-
公开(公告)号:US20070105935A1
公开(公告)日:2007-05-10
申请号:US10556043
申请日:2004-05-07
IPC分类号: A61K31/405 , C07D403/02
CPC分类号: C07D207/12
摘要: This invention provides an industrially useful process for producing 1,4-transcyclohexanecarboxylic acid derivative (1) which has excellent VLA-4 inhibitory action and safety, and an intermediate which is useful in such method. More particularly, this invention relates to a process for converting a compound of formula (I) into a compound of formula (VI) by the reaction scheme:
摘要翻译: 本发明提供了具有优异的VLA-4抑制作用和安全性的1,4-反式环己烷羧酸衍生物(1)的工业上有用的方法和可用于该方法的中间体。 更具体地,本发明涉及通过反应方案将式(I)化合物转化为式(VI)的化合物的方法:
-
公开(公告)号:US07345179B2
公开(公告)日:2008-03-18
申请号:US10556043
申请日:2004-05-07
IPC分类号: C07F9/02
CPC分类号: C07D207/12
摘要: This invention provides an industrially useful process for producing 1,4-transcyclohexanecarboxylic acid derivative (1) which has excellent VLA-4 inhibitory action and safety, and an intermediate which is useful in such method. More particularly, this invention relates to a process for converting a compound of formula (I) into a compound of formula (VI) by the reaction scheme:
摘要翻译: 本发明提供了具有优异的VLA-4抑制作用和安全性的1,4-反式环己烷羧酸衍生物(1)的工业上有用的方法和可用于该方法的中间体。 更具体地,本发明涉及通过反应方案将式(I)化合物转化为式(VI)的化合物的方法:
-
公开(公告)号:US08097622B2
公开(公告)日:2012-01-17
申请号:US12579175
申请日:2009-10-14
申请人: Kiyoshi Nakayama , Kazuyuki Sugita , Masaki Setoguchi , Yuichi Tominaga , Masanori Saitou , Takashi Odagiri
发明人: Kiyoshi Nakayama , Kazuyuki Sugita , Masaki Setoguchi , Yuichi Tominaga , Masanori Saitou , Takashi Odagiri
IPC分类号: A61K31/535 , C07D413/14
CPC分类号: C07D473/34
摘要: There is provided a novel compound that inhibits phosphatidylinositol 3-kinase (PI3K) and/or the mammalian target of rapamycin (mTOR) and exhibits anti-tumor activity. The present invention provides a compound represented by the following formula (1) having various substituents that inhibits PI3K and/or mTOR and exhibits anti-tumor activity: wherein R1, R2, R3, R4, Ra, Rb, Rc, and X each have the same meaning as defined in the specification.
-
公开(公告)号:US20100130492A1
公开(公告)日:2010-05-27
申请号:US12579175
申请日:2009-10-14
申请人: Kiyoshi Nakayama , Kazuyuki Sugita , Masaki Setoguchi , Yuichi Tominaga , Masanori Saitou , Takashi Odagiri
发明人: Kiyoshi Nakayama , Kazuyuki Sugita , Masaki Setoguchi , Yuichi Tominaga , Masanori Saitou , Takashi Odagiri
IPC分类号: A61K31/5377 , C07D487/04 , A61P43/00 , A61P35/00
CPC分类号: C07D473/34
摘要: There is provided a novel compound that inhibits phosphatidylinositol 3-kinase (PI3K) and/or the mammalian target of rapamycin (mTOR) and exhibits anti-tumor activity. The present invention provides a compound represented by the following formula (1) having various substituents that inhibits PI3K and/or mTOR and exhibits anti-tumor activity: wherein R1, R2, R3, R4, Ra, Rb, Rc, and X each have the same meaning as defined in the specification.
