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

Info

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
Authority
AR
Argentina
Prior art keywords
dihydro
carboxamide
oxo
triazol
methyl
Prior art date
Application number
ARP170103503A
Other languages
English (en)
Inventor
Gregory Hamilton
Snahel Patel
Original Assignee
Hoffmann La Roche
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of AR110368A1 publication Critical patent/AR110368A1/es

Links

Classifications

    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Veterinary Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Cardiology (AREA)
  • Vascular Medicine (AREA)
  • Pulmonology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Dermatology (AREA)
  • Gastroenterology & Hepatology (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)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201662435567P 2016-12-16 2016-12-16

Publications (1)

Publication Number Publication Date
AR110368A1 true AR110368A1 (es) 2019-03-20

Family

ID=60702777

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP170103503A AR110368A1 (es) 2016-12-16 2017-12-14 Inhibidores de la rip1 cinasa y métodos y uso de éstos

Country Status (7)

Country Link
US (1) US11072607B2 (es)
EP (2) EP4095138A1 (es)
JP (1) JP7209625B2 (es)
CN (1) CN110072863B (es)
AR (1) AR110368A1 (es)
TW (1) TW201827431A (es)
WO (1) WO2018109097A1 (es)

Families Citing this family (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2016287581B2 (en) 2015-07-02 2019-06-06 F. Hoffmann-La Roche Ag Bicyclic lactams and methods of use thereof
EP3526219B1 (en) 2016-10-17 2021-12-15 F. Hoffmann-La Roche AG Bicyclic pyridone lactams and methods of use thereof
EP3548484A1 (en) 2016-12-02 2019-10-09 H. Hoffnabb-La Roche Ag Bicyclic amide compounds and methods of use thereof
US11072607B2 (en) 2016-12-16 2021-07-27 Genentech, Inc. Inhibitors of RIP1 kinase and methods of use thereof
HRP20240354T1 (hr) 2017-07-14 2024-06-07 F. Hoffmann - La Roche Ag Biciklički ketonski spojevi i postupci njihove primjene
RU2020115915A (ru) 2017-10-31 2021-12-01 Ф. Хоффманн-Ля Рош Аг Бициклические сульфоны и сульфоксиды и способы их применения
JP7398391B2 (ja) * 2018-04-20 2023-12-14 エフ． ホフマン－ラ ロシュ アーゲー Ｎ－［４－オキソ－２，３－ジヒドロ－１，５－ベンズオキサゼピン－３－イル］－５，６－ジヒドロ－４Ｈ－ピロロ［１，２－ｂ］ピラゾール－２－カルボキサミド誘導体及び例えば過敏性腸症候群（ＩＢＳ）を処置するためのＲＩＰ１キナーゼ阻害剤としての関連化合物
FI3788045T3 (fi) 2018-05-03 2023-06-28 Rigel Pharmaceuticals Inc RIP1-inhibitorisia yhdisteitä ja samojen valmistus- ja käyttömenetelmiä
DK3788044T3 (da) 2018-05-03 2023-10-02 Rigel Pharmaceuticals Inc RIP1-hæmmende forbindelser og fremgangsmåder til fremstilling og anvendelse heraf
CN110642874B (zh) * 2018-06-26 2023-03-28 中国科学院上海有机化学研究所 一类细胞坏死抑制剂及其制备方法和用途
JP2022511213A (ja) * 2018-06-26 2022-01-31 シャンハイ インスティテュート オブ オーガニック ケミストリー，チャイニーズ アカデミー オブ サイエンシズ 細胞壊死阻害剤、その調製方法およびその使用
WO2020054670A1 (ja) * 2018-09-10 2020-03-19 科研製薬株式会社 新規ヘテロ芳香族アミド誘導体及びそれを含有する医薬
EP3908586B1 (en) * 2019-01-11 2022-12-21 F. Hoffmann-La Roche AG Bicyclic pyrrolotriazolr ketone compounds and methods of use thereof
JP7268921B2 (ja) * 2019-01-25 2023-05-08 北京賽特明強医薬科技有限公司 アミド基架橋複素環式化合物、その組成物および応用
CN114605400A (zh) 2019-03-19 2022-06-10 株式会社沃若诺伊 杂芳基衍生物、其制备方法、及含其作为有效成分的药物组合物
WO2021046515A1 (en) * 2019-09-06 2021-03-11 Board Of Regents, The University Of Texas System Inhibitors of receptor interacting protein kinase i for the treatment of disease
MX2022002717A (es) 2019-09-06 2022-08-10 Rigel Pharmaceuticals Inc Compuestos inhibidores de rip1 y metodos para prepararlos y usarlos.
KR20220042431A (ko) 2019-09-06 2022-04-05 리겔 파마슈티칼스, 인크. 헤테로시클릭 rip1 키나제 억제제
US11753381B2 (en) 2019-09-27 2023-09-12 Board Of Regents, The University Of Texas System Inhibitors of receptor interacting protein kinase I for the treatment of disease
CN115298184A (zh) 2019-11-07 2022-11-04 里格尔药品股份有限公司 杂环rip1抑制化合物
CN114981248A (zh) 2019-11-26 2022-08-30 德州大学系统董事会 用于治疗疾病的受体相互作用蛋白激酶i的抑制剂
TWI824259B (zh) 2020-07-01 2023-12-01 美商雷傑製藥公司 Rip1k抑制劑
WO2023020486A1 (zh) * 2021-08-17 2023-02-23 广州市恒诺康医药科技有限公司 Rip1激酶抑制剂类化合物及其组合物和用途
EP4209213A1 (en) 2022-01-05 2023-07-12 Universität zu Köln Signalling-pathway inhibitor combinations for use in the treatment of cancer diseases

