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1. 发明授权

US06531492B1 Heterocyclo-alkylsulfonyl pyrazole derivatives as anti-inflammatory/analgesic agents 失效
标题翻译：杂环烷基磺酰基吡唑衍生物作为抗炎/止痛剂
公开(公告)号：US06531492B1
公开(公告)日：2003-03-11
申请号：US09724446
申请日：2000-11-28
申请人： Kristin M. Lundy , Hengmiao Cheng , Subas M. Sakya , Jin Li , Martha L. Minich , Chikara Uchida
发明人： Kristin M. Lundy , Hengmiao Cheng , Subas M. Sakya , Jin Li , Martha L. Minich , Chikara Uchida
IPC分类号： C07D40104
CPC分类号： C07D401/14 , C07D403/04 , C07D405/14
摘要： The present invention relates to compounds of the formula wherein R2, R3, R6 and A are defined as in the specification, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the invention are useful in the treatment or alleviation of inflammation and other inflammation associated disorders, such as osteoarthritis, rheumatoid arthritis, colon cancer and Alzheimer's disease, in mammals (preferably humans, dogs, cats and livestock).
摘要翻译：本发明涉及式R 2，R 3，R 6和A的化合物在说明书中定义为含有它们的药物组合物及其药物用途。本发明的化合物可用于治疗或缓解哺乳动物（优选人，狗，猫和家畜）中的炎症和其它炎症相关疾病，例如骨关节炎，类风湿性关节炎，结肠癌和阿尔茨海默氏病。

2. 发明申请

US20100273794A1 Benzimidazolone Compounds Having 5-HT4 Receptor Agonistic Activity 审中-公开
标题翻译：具有5-HT4受体激动活性的苯并咪唑酮化合物
公开(公告)号：US20100273794A1
公开(公告)日：2010-10-28
申请号：US12831713
申请日：2010-07-07
申请人： Yasuhiro Katsu , Satoru Iguchi , Hiroki Sone , Chikara Uchida , Takashi Kojima
发明人： Yasuhiro Katsu , Satoru Iguchi , Hiroki Sone , Chikara Uchida , Takashi Kojima
IPC分类号： A61K31/5377 , C07D211/26 , A61K31/454 , C07D413/14 , A61P1/04 , A61P1/00 , A61P9/00 , A61P25/06 , A61P25/28 , A61P29/00
CPC分类号： C07D413/14 , C04B35/632 , C07D401/12 , C07D405/06 , C07D405/14
摘要： This invention provides a compound of the formula (I): or a pharmaceutically acceptable salt thereof, and compositions containing such compounds and the use of such compounds for the manufacture of medicament for gastroesophageal reflux disease, gastrointestinal disease, gastric motility disorder, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome (IBS), constipation, dyspepsia, esophagitis, gastroesophageral disease, nausea, central nervous system disease, Alzheimer's disease, cognitive disorder, emesis, migraine, neurological disease, pain, cardiovascular disorders, cardiac failure, heart arrhythmia, diabetes and apnea syndrome.These compounds have 5-HT4 receptor agonistic activity, and thus are useful for the treatment of gastroesophageal reflux disease, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome or the like in mammalian, especially humans.
摘要翻译：本发明提供式（I）化合物或其药学上可接受的盐，以及含有这些化合物的组合物以及这些化合物在制备胃食管反流疾病，胃肠道疾病，胃动力障碍，非溃疡的药物中的用途消化不良，功能性消化不良，肠易激综合征（IBS），便秘，消化不良，食管炎，胃食管疾病，恶心，中枢神经系统疾病，阿尔茨海默病，认知障碍，呕吐，偏头痛，神经系统疾病，疼痛，心血管疾病，心力衰竭，心脏心律失常，糖尿病和呼吸暂停综合征。这些化合物具有5-HT 4受体激动活性，因此可用于治疗哺乳动物特别是人类的胃食管反流病，非溃疡性消化不良，功能性消化不良，肠易激综合征等。

