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1. 发明授权

US06608070B1 2,3-substituted indole compounds as anti-inflammatory and analgesic agents 失效
标题翻译： 2,3-取代的吲哚化合物作为抗炎和止痛剂
公开(公告)号：US06608070B1
公开(公告)日：2003-08-19
申请号：US09355494
申请日：1999-07-28
申请人： Kazunari Nakao , Rodney William Stevens , Kiyoshi Kawamura , Chikara Uchida , Hiroki Koike , Stephane Caron
发明人： Kazunari Nakao , Rodney William Stevens , Kiyoshi Kawamura , Chikara Uchida , Hiroki Koike , Stephane Caron
IPC分类号： A01N4390
CPC分类号： C07D401/06 , C07D209/18 , C07D401/10 , C07D403/06 , C07D405/06 , C07D405/10 , C07D409/06 , C07D409/10 , C07D413/06 , C07D417/06 , C07D417/10
摘要： This invention provides a compound of the following formula: or the pharmaceutically acceptable salts thereof wherein Z is OH, C1-6 alkoxy, —NR2R3 or heterocycle; Q is selected from the following: (a) an optionally substituted phenyl, (b) an optionally substituted 6-membered monocyclic aromatic group containing one, two, three or four nitrogen atom(s), (c) an optionally substituted 5-membered monocyclic aromatic group containing one heteroatom selected from O, S and N and optionally containing one, two or three nitrogen atom(s) in addition to said heteroatom, (d) an optionally substituted C3-7 cycloalkyl and (e) an optionally substituted benzo-fuzed heterocycle; R1 is hydrogen, C1-4 alkyl or halo; R2 and R3 are independently hydrogen, OH, C1-4 alkoxy, C1-4 alkyl or C1-4 alkyl substituted with halo, OH, C1-4 alkoxy or CN; X is independently selected from H, halo, C1-4 alkyl, halo-substituted C1-4 alkyl, OH, C1-4 alkoxy, halo-substituted C1-4 alkoxy, C1-4 alkylthio, NO2, NH2, di-(C1-4 alkyl)amino and CN; and n is 0, 1, 2, 3 and 4. This invention also provides a pharmaceutical composition useful for the treatment of a medical condition in which prostaglandins are implicated as pathogens.
摘要翻译：本发明提供下式的化合物或其药学上可接受的盐，其中Z是OH，C 1-6烷氧基，-NR 2 R 3或杂环; Q选自以下：（a）任选取代的苯基，（b）含有一个，两个，三个或四个氮原子的任选取代的6元单环芳族基团，（c）任选取代的5元含有一个选自O，S和N的杂原子，并且除了所述杂原子之外任选含有一个，两个或三个氮原子的单环芳基，（d）任选取代的C 3-7环烷基和（e）任选取代的苯并杂环杂环 R1是氢，C1-4烷基或卤素; R2和R3独立地是氢，OH，C1-4烷氧基，C1-4烷基或被卤素，OH，C1-4烷氧基或CN取代的C1-4烷基; X独立地选自H，卤素，C 1-4烷基，卤素取代的C 1-4烷基，OH，C 1-4烷氧基，卤素取代的C 1-4烷氧基，C 1-4烷硫基，NO 2，NH 2，二（C 1 -4烷基）氨基和CN; 并且n为0,1,2,3和4.本发明还提供了可用于治疗前列腺素作为病原体的医疗状况的药物组合物。

2. 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。

3. 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。

4. 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。

5. 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。

6. 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。

7. 发明授权

US07723321B2 Chromane substituted benzimidazole derivatives 有权
标题翻译：苯并二氢苯并咪唑衍生物
公开(公告)号：US07723321B2
公开(公告)日：2010-05-25
申请号：US11612583
申请日：2006-12-19
申请人： Takeshi Hanazawa , Hiroki Koike
发明人： Takeshi Hanazawa , Hiroki Koike
IPC分类号： A61K31/4184 , C07D405/02 , C07D407/02
CPC分类号： C07D405/12 , C07D409/12
摘要： This invention relates to compounds of the formula (I): or a pharmaceutically acceptable salt thereof, wherein: A, B, X, R1, R2, R3, R4, R5, R6, R7 and R8 are each as described herein or a pharmaceutically acceptable salt, and compositions containing such compounds and the use of such compounds in 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-erosive 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：A，B，X，R 1，R 2，R 3，R 4，R 5，R 6，R 7和R 8各自如本文所述，可接受的盐和含有这些化合物的组合物，以及这些化合物在治疗由酸泵拮抗活性（例如但不限于胃肠疾病，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诱发的溃疡，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，非侵蚀性反流病（NERD），内脏痛，胃灼热，恶心，食管炎，吞咽困难，过度激素，气道障碍或哮喘。