Family Cites Families (47)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3773919A (en) 1969-10-23 1973-11-20 Du Pont Polylactide-drug mixtures
US4485045A (en) 1981-07-06 1984-11-27 Research Corporation Synthetic phosphatidyl cholines useful in forming liposomes
EP0102324A3 (de) 1982-07-29 1984-11-07 Ciba-Geigy Ag Lipide und Tenside in wässriger Phase
US4544545A (en) 1983-06-20 1985-10-01 Trustees University Of Massachusetts Liposomes containing modified cholesterol for organ targeting
HUT35524A (en) 1983-08-02 1985-07-29 Hoechst Ag Process for preparing pharmaceutical compositions containing regulatory /regulative/ peptides providing for the retarded release of the active substance
US5004697A (en) 1987-08-17 1991-04-02 Univ. Of Ca Cationized antibodies for delivery through the blood-brain barrier
US5268164A (en) 1990-04-23 1993-12-07 Alkermes, Inc. Increasing blood-brain barrier permeability with permeabilizer peptides
US5112596A (en) 1990-04-23 1992-05-12 Alkermes, Inc. Method for increasing blood-brain barrier permeability by administering a bradykinin agonist of blood-brain barrier permeability
US5206234A (en) 1990-10-22 1993-04-27 Merck & Co., Inc. Benzolactam analogs as antagonists of cck
CA2141216A1 (en) 1992-07-27 1994-02-03 Michael J. Micklus Targeting of liposomes to the blood-brain barrier
DE69736984T2 (de) 1996-12-06 2007-09-13 Vertex Pharmaceuticals Inc., Cambridge Inhibitoren des interleukin-1-beta konvertierenden enzyms
US6514221B2 (en) 2000-07-27 2003-02-04 Brigham And Women's Hospital, Inc. Blood-brain barrier opening
AU2001286930A1 (en) 2000-08-30 2002-03-13 The Board Of Trustees Of The Leland Stanford Junior University Glucocorticoid blocking agents for increasing blood-brain barrier permeability
GB0021831D0 (en) 2000-09-06 2000-10-18 Astrazeneca Ab Chemical compounds
US7034036B2 (en) 2000-10-30 2006-04-25 Pain Therapeutics, Inc. Inhibitors of ABC drug transporters at the blood-brain barrier
DE10121982B4 (de) 2001-05-05 2008-01-24 Lts Lohmann Therapie-Systeme Ag Nanopartikel aus Protein mit gekoppeltem Apolipoprotein E zur Überwindung der Blut-Hirn-Schranke und Verfahren zu ihrer Herstellung
DE60234057D1 (de) 2001-07-25 2009-11-26 Raptor Pharmaceutical Inc Zusammensetzungen und verfahren zur modulation des transports durch die blut-hirn-schranke
US20030113782A1 (en) 2001-11-26 2003-06-19 Karim Felix D. MAP4Ks as modifiers of branching morphogenesis and methods of use
US20030162695A1 (en) 2002-02-27 2003-08-28 Schatzberg Alan F. Glucocorticoid blocking agents for increasing blood-brain barrier permeability
US7057046B2 (en) 2002-05-20 2006-06-06 Bristol-Myers Squibb Company Lactam glycogen phosphorylase inhibitors and method of use
WO2004037986A2 (en) 2002-10-23 2004-05-06 Exelixis, Inc. Map2k6 as modifier of branching morphogenensis and methods of use
KR101111477B1 (ko) 2002-12-03 2012-02-23 블랜체트 록펠러 뉴로사이언시즈 인스티튜트 치료제와 연결된 콜레스테롤을 포함하는 접합체
