会员体验
专利管家（专利管理）
工作空间（专利管理）
风险监控（情报监控）
数据分析（专利分析）
侵权分析（诉讼无效）
联系我们
交流群
官方交流：
QQ群： 891211   
微信请扫码    >>>
现在联系顾问~
下载
著录项
PDF全文
热词
    • 39. 发明专利
      DE102007057718A1 New heteroaryl-substituted piperidine compounds are protease-activated receptor antagonists useful for the treatment and/or prophylaxis of e.g. cardiovascular diseases, thromboembolic diseases, tumors, stroke, hypertension and asthma 未知
    • New heteroaryl-substituted piperidine compounds are protease-activated receptor antagonists useful for the treatment and/or prophylaxis of e.g. cardiovascular diseases, thromboembolic diseases, tumors, stroke, hypertension and asthma
    • DE102007057718A1
    • 2009-07-30
    • DE102007057718
    • 2007-11-30
    • BAYER HEALTHCARE AG
    • HEIMBACH DIRK , ROEHRIG SUSANNE , SCHNEIDER DIRK , RESTER ULRICH , BENDER ECKHARD , MEININGHAUS MARK , ZIMMERMANN KATJA , ZUBOV DMITRY , BUCHMUELLER ANJA , DEGENFELD GEORGES , GERDES CHRISTOPH , GERISCH MICHAEL , GNOTH MARK JEAN
    • C07D413/04 , A61K31/4523 , A61P7/02 , A61P9/00 , A61P35/00 , C07D413/14 , C07D417/14
    • Heteroaryl-substituted piperidine compounds (I) and their salts, solvates or solvate of the salts, are new. Heteroaryl-substituted piperidine compounds of formula (I) and their salts, solvates or solvate of the salts, are new. A : [1,2,4]oxadiazole group of formula (a), thiazole group of formula (b) or (e), [1,3,4]oxadiazole group of formula (c), isoxazole group of formula (d), [1,3,4]thiadiazole group of formula (g) or oxazole group of formula (h); aa : connection with piperidine ring; aaa : connection with R 2>; R 1>phenyl substituted with 1-3 substituents of monofluoromethyl, difluoromethyl, trifluoromethyl, monofluoromethoxy, difluoromethoxy, trifluoromethoxy, monofluoromethylsulfanyl, difluoromethylsulfanyl, trifluoromethylsulfanyl, methylsulfonyl, 1-4C-alkyl, 1-4C-alkoxy, 1-4C-alkoxycarbonyl or 3-6C-cycloalkyl (where 2-4C-alkoxy is substituted by CH 3O or C 2H 5O and the cycloalkyl is substituted by 1-3 substituents of halo or 1-4C-alkyl); R 2>4-6-membered heterocycle, phenyl, 5- or 6-membered heteroaryl (all substituted by 1-3 substituents of halo, CN, amino, monofluoromethyl, difluoromethyl, trifluoromethyl, monofluoromethoxy, difluoromethoxy, trifluoromethoxy, monofluoromethylsulfanyl, difluoromethylsulfanyl, trifluoromethylsulfanyl, 1-4C-alkyl, 1-4C-alkoxy, 1-6C-alkylamino, 1-4C-alkoxycarbonylamino, 3-6C-cycloalkyl, 4-6 membered heterocycle, phenyl or 5-6 membered heteroaryl, where: alkyl amino is substituted by 1-4C-alkoxy or 1-6C-alkyl amino, 1-4C-alkyl is substituted by halo, OH, amino, aminocarbonyl, 1-4C-alkoxy, 1-6C-alkylamino, 1-4C-alkylthio, 1-4C-alkylcarbonyl, 1-4C-alkylcarbonyloxy, 