公开(公告)号：US07074813B2

公开(公告)日：2006-07-11

申请号：US10816893

申请日：2004-04-05

申请人： Sui Xiong Cai ,  Shailaja Kasibhatla ,  John Drewe ,  P. Sanjeeva Reddy ,  Han-Zhong Zhang

发明人： Sui Xiong Cai ,  Shailaja Kasibhatla ,  John Drewe ,  P. Sanjeeva Reddy ,  Han-Zhong Zhang

IPC分类号： A61K31/44 ,  C07D213/643 ,  C07D213/69 ,  C07D213/70

CPC分类号： A61K31/165 ,  A61K31/44 ,  C07D213/87 ,  C07D213/89 ,  C07D401/14

摘要： The present invention is directed to substituted N′-(arylcarbonyl)-benzhydrazides, N′-(arylcarbonyl)-benzylidene-hydrazides and analogs thereof, represented by the Formulae I and II: wherein Ar1, Ar2, and R1–R2 are defined herein. The present invention also relates to the discovery that compounds having Formulae I and II 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和II表示的取代的N' - （芳基羰基） - 苯甲酰肼，N' - （芳基羰基） - 亚苄基 - 酰肼及其类似物：其中Ar 1，Ar 本文定义了R 2，R 2和R 2 -R 2。 本发明还涉及具有式I和II的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：US07256219B2

公开(公告)日：2007-08-14

申请号：US10471720

申请日：2002-03-14

申请人： Sui Xiong Cai ,  P. Sanjeeva Reddy ,  John A. Drewe ,  Bao Ngoc Nguyen ,  Shailaja Kasibhatla

发明人： Sui Xiong Cai ,  P. Sanjeeva Reddy ,  John A. Drewe ,  Bao Ngoc Nguyen ,  Shailaja Kasibhatla

IPC分类号： A61K31/12 ,  C07C49/00 ,  C07D333/00 ,  C07D307/02 ,  C07D221/02 ,  C07D209/04 ,  C07D207/18

CPC分类号： C07D213/50 ,  A61K31/12 ,  A61K31/34 ,  A61K31/40 ,  A61K31/47 ,  A61K45/06 ,  C07C45/74 ,  C07C49/84 ,  C07C205/45 ,  A61K2300/00

摘要： The present invention is directed to multifluoro-substituted Chalcones and analogs thereof, represented by the general Formula I: wherein Ar and R6-R10 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： 本发明涉及由通式I表示的多氟取代的查尔酮及其类似物：其中Ar和R 6 -R 10是本文定义的。 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：US07226927B2

公开(公告)日：2007-06-05

申请号：US10704448

申请日：2003-11-10

申请人： Sui Xiong Cai ,  John A Drewe ,  P. Sanjeeva Reddy ,  Bao Nguyen ,  Azra Pervin

发明人： Sui Xiong Cai ,  John A Drewe ,  P. Sanjeeva Reddy ,  Bao Nguyen ,  Azra Pervin

IPC分类号： A61K31/53 ,  A61K31/505 ,  A61K31/506 ,  C07D239/02 ,  C07D409/00 ,  C07D251/00 ,  C07C49/00 ,  C07C255/17

CPC分类号： C07D239/42 ,  A61K31/50 ,  A61K31/505 ,  A61K31/506 ,  A61K31/53 ,  C07D239/48 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D405/14 ,  C07D417/04 ,  C07D417/14

摘要： The present invention is directed to substituted 2-aryl-4-arylaminopyrimidine and analogs thereof, represented by the general Formula I: wherein A, Ar1, Ar2, R1 and R3 are defined herein. The present invention also relates to the discovery that compounds having Formula I are activators of caspases and inducers of apoptosis. The compounds 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： 本发明涉及由通式I表示的取代的2-芳基-4-芳基氨基嘧啶及其类似物：其中A，Ar 1，Ar 2， 本文定义了SUB 1和R 3。 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。 本发明的化合物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：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。

公开(公告)号：US06794400B2

公开(公告)日：2004-09-21

申请号：US10158827

申请日：2002-06-03

申请人： Sui Xiong Cai ,  Bao Ngoc Nguyen ,  John Drewe ,  P. Sanjeeva Reddy ,  Shailaja Kasibhatla ,  Azra Pervin

发明人： Sui Xiong Cai ,  Bao Ngoc Nguyen ,  John Drewe ,  P. Sanjeeva Reddy ,  Shailaja Kasibhatla ,  Azra Pervin

IPC分类号： A61K3144

CPC分类号： C07D207/335 ,  A61K31/175 ,  A61K31/435 ,  A61K31/44 ,  A61K31/4965 ,  C07C281/14 ,  C07C337/08 ,  C07C2602/42 ,  C07D213/53 ,  C07D213/61 ,  C07D213/84 ,  C07D213/86 ,  C07D231/16 ,  C07D233/64 ,  C07D277/28 ,  C07D277/56 ,  C07D285/06 ,  C07D295/135 ,  C07D307/52 ,  C07D307/76 ,  C07D333/22 ,  C07D333/44 ,  A61K2300/00

摘要： The present invention is directed to optionally substituted 4-substituted-1-(arylmethylidene)thiosemicarbazide, 4-substituted-1-(arylcarbonyl)thiosemicarbazide and analogs thereof, represented by the Formulae I and II: wherein A1, A2, Q and R1-R3 are defined herein. The present invention also relates to the discovery that compounds having Formulae I and II 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和II表示的任选取代的4-取代-1-（芳基亚甲基）氨基硫脲，4-取代-1-（芳基羰基）氨基硫脲及其类似物：其中A1，A2，Q和R1- R3在本文中定义。 本发明还涉及具有式I和II的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：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。