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1. 发明申请

US20060199795A1 Receptor agonists 失效
标题翻译：受体激动剂
公开(公告)号：US20060199795A1
公开(公告)日：2006-09-07
申请号：US10543997
申请日：2004-01-27
申请人： Fumio Itoh , Shuji Hinuma , Naoyuki Kanzaki , Takashi Miki , Yuji Kawamata , Satoru Oi , Taisuke Tawaraishi , Yuji Ishichi , Mariko Hirohashi
发明人： Fumio Itoh , Shuji Hinuma , Naoyuki Kanzaki , Takashi Miki , Yuji Kawamata , Satoru Oi , Taisuke Tawaraishi , Yuji Ishichi , Mariko Hirohashi
IPC分类号： A61K31/554 , A61K31/553 , A61K31/5513
CPC分类号： C07D267/14 , A61K31/4353 , A61K31/5513 , A61K31/553
摘要： The present invention provides a TGR5 receptor agonist comprising a fused ring compound represented by the formula wherein ring A is an optionally substituted aromatic ring; and ring B′ is a 5- to 8-membered ring having one or more substituents or a salt thereof or a prodrug thereof, which is useful for the treatment of various diseases.
摘要翻译：本发明提供一种TGR5受体激动剂，其包含由下式表示的稠环化合物：其中环A为任选取代的芳环; 环B'是具有一个或多个取代基的5-至8-元环或其盐或其前药，其可用于治疗各种疾病。

2. 发明授权

US07625887B2 Receptor agonists 失效
标题翻译：受体激动剂
公开(公告)号：US07625887B2
公开(公告)日：2009-12-01
申请号：US10543997
申请日：2004-01-27
申请人： Fumio Itoh , Shuji Hinuma , Naoyuki Kanzaki , Yuji Kawamata , Taisuke Tawaraishi , Yuji Ishichi , Mariko Hirohashi
发明人： Fumio Itoh , Shuji Hinuma , Naoyuki Kanzaki , Yuji Kawamata , Taisuke Tawaraishi , Yuji Ishichi , Mariko Hirohashi
IPC分类号： A61K31/553 , A61K45/00 , C07D267/22 , C07D281/02
CPC分类号： C07D267/14 , A61K31/4353 , A61K31/5513 , A61K31/553
摘要： It is intended to provide a TGR5 receptor agonist containing a fused ring compound represented by the following general formula, its salt or a prodrug thereof: (1) wherein ring A represents an optionally substituted aromatic ring; and the ring B′ represents a 5- to 8-membered ring having one or more substituents; which is useful in treating various diseases.
摘要翻译：本发明提供一种TGR5受体激动剂，其含有下述通式表示的稠环化合物，其盐或其前药：（1）其中环A表示任选取代的芳环; 环B'表示具有一个或多个取代基的5-至8-元环; 其用于治疗各种疾病。

3. 发明申请

US20090082343A1 1,3-BENZOTHIAZINONE DERIVATIVES AND USE THEREOF 有权
标题翻译： 1,3-苯并噻嗪酮衍生物及其用途
公开(公告)号：US20090082343A1
公开(公告)日：2009-03-26
申请号：US12099779
申请日：2008-04-08
申请人： Masahiro Kajino , Yutaka Nakayama , Akira Kawada , Haruhide Kimura , Taisuke Tawaraishi
发明人： Masahiro Kajino , Yutaka Nakayama , Akira Kawada , Haruhide Kimura , Taisuke Tawaraishi
IPC分类号： A61K31/5415 , C07D401/04 , A61P9/00 , A61P1/00
CPC分类号： C07D417/04 , A61K31/5415 , C07D417/14
摘要： This invention provides a compound represented by the formula (I): wherein R1 is a hydrogen atom, a halogen atom, hydroxy, nitro, optionally halogenated alkyl, alkoxy optionally having substituents, acyl or amino optionally having substituents; R2 is pyridyl, furyl, thienyl, pyrrolyl, quinolyl, pyrazinyl, pyrimidinyl, pyridazinyl, indolyl, tetrahydroquinolyl or thiazolyl, each of which may have substituents; n is 1 or 2; or a salt. And this invention provides a safe pharmaceutical comprising the compound of the formula (I), which has an excellent apoptosis inhibitory effect and MIF binding effect, for preventing and/or treating heart disease, nervous degenerative disease, cerebrovascular disease, central nervous infectious disease, traumatorathy, demyelinating disease, bone and articular disease, kidney disease, liver disease, osteomyelodysplasia, AIDS, cancer, and the like.
摘要翻译：本发明提供由式（I）表示的化合物：其中R1是氢原子，卤素原子，羟基，硝基，任选卤代烷基，任选具有取代基的烷氧基，任选具有取代基的酰基或氨基; R 2是可以具有取代基的吡啶基，呋喃基，噻吩基，吡咯基，喹啉基，吡嗪基，嘧啶基，哒嗪基，吲哚基，四氢喹啉基或噻唑基。 n为1或2; 或盐。本发明提供了一种安全药物，其包含具有优异的细胞凋亡抑制作用和MIF结合作用的式（I）化合物，用于预防和/或治疗心脏病，神经退行性疾病，脑血管病，中枢神经感染性疾病，外伤，脱髓鞘疾病，骨和关节疾病，肾脏疾病，肝病，骨发育不良，艾滋病，癌症等。

