AR110368A1 - Inhibidores de la rip1 cinasa y métodos y uso de éstos - Google Patents

Inhibidores de la rip1 cinasa y métodos y uso de éstos

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Publication number
AR110368A1
AR110368A1 ARP170103503A ARP170103503A AR110368A1 AR 110368 A1 AR110368 A1 AR 110368A1 AR P170103503 A ARP170103503 A AR P170103503A AR P170103503 A ARP170103503 A AR P170103503A AR 110368 A1 AR110368 A1 AR 110368A1
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Argentina
Prior art keywords
dihydro
carboxamide
oxo
triazol
methyl
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ARP170103503A
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English (en)
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Gregory Hamilton
Snahel Patel
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Hoffmann La Roche
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—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 C07D453/00 or C07D455/00

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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Urology & Nephrology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Neurosurgery (AREA)
  • Vascular Medicine (AREA)
  • Pulmonology (AREA)
  • Cardiology (AREA)
  • Neurology (AREA)
  • Dermatology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Biomedical Technology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Compuestos que tienen actividad inhibidora de la RIP1 cinasa, composiciones farmacéuticas que incluyen los compuestos y métodos para utilizar los compuestos. Reivindicación 1: Un compuesto seleccionado entre el grupo que comprende: (5R)-5-(1,1-difluoropropil)-N-[(3S)-7,9-difluoro-2-oxo-1,3,4,5-tetrahidro-1-benzazepin-3-il]-6,7-dihidro-5H-pirrolo[1,2-b][1,2,4]triazol-2-carboxamida; (4R)-4-fenil-N-[(3S)-5-metil-4-oxo-2,3-dihidro-1,5-benzoxazepin-3-il]-5,6-dihidro-4H-pirrolo[1,2-b]pirazol-2-carboxamida; rac-(5R,7S)-7-fluoro-5-fenil-N-[(3S)-5-metil-4-oxo-2,3-dihidro-1,5-benzoxazepin-3-il]-6,7-dihidro-5H-pirrolo[1,2-b][1,2,4]triazol-2-carboxamida; rac-(5R,7S)-7-fluoro-5-fenil-N-[(3S)-7,9-difluoro-2-oxo-1,3,4,5-tetrahidro-1-benzazepin-3-il]-6,7-dihidro-5H-pirrolo[1,2-b][1,2,4]triazol-2-carboxamida; (5R,7R)-7-fluoro-5-fenil-N-[(3S)-7,9-difluoro-2-oxo-1,3,4,5-tetrahidro-1-benzazepin-3-il]-6,7-dihidro-5H-pirrolo[1,2-b][1,2,4]triazol-2-carboxamida; 1-(2,2-difluoropropil)-N-[(3S)-5-metil-4-oxo-2,3-dihidro-1,5-benzoxazepin-3-il]pirazolo[3,4-d]pirimidina-6-carboxamida; 1-ciclopropil-N-[(3S)-5-metil-4-oxo-2,3-dihidro-1,5-benzoxazepin-3-il]pirazolo[3,4-d]pirimidina-6-carboxamida; (5R)-5-fenil-N-[(3S)-7-metoxi-1-metil-2-oxo-4,5-dihidro-3H-pirido[3,4-b]azepin-3-il]-6,7-dihidro-5H-pirrolo[1,2-b][1,2,4]triazol-2-carboxamida; (5R)-5-fenil-N-[(7S)-6-oxo-5,7,8,9-tetrahidropirido[3,2-b]azepin-7-il]-6,7-dihidro-5H-pirrolo[1,2-b][1,2,4]triazol-2-carboxamida; 