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1. 发明授权

US08367708B2 Phenyl-isoxazol-3-ol derivative 有权
标题翻译：苯基异恶唑-3-醇衍生物
公开(公告)号：US08367708B2
公开(公告)日：2013-02-05
申请号：US12516025
申请日：2007-11-29
申请人： Noriaki Hashimoto , Yasuhiro Sasaki , Chisato Nakama , Makoto Ishikawa
发明人： Noriaki Hashimoto , Yasuhiro Sasaki , Chisato Nakama , Makoto Ishikawa
IPC分类号： A01N43/76 , A01N43/64 , A01N43/18 , A01N43/06 , A01N43/16 , A01N43/08 , A61K31/42 , A61K31/41 , A61K31/54 , A61K31/38 , A61K31/35 , A61K31/34
CPC分类号： C07D261/12 , C07D413/04 , C07D413/12 , C07D417/12
摘要： The present invention relates to a compound represented by formula (I), which has a GPR120 agonist action and thus is useful for treatment of diabetes mellitus or hyperlipidemia, or a pharmaceutically acceptable salt thereof. In the formula, (AA) represents a phenyl or the like, which may be substituted with a lower alkoxy group or the like; (BB) represents a divalent group or the like, derived by removal of two hydrogen atoms from a benzene which may be substituted with a halogen atom or the like; X represents a spacer having a main chain composed of 1-8 carbon atoms wherein 1-3 carbon atoms in the main chain may be substituted with an oxygen atom or the like; and Y represents a hydrogen atom or the like.
摘要翻译：本发明涉及由式（I）表示的化合物，其具有GPR120激动剂作用，因此可用于治疗糖尿病或高脂血症或其药学上可接受的盐。式中，（AA）表示可以被低级烷氧基等取代的苯基等，（BB）表示通过从可以被卤素原子等取代的苯中除去两个氢原子得到的二价基团等; X表示具有由1-8个碳原子构成的主链的间隔基，其中主链中的1-3个碳原子可以被氧原子等取代; Y表示氢原子等。

2. 发明申请

US20120028970A1 HETEROARYLTHIOMETHYL PYRIDINE DERIVATIVE 审中-公开
标题翻译：异丁基二甲基吡啶衍生物
公开(公告)号：US20120028970A1
公开(公告)日：2012-02-02
申请号：US13263809
申请日：2010-04-27
申请人： Minoru Kameda , Kensuke Kobayashi , Chisato Nakama , Makoto Ando , Nagaaki Sato
发明人： Minoru Kameda , Kensuke Kobayashi , Chisato Nakama , Makoto Ando , Nagaaki Sato
IPC分类号： A61K31/541 , C07D451/04 , C07D401/14 , C07D413/14 , A61K31/4545 , A61K31/46 , A61K31/5377 , A61P9/12 , A61P9/10 , A61P13/12 , A61P9/00 , A61P25/00 , A61P25/08 , A61P25/22 , A61P25/24 , A61P25/32 , A61P25/28 , A61P3/04 , A61P3/10 , A61P27/06 , A61P5/00 , C07D417/14
CPC分类号： C07D401/14 , C07D413/14 , C07D417/14 , C07D451/04
摘要： The present invention relates to a compound represented by a formula (I): wherein X is a group represented by or the like; Y is a group represented by or the like; and Ar1 is a group represented by or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明涉及由式（I）表示的化合物：其中X是由等表示的基团; Y是由等表示的基团; 和Ar 1是由其表示的基团或其药学上可接受的盐。

