- 专利标题: 2-(azaindol-2-yl) benzimidazoles as PAD4 inhibitors
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申请号: US15817562申请日: 2017-11-20
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公开(公告)号: US10039755B2公开(公告)日: 2018-08-07
- 发明人: Stephen John Atkinson , Michael David Barker , Matthew Campbell , Hawa Diallo , Clement Douault , Neil Stuart Garton , John Liddle , Robert John Sheppard , Ann Louise Walker , Christopher Wellaway , David Matthew Wilson
- 申请人: Glaxo Group Limited
- 申请人地址: GB Brentford
- 专利权人: Glaxo Group Limited
- 当前专利权人: Glaxo Group Limited
- 当前专利权人地址: GB Brentford
- 代理机构: Dechert LLP
- 代理商 Andrea L. C. Reid
- 主分类号: A61K31/4545
- IPC分类号: A61K31/4545
摘要:
Compounds of formula (I) wherein; R1 is hydrogen or C1-6alkyl; R2 is hydrogen, C1-6alkyl, perhalomethylC0-5alkyl-O—, or C1-6alkoxy; R3 is hydrogen, C1-6alkyl, or C1-6alkoxyC1-6alkyl; R4 is hydrogen, C1-6alkyl, perhalomethylC1-6alkyl; or unsubstituted C3-6cycloalkylC1-6alkyl; A is C—R5 or N; B is C—R6 or N; D is C—R7 or N; with the proviso that at least one of A, B, and D, is N; R5 is hydrogen or C1-6alkyl; R6 is hydrogen or C1-6alkyl; R7 is hydrogen, C1-6alkyl, C1-6alkoxy, or hydroxy; R8 is hydrogen or C1-6alkyl, with the proviso that one of R4 and R8 is hydrogen; R9 is hydrogen or hydroxy; R10 is hydrogen or C1-6alkyl; and salts thereof are PAD4 inhibitors and may be useful in the treatment of various disorders, for example rheumatoid arthritis, vasculitis, systemic lupus erythematosus, ulcerative colitis, cancer, cystic fibrosis, asthma, cutaneous lupus erythematosis, and psoriasis.
公开/授权文献
- US20180161316A1 2-(AZAINDOL-2-YL) BENZIMIDAZOLES AS PAD4 INHIBITORS 公开/授权日:2018-06-14
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