摘要翻译: 提供抑制磷脂酰肌醇3-激酶(PI3K)和/或雷帕霉素(mTOR)的哺乳动物靶标并表现出抗肿瘤活性的新型化合物。 本发明提供具有抑制PI3K和/或mTOR的各种取代基并表现出抗肿瘤活性的下述式(1)表示的化合物:其中R1,R2,R3,R4,Ra,Rb,Rc和X各自具有 与本说明书中定义的含义相同。
-
公开(公告)号:US20130165424A9
公开(公告)日:2013-06-27
申请号:US13416061
申请日:2012-03-09
申请人: Yuuichi Sugimoto , Kouichi Uoto , Takanori Wakabayashi , Masaki Miyazaki , Masaki Setoguchi , Toru Taniguchi , Keisuke Yoshida , Akitake Yamaguchi , Shoko Yoshida
发明人: Yuuichi Sugimoto , Kouichi Uoto , Takanori Wakabayashi , Masaki Miyazaki , Masaki Setoguchi , Toru Taniguchi , Keisuke Yoshida , Akitake Yamaguchi , Shoko Yoshida
IPC分类号: C07D487/10 , A61P35/02 , A61K31/438 , A61P35/00 , A61K31/407 , C07D471/10
CPC分类号: C07D487/20 , A61K9/14 , A61K9/1623 , A61K9/1652 , A61K9/2018 , A61K9/2054 , A61K9/2059 , C07D471/20 , C07D487/10
摘要: A compound that inhibits interaction between murine double minute 2 (Mdm2) protein and p53 protein and exhibits anti-tumor activity is provided. The present invention provides a dispiropyrrolidine derivative represented by the following formula (1), which has various substituents, inhibits interaction between Mdm2 protein and p53 protein and exhibits anti-tumor activity, wherein R1, R2, R3, ring A, and ring B in formula (1) respectively have the same meanings as defined in the specification.
摘要翻译: 提供抑制鼠双分钟2(Mdm2)蛋白和p53蛋白之间的相互作用并表现出抗肿瘤活性的化合物。 本发明提供由下式(1)表示的去甲吡咯烷衍生物,其具有各种取代基,抑制Mdm2蛋白与p53蛋白之间的相互作用并表现出抗肿瘤活性,其中R1,R2,R3,环A和环B在 式(1)分别具有与说明书中定义的相同的含义。
-
公开(公告)号:US08309546B2
公开(公告)日:2012-11-13
申请号:US13308239
申请日:2011-11-30
申请人: Kiyoshi Nakayama , Kazuyuki Sugita , Masaki Setoguchi , Yuichi Tominaga , Masanori Saitou , Takashi Odagiri
发明人: Kiyoshi Nakayama , Kazuyuki Sugita , Masaki Setoguchi , Yuichi Tominaga , Masanori Saitou , Takashi Odagiri
IPC分类号: A61K31/535 , C07D413/14
CPC分类号: C07D473/34
摘要: There is provided a novel compound that inhibits phosphatidylinositol 3-kinase (PI3K) and/or the mammalian target of rapamycin (mTOR) and exhibits anti-tumor activity. The present invention provides a compound represented by the following formula (1) having various substituents that inhibits PI3K and/or mTOR and exhibits anti-tumor activity: wherein R1, R2, R3, R4, Ra, Rb, Rc, and X each have the same meaning as defined in the specification.
摘要翻译: 提供抑制磷脂酰肌醇3-激酶(PI3K)和/或雷帕霉素(mTOR)的哺乳动物靶标并表现出抗肿瘤活性的新型化合物。 本发明提供具有抑制PI3K和/或mTOR的各种取代基并表现出抗肿瘤活性的下述式(1)表示的化合物:其中R1,R2,R3,R4,Ra,Rb,Rc和X各自具有 与本说明书中定义的含义相同。
-
公开(公告)号:US08629133B2
公开(公告)日:2014-01-14
申请号:US13416061
申请日:2012-03-09
申请人: Yuuichi Sugimoto , Kouichi Uoto , Takanori Wakabayashi , Masaki Miyazaki , Masaki Setoguchi , Toru Taniguchi , Keisuke Yoshida , Akitake Yamaguchi , Shoko Yoshida
发明人: Yuuichi Sugimoto , Kouichi Uoto , Takanori Wakabayashi , Masaki Miyazaki , Masaki Setoguchi , Toru Taniguchi , Keisuke Yoshida , Akitake Yamaguchi , Shoko Yoshida
IPC分类号: A61K31/407 , C07D487/10
CPC分类号: C07D487/20 , A61K9/14 , A61K9/1623 , A61K9/1652 , A61K9/2018 , A61K9/2054 , A61K9/2059 , C07D471/20 , C07D487/10
摘要: A compound that inhibits interaction between murine double minute 2 (Mdm2) protein and p53 protein and exhibits anti-tumor activity is provided. The present invention provides a dispiropyrrolidine derivative represented by the following formula (1), which has various substituents, inhibits interaction between Mdm2 protein and p53 protein and exhibits anti-tumor activity, wherein R1, R2, R3, ring A, and ring B in formula (1) respectively have the same meanings as defined in the specification.