4. 发明授权

US07767665B2 1,3-benzothiazinone derivatives and use thereof 有权
标题翻译： 1,3-苯并噻嗪酮衍生物及其用途
公开(公告)号：US07767665B2
公开(公告)日：2010-08-03
申请号：US12099779
申请日：2008-04-08
申请人： Masahiro Kajino , Yutaka Nakayama , Akira Kawada , Haruhide Kimura , Taisuke Tawaraishi
发明人： Masahiro Kajino , Yutaka Nakayama , Akira Kawada , Haruhide Kimura , Taisuke Tawaraishi
IPC分类号： C07D417/04 , A61K31/538
CPC分类号： C07D417/04 , A61K31/5415 , C07D417/14
摘要： This invention provides a compound represented by the formula (I): wherein R1 is a hydrogen atom, a halogen atom, hydroxy, nitro, optionally halogenated alkyl, alkoxy optionally having substituents, acyl or amino optionally having substituents; R2 is pyridyl, furyl, thienyl, pyrrolyl, quinolyl, pyrazinyl, pyrimidinyl, pyridazinyl, indolyl, tetrahydroquinolyl or thiazolyl, each of which may have substituents; n is 1 or 2; or a salt. And this invention provides a safe pharmaceutical comprising the compound of the formula (I), which has an excellent apoptosis inhibitory effect and MIF binding effect, for preventing and/or treating heart disease, nervous degenerative disease, cerebrovascular disease, central nervous infectious disease, traumatorathy, demyelinating disease, bone and articular disease, kidney disease, liver disease, osteomyelodysplasia, AIDS, cancer, and the like.
摘要翻译：本发明提供由式（I）表示的化合物：其中R1是氢原子，卤素原子，羟基，硝基，任选卤代烷基，任选具有取代基的烷氧基，任选具有取代基的酰基或氨基; R 2是可以具有取代基的吡啶基，呋喃基，噻吩基，吡咯基，喹啉基，吡嗪基，嘧啶基，哒嗪基，吲哚基，四氢喹啉基或噻唑基。 n为1或2; 或盐。本发明提供一种安全药物，其包含具有优异的细胞凋亡抑制作用和MIF结合作用的式（I）化合物，用于预防和/或治疗心脏病，神经退行性疾病，脑血管病，中枢神经感染性疾病，外伤，脱髓鞘疾病，骨和关节疾病，肾脏疾病，肝病，骨发育不良，艾滋病，癌症等。

