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41. 发明申请

US20110098297A1 FUSED RING COMPOUNDS AND USE THEREOF 失效
标题翻译：熔化环化合物及其用途
公开(公告)号：US20110098297A1
公开(公告)日：2011-04-28
申请号：US12936785
申请日：2009-04-09
申请人： Tsuneo Yasuma , Nobuyuki Takakura
发明人： Tsuneo Yasuma , Nobuyuki Takakura
IPC分类号： C07D417/04 , C07D417/14 , A61K31/427 , A61K31/4439 , A61K31/4178 , A61K31/4155 , A61K31/433 , A61K31/5377 , A61P3/10
CPC分类号： C07D417/04 , C07D417/14
摘要： The present invention aims to provide a glucokinase activator useful as a pharmaceutical agent such as an agent for the prophylaxis or treatment of diabetes, obesity and the like. The present invention provides a glucokinase activator containing a compound represented by the formula (I): wherein each symbol is defined in the specification, or a salt thereof or a prodrug thereof.
摘要翻译：本发明的目的在于提供一种用作预防或治疗糖尿病，肥胖症等药物的药剂的葡糖激酶活化剂。本发明提供含有式（I）表示的化合物的葡糖激酶活化剂：其中每个符号在说明书中定义，或其盐或其前药。

42. 发明申请

US20100144806A1 Cyclopropanecarboxylic Acid Compound 有权
标题翻译：环丙烷羧酸化合物
公开(公告)号：US20100144806A1
公开(公告)日：2010-06-10
申请号：US11989748
申请日：2006-07-28
申请人： Tsuneo Yasuma , Nobuyuki Negoro
发明人： Tsuneo Yasuma , Nobuyuki Negoro
IPC分类号： A61K31/426 , C07C69/753 , C07D335/02 , C07D305/06 , C07D277/38 , A61K31/216 , A61K31/382 , A61K31/337 , A61P3/00
CPC分类号： C07C229/46 , C07C62/34 , C07C69/757 , C07C2601/02 , C07D277/20 , C07D277/42 , C07D305/06 , C07D335/02
摘要： A compound of the formula (I): wherein each symbol is as defined in the description, a salt s thereof, and a prodrug thereof of the present invention unexpectedly have a superior GPR40 receptor agonist activity and superior properties as pharmaceutical products such as stability and the like, and can be safe and useful pharmaceutical agents for the prophylaxis or treatment of GPR40 receptor-related pathology or diseases in mammals.
摘要翻译：式（I）的化合物：其中每个符号如本说明书中所定义，其盐及其前药意外地具有优异的GPR40受体激动剂活性和优异的性能，如药物产品如稳定性和并且可以是用于预防或治疗哺乳动物中GPR40受体相关病理学或疾病的安全有用的药剂。

43. 发明申请

US20100137610A1 Indole compound 有权
公开(公告)号：US20100137610A1
公开(公告)日：2010-06-03
申请号：US12382622
申请日：2009-03-19
申请人： Tsuneo Yasuma , Osamu Ujikawa , Masahiro Itoh , Kazuko Aoki
发明人： Tsuneo Yasuma , Osamu Ujikawa , Masahiro Itoh , Kazuko Aoki
IPC分类号： C07D417/14
CPC分类号： C07D417/14
摘要： The purpose of the present invention is to provide a glucokinase activator useful as a pharmaceutical agent such as an agent for the prophylaxis or treatment of diabetes, obesity and the like.The present invention provides a glucokinase activator containing a compound represented by the formula (I): wherein R1 is a hydrogen atom or a halogen atom; R2 is a group represented by wherein each symbol is defined in the specification, or a salt thereof or a prodrug thereof.