8. 发明授权

US07718809B2 Chromane substituted benzimidazole derivatives as acid pump antagonists 有权
标题翻译：色烷取代的苯并咪唑衍生物作为酸泵拮抗剂
公开(公告)号：US07718809B2
公开(公告)日：2010-05-18
申请号：US11916671
申请日：2006-06-02
申请人： Hiroki Koike , Sachiko Sakakibara
发明人： Hiroki Koike , Sachiko Sakakibara
IPC分类号： A61K31/4184 , C07D405/12
CPC分类号： C07D405/12 , C07D405/14
摘要： This invention relates to compounds of the formula (I): or a pharmaceutically acceptable salt thereof, wherein: A, B, X, R1, R2, R3, R4, R5 and R6, R7, R8 and R9 are each as described herein or a pharmaceutically acceptable salt, and compositions containing such compounds and the use of such compounds in 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-erosive 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：A，B，X，R 1，R 2，R 3，R 4，R 5和R 6，R 7，R 8和R 9各自如本文所述或药学上可接受的盐，以及含有这些化合物的组合物，以及这些化合物在治疗由酸泵拮抗活性介导的病症中的用途，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 - 埃里森综合征，非侵蚀性反流疾病（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。

9. 发明申请

US20100107744A1 SPECIMEN ANALYZING APPARATUS AND SPECIMEN ANALYZING METHOD 有权
标题翻译：样本分析设备和样本分析方法
公开(公告)号：US20100107744A1
公开(公告)日：2010-05-06
申请号：US12607739
申请日：2009-10-28
申请人： Kazuya FUKUDA , Hiroki Koike , Hironori Katsumi , Takashi Yamato , Masayuki Ikeda , Tsuyoshi Fukuzaki , Daisuke Nakano , Masanori Imazu , Nobuhiro Kitagawa
发明人： Kazuya FUKUDA , Hiroki Koike , Hironori Katsumi , Takashi Yamato , Masayuki Ikeda , Tsuyoshi Fukuzaki , Daisuke Nakano , Masanori Imazu , Nobuhiro Kitagawa
IPC分类号： G01N1/10 , G01N35/00
CPC分类号： G01N35/1065 , G01N35/00722 , G01N35/0092 , G01N35/025 , G01N35/026 , G01N35/1016 , G01N35/1079 , G01N35/1081 , G01N2035/00752 , G01N2035/00801 , G01N2035/0403 , G01N2035/0444 , G01N2035/1086
摘要： A specimen analyzing apparatus comprising: a detector for detecting component information regarding a component in a specimen contained in each of analyzing containers, the analyzing containers comprising first and second analyzing containers; an analyzing part for analyzing the component information detected by the detector; a transporting device for transporting specimen containers each containing a specimen, the specimen containers comprising first and second specimen containers; an operation mode selector for selecting one of a first operation mode and a second operation mode; a first supplying device for supplying the specimen of a first amount; a second supplying device for supplying the specimen of a second amount grater than the first amount; and a supply controller for controlling the first and second supplying devices in accordance with an operation mode selected by the operation mode selector, is disclosed. A specimen analyzing method is also disclosed.
摘要翻译：一种样本分析装置，包括：检测器，用于检测包含在每个分析容器中的样本中的成分的成分信息，所述分析容器包括第一和第二分析容器; 用于分析由检测器检测到的分量信息的分析部件; 一个运送装置，用于运送每个包含试样的标本容器，该样本容器包括第一和第二标本容器; 操作模式选择器，用于选择第一操作模式和第二操作模式之一; 第一供给装置，其供给第一量的试样; 第二供给装置，其供给比第一量的第二量磨机的试样; 以及用于根据由操作模式选择器选择的操作模式来控制第一和第二供应装置的供应控制器。还公开了一种样本分析方法。

10. 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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