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公开(公告)号：US07790725B2
公开(公告)日：2010-09-07
申请号：US11774941
申请日：2007-07-09
申请人： Hiroshi Sakashita , Tomohiro Yoshida , Hiroshi Kitajima , Masahiro Takeuchi , Yoshihito Tanaka , Takuya Yoshimura , Fumihiko Akahoshi , Yoshiharu Hayashi
发明人： Hiroshi Sakashita , Tomohiro Yoshida , Hiroshi Kitajima , Masahiro Takeuchi , Yoshihito Tanaka , Takuya Yoshimura , Fumihiko Akahoshi , Yoshiharu Hayashi
IPC分类号： A61K31/435 , A61K31/496 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14
CPC分类号： C07D277/04
摘要： A thiazolidine derivative represented by the formula (I) wherein each symbol is as defined in the specification, and a pharmaceutically acceptable salt thereof exhibit a potent DPP-IV inhibitory activity, and can be provided as an agent for the prophylaxis or treatment of diabetes, an agent for the prophylaxis or treatment of obesity and the like.
摘要翻译： 由式（I）表示的噻唑烷衍生物，其中每个符号如说明书中所定义，及其药学上可接受的盐显示出有效的DPP-IV抑制活性，并且可以作为预防或治疗糖尿病， 用于预防或治疗肥胖症等的药剂。
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公开(公告)号：US20060173056A1
公开(公告)日：2006-08-03
申请号：US11351118
申请日：2006-02-10
IPC分类号： A61K31/427 , A61K31/4025 , C07D417/02 , C07D403/02
CPC分类号： C07D401/14 , C07D207/16 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/06 , C07D417/14 , C07D471/10 , C07D487/04
摘要： The present invention aims at providing compounds having therapeutic effects due to a DPP-IV inhibitory action, and satisfactory as pharmaceutical products. The present inventors have found that derivatives having a substituent introduced into the γ-position of proline represented by the formula (I) wherein each symbol is as defined in the specification, have a potent DPP-IV inhibitory activity, and completed the present invention by increasing the stability.
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公开(公告)号：US20050245538A1
公开(公告)日：2005-11-03
申请号：US11142523
申请日：2005-06-02
IPC分类号： A61P1/02 , A61P3/04 , A61P3/10 , A61P13/08 , A61P17/00 , A61P31/18 , A61P35/04 , A61P37/06 , A61P43/00 , C07D207/16 , C07D401/14 , C07D403/14 , C07D413/14 , C07D417/06 , C07D417/14 , C07D471/10 , C07D487/04 , C07D498/04 , A61K31/496 , A61K31/427 , A61K31/454 , C07D417/02
CPC分类号： C07D401/14 , C07D207/16 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/06 , C07D417/14 , C07D471/10 , C07D487/04
摘要： The present invention aims at providing compounds having therapeutic effects due to a DPP-IV inhibitory action, and satisfactory as pharmaceutical products. The present inventors have found that derivatives having a substituent introduced into the γ-position of proline represented by the formula (I) wherein each symbol is as defined in the specification, have a potent DPP-IV inhibitory activity, and completed the present invention by increasing the stability.
摘要翻译： 本发明旨在提供由于DPP-IV抑制作用而具有治疗作用的化合物，并且作为药物产品令人满意。 本发明人发现具有引入式（I）表示的脯氨酸的γ-位置的取代基的衍生物，其中每个符号如说明书中所定义，具有有效的DPP-IV抑制活性，并通过 增加稳定性。
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公开(公告)号：US07074794B2
公开(公告)日：2006-07-11
申请号：US10344255
申请日：2001-08-10
IPC分类号： A61K31/495 , C07D403/04
CPC分类号： C07D401/14 , C07D207/16 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/06 , C07D417/14 , C07D471/10 , C07D487/04
摘要： The present invention aims at providing compounds having therapeutic effects due to a DPP-IV inhibitory action, and satisfactory as pharmaceutical products.The present inventors have found that derivatives having a substituent introduced into the γ-position of proline represented by the formula (I) wherein each symbol is as defined in the specification, have a potent DPP-IV inhibitory activity, and completed the present invention by increasing the stability.
