公开(公告)号：US20100210591A1

公开(公告)日：2010-08-19

申请号：US12682097

申请日：2008-10-10

申请人： Yoshimitsu Suda ,  Hiromi Oshiumi ,  Koji Murakami

发明人： Yoshimitsu Suda ,  Hiromi Oshiumi ,  Koji Murakami

IPC分类号： A61K31/695 ,  C07F7/10

CPC分类号： C07F7/0812 ,  C07F7/081

摘要： The present invention provides a compound that exhibits an excellent antitumor effect and reduces side effects, such as skin disorders, of the existing retinoid by selectively activating on the nuclear receptor RARα, thereby possibly producing significant improvement of clinical profits. Specifically, the present invention provides a bis(trimethylsilyl)phenyl compound represented by Formula (I): wherein X is N or CH; Y is O or S; R1, R2, and R3 are the same or different and are hydrogen or lower alkyl; R4 and R5 are the same or different and are hydrogen, lower alkyl, or halogen; and a bond between a carbon atom to which R1 is attached and a carbon atom to which R2 is attached is a single bond or a double bond; or a salt thereof.

摘要翻译： 本发明提供通过选择性活化核受体RARα而显示出优异的抗肿瘤效果并降低现有类视色素的副作用，例如皮肤病，从而可能显着改善临床利益。 具体地说，本发明提供由式（I）表示的双（三甲基甲硅烷基）苯基化合物：其中X是N或CH; Y为O或S; R1，R2和R3相同或不同，为氢或低级烷基; R4和R5相同或不同，为氢，低级烷基或卤素; 并且R 1所连接的碳原子和R 2所连接的碳原子之间的键为单键或双键; 或其盐。

公开(公告)号：US07855300B2

公开(公告)日：2010-12-21

申请号：US12682097

申请日：2008-10-10

申请人： Yoshimitsu Suda ,  Hiromi Oshiumi ,  Koji Murakami

发明人： Yoshimitsu Suda ,  Hiromi Oshiumi ,  Koji Murakami

IPC分类号： C07F7/10

CPC分类号： C07F7/0812 ,  C07F7/081

摘要： The present invention provides a compound that exhibits an excellent antitumor effect and reduces side effects, such as skin disorders, of the existing retinoid by selectively activating on the nuclear receptor RARα, thereby possibly producing significant improvement of clinical profits. Specifically, the present invention provides a bis(trimethylsilyl)phenyl compound represented by Formula (I): wherein X is N or CH; Y is O or S; R1, R2, and R3 are the same or different and are hydrogen or lower alkyl; R4 and R5 are the same or different and are hydrogen, lower alkyl, or halogen; and a bond between a carbon atom to which R1 is attached and a carbon atom to which R2 is attached is a single bond or a double bond; or a salt thereof.

摘要翻译： 本发明提供通过选择性活化核受体RARα，显示出优异的抗肿瘤效果并降低现有类视黄醇的副作用，例如皮肤病，从而可能显着改善临床利益。 具体地说，本发明提供由式（I）表示的双（三甲基甲硅烷基）苯基化合物：其中X是N或CH; Y为O或S; R1，R2和R3相同或不同，为氢或低级烷基; R4和R5相同或不同，为氢，低级烷基或卤素; 并且R 1所连接的碳原子和R 2所连接的碳原子之间的键为单键或双键; 或其盐。

公开(公告)号：US08779142B2

公开(公告)日：2014-07-15

申请号：US13378527

申请日：2010-07-09

申请人： Makoto Kitade ,  Shuichi Ohkubo ,  Chihoko Yoshimura ,  Satoshi Yamashita ,  Hiromi Oshiumi ,  Takao Uno ,  Yuichi Kawai

发明人： Makoto Kitade ,  Shuichi Ohkubo ,  Chihoko Yoshimura ,  Satoshi Yamashita ,  Hiromi Oshiumi ,  Takao Uno ,  Yuichi Kawai

IPC分类号： A61K31/4365 ,  C07D471/04

CPC分类号： C07D471/04 ,  C07D209/08 ,  C07D519/00

摘要： It is intended to provide a novel azabicyclo compound which exhibits both HSP90 inhibitory activity and cell proliferation inhibitory effect. Specifically disclosed is a compound represented by the following general formula (I) or a salt thereof: wherein X1 represents CH or N; any one of X2, X3 and X4 represents N, and the others represent CH; any one or two of Y1, Y2, Y3 and Y4 represent C—R4, and the others are the same or different and represent CH or N; R1 represents an optionally substituted monocyclic or bicyclic unsaturated heterocyclic group having 1 to 4 heteroatoms selected from N, S and O; R2 represents an alkyl group having 1 to 6 carbon atoms, or the like; and R3 and R4 represent —CO—R5 or the like.

摘要翻译： 旨在提供表现出HSP90抑制活性和细胞增殖抑制作用的新型氮杂双环化合物。 具体公开的是由下列通式（I）表示的化合物或其盐：其中X1表示CH或N; X2，X3和X4中的任一个表示N，其余的表示CH; Y 1，Y 2，Y 3和Y 4中的任何一个或两个表示C-R 4，其余的相同或不同，表示CH或N; R1表示具有1至4个选自N，S和O的杂原子的任选取代的单环或双环不饱和杂环基; R2表示碳原子数1〜6的烷基等。 R3和R4表示-CO-R5等。

公开(公告)号：US20120108589A1

公开(公告)日：2012-05-03

申请号：US13378527

申请日：2010-07-09

申请人： Makoto Kitade ,  Shuichi Ohkubo ,  Chihoko Yoshimura ,  Satoshi Yamashita ,  Hiromi Oshiumi ,  Takao Uno ,  Yuichi Kawai

发明人： Makoto Kitade ,  Shuichi Ohkubo ,  Chihoko Yoshimura ,  Satoshi Yamashita ,  Hiromi Oshiumi ,  Takao Uno ,  Yuichi Kawai

IPC分类号： A61K31/437 ,  A61K31/5377 ,  A61P35/00 ,  C07D471/04

CPC分类号： C07D471/04 ,  C07D209/08 ,  C07D519/00

摘要： It is intended to provide a novel azabicyclo compound which exhibits both HSP90 inhibitory activity and cell proliferation inhibitory effect. Specifically disclosed is a compound represented by the following general formula (I) or a salt thereof: wherein X1 represents CH or N; any one of X2, X3 and X4 represents N, and the others represent CH; any one or two of Y1, Y2, Y3 and Y4 represent C—R4, and the others are the same or different and represent CH or N; R1 represents an optionally substituted monocyclic or bicyclic unsaturated heterocyclic group having 1 to 4 heteroatoms selected from N, S and O; R2 represents an alkyl group having 1 to 6 carbon atoms, or the like; and R3 and R4 represent —CO—R5 or the like.

摘要翻译： 旨在提供表现出HSP90抑制活性和细胞增殖抑制作用的新型氮杂双环化合物。 具体公开的是由下列通式（I）表示的化合物或其盐：其中X1表示CH或N; X2，X3和X4中的任一个表示N，其余的表示CH; Y 1，Y 2，Y 3和Y 4中的任何一个或两个表示C-R 4，其余的相同或不同，表示CH或N; R1表示具有1至4个选自N，S和O的杂原子的任选取代的单环或双环不饱和杂环基; R2表示碳原子数1〜6的烷基等。 R3和R4表示-CO-R5等。