您的位置: 首页 > 农业专利 > 详情页

取代的哌啶子基-二氫噻吩並嘧啶
专利权人:
BOEHRINGER INGELHEIM INTERNATIONAL GMBH
发明人:
POUZET, PASCALE,ANDERSKEWITZ, RALF,DOLLINGER, HORST,FIEGEN, DENNIS,FOX, THOMAS,GOEGGEL, ROLF,HOENKE, CHRISTOPH,MARTYRES, DOMNIC,NICKOLAUS, PETER,KLINDER, KLAUS
申请号:
HK10111978.1
公开号:
HK1145677B
申请日:
2010.12.22
申请国别(地区):
HK
年份:
2015
代理人:
摘要:
Substituted piperidino-dihydrothienopyrimidine compounds (I) and their salts, are new. Substituted piperidino-dihydrothienopyrimidine compounds of formula (I) and their salts, are new. Either R 1>; : H or 1-6C alkyl; and R 2>; : H, 1-10C alkyl or 2-6C alkenyl; or NR 1>;R 2>; : heterocyclic four to seven membered ring; either R 3>; : e.g. 6-10C-aryl; and R 4>; : e.g. H, CN, OH or CF 3; or R 3>;R 4>; : a mono- or bicyclic, unsaturated or or partially saturated heterocycle; and X : SO or SO 2. Full Definitions are given in the DEFINITIONS (Full Definitions) Field. [Image] ACTIVITY : Respiratory-Gen.; Gastrointestinal-Gen.; Antiinflammatory; Ophthalmological; Dermatological; Cytostatic; CNS-Gen.; Antiasthmatic; Antiulcer; Gastrointestinal-Gen.; Antidepressant; Neuroleptic; Tranquilizer; Neuroprotective; Nootropic; Antiparkinsonian; Analgesic; Vulnerary; Cerebroprotective. MECHANISM OF ACTION : Phosphodiesterase-4 inhibitor. The ability of (I) to inhibit phosphodiesterase-4 was tested by using scintillation proximity assays (GE healthcare, number TRKQ7090). The result showed that (R)-2-{2-[4-(4-chloro-phenyl)-piperidin-1-yl]-5-oxo-6,7-dihydro-5H-5-thieno[3,2-d]pyrimidin-4-ylamino}-3-methyl-butan-1-ol (I) at a concentration of 1 mu m exhibited a percentage inhibition of 93.
来源网站:
中国工程科技知识中心
来源网址:
http://www.ckcest.cn/home/

意 见 箱

匿名:登录

个人用户登录

找回密码

第三方账号登录

忘记密码

个人用户注册

必须为有效邮箱
6~16位数字与字母组合
6~16位数字与字母组合
请输入正确的手机号码

信息补充