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Azabicyclic carboxamide derivatives, their preparation and their therapeutic application.
专利权人:
SANOFI-AVENTIS
发明人:
LAURENT DUBOIS,YANNICK EVANNO,DAVID MACHNIK,ANDRÉ MALANDA
申请号:
BRPI0907381
公开号:
BRPI0907381A2
申请日:
2009.01.20
申请国别(地区):
BR
年份:
2015
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; Z 1-Z 4N, C or CR 2; 2C+R aR b5-membered ring containing a nitrogen atom and carbon atoms, and optionally saturated and optionally substituted; W 1O or S; n : 0-3; Y 1aryl or heteroaryl; 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; and R 2e.g. H, halo, 3-7C cycloalkyl-1-3C-alkylene-O-, OH, thiol or 1-6C fluoroalkoxy. Full Definitions are given in the DEFINITIONS (Full Definitions) Field. An independent claim is included for the preparation 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-(1H-pyrrolo[2,3-b]pyridin-5-yl)-5-fluoro-1-(3-fluorobenzyl)-1H-indole-2-carboxamide (1 nM) exhibited 82% inhibition in DRG patch.
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中国工程科技知识中心
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