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1. 发明申请

US20050038060A1 Spiropoperidine compounds as ligands for orl-1 receptor 审中-公开
标题翻译： Spiropoperidine化合物作为orl-1受体的配体
公开(公告)号：US20050038060A1
公开(公告)日：2005-02-17
申请号：US10481210
申请日：2002-06-17
申请人： Koji Ando , Fumitaka Ito , Hiroki Koike , Masaki Sudo , Tatsuya Yamagishi
发明人： Koji Ando , Fumitaka Ito , Hiroki Koike , Masaki Sudo , Tatsuya Yamagishi
IPC分类号： C07D491/107 , A61K31/438 , A61K31/454 , A61K31/4545 , A61K31/4709 , A61K31/496 , A61K31/498 , A61K31/517 , A61K31/537 , A61K31/538 , A61K31/541 , A61K31/55 , A61P1/04 , A61P1/16 , A61P3/04 , A61P7/12 , A61P11/00 , A61P13/12 , A61P15/00 , A61P25/00 , A61P25/02 , A61P25/04 , A61P25/08 , A61P25/16 , A61P25/22 , A61P25/28 , A61P43/00 , C07D401/06 , C07D401/14 , C07D413/06 , C07D413/14 , C07D417/06 , C07D417/14 , C07D471/10 , C07D491/10 , A61K31/4747
CPC分类号： C07D401/06 , C07D401/14 , C07D413/06 , C07D413/14 , C07D417/06 , C07D417/14 , C07D471/10 , C07D491/10
摘要： A compound of the formula (I) or a salt, prodrug or solvate thereof, wherein R1 and R2 groups are all hydrogen; A is a benzofuzed azahetero ring; W1—W2 is CH2—CH2; X1—X1 is CH2—CH2; and Z is methylene or carbonyl; or the like, is a ligand for ORL1-receptor and are useful for treating or preventing pain, a CNS disorder or the like in mammalian subjects.
摘要翻译：式（I）化合物或其盐，前药或溶剂合物，其中R 1和R 2均为氢; A是苯并呋喃氮杂环; W 1 -W 2是CH 2 -CH 2; X 1 -X 1是CH 2 -CH 2; Z是亚甲基或羰基; 等等是ORL1-受体的配体，可用于治疗或预防哺乳动物受试者的疼痛，CNS病症等。

2. 发明授权

US06423725B1 4-(2-keto-1-benzimidazolinyl)piperidine compounds as ORL1-receptor agonists 失效
标题翻译： 4-（2-酮-1-苯并咪唑啉基）哌啶化合物作为ORL1-受体激动剂
公开(公告)号：US06423725B1
公开(公告)日：2002-07-23
申请号：US09403408
申请日：2000-03-06
申请人： Fumitaka Ito , Hirohide Noguchi , Yoriko Ohashi , Hiroshi Kondo , Tatsuya Yamagishi
发明人： Fumitaka Ito , Hirohide Noguchi , Yoriko Ohashi , Hiroshi Kondo , Tatsuya Yamagishi
IPC分类号： A61K31454
CPC分类号： C07D401/04 , C07D401/14 , C07D409/14
摘要： A compound of the formula: or the pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4 and R5 are defined above are useful as ORL1-receptor agonists, and useful as analgesics or the like in mammalian subjects.
摘要翻译：下式化合物或其药学上可接受的盐，其中R 1，R 2，R 3，R 4和R 5如上定义，可用作ORL1-受体激动剂，并且可用作哺乳动物受试者中的止痛剂等。