3. 发明申请

US20110065739A1 NOVEL ISOXAZOLE DRIVATIVE 审中-公开
标题翻译：新的异丙唑驱动剂
公开(公告)号：US20110065739A1
公开(公告)日：2011-03-17
申请号：US12992387
申请日：2009-05-28
申请人： Makoto Ishikawa , Tasuku Haketa , Chisato Nakama , Teruyuki Nishimura , Jun Shibata , Tadashi Shimamura , Takeru Yamakawa
发明人： Makoto Ishikawa , Tasuku Haketa , Chisato Nakama , Teruyuki Nishimura , Jun Shibata , Tadashi Shimamura , Takeru Yamakawa
IPC分类号： A61K31/506 , C07D261/12 , A61K31/42 , A61P3/10 , A61P3/04 , A61P3/06 , C07D413/04 , A61K31/4439
CPC分类号： C07D261/12 , C07D413/04 , C07D413/12
摘要： Disclosed is a compound represented by formula (I) or a pharmaceutically acceptable salt thereof, which has an agonistic activity on GPR120 and is therefore useful for the treatment of diabetes, obesity or hyperlipemia. [In formula (I), the A represents a phenyl group which may be substituted by a lower alkoxy group or the like; the 13 represents a bivalent group produced by removing two hydrogen atoms from a benzene ring which may be substituted by a halogen atom or the like; X represents a lower alkylene group having 2 to 4 carbon atoms in its main chain or the like, wherein a carbon atom constituting the main chain may be substituted by an oxygen atom or the like; and Y represents a hydrogen atom or the like.]
摘要翻译：公开了由式（I）表示的化合物或其药学上可接受的盐，其对GPR120具有激动作用，因此可用于治疗糖尿病，肥胖症或高脂血症。 [式（I）中，A表示可被低级烷氧基等取代的苯基， 13表示通过从可被卤素原子等取代的苯环除去2个氢原子而生成的二价基团; X表示其主链等中具有2〜4个碳原子的低级亚烷基，其中构成主链的碳原子可以被氧原子等取代; Y表示氢原子等。]

4. 发明申请

US20110015181A1 ALKYLAMINOPYRIDINE DERIVATIVE 审中-公开
标题翻译：亚氨基吡啶衍生物
公开(公告)号：US20110015181A1
公开(公告)日：2011-01-20
申请号：US12920916
申请日：2009-03-04
申请人： Makoto Ando , Hirokatsu Ito , Minoru Kameda , Hiroshi Kawamoto , Kensuke Kobayashi , Hiroshi Miyazoe , Chisato Nakama , Nagaaki Sato , Toshiaki Tsujino
发明人： Makoto Ando , Hirokatsu Ito , Minoru Kameda , Hiroshi Kawamoto , Kensuke Kobayashi , Hiroshi Miyazoe , Chisato Nakama , Nagaaki Sato , Toshiaki Tsujino
IPC分类号： A61K31/55 , C07D498/04 , A61K31/5386 , C07D401/14 , A61K31/4545 , C07D417/14 , A61K31/541 , C07D413/14 , A61K31/5377 , A61K31/439 , A61P3/00
CPC分类号： C07D417/14 , C07D401/12 , C07D401/14 , C07D413/12 , C07D413/14 , C07D451/02 , C07D498/08
摘要： The present invention relates to a compound that is useful for treatment of, for example, hypertension, arteriosclerosis, bulimia and obesity because of having an antagonistic action to a neuropeptide Y receptor and is represented by formula (I) [wherein R1 represents hydrogen, cyano, or the like; R represents a group represented by formula (II); X1 represents C1-4 lower alkylene or the like; X2 represents lower alkylene or the like; and Het represents a 5-membered heteroaromatic ring that has at least one nitrogen atom and, in addition, one or two hetero atoms selected from the group consisting of nitrogen, sulfur and oxygen atoms] or to a pharmaceutically acceptable salt thereof.
摘要翻译：本发明涉及由于对神经肽Y受体具有拮抗作用而由式（I）表示的化合物，其可用于治疗例如高血压，动脉硬化，贪食症和肥胖症[其中R1表示氢，氰基，等等; R表示由式（II）表示的基团。 X1表示C1-4低级亚烷基等; X2表示低级亚烷基等; Het表示具有至少一个氮原子，另外还有一个或两个选自氮，硫和氧原子的杂原子的5元杂芳环]或其药学上可接受的盐。