5. 发明授权

US07399759B2 1, 3-benzothiazinone derivatives and use thereof 有权
标题翻译： 1,3-苯并噻嗪酮衍生物及其用途
公开(公告)号：US07399759B2
公开(公告)日：2008-07-15
申请号：US10488384
申请日：2002-09-02
申请人： Masahiro Kajino , Akira Kawada , Yutaka Nakayama , Haruhide Kimura , Taisuke Tawaraishi
发明人： Masahiro Kajino , Akira Kawada , Yutaka Nakayama , Haruhide Kimura , Taisuke Tawaraishi
IPC分类号： C07D417/04 , A61K31/538
CPC分类号： C07D417/04 , A61K31/5415 , C07D417/14
摘要： This invention provides a compound represented by the formula (I): wherein R1 is a hydrogen atom, a halogen atom, hydroxy, nitro, optionally halogenated alkyl, alkoxy optionally having substituents, acyl or amino optionally having substituents; R2 is pyridyl, furyl, thienyl, pyrrolyl, quinolyl, pyrazinyl, pyrimidinyl, pyridazinyl, indolyl, tetrahydroquinolyl or thiazolyl, each of which may have substituents; n is 1 or 2; or a salt. And this invention provides a safe pharmaceutical comprising the compound of the formula (I), which has an excellent apoptosis inhibitory effect and MIF binding effect, for preventing and/or treating heart disease, nervous degenerative disease, cerebrovascular disease, central nervous infectious disease, traumatorathy, demyelinating disease, bone and articular disease, kidney disease, liver disease, osteomyelodysplasia, AIDS, cancer, and the like.
摘要翻译：本发明提供由式（I）表示的化合物：其中R 1是氢原子，卤素原子，羟基，硝基，任选卤代烷基，任选具有取代基的烷氧基，任选具有取代基; R 2是吡啶基，呋喃基，噻吩基，吡咯基，喹啉基，吡嗪基，嘧啶基，哒嗪基，吲哚基，四氢喹啉基或噻唑基，它们各自可以具有取代基; n为1或2; 或盐。本发明提供了一种安全药物，其包含具有优异的细胞凋亡抑制作用和MIF结合作用的式（I）化合物，用于预防和/或治疗心脏病，神经退行性疾病，脑血管病，中枢神经感染性疾病，外伤，脱髓鞘疾病，骨和关节疾病，肾脏疾病，肝病，骨发育不良，艾滋病，癌症等。

6. 发明申请

US20110009384A1 FUSED RING COMPOUNDS AS PARTIAL AGONISTS OF PPAR-GAMMA 审中-公开
标题翻译：熔融环化合物作为PPAR-GAMMA的部分激发剂
公开(公告)号：US20110009384A1
公开(公告)日：2011-01-13
申请号：US12449388
申请日：2008-02-05
申请人： Taisuke Tawaraishi , Hiroshi Imoto , Nobuo Cho
发明人： Taisuke Tawaraishi , Hiroshi Imoto , Nobuo Cho
IPC分类号： A61K31/55 , C07D403/02 , A61K31/4155 , A61K31/4184 , C07D471/04 , A61K31/437 , C07D401/02 , A61K31/4709 , C07D417/14 , A61K31/427 , C07D413/14 , A61K31/4245 , A61K31/5377 , C07D403/14 , C07D401/14 , A61K31/454 , A61P3/10
CPC分类号： C07D403/04 , C07D231/12 , C07D401/14 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D491/113
摘要： The present invention provides an agent for the prophylaxis or treatment of diabetes, which has a superior hypoglycemic action, and is associated with a fewer side effects such as body weight gain and the like.The resent invention relates an agent for the prophylaxis or treatment of diabetes, which comprises a compound represented by wherein each symbol is as defined in the description, or a salt thereof or a prodrug thereof.
摘要翻译：本发明提供了预防或治疗糖尿病的药剂，其具有优异的降血糖作用，并且与较少的副作用如体重增加等有关。本发明涉及用于预防或治疗糖尿病的药剂，其包含其中每个符号如说明书中所定义的化合物或其盐或其前药。

7. 发明申请

US20080194617A1 Fused ring compound 审中-公开
标题翻译：稠环化合物
公开(公告)号：US20080194617A1
公开(公告)日：2008-08-14
申请号：US12068442
申请日：2008-02-06
申请人： Taisuke Tawaraishi , Hiroshi Imoto , Nobuo Cho
发明人： Taisuke Tawaraishi , Hiroshi Imoto , Nobuo Cho
IPC分类号： A61K31/437 , C07D403/02 , A61K31/4155 , A61P3/08 , C07D471/04
CPC分类号： C07D403/04 , C07D231/12 , C07D401/14 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D491/113
摘要： The present invention provides an agent for the prophylaxis or treatment of diabetes, which has a superior hypoglycemic action, and is associated with a fewer side effects such as body weight gain and the like.The present invention relates an agent for the prophylaxis or treatment of diabetes, which comprises a compound represented by wherein each symbol is as defined in the description, or a salt thereof or a prodrug thereof.
摘要翻译：本发明提供了预防或治疗糖尿病的药剂，其具有优异的降血糖作用，并且与较少的副作用如体重增加等有关。本发明涉及用于预防或治疗糖尿病的药剂，其包含其中每个符号如说明书中所定义的化合物或其盐或其前药。

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