3. 发明申请

US20050250818A1 Ortho substituted aryl or heteroaryl amide compounds 审中-公开
标题翻译：正构取代的芳基或杂芳基酰胺化合物
公开(公告)号：US20050250818A1
公开(公告)日：2005-11-10
申请号：US11118646
申请日：2005-04-29
申请人： Hiroki Koike , Yukari Matsumoto , Kazunari Nakao , Yoshiyuki Okumura , Tatsuya Yamagishi
发明人： Hiroki Koike , Yukari Matsumoto , Kazunari Nakao , Yoshiyuki Okumura , Tatsuya Yamagishi
IPC分类号： A61K31/195 , A61K31/4415 , C07C235/60 , C07C255/54 , C07D213/61 , C07D213/82 , C07D213/89 , C07D261/08 , C07D307/12 , C07D307/42 , C07D309/06
CPC分类号： C07D261/08 , C07C235/60 , C07C255/54 , C07C2601/04 , C07C2601/14 , C07D213/61 , C07D213/82 , C07D213/89 , C07D307/12 , C07D307/42 , C07D309/06 , C07D405/12
摘要： This invention provides a compound of the formula (I): wherein X represents a carbon atom or the like: Y represents imino, or the like: Z represents a hydrogen atom or the like: R1 represents an alkyl group having from 1 to 6 carbon atoms or the like: R2 and R3 independently represents a hydrogen atom 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X表示碳原子等：Y表示亚氨基等; Z表示氢原子等：R 1表示具有1至6个碳原子的烷基等：R 2和R 3独立地表示氢原子等。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。

4. 发明申请

US20050267170A1 Substituted methyl aryl or heteroaryl amide compounds 失效
标题翻译：取代的甲基芳基或杂芳基酰胺化合物
公开(公告)号：US20050267170A1
公开(公告)日：2005-12-01
申请号：US11118497
申请日：2005-04-29
申请人： Hiroki Koike , Kana Kon-i , Yukari Matsumoto , Kazunari Nakao , Yoshiyuki Okumura , Tatsuya Yamagishi
发明人： Hiroki Koike , Kana Kon-i , Yukari Matsumoto , Kazunari Nakao , Yoshiyuki Okumura , Tatsuya Yamagishi
IPC分类号： A61K31/195 , A61K31/455 , C07C235/42 , C07C235/46 , C07C235/70 , C07D213/56 , C07D213/65 , C07D213/74 , C07D213/82 , C07D213/89
CPC分类号： C07D213/74 , C07C235/42 , C07C235/46 , C07C2601/08 , C07C2601/14 , C07D213/65 , C07D213/82 , C07D213/89
摘要： This invention provides a compound of the formula (I): wherein X represents a carbon atom or the like: Y represents imino, or the like: R1 represents an alkyl group having from 1 to 6 carbon atoms or the like: R2 and R3 independently represents a hydrogen atom 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X表示碳原子等：Y表示亚氨基等：R 1表示具有1至6个碳原子的烷基 R 2，R 3和R 3独立地表示氢原子等。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。

5. 发明授权

US08084476B2 Substituted methyl aryl or heteroaryl amide compounds 有权
标题翻译：取代的甲基芳基或杂芳基酰胺化合物
公开(公告)号：US08084476B2
公开(公告)日：2011-12-27
申请号：US12368778
申请日：2009-02-10
申请人： Hiroki Koike , Kana Kon-i , Yukari Matsumoto , Kazunari Nakao , Yoshiyuki Okumura , Tatsuya Yamagishi
发明人： Hiroki Koike , Kana Kon-i , Yukari Matsumoto , Kazunari Nakao , Yoshiyuki Okumura , Tatsuya Yamagishi
IPC分类号： A61K31/44 , C07D211/72
CPC分类号： C07D213/74 , C07C235/42 , C07C235/46 , C07C2601/08 , C07C2601/14 , C07D213/65 , C07D213/82 , C07D213/89
摘要： This invention provides a compound of the formula (I): wherein X represents a carbon atom or the like: Y represents imino, or the like: R1 represents an alkyl group having from 1 to 6 carbon atoms or the like: R2 and R3 independently represents a hydrogen atom 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X表示碳原子等：Y表示亚氨基等：R 1表示具有1至6个碳原子的烷基等：R 2和R 3独立地表示氢原子等。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。

