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1. 发明申请

US20120094964A1 SULFAMOYL BENZOIC ACID DERIVATIVES AS TRPM8 ANTAGONISTS 审中-公开
标题翻译：磺酰胆碱衍生物作为TRPM8拮抗剂
公开(公告)号：US20120094964A1
公开(公告)日：2012-04-19
申请号：US13318212
申请日：2010-05-06
申请人： Tadashi Inoue , Masashi Ohmi , Kiyoshi Kawamura , Kazuo Ando , Yuji Shishido
发明人： Tadashi Inoue , Masashi Ohmi , Kiyoshi Kawamura , Kazuo Ando , Yuji Shishido
IPC分类号： A61K31/635 , A61K31/18 , A61K31/495 , A61K31/4453 , A61K31/5377 , A61K31/444 , A61K31/4439 , C07D213/76 , C07C311/21 , C07D295/192 , C07D413/12 , C07D401/12 , A61P29/00 , A61P13/00 , A61P19/08 , A61P25/00 , A61P25/06 , A61P9/10 , A61P1/00 , A61P25/22 , A61P25/24 , A61P11/06 , A61P11/00 , A61P9/12 , A61P13/10 , A61P35/00 , A61P13/02 , A61K31/44
CPC分类号： C07C311/21 , A61K31/18 , A61K31/196 , A61K31/44 , A61K31/443 , A61K31/4436 , A61K31/4439 , A61K31/444 , A61K31/4453 , A61K31/4709 , A61K31/495 , A61K31/5375 , A61K31/5377 , A61K45/06 , C07D213/42 , C07D213/75 , C07D295/13 , C07D295/185 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/12 , C07D413/12 , C07D417/12 , A61K2300/00
摘要： The present invention relates to sulfamoyl benzoic acid derivatives of formula (I) or a pharmaceutically acceptable salt thereof, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders which are mediated via the TRPM8 receptor.
摘要翻译：本发明涉及式（I）的氨磺酰苯甲酸衍生物或其药学上可接受的盐，其制备方法，含有它们的药物组合物及其用于治疗通过TRPM8受体介导的各种病症的用途。

2. 发明授权

US06603008B1 Sulfamoylheleroaryl pyrazole compounds as anti-inflammatory/analgesic agents 失效
标题翻译：磺酰基杂芳基吡唑化合物作为抗炎/止痛剂
公开(公告)号：US06603008B1
公开(公告)日：2003-08-05
申请号：US09723661
申请日：2000-11-28
申请人： Kazuo Ando , Kiyoshi Kawamura
发明人： Kazuo Ando , Kiyoshi Kawamura
IPC分类号： C07D40104
CPC分类号： C07D405/14 , C07D413/14 , C07D417/14
摘要： This invention relates to a compound of the formula: or a pharmaceutically acceptable salt thereof, wherein A and R1 are each an optionally substituted 5 to 6-membered heteroaryl, wherein the heteroaryl is optionally fused to a carbocyclic ring or 5 to 6-heteroaryl; R2 is NH2; R3 and R4 are each hydrogen, halo, (C1-C4)alkyl optionally substituted with halo and the like; and X1 to X4 are each hydrogen, halo, hydroxy, (C1-C4)alkyl optionally substituted with halo and the like. These compounds have COX-2 inhibiting activity and thus useful for treating or preventing inflammation or other COX-2 related diseases.
摘要翻译：本发明涉及下式的化合物或其药学上可接受的盐，其中A和R 1各自为任选取代的5至6元杂芳基，其中杂芳基任选地与碳环或5至6-杂芳基稠合; R2是NH2; R 3和R 4各自为氢，卤素，任选被卤素取代的（C 1 -C 4）烷基等; 且X 1至X 4各自为氢，卤素，羟基，任选被卤素取代的（C 1 -C 4）烷基等。这些化合物具有COX-2抑制活性，因此可用于治疗或预防炎症或其他COX-2相关疾病。

