公开(公告)号：US08158638B2

公开(公告)日：2012-04-17

申请号：US12442094

申请日：2007-09-14

申请人： Satoru Ohsuki ,  Atsushi Tengeiji ,  Masahiro Ikeda ,  Yoshihiro Shibata ,  Chikahiro Nagata ,  Takashi Shimada

发明人： Satoru Ohsuki ,  Atsushi Tengeiji ,  Masahiro Ikeda ,  Yoshihiro Shibata ,  Chikahiro Nagata ,  Takashi Shimada

IPC分类号： A61K31/505 ,  A61K31/415 ,  C07D491/00 ,  C07D487/02

CPC分类号： C07D495/16 ,  C07D495/20 ,  C07D495/22 ,  C07D498/22

摘要： Problem to be SolvedTo provide a novel compound inhibiting the effect of HSP90, in particular a novel compound inhibiting the function of HSP90 as a chaperone protein and having antitumor activity.SolutionThe present invention provides a pyrazolopyrimidine compound represented by the formula (1) having various substituents which inhibits the ATPase activity of HSP90 and which has antitumor activity, an HSP90 inhibitor comprising the compound represented by the formula (1), a medicament comprising the compound represented by the formula (1), an anticancer agent comprising the compound represented by the formula (1), a pharmaceutical composition comprising the compound represented by the formula (1) and a method for treating cancer using the compound represented by the formula (1).

摘要翻译： 要解决的问题提供抑制HSP90的作用的新型化合物，特别是抑制HSP90作为伴侣蛋白的功能并具有抗肿瘤活性的新化合物。 溶液本发明提供了具有抑制HSP90的ATP酶活性且具有抗肿瘤活性的各种取代基的式（1）表示的吡唑并嘧啶化合物，包含由式（1）表示的化合物的HSP90抑制剂，包含化合物 （1）代表的抗癌剂，包含由式（1）表示的化合物的抗癌剂，包含式（1）表示的化合物的药物组合物和使用式（1）表示的化合物治疗癌症的方法 ）。

公开(公告)号：US20100113410A1

公开(公告)日：2010-05-06

申请号：US12442094

申请日：2007-09-14

申请人： Satoru Ohsuki ,  Atsushi Tengeiji ,  Masahiro Ikeda ,  Yoshihiro Shibata ,  Chikahiro Nagata ,  Takashi Shimada

发明人： Satoru Ohsuki ,  Atsushi Tengeiji ,  Masahiro Ikeda ,  Yoshihiro Shibata ,  Chikahiro Nagata ,  Takashi Shimada

IPC分类号： A61K31/519 ,  C07D495/16 ,  C07D487/04 ,  C07D495/20 ,  A61K31/5377 ,  A61P35/00

CPC分类号： C07D495/16 ,  C07D495/20 ,  C07D495/22 ,  C07D498/22

摘要： Problem to be Solved To provide a novel compound inhibiting the effect of HSP90, in particular a novel compound inhibiting the function of HSP90 as a chaperone protein and having antitumor activity. Solution The present invention provides a pyrazolopyrimidine compound represented by the formula (1) having various substituents which inhibits the ATPase activity of HSP90 and which has antitumor activity, an HSP90 inhibitor comprising the compound represented by the formula (1), a medicament comprising the compound represented by the formula (1), an anticancer agent comprising the compound represented by the formula (1), a pharmaceutical composition comprising the compound represented by the formula (1) and a method for treating cancer using the compound represented by the formula (1).

摘要翻译： 要解决的问题提供抑制HSP90的作用的新型化合物，特别是抑制HSP90作为伴侣蛋白的功能并具有抗肿瘤活性的新化合物。 溶液本发明提供了具有抑制HSP90的ATP酶活性且具有抗肿瘤活性的各种取代基的式（1）表示的吡唑并嘧啶化合物，包含由式（1）表示的化合物的HSP90抑制剂，包含化合物 （1）代表的抗癌剂，包含由式（1）表示的化合物的抗癌剂，包含式（1）表示的化合物的药物组合物和使用式（1）表示的化合物治疗癌症的方法 ）。