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1. 发明授权

US06686373B2 Pyrazoloquinolinone derivatives as protein kinase C inhibitors 失效
标题翻译：吡唑啉酮衍生物作为蛋白激酶C抑制剂
公开(公告)号：US06686373B2
公开(公告)日：2004-02-03
申请号：US10191593
申请日：2002-07-09
申请人： Kiyoshi Kawamura , Sachiko Mihara , Seiji Nukui , Chikara Uchida
发明人： Kiyoshi Kawamura , Sachiko Mihara , Seiji Nukui , Chikara Uchida
IPC分类号： A61K314745
CPC分类号： C07D471/04
摘要： This invention provides a compound of the formula (I): or the pharmaceutically acceptable salts thereof wherein the dashed lines represent optional double bonds; C1, C2, C3 and C4 are carbon atom; R1 is C1-4 alkyl; R2 is H, amino, etc.; R3 is H, halo-CH2—, C2-8 alkyl or Q1-, wherein said C2-8 alkyl is optionally substituted with up to 3 substituents selected from halo, C1-3 alkyl, R4(R5)N, etc.; R4 is H, C1-7 alkyl, etc.; R5 is H, C1-7alkyl, etc.; R6 and R7 are independently selected from H and C1-4 alkyl; R8 is aryl or heteroaryl; Q1 is a 4-12 membered monocyclic or bicyclic aromatic, partially saturated or fully saturated ring optionally containing up to 4 heteroatoms selected from O, N and S, and is optionally substituted with halo, C1-4 alkyl, etc.; Y5, Y6, Y7 and Y8 are hydrogen; Y1, Y2, Y3 and Y4 are independently selected from hydrogen, halo, etc.; Q2 is a 5-12 membered monocyclic or bicyclic aromatic, partially saturated or fully saturated ring optionally containing up to 3 heteroatoms selected from O, N and S, and is optionally substituted with halo, C1-4alkyl-, etc.; These compounds have protein kinase C inhibitory activity and thus are useful for the treatment of neuropathic pain, acute or chronic inflammatory pain, auditory deficiency (synaptic repair), 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，其中虚线表示任选的双键; C 1，C 2，C 3和C 4是碳原子; R 1是C 1-4烷基; R 2是H，氨基等; R 3是H，卤代-CH 2 - ，C 2-8烷基或Q 1 - ，其中所述C 2-8烷基任选被至多3个选自卤素，C 1-3烷基，R 4，（R 5）N等; R 4是H，C 1-7烷基等; R 5是H，C 1-7烷基等; R 6和R 7独立地选自H和C 1-4烷基; R 8是芳基或杂芳基; Q 1是4-12元单环或双环芳族，部分饱和或完全饱和的环，任选地含有至多4个选自O，N和S的杂原子，并且任选地被卤素，C 1-4烷基等取代; Y 5，Y 6，Y 7和Y 8是氢; Y 1，Y 2，Y 3和Y 4独立地选自氢，卤素等; Q 2是5-12元单环或双环芳族，部分饱和或完全饱和的环，任选地含有至多3个选自O，N和S的杂原子，并且任选被卤素，C 1-4烷基等取代; 这些化合物具有蛋白激酶C抑制活性，因此可用于治疗哺乳动物，特别是人类的神经性疼痛，急性或慢性炎性疼痛，听觉缺陷（突触修复）等。本发明还提供了包含上述化合物的药物组合物。

2. 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.

3. 发明申请

US20080269211A1 Indazole Derivatives 失效
标题翻译：吲唑衍生物
公开(公告)号：US20080269211A1
公开(公告)日：2008-10-30
申请号：US11995179
申请日：2006-07-14
申请人： Asako Ishibashi , Tomoki Kato , Kiyoshi Kawamura , Sachiko Mihara , Mikio Morita
发明人： Asako Ishibashi , Tomoki Kato , Kiyoshi Kawamura , Sachiko Mihara , Mikio Morita
IPC分类号： A61K31/416 , A61P1/00 , A61P25/00 , A61P9/00 , C07D401/12 , C07D405/14 , A61K31/5377 , C07D403/12 , C07D413/14 , C07D401/14 , A61K31/454
CPC分类号： C07D401/12 , C07D403/12 , C07D405/14
摘要： This invention relates to compounds of the formula (I): or pharmaceutically acceptable salts thereof, wherein: R1, R2, R3, A and m are each as described herein 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, 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.
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 1，R 2，R 3， A和m各自如本文所述，含有这些化合物的组合物和这些化合物在治疗由5-HT 4激动剂活性介导的病症中的用途，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，阿尔茨海默氏病，认知障碍，呕吐，偏头痛，神经疾病，疼痛，心血管疾病，心力衰竭，心律失常，糖尿病和呼吸暂停综合征。