6. 发明申请

US20090163558A1 Substituted Methyl Aryl or Heteroaryl Amide Compounds 有权
标题翻译：取代的甲基芳基或杂芳基酰胺化合物
公开(公告)号：US20090163558A1
公开(公告)日：2009-06-25
申请号：US12368778
申请日：2009-02-10
申请人： Hiroki Koike , Kana Kon-i , Yukari Matsumoto , Kazunari Nakao , Yoshiyuki Okumura , Tatsuya Yamagishi
发明人： Hiroki Koike , Kana Kon-i , Yukari Matsumoto , Kazunari Nakao , Yoshiyuki Okumura , Tatsuya Yamagishi
IPC分类号： A61K31/44 , C07D213/56
CPC分类号： C07D213/74 , C07C235/42 , C07C235/46 , C07C2601/08 , C07C2601/14 , C07D213/65 , C07D213/82 , C07D213/89
摘要： This invention provides a compound of the formula (I): wherein X represents a carbon atom or the like: Y represents imino, or the like: R1 represents an alkyl group having from 1 to 6 carbon atoms or the like: R2 and R3 independently represents a hydrogen atom 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X表示碳原子等：Y表示亚氨基等：R 1表示具有1至6个碳原子的烷基等：R 2和R 3独立地表示氢原子等。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。

7. 发明授权

US07534914B2 Substituted methyl aryl or heteroaryl amide compounds 失效
标题翻译：取代的甲基芳基或杂芳基酰胺化合物
公开(公告)号：US07534914B2
公开(公告)日：2009-05-19
申请号：US11118497
申请日：2005-04-29
申请人： Hiroki Koike , Kana Kon-i , Yukari Matsumoto , Kazunari Nakao , Yoshiyuki Okumura , Tatsuya Yamagishi
发明人： Hiroki Koike , Kana Kon-i , Yukari Matsumoto , Kazunari Nakao , Yoshiyuki Okumura , Tatsuya Yamagishi
IPC分类号： C07C229/00
CPC分类号： C07D213/74 , C07C235/42 , C07C235/46 , C07C2601/08 , C07C2601/14 , C07D213/65 , C07D213/82 , C07D213/89
摘要： This invention provides a compound of the formula (I): wherein X represents a carbon atom or the like: Y represents imino, or the like: R1 represents an alkyl group having from 1 to 6 carbon atoms or the like: R2 and R3 independently represents a hydrogen atom 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X表示碳原子等：Y表示亚氨基等：R 1表示具有1至6个碳原子的烷基等：R 2和R 3独立地表示氢原子等。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。

8. 发明申请

US20110275628A1 NOVEL PYRAZOLE-3-CARBOXAMIDE DERIVATIVE HAVING 5-HT2B RECEPTOR ANTAGONIST ACTIVITY 有权
标题翻译：具有5-HT2B受体拮抗剂活性的新型吡唑-3-羧酰胺衍生物
公开(公告)号：US20110275628A1
公开(公告)日：2011-11-10
申请号：US13129916
申请日：2009-11-24
申请人： Tatsuya Yamagishi , Kiyoshi Kawamura , Tadashi Inoue , Yuji Shishido , Hiroaki Ito
发明人： Tatsuya Yamagishi , Kiyoshi Kawamura , Tadashi Inoue , Yuji Shishido , Hiroaki Ito
IPC分类号： A61K31/5377 , C07D413/14 , C07D471/04 , A61P1/00 , A61P25/24 , A61P19/02 , A61P25/28 , A61P31/14 , A61P31/12 , A61P25/00 , C07D413/12 , A61P17/02
CPC分类号： C07D487/04 , A61K31/415 , A61K31/4155 , A61K31/437 , A61K31/454 , A61K31/5377 , A61K31/553 , C07D231/14 , C07D401/04 , C07D401/14 , C07D403/04 , C07D409/04 , C07D413/14 , C07D417/04 , C07D471/04
摘要： Disclosed is a compound represented by general formula (I) or a pharmaceutically acceptable salt thereof, which is useful as a selective antagonist of a 5-HT2B receptor. The compound and salt are useful for treatment or prevention of various diseases and conditions associated with a 5-HT2B receptor.
摘要翻译：公开了通式（I）表示的化合物或其药学上可接受的盐，其可用作5-HT 2B受体的选择性拮抗剂。该化合物和盐可用于治疗或预防与5-HT 2B受体相关的各种疾病和病症。