摘要翻译: 提供抑制鼠双分钟2(Mdm2)蛋白和p53蛋白之间的相互作用并表现出抗肿瘤活性的化合物。 本发明提供由下式(1)表示的去甲吡咯烷衍生物,其具有各种取代基,抑制Mdm2蛋白与p53蛋白之间的相互作用并表现出抗肿瘤活性,其中R1,R2,R3,环A和环B在 式(1)分别具有与说明书中定义的相同的含义。
-
公开(公告)号:US20120264738A1
公开(公告)日:2012-10-18
申请号:US13416061
申请日:2012-03-09
申请人: Yuuichi Sugimoto , Kouichi Uoto , Takanori Wakabayashi , Masaki Miyazaki , Masaki Setoguchi , Toru Taniguchi , Keisuke Yoshida , Akitake Yamaguchi , Shoko Yoshida
发明人: Yuuichi Sugimoto , Kouichi Uoto , Takanori Wakabayashi , Masaki Miyazaki , Masaki Setoguchi , Toru Taniguchi , Keisuke Yoshida , Akitake Yamaguchi , Shoko Yoshida
IPC分类号: C07D487/10 , A61P35/02 , A61K31/438 , A61P35/00 , A61K31/407 , C07D471/10
CPC分类号: C07D487/20 , A61K9/14 , A61K9/1623 , A61K9/1652 , A61K9/2018 , A61K9/2054 , A61K9/2059 , C07D471/20 , C07D487/10
摘要: A compound that inhibits interaction between murine double minute 2 (Mdm2) protein and p53 protein and exhibits anti-tumor activity is provided. The present invention provides a dispiropyrrolidine derivative represented by the following formula (1), which has various substituents, inhibits interaction between Mdm2 protein and p53 protein and exhibits anti-tumor activity, wherein R1, R2, R3, ring A, and ring B in formula (1) respectively have the same meanings as defined in the specification.
摘要翻译: 提供抑制鼠双分钟2(Mdm2)蛋白和p53蛋白之间的相互作用并表现出抗肿瘤活性的化合物。 本发明提供由下式(1)表示的去甲吡咯烷衍生物,其具有各种取代基,抑制Mdm2蛋白与p53蛋白之间的相互作用并表现出抗肿瘤活性,其中R1,R2,R3,环A和环B在 式(1)分别具有与说明书中定义的相同的含义。
-
公开(公告)号:US20120071476A1
公开(公告)日:2012-03-22
申请号:US13308239
申请日:2011-11-30
申请人: Kiyoshi Nakayama , Kazuyuki Sugita , Masaki Setoguchi , Yuichi Tominaga , Masanori Saitou , Takashi Odagiri
发明人: Kiyoshi Nakayama , Kazuyuki Sugita , Masaki Setoguchi , Yuichi Tominaga , Masanori Saitou , Takashi Odagiri
IPC分类号: A61K31/5377 , A61P35/00 , C07D413/14
CPC分类号: C07D473/34
摘要: There is provided a novel compound that inhibits phosphatidylinositol 3-kinase (PI3K) and/or the mammalian target of rapamycin (mTOR) and exhibits anti-tumor activity. The present invention provides a compound represented by the following formula (1) having various substituents that inhibits PI3K and/or mTOR and exhibits anti-tumor activity: wherein R1, R2, R3, R4, Ra, Rb, Rc, and X each have the same meaning as defined in the specification.
摘要翻译: 提供抑制磷脂酰肌醇3-激酶(PI3K)和/或雷帕霉素(mTOR)的哺乳动物靶标并表现出抗肿瘤活性的新型化合物。 本发明提供具有抑制PI3K和/或mTOR的各种取代基并表现出抗肿瘤活性的下述式(1)表示的化合物:其中R1,R2,R3,R4,Ra,Rb,Rc和X各自具有 与本说明书中定义的含义相同。
-
-
-
-
-
-
-
-