5. 发明申请

US20100130559A1 NOVEL PHENYL-ISOXAZOL-3-OL DERIVATIVE 有权
标题翻译：新型PHENYL-ISOXAZOL-3-OL DERIVATIVE
公开(公告)号：US20100130559A1
公开(公告)日：2010-05-27
申请号：US12516025
申请日：2007-11-29
申请人： Noriaki Hashimoto , Yasuhiro Sasaki , Chisato Nakama , Makoto Ishikawa
发明人： Noriaki Hashimoto , Yasuhiro Sasaki , Chisato Nakama , Makoto Ishikawa
IPC分类号： A61K31/4439 , C07D413/12 , C07D417/12 , A61K31/422 , A61K31/427 , C07D261/02 , A61K31/421 , A61P3/04 , A61P3/06 , A61P3/10
CPC分类号： C07D261/12 , C07D413/04 , C07D413/12 , C07D417/12
摘要： The present invention relates to a compound represented by formula (I), which has a GPR120 agonist action and thus is useful for treatment of diabetes mellitus or hyperlipidemia, or a pharmaceutically acceptable salt thereof. In the formula, (AA) represents a phenyl or the like, which may be substituted with a lower alkoxy group or the like; (BB) represents a divalent group or the like, derived by removal of two hydrogen atoms from a benzene which may be substituted with a halogen atom or the like; X represents a spacer having a main chain composed of 1-8 carbon atoms wherein 1-3 carbon atoms in the main chain may be substituted with an oxygen atom or the like; and Y represents a hydrogen atom or the like.
摘要翻译：本发明涉及由式（I）表示的化合物，其具有GPR120激动剂作用，因此可用于治疗糖尿病或高脂血症或其药学上可接受的盐。式中，（AA）表示可以被低级烷氧基等取代的苯基等，（BB）表示通过从可以被卤素原子等取代的苯中除去两个氢原子得到的二价基团等; X表示具有由1-8个碳原子构成的主链的间隔基，其中主链中的1-3个碳原子可以被氧原子等取代; Y表示氢原子等。

6. 发明申请

US20080125429A1 Aryloxy-Substituted Benzimidazole Derivatives 有权
标题翻译：芳氧基取代的苯并咪唑衍生物
公开(公告)号：US20080125429A1
公开(公告)日：2008-05-29
申请号：US11666555
申请日：2005-11-01
申请人： Noriaki Hashimoto , Keiji Takahashi , Chisato Nakama , Yoshio Ogino , Fumiko Sakai , Teruyuki Nishimura , Jun-ichi Eiki
发明人： Noriaki Hashimoto , Keiji Takahashi , Chisato Nakama , Yoshio Ogino , Fumiko Sakai , Teruyuki Nishimura , Jun-ichi Eiki
IPC分类号： A61K31/5377 , C07D213/02 , C07D221/00 , C07D239/06 , C07D241/10 , C07D295/00 , A61P3/10 , A61K31/4439 , A61K31/4545 , A61K31/444 , A61K31/506 , A61K31/497
CPC分类号： A61K38/31 , A61K31/155 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/497 , A61K31/506 , A61K38/28 , A61K45/06 , C07D401/04 , C07D401/14 , C07D413/06 , C07D413/14 , A61K2300/00
摘要： A glucokinase activator is provided; and a treatment and/or a preventive for diabetes, or a treatment and/or a preventive for diabetes such as retinopathy, nephropathy, neurosis, ischemic cardiopathy, arteriosclerosis, and further a treatment and/or a preventive for obesity are provided.The invention relates to a compound of a formula (I): [wherein R1 and R2 represent a hydrogen, etc.; R3 represents a hydrogen atom, a halogen atom, etc.; R4 each independently represents a hydrogen atom, a lower alkyl group, etc.; Q represents a carbon atom, a nitrogen atom or a sulfur atom (the sulfur atom may be mono- or di-substituted with an oxo group); R5 and R6 each represent a hydrogen atom, a lower alkyl group, etc.; X1, X2, X3 and X4 each independently represent a carbon atom or a nitrogen atom; Z represents an oxygen atom, a sulfur atom or a nitrogen atom; Ar represents an aryl or heteroaryl group optionally mono to tri-substituted with a group selected from the substituent group β; ring A represents a 5- or 6-membered nitrogen-containing heteroaromatic group; m indicates an integer of from 1 to 6; n indicates an integer of from 0 to 3; p indicates an integer of from 0 to 2 (provided that at least two of X1 to X4 are carbon atoms); q indicates 0 or 1] or its pharmaceutically-acceptable salt, which has an effect of glucokinase activation and is useful as a treatment for diabetes.
摘要翻译：提供葡糖激酶活化剂; 提供糖尿病的治疗和/或预防，或治疗和/或预防糖尿病如视网膜病，肾病，神经症，缺血性心脏病，动脉硬化，以及进一步的治疗和/或预防肥胖症。本发明涉及式（I）的化合物：其中R 1和R 2代表氢等; R 3表示氢原子，卤素原子等; R 4各自独立地表示氢原子，低级烷基等; Q表示碳原子，氮原子或硫原子（硫原子可以被氧代基单取代或二取代）。 R 5和R 6各自表示氢原子，低级烷基等; X 1，X 2，X 3和X 4各自独立地表示碳原子或氮原子; Z表示氧原子，硫原子或氮原子; Ar表示任选被选自取代基组β的基团单取代至三取代的芳基或杂芳基; 环A表示5-或6-元含氮杂芳基; m表示1〜6的整数， n表示0〜3的整数， p表示0〜2的整数（条件是X 1〜X 4中的至少2个为碳原子）; q表示0或1]或其药学上可接受的盐，其具有葡糖激酶活化的作用，并且可用作糖尿病的治疗。