3. 发明授权

US06951876B2 Sulfamoylheteroaryl pyrazole compounds as anti-inflammatory/analgesic agents 失效
标题翻译：磺酰基杂芳基吡唑化合物作为抗炎/止痛剂
公开(公告)号：US06951876B2
公开(公告)日：2005-10-04
申请号：US10334329
申请日：2002-12-31
申请人： Kazuo Ando , Kiyoshi Kawamura
发明人： Kazuo Ando , Kiyoshi Kawamura
IPC分类号： A61K31/443 , A61K31/4439 , A61P1/00 , A61P1/04 , A61P7/00 , A61P7/02 , A61P7/04 , A61P7/06 , A61P11/06 , A61P13/12 , A61P15/00 , A61P15/06 , A61P17/02 , A61P19/02 , A61P19/06 , A61P19/08 , A61P25/00 , A61P25/16 , A61P25/28 , A61P27/02 , A61P29/00 , A61P31/12 , A61P35/00 , A61P43/00 , C07D405/14 , C07D413/14 , C07D417/14 , C07D401/04
CPC分类号： C07D405/14 , C07D413/14 , C07D417/14
摘要： This invention relates to a compound of the formula: or a pharmaceutically acceptable salt thereof, wherein A and R1 are each an optionally substituted 5 to 6-membered heteroaryl, wherein the heteroaryl is optionally fused to a carbocyclic ring or 5 to 6-heteroaryl; R2 is NH2; R3 and R4 are each hydrogen, halo, (C1-C4)alkyl optionally substituted with halo and the like; and X1 to X4 are each hydrogen, halo, hydroxy, (C1-C4)alkyl optionally substituted with halo and the like. These compounds have COX-2 inhibiting activity and thus useful for treating or preventing inflammation or other COX-2 related diseases.
摘要翻译：本发明涉及下式化合物或其药学上可接受的盐，其中A和R 1各自为任选取代的5至6元杂芳基，其中杂芳基任选地与碳环稠合环或5至6-杂芳基; R 2是NH 2; R 3和R 4各自为氢，卤素，（C 1 -C 4 -C 4）烷基，任选被卤素等; 和X 1至X 4各自为氢，卤素，羟基，（C 1 -C 4 -C 4）烷基任选被卤素等取代。这些化合物具有COX-2抑制活性，因此可用于治疗或预防炎症或其他COX-2相关疾病。

4. 发明授权

US06649636B1 Heteroaryl phenyl pyrazole compounds as anti-inflammatory/analgesic agents 失效
标题翻译：杂芳基苯基吡唑化合物作为抗炎/止痛剂
公开(公告)号：US06649636B1
公开(公告)日：2003-11-18
申请号：US09723608
申请日：2000-11-28
申请人： Kazuo Ando , Martha L. Minich , Jin Li , Subas M. Sakya , Kristin M. Lundy , Hengmiao Cheng , Brian S. Bronk , Kiyoshi Kawamura , Tomoki Kato
发明人： Kazuo Ando , Martha L. Minich , Jin Li , Subas M. Sakya , Kristin M. Lundy , Hengmiao Cheng , Brian S. Bronk , Kiyoshi Kawamura , Tomoki Kato
IPC分类号： C07D40114
CPC分类号： C07D405/14 , C07D413/14 , C07D417/14
摘要： This invention relates to a compound of the formula: or a pharmaceutically acceptable salt thereof, wherein A and R1 are each an optionally substituted 5 to 6-membered heteroaryl, wherein the heteroaryl is optionally fused to a carbocyclic ring or 5 to 6-heteroaryl; R2 is (C1-C4)alkyl optionally substituted with halo, amino or an alkyl amino; R3 and R4 are each hydrogen, halo, (C1-C4)alkyl optionally substituted with halo and the like; and X1 to X4 are each hydrogen, halo, hydroxy, (C1-C4)alkyl optionally substituted with halo and the like. These compounds have COX-2 inhibiting activity and thus useful for treating or preventing inflammation or other COX-2 related diseases.
摘要翻译：本发明涉及下式的化合物或其药学上可接受的盐，其中A和R 1各自为任选取代的5至6元杂芳基，其中杂芳基任选地稠合于碳环或5至6个杂芳基 R 2是任选被卤素，氨基或烷基氨基取代的（C 1 -C 4）烷基; R 3和R 4各自为氢，卤素，任选被卤素取代的（C 1 -C 4）烷基等; X 1至X 4各自为氢，卤素，羟基，任选被卤素取代的（C 1 -C 4）烷基等。这些化合物具有COX-2抑制活性，因此可用于治疗或预防炎症或其他COX-2相关疾病。

