDS
Compounds having the following formula (I) or a stereoisomer or pharmaceutically-acceptable salt thereof, where all substituents are as defined herein, are inhibitors of USP1 useful for treating diseases including, among others, treating proliferative, metabolic, allergic, autoimmune and inflammatory diseases.
A61P 35/02 - Antineoplastic agents specific for leukemia
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
84.
UBIQUITIN SPECIFIC PROCESSING PROTEASE 1 (USP1) COMPOUNDS
Compounds having the following formula I or a stereoisomer or pharmaceutically acceptable salt thereof, where all substituents are as defined herein, are inhibitors of USP1 useful for treating diseases including, among others, treating proliferative, metabolic, allergic, autoimmune and inflammatory diseases.
A61P 35/02 - Antineoplastic agents specific for leukemia
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 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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 a particular embodiment, the compounds are of Formula (I):, wherein values for the variables are as described herein.
C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
Provided herein 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 a particular embodiment, the compounds are of Formula (I):, wherein values for the variables are as described herein.
A61P 37/00 - Drugs for immunological or allergic disorders
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
C07D 411/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms containing three or more hetero rings
C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
Methods of treatment with a myosin inhibitor using protein levels; methods of monitoring response to treatment based on such protein levels; and methods of determining whether to treat a patient with a myosin inhibitor based on such protein levels are described herein. Such methods may include obtaining a biological sample of a subject, measuring one or more protein levels in the sample, analyzing the one or more protein levels, and determining the treatment response based on the analysis, and may further include treating the subject based on the determination of treatment response.
Disclosed are macrocyclic peptide compounds or a salt thereof, which are useful as modulators of TNFα, and pharmaceutical compositions comprising such compounds. These compounds may be useful in treating cancers, inflammatory and autoimmune 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
This disclosure provides methods for treating a subject afflicted with a tumor derived from a renal cell carcinoma. The methods comprise administering a first dose to a subject of an anti-PD-1 antibody or antigen-binding portion thereof and/or an anti-PD-L1 antibody or antigen-binding portion thereof, and administering a second dose to the subject, wherein the subject exhibited differential expression in one or more biomarker genes, e.g., CTLA-4, TIGIT, and/or PD-L2, following administration of the first dose.
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
A61P 1/00 - Drugs for disorders of the alimentary tract or the digestive system
A61P 31/00 - Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
Compounds having the following formula I or a stereoisomer or pharmaceutically-acceptable salt thereof, where all substituents are as defined herein, are inhibitors of USP1 useful for treating diseases including, among others, treating proliferative, metabolic, allergic, autoimmune and inflammatory diseases.
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 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
91.
UBIQUITIN SPECIFIC PROCESSING PROTEASE 1 (USP1) COMPOUNDS
Compounds having the following formula (I) or a stereoisomer or pharmaceutically-acceptable salt thereof, where all substituents are as defined herein, are inhibitors of USP1 useful for treating diseases including, among others, treating proliferative, metabolic, allergic, autoimmune and inflammatory diseases.
Compounds having the following formula I or a stereoisomer or pharmaceutically-acceptable salt thereof, where all substituents are as defined herein, are inhibitors of USP1 useful for treating diseases including, among others, treating proliferative, metabolic, allergic, autoimmune and inflammatory diseases.
Compounds having the following formula (I) or a stereoisomer or pharmaceutically-acceptable salt thereof, where all substituents are as defined herein, are inhibitors of USP1 useful for treating diseases including, among others, treating proliferative, metabolic, allergic, autoimmune and inflammatory diseases.
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
Compounds having the following formula or a stereoisomer or pharmaceutically-acceptable salt thereof, where all substituents are as defined herein, are inhibitors of USP1 useful for treating diseases including, among others, treating proliferative, metabolic, allergic, autoimmune and inflammatory diseases: formula (I)
A61P 35/02 - Antineoplastic agents specific for leukemia
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 403/10 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing aromatic rings
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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.
A61K 31/435 - 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
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
