Invention Grant
US07935832B2 Pyrrole and isoindole carboxamide derivatives as P2X7 modulators
失效
吡咯和异吲哚羧酰胺衍生物作为P2X7调节剂
- Patent Title: Pyrrole and isoindole carboxamide derivatives as P2X7 modulators
- Patent Title (中): 吡咯和异吲哚羧酰胺衍生物作为P2X7调节剂
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Application No.: US12532868Application Date: 2008-03-20
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Publication No.: US07935832B2Publication Date: 2011-05-03
- Inventor: Robert James Gleave , David George Hubert Livermore , Daryl Simon Walter
- Applicant: Robert James Gleave , David George Hubert Livermore , Daryl Simon Walter
- Applicant Address: GB Greenford, Middlesex
- Assignee: Glaxo Group Limited
- Current Assignee: Glaxo Group Limited
- Current Assignee Address: GB Greenford, Middlesex
- Agent Duke M. Fitch; Kathryn L. Sieburth; John L. Lemanowicz
- Priority: GB0705882.9 20070327
- International Application: PCT/EP2008/053343 WO 20080320
- International Announcement: WO2008/116814 WO 20081002
- Main IPC: C07D209/44
- IPC: C07D209/44 ; C07D207/24 ; C07D213/02 ; C07D401/06 ; A61K31/44 ; A61K31/40

Abstract:
The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof: wherein: R2 represents hydrogen, halogen, C1-6 alkyl, C6-10 arylmethyl-, C2-6 alkenyl, C2-6 alkynyl or C3-6 cycloalkylmethyl-; and any of said C1-6 alkyl, C6-10 arylmethyl-, C2-6 alkenyl, C2-6 alkynyl or C3-6 cycloalkylmethyl- is optionally substituted with 1, 2 or 3 halogen atoms; and R3 represents hydrogen, fluorine or methyl; or R2 and R3 together with the carbon atoms to which they are attached form a benzene ring optionally substituted with 1, 2 or 3 substituents, which may be the same or different, selected from the group consisting of C1-6 alkyl, C2-6 alkenyl and C2-6 alkynyl. The compounds or salts modulate P2X7 receptor function and are capable of antagonizing the effects of ATP at the P2X7 receptor. The invention also provides the use of such compounds or salts, or pharmaceutical compositions thereof, in the treatment of disorders mediated by the P2X7 receptor, for example pain, inflammation or neurodegeneration.
Public/Granted literature
- US20100210705A1 Pyrrole and Isoindole Carboxamide Derivatives as P2X7 Modulators Public/Granted day:2010-08-19
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