摘要翻译： 本发明旨在提供由于DPP-IV抑制作用而具有治疗作用的化合物，并且作为药物产品令人满意。 本发明人发现具有引入式（I）表示的脯氨酸的γ-位置的取代基的衍生物，其中每个符号如说明书中所定义，具有有效的DPP-IV抑制活性，并通过 增加稳定性。
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公开(公告)号：US07060722B2
公开(公告)日：2006-06-13
申请号：US11142523
申请日：2005-06-02
IPC分类号： A61K31/4025 , A61K31/427
CPC分类号： C07D401/14 , C07D207/16 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/06 , C07D417/14 , C07D471/10 , C07D487/04
摘要： The present invention aims at providing compounds having therapeutic effects due to a DPP-IV inhibitory action, and satisfactory as pharmaceutical products.The present inventors have found that derivatives having a substituent introduced into the γ-position of proline represented by the formula (I) wherein each symbol is as defined in the specification, have a potent DPP-IV inhibitory activity, and completed the present invention by increasing the stability.
摘要翻译： 本发明旨在提供由于DPP-IV抑制作用而具有治疗作用的化合物，并且作为药物产品令人满意。 本发明人发现具有引入式（I）表示的脯氨酸的γ-位置的取代基的衍生物，其中每个符号如说明书中所定义，具有有效的DPP-IV抑制活性，并通过 增加稳定性。
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公开(公告)号：US6080738A
公开(公告)日：2000-06-27
申请号：US284877
申请日：1999-04-22
申请人： Fumihiko Akahoshi , Atsuyuki Ashimori , Takuya Yoshimura , Masahiro Eda , Hiroshi Sakashita , Masahide Nakajima , Teruaki Imada
发明人： Fumihiko Akahoshi , Atsuyuki Ashimori , Takuya Yoshimura , Masahiro Eda , Hiroshi Sakashita , Masahide Nakajima , Teruaki Imada
IPC分类号： C07D413/12 , A61K31/435 , A61K38/00 , C07K5/078 , A61K31/505 , C07D239/47 , C07D417/12 , C07D498/04 , C07K5/04
CPC分类号： C07K5/06139 , A61K38/00
摘要： A heterocyclic amide compound of the formula (I) ##STR1## wherein each symbol is as defined in the specification, a pharmacologically acceptable salt thereof, a pharmaceutical composition thereof and a pharmaceutical use thereof. The heterocyclic amide compound and a pharmacologically acceptable salt thereof of the present invention have superior inhibitory action on chymase group in mammals inclusive of human, and can be administered orally or parenterally. Therefore, they are useful as chymase inhibitors and can be used for the prophylaxis and treatment of various diseases caused by chymase, such as those caused by angiotensin II.
摘要翻译： PCT No.PCT / JP97 / 03839 Sec。 371日期1999年4月22日 102（e）1999年4月22日PCT 1997年10月22日PCT公布。 第WO98 / 18794号公报 日期：1998年5月7日一种式（I）的杂环酰胺化合物，其中各符号如说明书中所定义，其药理学上可接受的盐，其药物组合物及其药物用途。 本发明的杂环酰胺化合物及其药理学上可接受的盐对包含人的哺乳动物中的胃促胰酶组具有优异的抑制作用，可以口服或肠胃外给药。 因此，它们可用作胃促胰酶抑制剂，可用于预防和治疗由胃促胰岛素引起的各种疾病，例如由血管紧张素II引起的疾病。
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7.发明授权公开(公告)号：US08003790B2
公开(公告)日：2011-08-23
申请号：US11816493
申请日：2006-02-17
申请人： Tomohiro Yoshida , Hiroshi Sakashita , Naoko Ueda , Shinji Kirihara , Satoru Uemori , Reiko Tsutsumiuchi , Fumihiko Akahoshi
发明人： Tomohiro Yoshida , Hiroshi Sakashita , Naoko Ueda , Shinji Kirihara , Satoru Uemori , Reiko Tsutsumiuchi , Fumihiko Akahoshi
IPC分类号： C07D417/14
CPC分类号： C07D417/14
摘要： The present invention provides 3-{(2S,4S)-4-[4-(3-methyl-1-phenyl-1H-pyrazol-5-yl)piperazin-1-yl]pyrrolidin-2-ylcarbonyl}thiazolidine (compound I) useful as a dipeptidyl peptidase-IV inhibitor, which has superior properties of stability and hygroscopicity, and reproducible crystal structure, and a production method thereof.