3. 发明申请

US20080108660A1 Benzimidazolone Carboxylic Acid Derivatives 审中-公开
标题翻译：苯并咪唑酮羧酸衍生物
公开(公告)号：US20080108660A1
公开(公告)日：2008-05-08
申请号：US11971265
申请日：2008-01-09
申请人： Koji Ando , Satoru Iguchi , Noriaki Murase , Yoshinori Murata , Toyoharu Numata , Hiroki Sone , Chikara Uchida , Tatsuo Ueki
发明人： Koji Ando , Satoru Iguchi , Noriaki Murase , Yoshinori Murata , Toyoharu Numata , Hiroki Sone , Chikara Uchida , Tatsuo Ueki
IPC分类号： A61K31/445 , C07D403/02 , A61P1/00 , C07D211/06 , A61K31/4164
CPC分类号： C07D401/12 , C07D211/26 , C07D401/06 , C07D401/14 , C07D405/06 , C07D405/14
摘要： This invention relates to compounds of the formula (I): wherein R1, R2, R3, A and m are each as described herein or a pharmaceutically acceptable salt or solvate thereof, and compositions containing such compounds and the use of such compounds in the treatment of a condition mediated by 5-HT4 receptor activity such as, but not limited to, gastroesophageal reflux disease, gastrointestinal disease, gastric motility disorder, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome (IBS), constipation, dyspepsia, esophagitis, gastroesophageal disease, nausea, central nervous system disease, Alzheimer's disease, cognitive disorder, emesis, migraine, neurological disease, pain, cardiovascular disorders such as cardiac failure and heart arrhythmia, diabetes and apnea syndrome.
摘要翻译：本发明涉及式（I）化合物：其中R 1，R 2，R 3，A和m各自如上所述本文或其药学上可接受的盐或溶剂合物，以及含有这些化合物的组合物以及这些化合物在治疗由5-HT 4受体活性介导的病症中的用途，所述活性例如但不限于，胃食管反流病，胃肠道疾病，胃动力障碍，非溃疡性消化不良，功能性消化不良，肠易激综合征（IBS），便秘，消化不良，食管炎，胃食管疾病，恶心，中枢神经系统疾病，阿尔茨海默病，认知障碍，呕吐，偏头痛，神经系统疾病，疼痛，心血管疾病如心力衰竭和心律失常，糖尿病和呼吸暂停综合征。

4. 发明申请

US20060194842A1 Oxyindole derivatives 失效
标题翻译：氧吲哚衍生物
公开(公告)号：US20060194842A1
公开(公告)日：2006-08-31
申请号：US11360095
申请日：2006-02-22
申请人： Chikara Uchida , Hiroki Sone , Kiyoshi Kawamura
发明人： Chikara Uchida , Hiroki Sone , Kiyoshi Kawamura
IPC分类号： A61K31/454 , C07D417/14 , C07D413/14 , C07D403/14
CPC分类号： C07D401/12 , C07D401/14 , C07D405/14
摘要： This invention relates to compounds of the formula (I): or a pharmaceutically acceptable salt thereof, wherein: A, R1, R2, R3, R4 and R5 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 5-HT4 agonistic activity such as, but not limited to, as gastroesophageal reflux disease, gastrointestinal disease, gastric motility disorder, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome (IBS), constipation, dyspepsia, esophagitis, gastroesophageal disease, nausea, central nervous system disease, Alzheimer's disease, cognitive disorder, emesis, migraine, neurological disease, pain, cardiovascular disorders, cardiac failure, heart arrhythmia, diabetes or apnea syndrome.
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，R 1，R 2，R 3， SUP，R 4和R 5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和这些化合物在治疗病症中的用途由5-HT 4激动剂活性介导，例如但不限于胃食管反流疾病，胃肠道疾病，胃动力障碍，非溃疡性消化不良，功能性消化不良，肠易激综合征（IBS），便秘，消化不良，食管炎，胃食管疾病，恶心，中枢神经系统疾病，阿尔茨海默病，认知障碍，呕吐，偏头痛，神经系统疾病，疼痛，心血管疾病，心力衰竭，心律失常，糖尿病或呼吸暂停综合征。