44. 发明授权

US07718798B2 Indole compound 有权
标题翻译：吲哚化合物
公开(公告)号：US07718798B2
公开(公告)日：2010-05-18
申请号：US12382623
申请日：2009-03-19
申请人： Tsuneo Yasuma , Osamu Ujikawa
发明人： Tsuneo Yasuma , Osamu Ujikawa
IPC分类号： C07D413/14
CPC分类号： C07D417/14
摘要： The purpose of the present invention is to provide a glucokinase activator useful as a pharmaceutical agent such as an agent for the prophylaxis or treatment of diabetes, obesity and the like.The present invention provides a glucokinase activator containing a compound represented by the formula (I): wherein R1 is a hydrogen atom or a halogen atom; R2 is a group represented by wherein each symbol is defined in the specification, or a salt thereof or a prodrug thereof.
摘要翻译：本发明的目的是提供可用作药物的葡糖激酶活化剂，例如用于预防或治疗糖尿病，肥胖症等的药剂。本发明提供含有式（I）表示的化合物的葡糖激酶活化剂：其中R1是氢原子或卤素原子; R2是由其中每个符号在说明书中定义的基团，或其盐或其前药。

45. 发明授权

US07585880B2 Phenylpropanoic acid derivatives 失效
标题翻译：苯丙酸衍生物
公开(公告)号：US07585880B2
公开(公告)日：2009-09-08
申请号：US10584730
申请日：2004-12-24
申请人： Tsuneo Yasuma , Shinobu Sasaki , Nozomu Sakai
发明人： Tsuneo Yasuma , Shinobu Sasaki , Nozomu Sakai
IPC分类号： A61K31/443 , A61K31/4439 , A61K31/427 , A61K31/422 , C07D277/22 , C07D263/32 , C07D417/10 , C07D413/10
CPC分类号： C07D277/42 , C07D263/48 , C07D417/04 , C07D417/12
摘要： The present invention provides a novel compound having a GPR40 receptor function modulating action, which is useful as an insulin secretagogue, a drug for the prophylaxis or treatment of diabetes and the like.A compound represented by the formula (I) wherein each symbol is as defined in the specification, a salt thereof and a prodrug thereof have unexpectedly superior GPR40 receptor agonist activity and also show superior properties as a pharmaceutical product, such as stability and the like. Thus, they can be safe and useful drugs for the prophylaxis or treatment of GPR40 receptor related conditions or diseases in mammals.
摘要翻译：本发明提供具有GPR40受体功能调节作用的新化合物，其可用作胰岛素促分泌素，用于预防或治疗糖尿病等的药物。由式（I）表示的化合物，其中每个符号如说明书中所定义，其盐和前药具有出人意料的优异的GPR40受体激动剂活性，并且还表现出作为药物的优异性质，例如稳定性等。因此，它们可以是用于预防或治疗哺乳动物中GPR40受体相关病症或疾病的安全有用的药物。

46. 发明授权

US07067527B2 Thienopyridine derivatives, their production and use 失效
标题翻译：噻吩并吡啶衍生物，其生产和使用
公开(公告)号：US07067527B2
公开(公告)日：2006-06-27
申请号：US10662165
申请日：2003-09-03
申请人： Tsuneo Yasuma , Atsuo Baba , Haruhiko Makino , Isao Aoki , Toshiaki Nagata
发明人： Tsuneo Yasuma , Atsuo Baba , Haruhiko Makino , Isao Aoki , Toshiaki Nagata
IPC分类号： C07D495/14 , A61K31/38
CPC分类号： C07D495/04 , C07D495/14
摘要： The present invention provides thienopyridine derivatives, which are useful as anti-inflammatory drugs, particularly as remedies for arthritis; processes for producing them, and pharmaceutical compositions containing them. The thienopyridine derivatives are represented by the formula (I): wherein G is a halogen atom, hydroxyl group, an optionally substituted amino group, etc.; alk is an optionally substituted lower alkylene group; X is O, S, —(CH2)q—, etc.; R is an optionally substituted amino group, etc.; ring B is an optionally substituted Y-containing 5- to 8-membered ring whose ring constituent atoms contain no nitrogen atom; Y is O, S, a group of (wherein Ra, Rb and Rc are the same or different and, each is H, a halogen atom, an optionally substituted hydrocarbon group, etc.), etc.; and ring A may be substituted.
摘要翻译：本发明提供可用作抗炎药物的噻吩并吡啶衍生物，特别是作为关节炎的补救剂; 制备它们的方法和含有它们的药物组合物。噻吩并吡啶衍生物由式（I）表示：其中G是卤素原子，羟基，任选取代的氨基等; 烷基是任选取代的低级亚烷基; X是O，S， - （CH 2 CH 2）q - 等; R是任选取代的氨基等; 环B是任选取代的含有Y的5至8元环，其环组成原子不含氮原子; Y是O，S，（其中Ra，Rb和Rc相同或不同，并且各自为H，卤素原子，任选取代的烃基等）等; 并且环A可以被取代。

