| 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. |
