公开(公告)号：US07968595B2

公开(公告)日：2011-06-28

申请号：US11822535

申请日：2007-07-06

申请人： Sui Xiong Cai ,  John A. Drewe ,  Shailaja Kasibhatla ,  William D. Kemnitzer ,  Ben Y. Tseng ,  Charles Blais ,  Denis Labrecque ,  Henriette Gourdeau

发明人： Sui Xiong Cai ,  John A. Drewe ,  Shailaja Kasibhatla ,  William D. Kemnitzer ,  Ben Y. Tseng ,  Charles Blais ,  Denis Labrecque ,  Henriette Gourdeau

IPC分类号： A61K31/353 ,  C07D311/58

CPC分类号： C07D405/12 ,  C07D311/58

摘要： The present invention is directed to a substituted 4H-chromene represented by the Formula 1R, substantially free from the corresponding (S)-stereoisomer: The present invention also relates to the discovery that compound 1R, substantially free from the corresponding (S)-stereoisomer, is an activator of caspases and inducer of apoptosis, as well as an antivascular agent. Therefore, compound 1R, substantially free from the corresponding (S)-stereoisomer, can be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs. Compound 1R, substantially free from the corresponding (S)-stereoisomer, also can be used for the treatment of diseases due to overgrowth of vasculature, such as solid tumors and ocular neovascularization.

摘要翻译： 本发明涉及基本上不含相应（S） - 立体异构体的由式1R表示的取代的4H-色烯。本发明还涉及发现基本上不含相应的（S） - 立体异构体的化合物1R 是胱天蛋白酶和凋亡诱导剂的激活剂，以及抗血管性药剂。 因此，基本上不含相应（S） - 立体异构体的化合物1R可用于诱发异常细胞发生不受控制的生长和扩散的各种临床条件下的细胞死亡。 基本上不含相应（S） - 立体异构体的化合物1R也可用于治疗由于脉管系统过度生长（如实体瘤和眼新生血管形成）引起的疾病。

公开(公告)号：US20080085328A1

公开(公告)日：2008-04-10

申请号：US11822535

申请日：2007-07-06

申请人： Sui Xiong Cai ,  John A. Drewe ,  Shailaja Kasibhatla ,  William E. Kemnitzer ,  Ben Y. Tseng ,  Charles Blais ,  Denis Labrecque ,  Henriette Gourdeau

发明人： Sui Xiong Cai ,  John A. Drewe ,  Shailaja Kasibhatla ,  William E. Kemnitzer ,  Ben Y. Tseng ,  Charles Blais ,  Denis Labrecque ,  Henriette Gourdeau

IPC分类号： A61K31/352 ,  A61K31/351 ,  A61K31/403 ,  A61K31/4035 ,  A61K31/436 ,  A61K31/4412 ,  A61K31/502 ,  A61K31/513 ,  A61K31/661 ,  A61K33/24 ,  A61P17/00 ,  A61P35/00 ,  A61P35/02 ,  A61P37/00 ,  C07D311/68

CPC分类号： C07D405/12 ,  C07D311/58

摘要： The present invention is directed to a substituted 4H-chromene represented by the Formula 1R, substantially free from the corresponding (S)-stereoisomer: The present invention also relates to the discovery that compound 1R, substantially free from the corresponding (S)-stereoisomer, is an activator of caspases and inducer of apoptosis, as well as an antivascular agent. Therefore, compound 1R, substantially free from the corresponding (S)-stereoisomer, can be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs. Compound 1R, substantially free from the corresponding (S)-stereoisomer, also can be used for the treatment of diseases due to overgrowth of vasculature, such as solid tumors and ocular neovascularization.

摘要翻译： 本发明涉及基本上不含相应（S） - 立体异构体的由式1R表示的取代的4H-色烯。本发明还涉及发现基本上不含相应的（S） - 立体异构体的化合物1R 是胱天蛋白酶和凋亡诱导剂的激活剂，以及抗血管性药剂。 因此，基本上不含相应（S） - 立体异构体的化合物1R可用于诱发异常细胞发生不受控制的生长和扩散的各种临床条件下的细胞死亡。 基本上不含相应（S） - 立体异构体的化合物1R也可用于治疗由于脉管系统过度生长（如实体瘤和眼新生血管形成）引起的疾病。