DUBOIS, LAURENT,EVANNO, YANNICK,GILLE, CATHERINE,MALANDA, ANDRE
申请号：
EP09718719.9
公开号：
EP2235014B1
申请日:
2009.01.20
申请国别(地区):
EP
年份:
2013
代理人:
摘要：
Azabicyclic carboxamide compounds (I) and their acid or base addition salts, hydrates or solvates are new. Azabicyclic carboxamide compounds of formula (I) and their acid or base addition salts, hydrates or solvates are new. X 1-X 4N or CR 1； A : heteroaryl group； W 1O or S； n : 0-3； Y 1aryl or heteroaryl； and R 1e.g. H, halo, 1-6C alkyl, 3-7C cycloalkyl, 3-7C cycloalkyl-1-3C alkylene, 1-6C fluoroalkyl, aryloxy-1-6C alkyl or heteroaryloxy-1-6C alkyl. Full Definitions are given in the DEFINITIONS (Full Definitions) Field. An independent claim is included for the preparations of (I). [Image] ACTIVITY : Analgesic； Antiinflammatory； Metabolic； Gynecological； Gastrointestinal-Gen.； Respiratory-Gen.； Antipsoriatic； Antipruritic； Virucide； Neuroprotective； Antidepressant； Antiarthritic； Osteopathic； Muscular-Gen.； Antimigraine； Vulnerary； Dermatological； Cerebroprotective； Vasotropic； Antidiabetic； Uropathic； Nephrotropic； Antiulcer； Antiasthmatic； Antitussive； CNS-Gen.； Antiallergic； Immunosuppressive. MECHANISM OF ACTION : Transient receptor potential vanilloid type 1 (TRPV1) receptor modulator. The ability of (I) to inhibit current induced by capsaicin was tested in primary cells of dorsal root ganglia (DRG) of rat. The result showed that N-(2-hydroxymethyl-thiazolo[5,4-b]pyridin-6-yl)-5-fluoro-1-(3-fluorobenzyl)-1H-indole-2-carboxamide (0.1 nM) exhibited 65.5% inhibition in DRG patch.
