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21. 发明授权

US06979690B2 Oxo or oxy-pyridine compounds as 5-HT4 receptor modulators 失效
公开(公告)号：US06979690B2
公开(公告)日：2005-12-27
申请号：US10337497
申请日：2003-01-07
申请人： Geoffrey Gymer , Kiyoshi Kawamura , Sachiko Mihara , Mikio Morita , Alan Stobie , Chikara Uchida , Seiji Nukui
发明人： Geoffrey Gymer , Kiyoshi Kawamura , Sachiko Mihara , Mikio Morita , Alan Stobie , Chikara Uchida , Seiji Nukui
IPC分类号： A61K31/4545 , A61P1/00 , A61P1/04 , A61P1/08 , A61P1/10 , A61P1/14 , A61P9/00 , A61P9/10 , A61P25/00 , A61P25/04 , A61P25/06 , A61P25/22 , A61P25/28 , A61P43/00 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/14 , A61K31/445
CPC分类号： C07D401/06 , C07D401/12 , C07D401/14
摘要： This invention provides compounds of the formula (I) and (II): or the pharmaceutically acceptable esters thereof, and the pharmaceutically acceptable salts thereof: wherein R1 is hydrogen or halo; R2 and R3 are independently hydrogen or C1-6 alkyl; R4 and R5 are independently hydrogen or C1-6 alkyl; R6 is hydrogen, C1-12 alkyl, C1-6 alkoxy (C1-6)alkyl or C1-12 alkyl substituted by up to 3 substituents selected from the groups consisting of C3-8 cycloalkyl, aryl, heteroaryl and heterocyclic; R7 and R8 are hydrogen or taken together may form alkylene chain having one or two carbon atoms; R9 is C1-6 alkyl or C3-8 cycloalkyl; R10 is C1-6 alkyl or NR11R12; L is (CR11R12)n or NR11; M is NR11 or (CR11R12)n; R11 and R12 are independently hydrogen or C1-6 alkyl; n is an integer from 0 to 5; and m is an integer from 0 to 2; said heterocyclic, aryl and heteroaryl are unsubstituted or are substituted by at least one substituent selected from the group consisting of halo and C1-6 alkyl; with the proviso that when R9 is C1-6 alkyl, L is not NR11. These compounds have 5-HT4 receptor binding activity, and thus are useful for the treatment of gastroesophageal reflux disease, non-ulcer dyspepsia, irritable bowel syndrome or the like in mammalian, especially humans. This invention also provides a pharmaceutical composition comprising the above compound.

22. 发明申请

US20050065188A1 Aryl or heteroaryl amide compounds 有权
标题翻译：芳基或杂芳基酰胺化合物
公开(公告)号：US20050065188A1
公开(公告)日：2005-03-24
申请号：US10932463
申请日：2004-09-02
申请人： Kazunari Nakao , Seiji Nukui , Yoshiyuki Okumura , Tatsuya Yamagishi
发明人： Kazunari Nakao , Seiji Nukui , Yoshiyuki Okumura , Tatsuya Yamagishi
IPC分类号： A61P29/00 , C07C233/87 , C07C235/60 , C07C255/57 , C07D213/64 , C07D213/643 , C07D213/65 , C07D213/82 , C07D257/04 , C07D401/12 , C07D417/12 , A61K31/4439 , A61K31/18 , A61K31/195 , A61K31/198 , A61K31/355
CPC分类号： C07C233/87 , C04B35/632 , C07C235/60 , C07C255/57 , C07D213/643 , C07D213/65 , C07D213/82 , C07D257/04 , C07D401/12 , C07D417/12
摘要： This invention provides a compound of the formula (I): wherein A represents a phenyl group or the like: B represents an aryl or the like: E represents a 1,4-phenylene group; R1 and R2 independently represent a hydrogen atom or the like: R3 and R4 independently represent a hydrogen atom or the like: R5 represents —CO2H or the like: R6 represents an alkyl group having from 1 to 6 carbon atoms or the like: X represents a methylene group or the like. These compounds are useful for the treatment of disease conditions mediated by prostaglandin such as pain, or the like in mammalian. This invention also provides a pharmaceutical composition comprising the above compound.
摘要翻译：本发明提供式（I）的化合物：其中A表示苯基等：B表示芳基等：E表示1,4-亚苯基; R 1和R 2独立地表示氢原子等：R 3和R 4独立地表示氢原子等：R 5表示-CO 2 H等：R 6 >表示具有1〜6个碳原子的烷基等：X表示亚甲基等。这些化合物可用于治疗由前列腺素介导的疾病状况，例如哺乳动物中的疼痛等。本发明还提供了包含上述化合物的药物组合物。

23. 发明授权

US06734306B2 N-benzenesulfonyl L-proline compounds as bradykinin antagonists 失效
标题翻译： N-苯磺酰基L-脯氨酸化合物作为缓激肽拮抗剂
公开(公告)号：US06734306B2
公开(公告)日：2004-05-11
申请号：US10010863
申请日：2001-12-05
申请人： Yasuhiro Katsu , Makoto Kawai , Hiroki Koike , Seiji Nukui
发明人： Yasuhiro Katsu , Makoto Kawai , Hiroki Koike , Seiji Nukui
IPC分类号： C07D40114
CPC分类号： C07D451/02 , C07D401/12 , C07D401/14 , C07D451/04 , C07D453/02 , C07D487/08
摘要： This invention provides a compound of the formula (I): or the pharmaceutically acceptable salts thereof wherein X1 and X2 are halo; R1 and R2 are independently hydrogen or C1-4 alkyl; R3 and R4 are each hydrogen or halo; and R5 is (a) —C3-9 diazacycloalkyl optionally substituted with C5-11 azabicycloalkyl; (b) —C3-9 azacycloalkyl-NH—(C5-11 azabicycloalkyl optionally substituted with C1-4 alkyl); (c) —NH—C1-3 alkyl-C(O)—C5-11 diazabicycloalkyl; (d) —NH—C1-3 alkyl-C(O)—NH—C5-11 azabicycloalkyl, the C5-11 azabicycloalkyl being optionally substituted with C1-4 alkyl; (e) —C3-9 azacycloalkyl optionally substituted with C3-9 azacycloalkyl; or (f) —NH—C1-5 alkyl-NH—C(O)—C4-9 cycloalkyl-NH2. These compounds are useful for the treatment of medical conditions mediated by bradykinin such as inflammation, allergic rhinitis, pain, etc. This invention also provides a pharmaceutical composition comprising the above compound.
摘要翻译：本发明提供式（I）化合物或其药学上可接受的盐，其中X 1和X 2为卤素; R 1和R 2独立地是氢或C 1-4烷基; R 3和R 4各自为氢或卤素; （b）-C3-9氮杂环烷基-NH-（任选被C 1-4烷基取代的C 5-10氮杂双环烷基）;（c）-C（= NH-C 1-3烷基-C（O）-C 5-11二氮杂双环烷基;（d）-NH-C 1-3烷基-C（O）-NH-C 5-11氮杂双环烷基，C 5-11氮杂双环烷基任选被C 1 -4-烷基;（e）任选被C 3-9氮杂环烷基取代的-C3-9氮杂环烷基; 或（f）-NH-C 1-5烷基-NH-C（O）-C 4-9环烷基-NH 2。这些化合物可用于治疗由缓激肽介导的医学病症如炎症，过敏性鼻炎，疼痛等。本发明还提供了包含上述化合物的药物组合物。

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