7. 发明授权

US07932394B2 Aryloxy-substituted benzimidazole derivatives 有权
标题翻译：芳氧基取代的苯并咪唑衍生物
公开(公告)号：US07932394B2
公开(公告)日：2011-04-26
申请号：US11666555
申请日：2005-11-01
申请人： Noriaki Hashimoto , Keiji Takahashi , Chisato Nakama , Yoshio Ogino , Fumiko Sakai , Teruyuki Nishimura , Jun-ichi Eiki
发明人： Noriaki Hashimoto , Keiji Takahashi , Chisato Nakama , Yoshio Ogino , Fumiko Sakai , Teruyuki Nishimura , Jun-ichi Eiki
IPC分类号： C07D401/00 , A61K31/445
CPC分类号： A61K38/31 , A61K31/155 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/497 , A61K31/506 , A61K38/28 , A61K45/06 , C07D401/04 , C07D401/14 , C07D413/06 , C07D413/14 , A61K2300/00
摘要： A glucokinase activator is provided; and a treatment and/or a preventive for diabetes, or a treatment and/or a preventive for diabetes such as retinopathy, nephropathy, neurosis, ischemic cardiopathy, arteriosclerosis, and further a treatment and/or a preventive for obesity are provided.The invention relates to a compound of a formula (I): [wherein R1 and R2 represent a hydrogen, etc.; R3 represents a hydrogen atom, a halogen atom, etc.; R4 each independently represents a hydrogen atom, a lower alkyl group, etc.; Q represents a carbon atom, a nitrogen atom or a sulfur atom (the sulfur atom may be mono- or di-substituted with an oxo group); R5 and R6 each represent a hydrogen atom, a lower alkyl group, etc.; X1, X2, X3 and X4 each independently represent a carbon atom or a nitrogen atom; Z represents an oxygen atom, a sulfur atom or a nitrogen atom; Ar represents an aryl or heteroaryl group optionally mono to tri-substituted with a group selected from the substituent group β; ring A represents a 5- or 6-membered nitrogen-containing heteroaromatic group; m indicates an integer of from 1 to 6; n indicates an integer of from 0 to 3; p indicates an integer of from 0 to 2 (provided that at least two of X1 to X4 are carbon atoms); q indicates 0 or 1] or its pharmaceutically-acceptable salt, which has an effect of glucokinase activation and is useful as a treatment for diabetes.
摘要翻译：提供葡糖激酶活化剂; 提供糖尿病的治疗和/或预防，或治疗和/或预防糖尿病如视网膜病，肾病，神经症，缺血性心脏病，动脉硬化，以及进一步的治疗和/或预防肥胖症。本发明涉及式（I）化合物：其中R 1和R 2表示氢等; R3表示氢原子，卤原子等; R4各自独立地表示氢原子，低级烷基等; Q表示碳原子，氮原子或硫原子（硫原子可以被氧代基单取代或二取代）。 R5和R6各自表示氢原子，低级烷基等; X1，X2，X3和X4各自独立地表示碳原子或氮原子; Z表示氧原子，硫原子或氮原子; Ar表示任选被选自取代基组中的基团单取代至三取代的芳基或杂芳基; 环A表示5-或6-元含氮杂芳基; m表示1〜6的整数， n表示0〜3的整数， p表示0〜2的整数（X1〜X4中的至少2个为碳原子）。 q表示0或1]或其药学上可接受的盐，其具有葡糖激酶活化的作用，并且可用作糖尿病的治疗。

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