5-(1,1-difluoropropil)-N-[(3S)-7,9-difluoro-2-oxo-1,3,4,5-tetrahidro-1-benzazepin-3-il]-6,7-dihidro-5H-pirrolo[1,2-b][1,2,4]triazol-2-carboxamida; rac-(5S,7S)-7-fluoro-5-fenil-N-[(3S)-5-metil-4-oxo-1 2,3-dihidro-1,5-benzoxazepin-3-il]-6,7-dihidro-5H-pirrolo[1,2-b][1,2,4]triazol-2-carboxamida; rac-(5S,7S)-7-fluoro-5-fenil-N-[(6S)-4-metil-5-oxo-7,8-dihidro-6H-pirazolo[1,5-a][1,3]diazepin-6-il]-6,7-dihidro-5H-pirrolo[1,2-b][1,2,4]triazol-2-carboxamida; (5S)-5-(2-fluorofenil)-N-[(3S)-7-metoxi-1-metil-2-oxo-4,5-dihidro-3H-pirido[3,4-b]azepin-3-il]-6,7-dihidro-5H-pirrolo[1,2-b][1,2,4]triazol-2-carboxamida; (5S)-5-(2-fluorofenil)-N-[(7S)-6-oxo-5,7,8,9-tetrahidropirido[3,2-b]azepin-7-il]-6,7-dihidro-5H-pirrolo[1,2-b][1,2,4]triazol-2-carboxamida; (5R)-5-(2-fluorofenil)-N-[(7S)-5-metil-6-oxo-8,9-dihidro-7H-pirido[3,2-b]azepin-7-il]-6,7-dihidro-5H-pirrolo[1,2-b][1,2,4]triazol-2-carboxamida; 4-fenil-N-[(3S)-5-metil-4-oxo-2,3-dihidro-1,5-benzoxazepin-3-il]-5,6-dihidro-4H-pirrolo[1,2-b]pirazol-2-carboxamida; (4S)-4-fenil-N-[(3S)-5-metil-4-oxo-2,3-dihidro-1,5-benzoxazepin-3-il]-6,7-dihidro-4H-pirazolo[5,1-c][1,4]oxazina-2-carboxamida; 4-fenil-N-[(3S)-7,9-difluoro-2-oxo-1,3,4,5-tetrahidro-1-benzazepin-3-il]-6,7-dihidro-4H-pirazolo[5,1-c][1,4]oxazina-2-carboxamida; 1-(2,2-difluoropropil)-N-[(3S)-5-metil-4-oxo-2,3-dihidro-1,5-benzoxazepin-3-il]pirazolo[4,3-c]piridina-6-carboxamida; 1-ciclopropil-N-[(3S)-5-metil-4-oxo-2,3-dihidro-1,5-benzoxazepin-3-il]pirazolo[4,3-c]piridina-6-carboxamida; (7S)-7-(2-fluorofenil)-N-[(7S)-5-metil-6-oxo-8,9-dihidro-7H-pirido[3,2-b]azepin-7-il]-6,7-dihidro-5H-pirrolo[1,2-b][1,2,4]triazol-2-carboxamida; (7S)-7-fenil-N-[(7S)-5-metil-6-oxo-8,9-dihidro-7H-pirido[3,2-b]azepin-7-il]-6,7-dihidro-5H-pirrolo[1,2-b][1,2,4]triazol-2-carboxamida; (5S)-5-fenil-N-[(7S)-5-metil-6-oxo-8,9-dihidro-7H-pirido[3,2-b]azepin-7-il]-6,7-dihidro-5H-pirrolo[1,2-b][1,2,4]triazol-2-carboxamida; (5S,7R)-7-fluoro-5-fenil-N-[(3S)-7,9-difluoro-2-oxo-1,3,4,5-tetrahidro-1-benzazepin-3-il]-6,7-dihidro-5H-pirrolo[1,2-b][1,2,4]triazol-2-carboxamida; (5S,7R)-7-fluoro-5-fenil-N-[(3S)-5-metil-4-oxo-2,3-dihidro-1,5-benzoxazepin-3-il]-6,7-dihidro-5H-pirrolo[1,2-b][1,2,4]triazol-2-carboxamida; (5R,7S)-7-fluoro-5-fenil-N-[(6S)-2,4-dimetil-5-oxo-7,8-dihidro-6H-pirazolo[1,5-a][1,3]diazepin-6-il]-6,7-dihidro-5H-pirrolo[1,2-b][1,2,4]triazol-2-carboxamida; (5R,7S)-7-fluoro-5-fenil-N-[(6S)-4-metil-5-oxo-7,8-dihidro-6H-pirazolo[1,5-a][1,3]diazepin-6-il]-6,7-dihidro-5H-pirrolo[1,2-b][1,2,4]triazol-2-carboxamida; 4-fenil-N-[(3S)-5-metil-4-oxo-2,3-dihidro-1,5-benzoxazepin-3-il]-6,7-dihidro-4H-pirazolo[5,1-c][1,4]oxazina-2-carboxamida; 7,7-difluoro-5-fenil-N-[(3S)-7,9-difluoro-2-oxo-1,3,4,5-tetrahidro-1-benzazepin-3-il]-5,6-dihidropirrolo[1,2-b][1,2,4]triazol-2-carboxamida; 