4. 发明授权

US07906532B2 Indazole derivatives 失效
标题翻译：吲唑衍生物
公开(公告)号：US07906532B2
公开(公告)日：2011-03-15
申请号：US11995179
申请日：2006-07-14
申请人： Asako Ishibashi , Tomoki Kato , Kiyoshi Kawamura , Sachiko Mihara , Mikio Morita
发明人： Asako Ishibashi , Tomoki Kato , Kiyoshi Kawamura , Sachiko Mihara , Mikio Morita
IPC分类号： A61K31/454 , A61K31/416 , C07D211/56 , C07D231/56
CPC分类号： C07D401/12 , C07D403/12 , C07D405/14
摘要： This invention relates to compounds of the formula (I): or pharmaceutically acceptable salts thereof, wherein: R1, R2, R3, A and m are each as described herein 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, 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.
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：R1，R2，R3，A和m各自如本文所述，含有这些化合物的组合物和这些化合物在治疗中的用途由5-HT4激动活性介导的病症，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，中枢神经系统疾病，阿尔茨海默病，认知障碍，呕吐，偏头痛，神经疾病，疼痛，心血管疾病，心力衰竭，心律失常，糖尿病和呼吸暂停综合征。

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

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。

9. 发明授权

US06300363B1 Indole compounds as COX-2 inhibitors 失效
标题翻译：吲哚化合物作为COX-2抑制剂
公开(公告)号：US06300363B1
公开(公告)日：2001-10-09
申请号：US09424837
申请日：1999-12-03
申请人： Rodney William Stevens , Kasumari Nakao , Kiyoshi Kawamura , Chikara Uchida , Shinya Fujiwara
发明人： Rodney William Stevens , Kasumari Nakao , Kiyoshi Kawamura , Chikara Uchida , Shinya Fujiwara
IPC分类号： A61K3140
CPC分类号： C07D401/06 , C07D209/40 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/06 , C07D405/12 , C07D409/06 , C07D409/12 , C07D413/06 , C07D413/12 , C07D417/06 , C07D417/12
摘要： This invention provides a compound of the following formula: and the pharmaceutically acceptable salts thereof, wherein L is oxygen or sulfur; Y is a direct bond or C1-4 alkylidene; Q is C1-6 alkyl, C3-7 cycloalkyl, phenyl, naphthyl, heteroaryl or the like; R1 is hydrogen, C1-6 alkyl or the like; R2 is hydrogen, C1-4 alkyl, C(O)R5 wherein R5 is C1-22 alkyl or C2-22 alkenyl, halosubstituted C1-8 alkyl, halosubstituted C2-8alkenyl, —Y—C3-7 cycloalkyl, —Y—C3-7 cycloalkenyl, phenyl, naphthyl, heteroaryl or the like; X is halo, C1-4 alkyl, hydroxy, C1-4 alkoxy or the like; and n is 0, 1, 2 or 3, with the proviso that a group of formula —Y—Q is not methyl or ethyl when X is hydrogen; L is oxygen; R1 is hydrogen; and R2 is acetyl. 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及其药学上可接受的盐，其中L是氧或硫; Y是直接键或C1-4亚烷基; Q为C 1-6烷基，C 3-7环烷基，苯基，萘基，杂芳基等; R1是氢，C1-6烷基等; R2是氢，C1-4烷基，C（O）R5，其中R5是C1-22烷基或C2-22链烯基，卤代C 1-8烷基，卤代C 2-8烯基，-Y-C 3-7环烷基，-Y-C 3 -7环烯基，苯基，萘基，杂芳基等; X是卤素，C 1-4烷基，羟基，C 1-4烷氧基等; 且n为0,1,2或3，条件是当X为氢时，式-Y-Q基团不是甲基或乙基; L是氧; R1是氢; 并且R 2是乙酰基。本发明还提供了可用于治疗前列腺素作为病原体的医学病症的药物组合物。

10. 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。

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