47. 发明授权

US5498728A Derivatives of L-tryptophanal and their use as medicinals 失效
标题翻译： L-色氨酸的衍生物及其作为药物的用途
公开(公告)号：US5498728A
公开(公告)日：1996-03-12
申请号：US192038
申请日：1994-02-04
申请人： Takashi Sohda , Yukio Fujisawa , Tsuneo Yasuma , Junji Mizoguchi , Masakuni Kori , Masayuki Takizawa
发明人： Takashi Sohda , Yukio Fujisawa , Tsuneo Yasuma , Junji Mizoguchi , Masakuni Kori , Masayuki Takizawa
IPC分类号： A61K38/55 , A61K31/16 , A61K31/165 , A61K31/18 , A61K31/27 , A61K38/00 , A61P3/00 , A61P3/02 , A61P43/00 , C07C231/12 , C07C233/18 , C07C233/22 , C07C233/31 , C07C237/10 , C07C237/22 , C07C271/16 , C07C271/18 , C07C271/22 , C07C303/40 , C07C311/19 , C07C337/02 , C07D209/14 , C07D209/16 , C07K1/113 , C07K5/06 , C07K5/062 , C07K14/81 , A61K31/40
CPC分类号： C07D209/16 , C07C233/18 , C07C233/22 , C07C233/31 , C07C271/16 , C07C271/18 , C07C271/22 , C07C311/19 , C07K5/06034 , A61K38/00 , Y02P20/55
摘要： The present invention provides a cathepsin L inhibitor containing a compound of the formula: ##STR1## wherein R.sup.1 is a hydrogen atom or an arylalkyl, heterocyclic-alkyl or lower alkyl group which may be substituted; R.sup.2 and R.sup.3 independently are a hydrogen atom or a hydrocarbon residue which may be substituted; R.sup.4 is an alkanoyl, sulfonyl, carbonyloxy, carbamoyl or thiocarbamoyl group which may be substituted; X is formula: --CHO or --CH.sub.2 OB (wherein B is a hydrogen atom or a protecting group of hydroxyl group); m and n independently are an integer of 0 or 1; provided that R.sup.4 is an alkanoyl group substituted by aryl, a sulfonyl group substituted by aryl having more than 9 carbon atoms or by lower alkyl, or a carbamoyl or thiocarbamoyl group which may be substituted when R.sup.1 is an unsubstituted lower alkyl, arylalkyl on methylthioethyl group, R.sup.2 and R.sup.3 independently are a lower alkyl or arylalkyl, X is --CHO, m is 1 and n is 0 or 1, or a salt thereof.Compound (I) is useful as a prophylactic/therapeutic agent for osteoporosis.
摘要翻译：本发明提供了含有下式化合物的组蛋白酶L抑制剂：其中R1是氢原子或可被取代的芳基烷基，杂环烷基或低级烷基; R2和R3独立地是氢原子或可以被取代的烃残基; R4是可以被取代的烷酰基，磺酰基，羰基氧基，氨基甲酰基或硫代氨基甲酰基; X是式：-CHO或-CHOOB（其中B是氢原子或羟基保护基）; m和n独立地为0或1的整数; 条件是R4是被芳基取代的烷酰基，被具有多于9个碳原子的芳基取代的磺酰基或低级烷基，或当R 1是未取代的低级烷基时可被取代的氨基甲酰基或硫代氨基甲酰基，甲基硫代乙基上的芳基烷基，R2和R3独立地是低级烷基或芳烷基，X是-CHO，m是1，n是0或1，或其盐。化合物（I）可用作骨质疏松症的预防/治疗剂。