7,7-difluoro-5-fenil-N-[rac-(3S)-5-metil-4-oxo-2,3-dihidro-1,5-benzoxazepin-3-il]-5,6-dihidropirrolo[1,2-b][1,2,4]triazol-2-carboxamida; 7-fluoro-5-fenil-N-[rac-(3S)-7,9-difluoro-2-oxo-1,3,4,5-tetrahidro-1-benzazepin-3-il]-6,7-dihidro-5H-pirrolo[1,2-b][1,2,4]triazol-2-carboxamida; 7-fluoro-5-fenil-N-[rac-(3S)-5-metil-4-oxo-2,3-dihidro-1,5-benzoxazepin-3-il]-6,7-dihidro-5H-pirrolo[1,2-b][1,2,4]triazol-2-carboxamida; 7-fluoro-5-fenil-N-[(6S)-4-metil-5-oxo-7,8-dihidro-6H-pirazolo[1,5-a][1,3]diazepin-6-il]-6,7-dihidro-5H-pirrolo[1,2-b][1,2,4]triazol-2-carboxamida; (7S)-7-(2-fluorofenil)-N-[(6S)-4-metil-5-oxo-7,8-dihidro-6H-pirazolo[1,5-a][1,3]diazepin-6-il]-6,7-dihidro-5H-pirrolo[1,2-b][1,2,4]triazol-2-carboxamida; (7S)-7-(2-fluorofenil)-N-[(6S)-2,4-dimetil-5-oxo-7,8-dihidro-6H-pirazolo[1,5-a][1,3]diazepin-6-il]-6,7-dihidro-5H-pirrolo[1,2-b][1,2,4]triazol-2-carboxamida; 1-[(2-fluorofenil)metil]-N-[(6S)-2,4-dimetil-5-oxo-7,8-dihidro-6H-pirazolo[4,3-b]azepin-6-il]-1,2,4-triazol-3-carboxamida; 1-bencil-N-[(6S)-2,4-dimetil-5-oxo-7,8-dihidro-6H-pirazolo[4,3-b]azepin-6-il]-1,2,4-triazol-3-carboxamida; 1-[(2-fluorofenil)metil]-N-[(6S)-1,4-dimetil-5-oxo-7,8-dihidro-6H-pirazolo[4,3-b]azepin-6-il]-1,2,4-triazol-3-carboxamida; 1-bencil-N-[(6S)-1,4-dimetil-5-oxo-7,8-dihidro-6H-pirazolo[4,3-b][azepin-6-il]-1,2,4-triazol-3-carboxamida; 1-bencil-N-[rac-(6S)-4-metil-5-oxo-2-(tetrahidrofuran-3-ilmetil)-7,8-dihidro-6H-pirazolo[1,5-a][1,3]diazepin-6-il]-1,2,4-triazol-3-carboxamida; rac-(5S,7S)-7-fluoro-5-fenil-N-[rac-(6S)-4-metil-5-oxo-7,8-dihidro-6H-pirazolo[1,5-a][1,3]diazepin-6-il]-6,7-dihidro-5H-pirrolo[1,2-b][1,2,4]triazol-2-carboxamida; rac-(5S,7S)-7-fluoro-5-fenil-N-[rac-(6S)-2,4-dimetil-5-oxo-7,8-dihidro-6H-pirazolo[1,5-a][1,3]diazepin-6-il]-6,7-dihidro-5H-pirrolo[1,2-b][1,2,4]triazol-2-carboxamida; rac-(5S,7S)-7-fluoro-5-fenil-N-[rac-(3S)-5-metil-4-oxo-2,3-dihidro-1,5-benzoxazepin-3-il]-6,7-dihidro-5H-pirrolo[1,2-b][1,2,4]triazol-2-carboxamida; rac-(5R)-7,7-difluoro-5-fenil-N-[rac-(6S)-2,4-dimetil-5-oxo-7,8-dihidro-6H-pirazolo[1,5-a][1,3]diazepin-6-il]-5,6-dihidropirrolo[1,2-b][1,2,4]triazol-2-carboxamida; rac-(5R)-7,7-difluoro-5-fenil-N-[rac-(3S)-5-metil-4-oxo-2,3-dihidro-1,5-benzoxazepin-3-il]-5,6-dihidropirrolo[1,2-b][1,2,4]triazol-2-carboxamida; rac-(5R)-7,7-difluoro-5-fenil-N-[rac-(6S)-4-metil-5-oxo-7,8-dihidro-6H-pirazolo[1,5-a][1,3]diazepin-6-il]-5,6-dihidropirrolo[1,2-b][1,2,4]triazol-2-carboxamida; y 5-(1,1-difluoropropil)-N-[(3S)-5-metil-4-oxo-2,3-dihidro-1,5-benzoxazepin-3-il]-6,7-dihidro-5H-pirrolo[1,2-b][1,2,4]triazol-2-carboxamida; o un enantiómero de ellos o una sal farmacéuticamente aceptable de ellos.
ARP170103503A 2016-12-16 2017-12-14 Inhibidores de la rip1 cinasa y métodos y uso de éstos AR110368A1 (es)

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