9. 发明申请

US20140336377A1 ARYLAMIDE DERIVATIVES AS TTX-S BLOCKERS 有权
标题翻译： ARYLAMIDE衍生物作为TTX-S阻挡剂
公开(公告)号：US20140336377A1
公开(公告)日：2014-11-13
申请号：US13879673
申请日：2011-10-18
申请人： Tatsuya Yamagishi , Kiyoshi Kawamura , Yoshimasa Arano , Mikio Morita
发明人： Tatsuya Yamagishi , Kiyoshi Kawamura , Yoshimasa Arano , Mikio Morita
IPC分类号： C07D213/64 , C07D213/75 , C07D239/42 , C07D471/04 , C07D413/12 , C07D413/14 , C07D401/12 , C07D401/14
CPC分类号： C07D213/64 , A61K31/44 , A61K31/4427 , A61K31/444 , A61K31/506 , C07D213/75 , C07D213/81 , C07D239/42 , C07D401/12 , C07D401/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04
摘要： The present invention relates to arylamide derivatives which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of disorders and diseases in which voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which voltage gated sodium channels are involved.
摘要翻译：本发明涉及具有电压门控钠通道作为TTX-S通道的阻断活性的芳基酰胺衍生物，其可用于治疗或预防涉及电压门控钠通道的疾病和疾病。本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及电压门控钠通道的疾病中的用途。

10. 发明申请

US20090291977A1 Chromane Derivatives Useful As Acid Pump Antagonists 审中-公开
标题翻译：色氨酸衍生物可用作酸泵拮抗剂
公开(公告)号：US20090291977A1
公开(公告)日：2009-11-26
申请号：US11721453
申请日：2005-12-07
申请人： Madoka Jinno , Hirohisa Shimokawa , Tatsuya Yamagishi
发明人： Madoka Jinno , Hirohisa Shimokawa , Tatsuya Yamagishi
IPC分类号： A61K31/437 , C07D471/04
CPC分类号： C07D471/04
摘要： This invention relates to compounds of the formula (I): or a pharmaceutically acceptable salt thereof, wherein: R′, R2, R3, R4, R5, R6, R7, R8 A and B are each as described herein or a pharmaceutically acceptable salt, and compositions containing such compounds and the method of treatment and the use, comprising such compounds for the treatment of a condition mediated by acid pump antagonistic activity such as, but not limited to, as gastrointestinal disease, gastroesophageal disease, gastroesophageal reflux disease (GERD), peptic ulcer, gastric ulcer, duodenal ulcer, NSAID-induced ulcers, gastritis, infection of Helicobacter pylori, dyspepsia, functional dyspepsia, Zollinger-Ellison syndrome, non-crosive reflux disease (NERD), visceral pain, heartburn, nausea, esophagitis, dysphagia, hypersalivation, airway disorders or asthma.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐，其中：R'，R 2，R 3，R 4，R 5，R 6，R 7，R 8 A和B各自如本文所述，或其药学上可接受的盐，以及含有这些化合物的组合物及其治疗和使用方法，包括用于治疗由酸泵拮抗活性（例如但不限于胃肠道疾病，胃食管疾病，胃食管反流病（GERD）），消化性溃疡，胃溃疡，十二指肠溃疡，NSAID诱导的溃疡，胃炎，幽门螺杆菌感染，消化不良，功能性消化不良，佐林格 - 埃利森综合征，非交叉性反流病（NERD），内脏痛，胃灼热，恶心，食管炎，吞咽困难，过度激活，气道障碍或哮喘。

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