5. 发明授权

US07964727B2 Quinolonecarboxylic acid compounds having 5-HT4 receptor agonistic activity 失效
标题翻译：具有5-HT 4受体激动活性的喹诺酮羧酸化合物
公开(公告)号：US07964727B2
公开(公告)日：2011-06-21
申请号：US10595948
申请日：2004-11-10
申请人： Tomoki Kato , Kiyoshi Kawamura , Mikio Morita , Chikara Uchida
发明人： Tomoki Kato , Kiyoshi Kawamura , Mikio Morita , Chikara Uchida
IPC分类号： C07D221/02 , C07D215/00 , C07D413/00 , A01N43/40 , A01N43/42 , A61K31/435 , A61K31/44
CPC分类号： C04B35/632 , C07D401/12 , C07D401/14 , C07D405/14
摘要： This invention provides a compound of the formula (I): wherein Het represents a heterocyclic group having one nitrogen atom, to which B binds directly, and from 4 to 7 carbon atoms, and said heterocyclic group being unsubstituted or substituted by 1 to 4 substituents independently selected from the group consisting of substituents α1; A represents an alkylene group having from 1 to 4 carbon atoms; B represents a covalent bond or an alkylene group having from 1 to 5 carbon atoms; R1 represents an isopropyl group, a n-propyl group or a cyclopentyl group; R2 represents a methyl group, a fluorine atom or a chlorine atom; R3 independently represents (i) an oxo group, a hydroxy group, an amino group, an alkylamino group or a carboxyl group; (ii) a cycloalkyl group having from 3 to 8 carbon atoms, and said cycloalkyl group being substituted by 1 to 5 substituents, or (iii) a heterocyclic group having from 3 to 8 atoms, and said heterocyclic group being unsubstituted or substituted by 1 to 5 substituents, and n is 1, 2 or 3, or a pharmaceutically acceptable salts thereof. These compounds have 5-HT4 receptor agonistic activity, and thus are useful for the treatment of gastroesophageal reflux disease, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome or the like in mammalian, especially humans.
摘要翻译：本发明提供式（I）化合物：其中Het表示具有一个氮原子的杂环基团，B直接与该碳原子结合，并且具有4至7个碳原子，所述杂环基团未被取代或被1至4个取代基取代独立地选自取代基α1; A表示具有1至4个碳原子的亚烷基; B表示共价键或具有1至5个碳原子的亚烷基; R1表示异丙基，正丙基或环戊基; R2表示甲基，氟原子或氯原子; R3独立地表示（i）氧代基，羟基，氨基，烷基氨基或羧基; （ii）具有3至8个碳原子的环烷基，所述环烷基被1至5个取代基取代，或（iii）具有3至8个原子的杂环基，所述杂环基未被取代或被1 至5个取代基，n为1,2或3，或其药学上可接受的盐。这些化合物具有5-HT 4受体激动活性，因此可用于治疗哺乳动物特别是人类的胃食管反流病，非溃疡性消化不良，功能性消化不良，肠易激综合征等。

6. 发明授权

US07589109B2 Oxyindole derivatives 失效
标题翻译：氧吲哚衍生物
公开(公告)号：US07589109B2
公开(公告)日：2009-09-15
申请号：US11360095
申请日：2006-02-22
申请人： Chikara Uchida , Hiroki Sone , Kiyoshi Kawamura
发明人： Chikara Uchida , Hiroki Sone , Kiyoshi Kawamura
IPC分类号： A61K31/454 , C07D403/14
CPC分类号： C07D401/12 , C07D401/14 , C07D405/14
摘要： This invention relates to compounds of the formula (I): or a pharmaceutically acceptable salt thereof, wherein: A, R1, R2, R3, R4 and R5 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 5-HT4 agonistic activity such as, but not limited to, as gastroesophageal reflux disease, gastrointestinal disease, gastric motility disorder, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome (IBS), constipation, dyspepsia, esophagitis, gastroesophageal disease, nausea, central nervous system disease, Alzheimer's disease, cognitive disorder, emesis, migraine, neurological disease, pain, cardiovascular disorders, cardiac failure, heart arrhythmia, diabetes or apnea syndrome.
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，R 1，R 2，R 3，R 4和R 5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和使用这些化合物治疗由5-HT4激动活性介导的病症，例如但不限于胃食道反流病，胃肠道疾病，胃动力障碍，非溃疡性消化不良，功能性消化不良，肠易激综合征（IBS）），便秘，消化不良，食道炎，胃食管疾病，恶心，中枢神经系统疾病，阿尔茨海默病，认知障碍，呕吐，偏头痛，神经系统疾病，疼痛，心血管疾病，心力衰竭，心律失常，糖尿病或呼吸暂停综合征。

