公开(公告)号：US07176234B2

公开(公告)日：2007-02-13

申请号：US10609670

申请日：2003-07-01

申请人： Sui Xiong Cai ,  Shailaja Kasibhatla ,  Kristin P. Ollis ,  Han-Zhong Zhang ,  John A. Drewe ,  Ben Tseng ,  Nilantha Sudath Sirisoma

发明人： Sui Xiong Cai ,  Shailaja Kasibhatla ,  Kristin P. Ollis ,  Han-Zhong Zhang ,  John A. Drewe ,  Ben Tseng ,  Nilantha Sudath Sirisoma

IPC分类号： A61K31/352 ,  C07D313/06

CPC分类号： A61K31/00 ,  C07D493/20

摘要： The present invention is directed to derivatives of gambogic acid and analogs thereof. Exemplary gambogic acid derivatives of the present invention include, among others, derivatives substituted in the C10 and C28 positions of gambogic acid. The present invention also relates to the discovery that certain preferred compounds of the present invention are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention can be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.

摘要翻译： 本发明涉及吡啶酸及其类似物的衍生物。 本发明的示例性的吡咯烷酸衍生物包括其中取代为吡咯烷酸的C10和C28位置的衍生物。 本发明还涉及本发明的某些优选化合物是胱天蛋白酶的活化剂和凋亡诱导剂的发现。 因此，本发明的胱天蛋白酶和细胞凋亡诱导剂的激活剂可用于诱导异常细胞发生不受控制的生长和扩散的各种临床病症中的细胞死亡。

公开(公告)号：US07435750B2

公开(公告)日：2008-10-14

申请号：US11074077

申请日：2005-03-08

申请人： Sui Xiong Cai ,  Han-Zhong Zhang ,  John A. Drewe ,  P. Sanjeeva Reddy ,  Shailaja Kasibhatla ,  Jared Daniel Kuemmerle ,  Kristin P. Ollis

发明人： Sui Xiong Cai ,  Han-Zhong Zhang ,  John A. Drewe ,  P. Sanjeeva Reddy ,  Shailaja Kasibhatla ,  Jared Daniel Kuemmerle ,  Kristin P. Ollis

IPC分类号： A61K31/422 ,  A61K31/4245 ,  A61K31/443 ,  A61K31/4709 ,  A61K31/4155 ,  A61K31/4178 ,  A61K31/4025 ,  A61K31/381 ,  A61K31/341 ,  A61K31/519 ,  A61K31/4725

CPC分类号： C07D413/14 ,  A61K31/335 ,  A61K31/38 ,  A61K31/395 ,  C07D409/04 ,  C07D409/14 ,  C07D413/04 ,  C07D417/14 ,  C07D471/04

摘要： The present invention is directed to substituted 3-aryl-5-aryl-[1,2,4]-oxadiazoles and analogs thereof, represented by the Formula I: wherein Ar1, Ar3, A, B and D are defined herein. The present invention also relates to the discovery that compounds having Formula I are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention may be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.

摘要翻译： 本发明涉及由式I表示的取代的3-芳基-5-芳基 - [1,2,4] - 恶二唑及其类似物：其中Ar 1，Ar 3 A，B和D在本文中定义。 本发明还涉及发现具有式I的化合物是胱天蛋白酶的活化剂和凋亡诱导剂。 因此，本发明的胱天蛋白酶和细胞凋亡诱导剂的激活剂可用于在异常细胞发生不受控制的生长和扩散的各种临床病症中诱导细胞死亡。

公开(公告)号：US07041685B2

公开(公告)日：2006-05-09

申请号：US10164705

申请日：2002-06-10

申请人： Sui Xiong Cai ,  Han-Zhong Zhang ,  John A. Drewe ,  P. Sanjeeva Reddy ,  Shailaja Kasibhatla ,  Jared Daniel Kuemmerle ,  Kristin P. Ollis

发明人： Sui Xiong Cai ,  Han-Zhong Zhang ,  John A. Drewe ,  P. Sanjeeva Reddy ,  Shailaja Kasibhatla ,  Jared Daniel Kuemmerle ,  Kristin P. Ollis

IPC分类号： A61K31/44 ,  C07D413/14

CPC分类号： C07D413/14 ,  A61K31/335 ,  A61K31/38 ,  A61K31/395 ,  C07D409/04 ,  C07D409/14 ,  C07D413/04 ,  C07D417/14 ,  C07D471/04

摘要： The present invention is directed to substituted 3-aryl-5-aryl-[1,2,4]-oxadiazoles and analogs thereof, represented by the Formula I: wherein Ar1, Ar3, A, B and D are defined herein. The present invention also relates to the discovery that compounds having Formula I are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention may be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.

摘要翻译： 本发明涉及由式I表示的取代的3-芳基-5-芳基 - [1,2,4] - 恶二唑及其类似物：其中Ar 1，Ar 3 A，B和D在本文中定义。 本发明还涉及发现具有式I的化合物是胱天蛋白酶的活化剂和凋亡诱导剂。 因此，本发明的胱天蛋白酶和细胞凋亡诱导剂的激活剂可用于在异常细胞发生不受控制的生长和扩散的各种临床病症中诱导细胞死亡。