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Bicyclic derivatives of azabicyclic carboxamides, their preparation and therapeutic use
专利权人:
サノフイ
发明人:
デユボワ,ローラン,エバノ,ヤニク,ジル,カトリンヌ,マランダ,アンドレ,デユボワ,ローラン,エバノ,ヤニク,ジル,カトリンヌ,マランダ,アンドレ
申请号:
JP2010543538
公开号:
JP5457370B2
申请日:
2009.01.20
申请国别(地区):
JP
年份:
2014
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.
来源网站:
中国工程科技知识中心
来源网址:
http://www.ckcest.cn/home/
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