1-4C-alkylsulfonyl, 1-4C-alkoxycarbonyl, 1-4C-alkoxycarbonylamino, 3-6C-cycloalkyl, 3-6C-cycloalkylamino, 4-6-membered heterocyclyl, phenyl, phenoxy, 5- or 6-membered heteroaryl or 5- or 6-membered heteroarylthio, and the cycloalkyl, heterocycle, phenyl, phenoxy, heteroaryl or heteroarylthio is substituted by 1-3 substituents of halo, CN, hydroxymethyl, monofluoromethyl, difluoromethyl, trifluoromethyl, monofluoromethoxy, difluoromethoxy, trifluoromethoxy, monofluoromethylsulfanyl, difluoromethylsulfanyl, trifluoromethylsulfanyl, 1-4C-alkyl, 1-4C-alkoxy, 3-6C-cycloalkyl, 4-6-membered heterocycle, phenyl or 5- or 6-membered heteroaryl); and R 3>1-6C-alkyl, 1-6C-alkoxy, 1-6C-alkylamino, 3-7C-cycloalkyl, 4-6-membered heterocycle, phenyl or 5- or 6-membered heteroaryl (where: the alkyl, 2-6C-alkoxy and alkylamino is substituted by OH, amino, CN or 1-4C-alkoxy, and the cycloalkyl, heterocycle, phenol or heteroaryl is substituted by 1-3 substituents of halo, CN, NO 2, oxo, OH, amino, aminomethyl, monofluoromethyl, difluoromethyl, trifluoromethyl, monofluoromethoxy, difluoromethoxy, trifluoromethoxy, monofluoromethylsulfanyl, difluoromethylsulfanyl, trifluoromethylsulfanyl, hydroxy carbonyl, amino carbonyl, 1-4C-alkyl, 1-4C-alkoxy, 1-6C-alkyl amino, 1-4C-alkoxy carbonyl or 1-4C-alkyl aminocarbonyl), H, trifluoromethyl, aminomethyl, 1-6C-alkyl, 2-6C-alkenyl, 1-4C-alkoxycarbonyl, 3-6C-cycloalkyl, cyclopentenyl, 1,3-benzodioxolyl or pyridylaminocarbonyl. An independent claim is included for the preparations of (I). [Image] [Image] [Image] ACTIVITY : Cardiovascular-Gen.; Thrombolytic; Cytostatic; Anticoagulant; Hemostatic; Cardiant; Antianginal; Vasotropic; Cerebroprotective; Antiarrhythmic; Muscular-Gen.; Osteopathic; Hypotensive; Antiasthmatic; Nephrotropic; Neuroprotective; Nootropic; Immunosuppressive; Antiinflammatory; Gastrointestinal-Gen.; Antiulcer; Ophthalmological; Antiarthritic; Antirheumatic; Respiratory-Gen.; Antiarteriosclerotic; Antibacterial; Antipyretic; Fungicide; Virucide; Antimicrobial; Uropathic; Vulnerary. MECHANISM OF ACTION : Protease-activated receptor antagonist. The antagonistic activity of (I) was tested in recombinant cell line. The results showed that (I), preferably {3-[3-(2-methoxyethyl)-1,2,4-oxadiazol-5-yl]-5-[3-methyl-4-(trifluoromethoxy)phenyl]piperidin-1-yl}(morpholin-4-yl)methanone exhibited an IC 5 0value of 3.01 nM.
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
每页展示10个专利
每页展示10个专利
每页展示20个专利
每页展示50个专利
每页展示100个专利

IPRDB

最新中国发明专利 最新美国发明专利 技术领域 专利库 专利分类库 国际专利分类库

热门服务

会员版试用 API 数据接口 找代理 知嘟嘟专利交易 排行榜 大学排行榜 专利百科

关于我们

平台介绍 战略合作 网站地图

友情链接

知嘟嘟专利交易 国家知识产权局 中国商标网

联系方式


©2019-2023 上海吉码数字技术有限公司 版权所有，并保留所有权利 沪ICP备20016256号-6 沪公网安备31011702005475号