摘要翻译： 本发明提供3 - {（2S，4S）-4- [4-（3-甲基-1-苯基-1H-吡唑-5-基）哌嗪-1-基]吡咯烷-2-基羰基}噻唑烷（化合物 I）作为二肽基肽酶-IV抑制剂，其具有优异的稳定性和吸湿性，以及可再现的晶体结构及其制备方法。
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8.发明授权公开(公告)号：US08604198B2
公开(公告)日：2013-12-10
申请号：US13194501
申请日：2011-07-29
申请人： Tomohiro Yoshida , Hiroshi Sakashita , Naoko Ueda , Shinji Kirihara , Satoru Uemori , Reiko Tsutsumiuchi , Fumihiko Akahoshi
发明人： Tomohiro Yoshida , Hiroshi Sakashita , Naoko Ueda , Shinji Kirihara , Satoru Uemori , Reiko Tsutsumiuchi , Fumihiko Akahoshi
IPC分类号： C07D417/14
CPC分类号： C07D417/14
摘要： The present invention provides 3-{(2S,4S)-4-[4-(3-methyl -1-phenyl-1H-pyrazol-5-yl)piperazin-1-yl]pyrrolidin-2 -ylcarbonyl}thiazolidine (compound I) useful as a dipeptidyl peptidase-IV inhibitor, which has superior properties of stability and hygroscopicity, and reproducible crystal structure, and a production method thereof.
摘要翻译： 本发明提供3 - {（2S，4S）-4- [4-（3-甲基-1-苯基-1H-吡唑-5-基）哌嗪-1-基]吡咯烷-2-基羰基}噻唑烷（化合物 I）作为二肽基肽酶-IV抑制剂，其具有优异的稳定性和吸湿性，以及可再现的晶体结构及其制备方法。
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9.发明申请公开(公告)号：US20090216016A1
公开(公告)日：2009-08-27
申请号：US11816493
申请日：2006-02-17
申请人： Tomohiro Yoshida , Hiroshi Sakashita , Naoko Ueda , Shinji Kirihara , Satoru Uemori , Reiko Tsutsumiuchi , Fumihiko Akahoshi
发明人： Tomohiro Yoshida , Hiroshi Sakashita , Naoko Ueda , Shinji Kirihara , Satoru Uemori , Reiko Tsutsumiuchi , Fumihiko Akahoshi
IPC分类号： C07D417/14
CPC分类号： C07D417/14
摘要： The present invention provides 3-{(2S,4S)-4-[4-(3-methyl-1-phenyl-1H -pyrazol-5-yl)piperazin-1-yl]pyrrolidin-2-ylcarbonyl}thiazolidine (compound I) useful as a dipeptidyl peptidase-IV inhibitor, which has superior properties of stability and hygroscopicity, and reproducible crystal structure, and a production method thereof.
摘要翻译： 本发明提供3 - {（2S，4S）-4- [4-（3-甲基-1-苯基-1H-吡唑-5-基）哌嗪-1-基]吡咯烷-2-基羰基}噻唑烷（化合物 I）作为二肽基肽酶-IV抑制剂，其具有优异的稳定性和吸湿性，以及可再现的晶体结构及其制备方法。
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公开(公告)号：US5948785A
公开(公告)日：1999-09-07
申请号：US952319
申请日：1997-10-27
申请人： Fumihiko Akahoshi , Takuya Yoshimura , Masahiro Eda , Atsuyuki Ashimori , Hajime Fukuyama , Masahide Nakajima , Teruaki Imada , Hideki Okunishi , Mizuo Miyazaki
发明人： Fumihiko Akahoshi , Takuya Yoshimura , Masahiro Eda , Atsuyuki Ashimori , Hajime Fukuyama , Masahide Nakajima , Teruaki Imada , Hideki Okunishi , Mizuo Miyazaki
IPC分类号： C07D213/73 , C07D213/75 , C07D239/46 , A61K31/44 , C07D213/64
CPC分类号： C07D213/73 , C07D213/75 , C07D239/47
摘要： Heterocyclic amide compounds of the formula (I) ##STR1## wherein each symbol is as defined in the specification, pharmacologically acceptable salts thereof, pharmaceutical compositions thereof and pharmaceutical use thereof. The heterocyclic amide compounds and pharmacologically acceptable salts thereof of the present invention have superior inhibitory activity against chymase groups in mammals inclusive of human, and can be administered orally or parenterally. Therefore, they are useful as chymase inhibitors and can be effective for the prophylaxis and treatment of various diseases caused by chymase, such as those caused by angiotensin II.
摘要翻译： PCT No.PCT / JP96 / 01171 Sec。 371日期1997年10月27日第 102（e）1997年10月27日PCT PCT 1996年4月26日PCT公布。 第WO96 / 33974号公报 日期：1996年10月31日式（I）的杂环酰胺化合物，其中每个符号如说明书中所定义，其药理学上可接受的盐，其药物组合物和药物用途。 本发明的杂环酰胺化合物及其药理学上可接受的盐对包括人在内的哺乳动物中的食糜酶基具有优异的抑制活性，可以口服或非肠道给药。 因此，它们可用作胃促胰酶抑制剂，并且可用于预防和治疗由胃促胰岛素引起的各种疾病，例如由血管紧张素II引起的疾病。
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