Invention Grant
- Patent Title: 2-(azaindol-2-yl)benzimidazoles as PAD4 inhibitors
- Patent Title (中): 2-(氮杂吲哚-2-基)苯并咪唑作为PAD4抑制剂
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Application No.: US14416937Application Date: 2012-07-26
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Publication No.: US09127003B2Publication Date: 2015-09-08
- Inventor: 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
- Applicant: 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
- Applicant Address: GB Brentford
- Assignee: Glaxo Group Limited
- Current Assignee: Glaxo Group Limited
- Current Assignee Address: GB Brentford
- Agency: Choate, Hall & Stewart LLP
- Agent Andrea L.C. Reid
- International Application: PCT/EP2012/064649 WO 20120726
- International Announcement: WO2014/015905 WO 20140130
- Main IPC: C07D471/04
- IPC: C07D471/04 ; A61K31/407 ; A61K31/4184

Abstract:
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 C3-6cycloalkylC1-6 alkyl; 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.
Public/Granted literature
- US20150175600A1 2-(AZAINDOL-2-YL)BENZIMIDAZOLES AS PAD4 INHIBITORS Public/Granted day:2015-06-25
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