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1. 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。

2. 发明申请

US20080207690A1 Benzisoxazole Derivatives 有权
标题翻译：苯并异恶唑衍生物
公开(公告)号：US20080207690A1
公开(公告)日：2008-08-28
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： A61K31/454 , C07D401/12 , A61P1/04 , C07D401/14
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）化合物：其中A，B，R 1，R 4，m和n各自如本文所述，或药学上可接受的其盐和含有这些化合物的组合物以及这些化合物在治疗5-HT 4受体活性介导的病症中的用途，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。

3. 发明授权

US06624162B2 Imidazopyridine compounds as 5-HT4 receptor modulators 失效
标题翻译：咪唑并吡啶化合物作为5-HT4受体调节剂
公开(公告)号：US06624162B2
公开(公告)日：2003-09-23
申请号：US10251109
申请日：2002-09-20
申请人： Chikara Uchida , Hirohide Noguchi , Alan Stobie , Geoffrey Gymer , David Fenwick
发明人： Chikara Uchida , Hirohide Noguchi , Alan Stobie , Geoffrey Gymer , David Fenwick
IPC分类号： A61K31437
CPC分类号： C07D471/04
摘要： This invention provides a compound of the formula (I): or the pharmaceutically acceptable salts thereof wherein R1 is hydrogen, halo or alkyl; R2 and R3 are independently hydrogen, alkyl, alkenyl, alkynyl, aminoalkyl or hydroxyalkyl; or R2 and R3 taken together with the nitrogen atom to which they are attached may form hetrocyclic; R4 is hydrogen, halo, acyl, amino, amido, aryl, arylalkyl, or heteroaryl; R5 is hydrogen, halo, alkyl alkenyl, alkynyl, acyl, amino, amido, aryl, arylalkyl, or heteroaryl; R6 is hydrogen, alkyl or alkoxyalkyl; X is NR9 wherein R9 is hydrogen or alkyl; and Y is (CR7R8)n wherein n is an integer from 0 to 5. These compounds have 5-HT4 receptor binding 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. 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R 1是氢，卤素或烷基; R 2和R 3独立地是氢，烷基，烯基，炔基，氨基烷基或羟烷基; 或R 2和R 3与它们所连接的氮原子一起可以形成环状的; R 4是氢，卤素，酰基，氨基，酰氨基，芳基，芳基烷基或杂芳基; R 5是氢，卤素，烷基烯基，炔基，酰基，氨基，酰氨基，芳基，芳基烷基或杂芳基; R 6是氢，烷基或烷氧基烷基; X是NR 9，其中R 9是氢或烷基; 并且Y是（CR 7 R 8）n，其中n是0至5的整数。这些化合物具有5-HT 4受体结合活性，因此可用于治疗胃食管反流病，非溃疡性消化不良，功能性消化不良，肠易激综合征等。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

US06951867B2 N-substituted piperidinyl-imidazopyridine compounds as 5-HT4 receptor modulators 失效
标题翻译： N-取代的哌啶基 - 咪唑并吡啶化合物作为5-HT 4受体调节剂
公开(公告)号：US06951867B2
公开(公告)日：2005-10-04
申请号：US10667182
申请日：2003-09-17
申请人： Yasuhiro Katsu , Kana Kon-I , Mikio Morita , Hirohide Noguchi , Chikara Uchida
发明人： Yasuhiro Katsu , Kana Kon-I , Mikio Morita , Hirohide Noguchi , Chikara Uchida
IPC分类号： C07D471/04 , A61K31/437 , A61P1/04
CPC分类号： C07D471/04
摘要： This invention provides a compound of the formula (I): or a pharmaceutically acceptable salt, amide or ester thereof, wherein R1 represents a hydrogen atom or a halogen atom; R2 represents a hydrogen atom, etc.; R3 represents an alkyl group having from 1 to 10 carbon atoms; said alkyl group of R3 is substituted by at least one substituent selected from the group consisting of substituents α; said substituents α is aryl, hydroxy, oxo, etc.; said aryl having 6 to 10 carbon atoms; said aryl is unsubstituted or substituted by at least one alkyl group having from 1 to 6 carbon atoms; said heterocyclic and the heterocyclic moiety of said heterocycliccarbonyl, both of substituents α, are 5- to 10-membered cyclic groups containing from 1 to 4 heteroatoms selected from the group consisting of nitrogen atoms, oxygen atoms and sulfur atoms These compounds have 5-HT4 receptor binding 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. 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，酰胺或酯，其中R 1表示氢原子或卤素原子; R 2表示氢原子等; R 3表示具有1至10个碳原子的烷基; 所述R 3的烷基被至少一个选自取代基α的取代基取代; 所述取代基α是芳基，羟基，氧代等; 所述芳基具有6至10个碳原子; 所述芳基是未取代的或被至少一个具有1至6个碳原子的烷基取代; 所述杂环基和所述杂环羰基的杂环部分，两个取代基α为含有1至4个选自氮原子，氧原子和硫原子的杂原子的5至10元环基这些化合物具有5-HT 受体结合活性，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。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

US07012080B2 Imidazopyridine compounds as 5-HT4 receptor agonists 失效
标题翻译：咪唑并吡啶化合物作为5-HT4受体激动剂
公开(公告)号：US07012080B2
公开(公告)日：2006-03-14
申请号：US10667188
申请日：2003-09-17
申请人： Satoru Iguchi , Yasuhiro Katsu , Kana Kon-I , Hirohide Noguchi , Chikara Uchida
发明人： Satoru Iguchi , Yasuhiro Katsu , Kana Kon-I , Hirohide Noguchi , Chikara Uchida
IPC分类号： A61K31/437 , C07D471/04 , A61P1/04
CPC分类号： C07D471/04
摘要： This invention provides a compound of the formula (I): or a pharmaceutically acceptable salt thereof, wherein R1 represents a hydrogen atom or a halogen atom; R2 represents a methyl group or an ethyl group; R3 represents a branched alkyl group having from 3 to 6 carbon atoms or an alkyl group having from 3 to 6 carbon atoms substituted by an alkoxy group having from 1 to 6 carbon atoms; with the proviso that when the terminal carbon atom of said alkyl group of R3 is substituted by said alkoxy group, said alkyl group is a branched alkyl group. These compounds have 5-HT4 receptor binding 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. 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R 1表示氢原子或卤素原子; R 2表示甲基或乙基; R 3表示具有3至6个碳原子的支链烷基或具有3至6个碳原子的烷基，被具有1至6个碳原子的烷氧基取代; 条件是当所述R 3烷基的末端碳原子被所述烷氧基取代时，所述烷基是支链烷基。这些化合物具有5-HT 4受体结合活性，因此可用于治疗哺乳动物，特别是人类中的胃食管反流病，非溃疡性消化不良，功能性消化不良，肠易激综合征等。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

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。

7. 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。

8. 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。

9. 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。

10. 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。

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