US20050089473A1 (en) 2003-09-10 2005-04-28 Cedars-Sinai Medical Center Potassium channel mediated delivery of agents through the blood-brain barrier
US7390798B2 (en) 2004-09-13 2008-06-24 Merck & Co., Inc. Carboxamide spirolactam CGRP receptor antagonists
KR20080090484A (ko) 2005-12-30 2008-10-08 메르크 파텐트 게엠베하 ＧＰ130 에 대한, ＩＬ-6Ｒα 와 복합체를 형성한 ＩＬ-6의 결합을 방해하는 항-ＩＬ-6 항체
CA2658573A1 (en) 2006-07-21 2008-01-24 Vertex Pharmaceuticals Incorporated Cgrp receptor antagonists
US8507488B2 (en) 2008-05-13 2013-08-13 Irm Llc Fused nitrogen containing heterocycles and compositions thereof as kinase inhibitors
US20140357570A1 (en) 2011-10-21 2014-12-04 Massachusetts Eye And Ear Infirmary Compositions comprising necrosis inhibitors, such as necrostatins, alone or in combination, for promoting axon regeneration and nerve function, thereby treating cns disorders
US9611224B2 (en) 2012-07-13 2017-04-04 Hoffmann-La Roche Inc. Antiproliferative benzo [B] azepin-2-ones
US9394263B2 (en) 2012-08-09 2016-07-19 F. Hoffmann-La Roche Ag Substituted hetero-azepinones
TWI637951B (zh) 2013-02-15 2018-10-11 英商葛蘭素史克智慧財產發展有限公司 作為激酶抑制劑之雜環醯胺類
US9725452B2 (en) 2013-03-15 2017-08-08 Presidents And Fellows Of Harvard College Substituted indoles and pyrroles as RIP kinase inhibitors
EP2986317A4 (en) 2013-04-15 2016-10-05 Yeda Res & Dev INHIBITION OF RIP KINASES FOR THE TREATMENT OF LYSOSOMAL STORAGE DISEASES
CN106573006A (zh) 2014-08-21 2017-04-19 葛兰素史密斯克莱知识产权发展有限公司 作为药物的rip1激酶抑制剂杂环酰胺
MX2017016788A (es) 2015-07-02 2018-07-06 Janssen Sciences Ireland Uc Compuestos antibacterianos.
TW202108592A (zh) 2015-07-02 2021-03-01 瑞士商赫孚孟拉羅股份公司 苯并氧氮呯噁唑啶酮化合物及其用途
KR20170004814A (ko) 2015-07-02 2017-01-11 주식회사 녹십자 헌터증후군 치료제
US10875876B2 (en) 2015-07-02 2020-12-29 Janssen Sciences Ireland Uc Cyclized sulfamoylarylamide derivatives and the use thereof as medicaments for the treatment of hepatitis B
AU2016287581B2 (en) 2015-07-02 2019-06-06 F. Hoffmann-La Roche Ag Bicyclic lactams and methods of use thereof
US10709692B2 (en) 2015-12-04 2020-07-14 Denali Therapeutics Inc. Isoxazolidine derived inhibitors of receptor interacting protein kinase 1 (RIPK1)
AR107044A1 (es) 2015-12-17 2018-03-14 Astex Therapeutics Ltd Compuesto de quinolin-3-carboxamida, composición farmacéutica que lo comprende y su uso para prepararla
WO2017109724A1 (en) 2015-12-21 2017-06-29 Glaxosmithkline Intellectual Property Development Limited Heterocyclic amides as kinase inhibitors
CA3009324A1 (en) 2015-12-23 2017-06-29 President And Fellows Of Harvard College Cortistatin analogs and uses thereof
WO2017136727A2 (en) 2016-02-05 2017-08-10 Denali Therapeutics Inc. Compounds, compositions and methods
EP3526219B1 (en) 2016-10-17 2021-12-15 F. Hoffmann-La Roche AG Bicyclic pyridone lactams and methods of use thereof
US11072607B2 (en) 2016-12-16 2021-07-27 Genentech, Inc. Inhibitors of RIP1 kinase and methods of use thereof
JP7398391B2 (ja) 2018-04-20 2023-12-14 エフ． ホフマン－ラ ロシュ アーゲー Ｎ－［４－オキソ－２，３－ジヒドロ－１，５－ベンズオキサゼピン－３－イル］－５，６－ジヒドロ－４Ｈ－ピロロ［１，２－ｂ］ピラゾール－２－カルボキサミド誘導体及び例えば過敏性腸症候群（ＩＢＳ）を処置するためのＲＩＰ１キナーゼ阻害剤としての関連化合物