7. 发明申请

US20080293767A1 1-Isopropyl-2-Oxo-1,2-Dihydropyridine-3-Carboxamide Derivatives Having 5-Ht4 Receptor Agonistic Activity 失效
标题翻译：具有5-Ht4受体激动活性的1-异丙基-2-氧代-1,2-二氢吡啶-3-甲酰胺衍生物
公开(公告)号：US20080293767A1
公开(公告)日：2008-11-27
申请号：US10597480
申请日：2005-01-18
申请人： Tomoki Kato , Kiyoshi Kawamura , Chikara Uchida
发明人： Tomoki Kato , Kiyoshi Kawamura , Chikara Uchida
IPC分类号： A61K31/4545 , A61P3/00 , A61P25/00 , A61P1/00 , A61P9/00 , C07D405/14 , C07D401/12
CPC分类号： C07D401/12 , C07D405/14
摘要： This invention provides a compound of formula (I): wherein R1 represents an alkyl group having from 1 to 4 carbon atoms or a halogen atom, R2 represents an alkyl group having from 1 to 4 carbon atoms, R3 represents a hydrogen atom or a hydroxy group, and A represents an oxygen atom or a group of the formula —C(R4)(R5)— (in which R4 represents a hydrogen atom or an alkyl group having from 1 to 4 carbon atoms and R5 represents a hydroxy group or an alkoxy group having from 1 to 4 carbon atoms) or a pharmaceutically acceptable salts thereof. These compounds have 5-HT4 receptor agonistic activity, and thus are useful for the treatment of gastroesophageal reflux disease, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome or the like in mammalian, especially humans.
摘要翻译：本发明提供式（I）化合物：其中R 1表示具有1至4个碳原子的烷基或卤原子，R 2表示具有1至4个碳原子的烷基，R 3表示氢原子或羟基基团，A表示氧原子或式-C（R4）（R5） - （其中R4表示氢原子或具有1至4个碳原子的烷基，R5表示羟基或式具有1至4个碳原子的烷氧基）或其药学上可接受的盐。这些化合物具有5-HT 4受体激动活性，因此可用于治疗哺乳动物特别是人类的胃食管反流病，非溃疡性消化不良，功能性消化不良，肠易激综合征等。

8. 发明授权

US08816090B2 Benzisoxazole derivatives 有权
标题翻译：苯并异恶唑衍生物
公开(公告)号：US08816090B2
公开(公告)日：2014-08-26
申请号：US11814588
申请日：2006-02-15
申请人： Hirohide Noguchi , Isao Sakurada , Chikara Uchida , Nobuaki Waizumi
发明人： Hirohide Noguchi , Isao Sakurada , Chikara Uchida , Nobuaki Waizumi
IPC分类号： C07D261/20 , A61K31/4439
CPC分类号： C07D413/12 , C07D413/14
摘要： This invention relates to compounds of the formula (I): wherein A, B, R1, R4, m, and n are each as described herein or a pharmaceutically acceptable salt thereof, and compositions containing such compounds and the use of such compounds in the treatment of a condition mediated by 5-HT4 receptor activity such as, but not limited to, gastroesophageal reflux disease, gastrointestinal disease, gastric motility disorder, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome (IBS), constipation, dyspepsia, esophagitis, gastroesophageral disease, nausea, central 10 nervous system disease, Alzheimer's disease, cognitive disorder, emesis, migraine, neurological disease, pain, cardiovascular disorders such as cardiac failure and heart arrhythmia, diabetes and apnea syndrome.
摘要翻译：本发明涉及式（I）的化合物：其中A，B，R 1，R 4，m和n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和这些化合物在治疗由5-HT4受体活性介导的病症，例如但不限于胃食管反流病，胃肠道疾病，胃动力障碍，非溃疡性消化不良，功能性消化不良，肠易激综合征（IBS），便秘，消化不良，食管炎，胃肠疾病，恶心，中枢10神经系统疾病，阿尔茨海默病，认知障碍，呕吐，偏头痛，神经系统疾病，疼痛，心力衰竭和心律失常等心血管疾病，糖尿病和呼吸暂停综合征。