5. 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。

6. 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。

7. 发明授权

US07645830B2 Polymer, crosslinked polymer, composition for solid polymer electrolyte, solid polymer electrolyte, and adhesive composition 有权
标题翻译：聚合物，交联聚合物，固体聚合物电解质的组合物，固体聚合物电解质和粘合剂组合物
公开(公告)号：US07645830B2
公开(公告)日：2010-01-12
申请号：US11795783
申请日：2006-01-18
申请人： Takeshi Niitani , Masato Amaike , Mikiya Shimada , Kiyoshi Kawamura
发明人： Takeshi Niitani , Masato Amaike , Mikiya Shimada , Kiyoshi Kawamura
IPC分类号： C08F118/02 , C08L31/02 , C09J167/06
CPC分类号： C08F293/005 , C08F290/06 , C08F293/00 , C08F297/02 , C08F297/026 , C08G18/6229 , C08L25/04 , C08L27/16 , C08L29/02 , C08L53/00 , C08L71/02 , C08L75/04 , C08L2205/05 , C08L2666/02 , C09J153/00 , H01M10/052 , H01M10/0565 , H01M2300/0082 , C08L2666/04
摘要： A polymer including a block chain A which is formed from a random copolymer containing a repeating unit (I) represented by the formula (I) wherein R1 to R3 each independently represents hydrogen or C1-10 hydrocarbon and R1 and R3 may bond to form a ring; R4a and R4b each independently represents hydrogen or methyl; R5 represents hydrogen, hydrocarbon, acyl, or silyl; and m represents any integer of 1 to 100 and when m is 2 or more and each R4a may be the same or different from one another and each R4b may be the same or different from one another; and a repeating unit (II) represented by the formula (II) wherein R6 and R8 each independently represents hydrogen or C1-10 hydrocarbon and R6 and R8 may bond to form a ring; R7 represents hydrogen, C1-10 hydrocarbon, hydroxyl, hydrocarbonoxy, carboxyl, acid anhydride, amino, ester, or an organic group having at least one functional group selected from the group consisting of hydroxyl, carboxyl, epoxy, acid anhydride, and amino; and R9 represents an organic group having at least one functional group selected from the group consisting of hydroxyl, carboxyl, epoxy, acid anhydride, and amino; and a block chain B having a repeating unit (III) represented by the formula (III) wherein R10 to R12 each independently represents hydrogen or C1-10 hydrocarbon and R13 represents aryl or heteroaryl; and wherein an arrangement order thereof is B, A, B.
摘要翻译：一种包含嵌段链A的聚合物，其由含有式（I）表示的重复单元（I）的无规共聚物形成，其中R 1至R 3各自独立地表示氢或C 1-10烃，并且R 1和R 3可以键合形成环; R4a和R4b各自独立地表示氢或甲基; R5表示氢，烃，酰基或甲硅烷基; m表示1〜100的整数，m为2以上时，各R 4a可以相同也可以不同，各R 4a可以相同也可以不同。和由式（II）表示的重复单元（II），其中R6和R8各自独立地表示氢或C1-10烃，R6和R8可以键合形成环; R7表示氢，C1-10烃，羟基，烃氧基，羧基，酸酐，氨基，酯或具有至少一个选自羟基，羧基，环氧基，酸酐和氨基的官能团的有机基团; 并且R 9表示具有至少一个选自羟基，羧基，环氧基，酸酐和氨基的官能团的有机基团; 和具有由式（III）表示的重复单元（III）的嵌段链B，其中R10至R12各自独立地表示氢或C1-10烃，R13表示芳基或杂芳基; 其布置顺序为B，A，B。

8. 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。

9. 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。

10. 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。

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