Also Published As

Publication number Publication date
JP2020502146A (ja) 2020-01-23
EP3555093A1 (en) 2019-10-23
TW201827431A (zh) 2018-08-01
US20180170927A1 (en) 2018-06-21
US11072607B2 (en) 2021-07-27
EP4095138A1 (en) 2022-11-30
CN110072863B (zh) 2022-08-30
CN110072863A (zh) 2019-07-30
EP3555093B1 (en) 2022-09-21
WO2018109097A1 (en) 2018-06-21
JP7209625B2 (ja) 2023-01-20

Similar Documents

Publication Publication Date Title
AR110368A1 (es) Inhibidores de la rip1 cinasa y métodos y uso de éstos
EP3875078A1 (en) Compounds for the treatment of covid-19
JP2016504363A5 (es)
RU2015131148A (ru) СОЕДИНЕНИЯ, ГЕТЕРОБИЦИКЛО-ЗАМЕЩЕННЫЕ-[1, 2, 4]ТРИАЗОЛО[1, 5c]ХИНАЗОЛИН-5-АМИНА, ОБЛАДАЮЩИЕ СВОЙСТВАМИ А2А АНТАГОНИСТОВ
PE20211001A1 (es) Imidazopirimidinas y triazolopirimidinas como inhibidores de a2a / a2b
HRP20191283T1 (hr) Diaril makrocikli kao modulatori protein kinaze
ES2898938T3 (es) Compuestos de heteroarilpiridona y aza-piridona como inhibidores de la actividad Btk
JP2015508075A5 (es)
RU2018112230A (ru) Бициклические соединения в качестве ингибиторов atx
IL261231B (en) Mcl-1 (r)-4-methyl-3,4-dihydropyrazino[1,2-a]indol-1(2h)-one inhibitors
JP2015504057A5 (es)
IL257587A (en) Compounds for the treatment of lateral amyotrophic sclerosis
HRP20211864T1 (hr) Inhibitori hetero-halo histonske deacetilaze
MX2020002711A (es) Proceso para preparacion de 7-(4,7-diazaespiro[2.5]octan-7-il)-2-( 2,8-dimetilimidazo[1,2-b]piridazin-6-il)pirido[1,2-a]pirimidin-4- ona.
JP2017510564A5 (es)
HRP20211483T1 (hr) Derivati 2-(3-(1h-benzo[d]imidazol-1-il)propil)piperidin-3-ola i povezani spojevi kao inhibitori prs za liječenje npr. raka
NZ590922A (en) Piperidine derivatives as jak3 inhibitors
MX2021004487A (es) Nuevas formas de derivados de pirido[1,2-a]pirimidin-4-ona, su formulacion y su proceso de elaboracion.
FI3652178T3 (fi) Bisyklisiä ketoniyhdisteitä ja niiden käyttömenetelmiä
HRP20110942T1 (hr) (dihidro)pirolo[2,1-a]izohinolini
JP2019530725A5 (es)
EP3856743A4 (en) SUBSTITUTED IMIDAZO[1,2-A]PYRIDINE AND [1,2,4]TRIAZOLO[1,5-A]PYRIDINE COMPOUNDS AS RET KINASE INHIBITORS
EA202092251A1 (ru) Комбинированные продукты для лечения rsv
JP2019504102A5 (es)
RU2018115716A (ru) Пиранодипиридиновое соединение

Legal Events

Date Code Title Description
FB Suspension of granting procedure