9. 发明授权

US08362038B2 1-isopropyl-2-oxo-1,2-dihydropyridine-3-carboxamide derivatives having 5-HT4 receptor agonistic activity 失效
标题翻译：具有5-HT 4受体激动活性的1-异丙基-2-氧代-1,2-二氢吡啶-3-甲酰胺衍生物
公开(公告)号：US08362038B2
公开(公告)日：2013-01-29
申请号：US12708012
申请日：2010-02-18
申请人： Tomoki Kato , Kiyoshi Kawamura , Chikara Uchida
发明人： Tomoki Kato , Kiyoshi Kawamura , Chikara Uchida
IPC分类号： A61K31/4545 , C07D401/12
CPC分类号： C07D401/12 , C07D405/14
摘要： This invention provides a compound of formula (I): wherein R1 represents an alkyl group having from 1 to 4 carbon atoms or a halogen atom, R2 represents an alkyl group having from 1 to 4 carbon atoms, R3 represents a hydrogen atom or a hydroxy group, and A represents an oxygen atom or a group of the formula —C(R4)(R5)— (in which R4 represents a hydrogen atom or an alkyl group having from 1 to 4 carbon atoms and R5 represents a hydroxy group or an alkoxy group having from 1 to 4 carbon atoms) or a pharmaceutically acceptable salts thereof. These compounds have 5-HT4 receptor agonistic activity, and thus are useful for the treatment of gastroesophageal reflux disease, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome or the like in mammalian, especially humans.
摘要翻译：本发明提供式（I）化合物：其中R 1表示具有1至4个碳原子的烷基或卤原子，R 2表示具有1至4个碳原子的烷基，R 3表示氢原子或羟基基团，A表示氧原子或式-C（R4）（R5） - （其中R4表示氢原子或具有1至4个碳原子的烷基，R5表示羟基或式具有1至4个碳原子的烷氧基）或其药学上可接受的盐。这些化合物具有5-HT 4受体激动活性，因此可用于治疗哺乳动物特别是人类的胃食管反流病，非溃疡性消化不良，功能性消化不良，肠易激综合征等。

10. 发明授权

US07776885B2 Benzimidazolone compounds having 5-HT4 receptor agonistic activity 有权
标题翻译：具有5-HT 4受体激动活性的苯并咪唑酮化合物
公开(公告)号：US07776885B2
公开(公告)日：2010-08-17
申请号：US10933629
申请日：2004-09-02
申请人： Yasuhiro Katsu , Satoru Iguchi , Hiroki Sone , Chikara Uchida , Takashi Kojima
发明人： Yasuhiro Katsu , Satoru Iguchi , Hiroki Sone , Chikara Uchida , Takashi Kojima
IPC分类号： A61K31/454 , C07D471/04
CPC分类号： C07D413/14 , C04B35/632 , C07D401/12 , C07D405/06 , C07D405/14
摘要： This invention provides a compound of the formula (I): or a pharmaceutically acceptable salt thereof, and compositions containing such compounds and the use of such compounds for the manufacture of medicament for gastroesophageal reflux disease, gastrointestinal disease, gastric motility disorder, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome (IBS), constipation, dyspepsia, esophagitis, gastroesophageral disease, nausea, central nervous system disease, Alzheimer's disease, cognitive disorder, emesis, migraine, neurological disease, pain, cardiovascular disorders, cardiac failure, heart arrhythmia, diabetes and apnea syndrome. These compounds have 5-HT4 receptor agonistic activity, and thus are useful for the treatment of gastroesophageal reflux disease, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome or the like in mammalian, especially humans.
摘要翻译：本发明提供式（I）化合物或其药学上可接受的盐，以及含有这些化合物的组合物以及这些化合物在制备胃食管反流疾病，胃肠道疾病，胃动力障碍，非溃疡的药物中的用途消化不良，功能性消化不良，肠易激综合征（IBS），便秘，消化不良，食管炎，胃食管疾病，恶心，中枢神经系统疾病，阿尔茨海默病，认知障碍，呕吐，偏头痛，神经系统疾病，疼痛，心血管疾病，心力衰竭，心脏心律失常，糖尿病和呼吸暂停综合征。这些化合物具有5-HT 4受体激动活性，因此可用于治疗哺乳动物特别是人类的胃食管反流病，非溃疡性消化不良，功能性消化不良，肠易激综合征等。

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