48. 发明授权

US08492405B2 Glucokinase-activating fused heterocyclic compounds and methods of treating diabetes and obesity 失效
标题翻译：葡萄糖激酶活化融合杂环化合物和治疗糖尿病和肥胖症的方法
公开(公告)号：US08492405B2
公开(公告)日：2013-07-23
申请号：US12311892
申请日：2007-10-17
申请人： Tsuneo Yasuma , Yasufumi Miyamoto
发明人： Tsuneo Yasuma , Yasufumi Miyamoto
IPC分类号： A01N43/52 , A01N43/78 , A01N43/40 , A01N43/82 , A61K31/415 , A61K31/425 , A61K31/445 , A61K31/41 , C07D261/20
CPC分类号： C07D487/04 , C07D495/04 , C07D519/00
摘要： The present invention aims to provide a glucokinase activator useful as a pharmaceutical agent such as an agent for the prophylaxis or treatment of diabetes, obesity and the like, and the like.A glucokinase activator containing a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof or a prodrug thereof.
摘要翻译：本发明的目的在于提供一种用作药剂的糖激酶活化剂，例如用于预防或治疗糖尿病，肥胖症等的药剂。含有由式（I）表示的化合物的葡糖激酶活化剂：其中每个符号如说明书中所定义，或其盐或其前药。

49. 发明授权

US08153694B2 Cyclopropanecarboxylic acid compound 有权
标题翻译：环丙烷羧酸化合物
公开(公告)号：US08153694B2
公开(公告)日：2012-04-10
申请号：US11989748
申请日：2006-07-28
申请人： Tsuneo Yasuma , Nobuyuki Negoro
发明人： Tsuneo Yasuma , Nobuyuki Negoro
IPC分类号： A61K31/19
CPC分类号： C07C229/46 , C07C62/34 , C07C69/757 , C07C2601/02 , C07D277/20 , C07D277/42 , C07D305/06 , C07D335/02
摘要： A compound of the formula (I): wherein each symbol is as defined in the description, a salt thereof, and a prodrug thereof of the present invention unexpectedly have a superior GPR40 receptor agonist activity and superior properties as pharmaceutical products such as stability and the like, and can be safe and useful pharmaceutical agents for the prophylaxis or treatment of GPR40 receptor-related pathology or diseases in mammals.
摘要翻译：式（I）的化合物：其中每个符号如本说明书中所定义，其盐及其前药意外地具有优异的GPR40受体激动剂活性和优异的药物产品的性质，如稳定性和并且可以是用于预防或治疗哺乳动物中GPR40受体相关病理学或疾病的安全有用的药物。

50. 发明申请

US20120035163A1 NOVEL FUSED RING COMPOUND AND USE THEREOF 失效
标题翻译：新型熔融环化合物及其用途
公开(公告)号：US20120035163A1
公开(公告)日：2012-02-09
申请号：US13142507
申请日：2009-12-28
申请人： Tsuneo Yasuma , Nobuyuki Takakura , Yasufumi Miyamoto
发明人： Tsuneo Yasuma , Nobuyuki Takakura , Yasufumi Miyamoto
IPC分类号： A61K31/541 , C07D417/14 , C07D279/12 , A61P3/04 , A61K31/427 , A61K31/4439 , A61K31/5355 , A61P3/10 , C07D277/10 , C07D413/14
CPC分类号： C07D417/14 , A61K31/427 , A61K31/4439 , A61K31/5377 , A61K31/541
摘要： The present invention provides an agent for the prophylaxis or treatment of diabetes, obesity and the like, a glucokinase activator, containing a compound represented by the formula (I): wherein each symbol is as defined in the description, or a salt thereof or a prodrug thereof.
摘要翻译：本发明提供了用于预防或治疗糖尿病，肥胖症等的药剂，含有式（I）表示的化合物的葡糖激酶活化剂：其中每个符号如说明书中所定义，或其盐或前药。

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