Inhibitors of RIP1 kinase and methods of use thereof

US11072607B2 · US · B2

Patent metadata
FieldValue
Publication numberUS-11072607-B2
Application numberUS-201715839788-A
CountryUS
Kind codeB2
Filing dateDec 12, 2017
Priority dateDec 16, 2016
Publication dateJul 27, 2021
Grant dateJul 27, 2021

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  1. Title

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  2. Abstract

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  5. First independent claim

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Abstract

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The invention provides novel compounds having RIP1 kinase inhibitory activity, pharmaceutical compositions including the compounds and methods of using the compounds.

First claim

Opening claim text (preview).

The invention claimed is: 1. A compound selected from the group consisting of: (5R)-5 -(1, 1-difluoropropyl)-N-[(3S)-7,9-difluoro-2-oxo-1,3,4,5-tetrahydro-1-benzazepin-3-yl]-6,7-dihydro-5H-pyrrolo[1,2-b][1,2,4]triazole-2-carboxamide; rac-(5R,7S)-7-fluoro-5-phenyl-N-[(3S)-5-methyl-4-oxo-2,3-dihydro-1,5-benzoxazepin-3-yl]-6,7-dihydro-5H-pyrrolo[1,2-b][1,2,4]triazole-2-carboxamide; rac-(5R, 7S)-7-fluoro-5-phenyl-N-[(3S)-7,9-difluoro-2-oxo-1,3,4,5-tetrahydro-1-benzazepin-3-yl]-6,7-dihydro-5H-pyrrolo[1,2-b][1,2,4]triazole-2-carboxamide; (5R,7R)-7-fluoro-5-phenyl-N-[(3S)-7,9-difluoro-2-oxo-1,3,4,5-tetrahydro-1-benzazepin-3-yl]-6,7-dihydro-5H-pyrrolo[1,2-b][1,2,4]triazole-2-carboxamide; 1-(2,2-difluoropropyl)-N-[(3S)-5-methyl-4-oxo-2,3-dihydro-1,5-benzoxazepin-3-yl]pyrazolo[3,4-d]pyrimidine-6-carboxamide; 1-cyclopropyl-N-[(3S)-5-methyl-4-oxo-2,3-dihydro-1,5-benzoxazepin-3-yl]pyrazolo [3,4-d]pyrimidine-6-carboxamide; (5R)-5-phenyl-N-[(3S)-7-methoxy-1-methyl-2-oxo-4,5-dihydro-3H-pyrido[3,4-b]azepin-3-yl]-6,7-dihydro-5H-pyrrolo[1,2-b][1,2,4]triazole-2-carboxamide; (5R)-5-phenyl-N-[(7S)-6-oxo-5,7,8,9-tetrahydropyrido[3,2-b]azepin-7-yl]-6,7-dihydro-5H-pyrrolo[1,2-b][1,2,4]triazole-2-carboxamide; 5-(1,1-difluoropropyl)-N-[(3S)-7,9-difluoro-2-oxo-1,3,4,5-tetrahydro-1-benzazepin-3-yl]-6,7-dihydro-5H-pyrrolo[1,2-b][1,2,4]triazole-2carboxamide; rac-(5S,7S)-7-fluoro-5-phenyl-N-[(3S)-5-methyl-4-oxo-2,3-dihydro-1,5-benzoxazepin-3-yl]-6,7-dihydro-5H-pyrrolo[1,2-b][1,2,4]triazole-2-carboxamide; rac-(5S,7S)-7-fluoro-5-phenyl-N-[(6S)-4-methyl-5-oxo-7,8-dihydro-6H-pyrazolo[1,5-a][1,3]diazepin-6-yl]-6,7-dihydro-5H-pyrrolo[1,2-b][1,2,4]triazole-2-carboxamide; (5S)-5-(2-fluorophenyl)-N-[(3S)-7-methoxy-1-methyl-2-oxo-4,5-dihydro-3H-pyrido[3,4-b]azepin-3-yl]-6,7-dihydro-5H-pyrrolo[1,2-b][1,2,4]triazole-2-carboxamide; (5S)-5-(2-fluorophenyl)-N-[(7S)-6-oxo-5,7,8,9-tetrahydropyrido[3,2-b]azepin-7-yl]-6,7-dihydro-5H-pyrrolo[1,2-b][1,2,4]triazole-2-carboxamide; (5R)-5-(2-fluorophenyl)-N-[(7S)-5-methyl-6-oxo-8,9-dihydro-7H-pyrido[3,2-b]azepin-7-yl]-6,7-dihydro-5H-pyrrolo[1,2-b][1,2,4]triazole-2-carboxamide; (4S)-4-phenyl-N- [(3S)-5-methyl-4-oxo-2,3-dihydro-1,5-benzoxazepin-3-6,7-dihydro-4H-pyrazolo[5,1-c][1,4]oxazine-2-carboxamide; 4-phenyl-N- [(3S)-7,9-difluoro-2-oxo-1,3,4,5-tetrahydro-1-benzazepin-3-6,7-dihydro-4H-pyrazolo[5,1-c][1,4]oxazine-2-carboxamide; 1-(2,2-difluoropropyl)-N-[(3S)-5-methyl -4-oxo-2,3-dihydro-1,5-benzoxazepin-3-yl]pyrazolo[4,3-c]pyridine-6-carboxamide; 1-cyclopropyl-N-[(3S)-5-methyl-4-oxo-2,3-dihydro- 1,5-benzoxazepin-3-yl]pyrazolo[4,3-c]pyridine-6-carboxamide; (7S)-7-(2-fluorophenyl)-N-[(7S)-5-methyl-6-oxo-8,9-dihydro-7H-pyrido[3,2-b ]-azepin-7-yl]-6,7-dihydro-5H-pyrrolo[1,2-b][1,2,4]triazole-2-carboxamide; (7S)-7-phenyl-N-[(7S)-5-methyl-6-oxo-8,9-dihydro-7H-pyrido[3,2-b]azepin-7-yl]-6,7-dihydro-5H-pyrrolo[1,2-b][1,2,4]triazole-2carboxamide; (5S)-5-phenyl-N-[(7S)-5-methyl-6-oxo-8,9-dihydro-7H-pyrido[3,2-b ]azepin-7-yl]-6,7-dihydro-5H-pyrrolo[1,2-b][1,2,4]triazole-2carboxamide; (5S,7R)-7-fluoro-5-phenyl-N-[(3S)-7,9-difluoro-2-oxo-1,3,4,5-tetrahydro-1-benzazepin-3-yl]-6,7-dihydro-5H-pyrrolo[1,2-b][1,2,4]triazole-2-carboxamide; (5S,7R)-7-fluoro-5-phenyl-N-[(3S)-5-methyl-4-oxo-2,3-dihydro-1,5-benzoxazepin-3-yl]-6,7-dihydro-5H-pyrrolo[1,2-b][1,2,4]triazole-2-carboxamide; (5R,7S)-7-fluoro-5-phenyl-N-[(6S)-2,4-dimethyl-5-oxo-7,8-dihydro-6H-pyrazolo [1,5-a][1,3]diazepin-6-yl]-6,7-dihydro-5H-pyrrolo[1,2-b][1,2,4]triazole-2-carboxamide; (5R,7S)-7-fluoro-5-phenyl-N-[(6S)-4-methyl-5-oxo-7,8-dihydro-6H-pyrazolo[1,5-a][1,3]diazepin-6-yl]-6,7-dihydro-5H-pyrrolo[1,2-b][1,2,4]triazole-2-carboxamide; 4-phenyl-N-[(3S)-5-methyl-4-oxo-2,3-dihydro-1,5-benzoxazepin-3-yl]-6,7-dihydro-4H-pyrazolo[5,1-c][1,4]oxazine-2-carboxamide; 7,7-difluoro-5-phenyl-N-[(3S)-7,9-difluoro-2-oxo-1,3,4,5-tetrahydro-1-benzazepin-3-yl]-5,6-dihydropyrrolo[1,2-b][1,2,4]triazole-2-carboxamide; 7,7-difluoro-5-phenyl-N-[rac-(3S)-5-methyl-4-oxo-2,3-dihydro-1,5-benzoxazepin-3-yl]-5,6-dihydropyrrolo[1,2-b][1,2,4]triazole-2-carboxamide; 7-fluoro-5-phenyl-N-[rac-(3S)-7,9-difluoro-2-oxo-1,3,4,5-tetrahydro-1-benzazepin-3-yl]-6,7-dihydro-5H-pyrrolo[1,2-b][1,2,4]triazole-2-carboxamide; 7-fluoro-5-phenyl-N-[rac-(3S)-5-methyl-4-oxo-2,3-dihydro-1,5-benzoxazepin-3-yl]-6,7-dihydro-5H-pyrrolo[1,2-b][1,2,4]triazole-2-carboxamide; 7-fluoro-5-phenyl-N-[6S)-4-methyl-5-oxo-7,8-dihydro-6H-pyrazolo[1,5-a][1,3]diazepin-6-yl]-6,7-dihydro-5H-pyrrolo[1,2-b][1,2,4]

Assignees

Inventors

Classifications

  • 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 · CPC title

  • Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] · CPC title

  • Drugs for disorders of the alimentary tract or the digestive system · CPC title

  • for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics · CPC title

  • for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis · CPC title

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What does patent US11072607B2 cover?
The invention provides novel compounds having RIP1 kinase inhibitory activity, pharmaceutical compositions including the compounds and methods of using the compounds.
Who is the assignee on this patent?
Genentech Inc
What technology area does this patent fall under?
Primary CPC classification C07D471/04. Mapped technology areas include Chemistry & Metallurgy.
When was this patent published?
Publication date Tue Jul 27 2021 00:00:00 GMT+0000 (Coordinated Universal Time) (B2). Legal status and post-grant events are not shown on this page.
What related patents are in patentsdb?
We list 3 related publications on this page (citations in our corpus or others sharing the same primary CPC).