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2. 发明申请

US20080032974A1 COMPOUNDS AND THERAPEUTICAL USE THEREOF 审中-公开
公开(公告)号：US20080032974A1
公开(公告)日：2008-02-07
申请号：US11779086
申请日：2007-07-17
申请人： Sui Xiong Cai , Nilantha Sirisoma , Azra Pervin , John Drewe , Shailaja Kasibhatla , Songchun Jiang , Hong Zhang , Chris Pleiman , Vijay Baichwal , John Manfredi , Leena Bhoite
发明人： Sui Xiong Cai , Nilantha Sirisoma , Azra Pervin , John Drewe , Shailaja Kasibhatla , Songchun Jiang , Hong Zhang , Chris Pleiman , Vijay Baichwal , John Manfredi , Leena Bhoite
IPC分类号： A61K31/517 , A61K31/52 , A61K31/5377 , A61P31/10 , A61P35/00 , C07D239/94 , C07D401/12 , C07D413/12 , C07D473/16
CPC分类号： C07D239/94 , C07D239/95 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/12 , C07D471/04 , C07D473/34 , C07D487/04
摘要： Disclosed are 4-arylamino-quinazolines and analogs thereof effective as activators of caspases and inducers of apoptosis. The compounds of this invention are useful in the treatment of a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.

3. 发明申请

US20070244114A1 COMPOUNDS AND THERAPEUTICAL USE THEREOF 审中-公开
标题翻译：化合物及其治疗用途
公开(公告)号：US20070244114A1
公开(公告)日：2007-10-18
申请号：US11685342
申请日：2007-03-13
申请人： Sui Cai , Nilantha Sirisoma , Azra Pervin , John Drewe , Shailaja Kasibhatla , Songchun Jiang , Hong Zhang , Chris Pleiman , Vijay Baichwal , John Manfredi , Leena Bhoite
发明人： Sui Cai , Nilantha Sirisoma , Azra Pervin , John Drewe , Shailaja Kasibhatla , Songchun Jiang , Hong Zhang , Chris Pleiman , Vijay Baichwal , John Manfredi , Leena Bhoite
IPC分类号： A61K31/517 , A61K31/5355 , C07D239/94 , C07D401/12 , C07D413/12 , C07D473/00
CPC分类号： C07D239/94 , C07D239/95 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/12 , C07D487/04
摘要： Disclosed are 4-arylamino-quinazolines and analogs thereof effective as activators of caspases and inducers of apoptosis. The compounds of this invention are useful in the treatment of a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.
摘要翻译：公开了作为胱天蛋白酶的活化剂和凋亡诱导剂的4-芳基氨基 - 喹唑啉及其类似物。本发明的化合物可用于治疗异常细胞发生不受控制的生长和扩散的各种临床病症。

4. 发明授权

US07135480B2 Substituted 1-benzoyl-3-cyano-pyrrolo [1,2-a] quinolines and analogs as activators of caspases and inducers of apoptosis 失效
标题翻译：取代的1-苯甲酰基-3-氰基 - 吡咯并[1,2-a]喹啉和类似物作为胱天蛋白酶和凋亡诱导剂的活化剂
公开(公告)号：US07135480B2
公开(公告)日：2006-11-14
申请号：US10733229
申请日：2003-12-12
申请人： Sui Xiong Cai , John A Drewe , Sungchun Jiang , Shailaja Kasibhatla , Jared Daniel Kuemmerle , Nilantha Sudath Sirisoma , Han-Zhong Zhang
发明人： Sui Xiong Cai , John A Drewe , Sungchun Jiang , Shailaja Kasibhatla , Jared Daniel Kuemmerle , Nilantha Sudath Sirisoma , Han-Zhong Zhang
IPC分类号： A61K31/4745 , C07D471/02
CPC分类号： C07D471/04 , A61K31/4745 , A61K31/496 , A61K31/4985 , C07D471/14 , C07D487/04
摘要： The present invention is directed to substituted 1-benzoyl-3-cyano-pyrrolo[1,2-α]quinolines and analogs thereof, represented by the general Formula I: wherein R1–R8, L, Q, dash line and Ar 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 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：本发明涉及由通式I表示的取代的1-苯甲酰基-3-氰基 - 吡咯并[1,2-a]喹啉及其类似物：其中R 1〜 8，L，Q，虚线和Ar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。

5. 发明授权

US07041685B2 Substituted 3-aryl-5-aryl-[1,2,4]-oxadiazoles and analogs as activators of caspases and inducers of apoptosis and the use thereof 失效
标题翻译：取代的3-芳基-5-芳基 - [1,2,4] - 恶二唑和类似物作为胱天蛋白酶的激活剂和凋亡诱导剂及其用途
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。

6. 发明授权

US06828091B2 Method of identifying immunosuppressive agents 失效
标题翻译：识别免疫抑制剂的方法
公开(公告)号：US06828091B2
公开(公告)日：2004-12-07
申请号：US09920332
申请日：2001-08-02
申请人： Shailaja Kasibhatla , Douglas R. Green , Ben Tseng
发明人： Shailaja Kasibhatla , Douglas R. Green , Ben Tseng
IPC分类号： C12Q125
CPC分类号： G01N33/505
摘要： A method for identifying therapeutically effective immunosuppressive agents by screening such agents for those which induce apoptosis in activated T cells is disclosed. T cells were isolated then activated and treating with various test compounds. A caspase substrate is added to detect caspase activation and apoptosis in the cells. Compounds which stimulate caspase activation and apoptosis are also tested against resting T cells to determine those agents which are more effective in activated T cells compared to resting T cells. Compounds with this selectivity are effective in treating immunopathological disorders such as arthritis, graft rejection, graft versus host disease, inflammatory bowel syndrome and the like.
摘要翻译：公开了通过筛选诱导活化的T细胞凋亡的那些试剂来鉴定治疗有效的免疫抑制剂的方法。分离T细胞，然后活化并用各种试验化合物处理。加入半胱天冬酶底物以检测细胞中的半胱天冬酶活化和细胞凋亡。还针对静息T细胞测试刺激半胱天冬酶活化和凋亡的化合物，以确定与静息T细胞相比在活化的T细胞中更有效的那些试剂。具有这种选择性的化合物在治疗免疫病理学疾病如关节炎，移植排斥反应，移植物抗宿主病，炎性肠综合征等方面是有效的。

7. 发明授权

US06794400B2 4-substituted-1-(arylmethylidene)thiosemicarbazide, 4-substituted-1-(arylcarbonyl)thiosemicarbazide and analogs as activators of caspases and inducers of apoptosis and the use thereof 失效
标题翻译： 4-取代-1-（芳基亚甲基）氨基硫脲，4-取代-1-（芳基羰基）氨基硫脲和类似物作为胱天蛋白酶的活化剂和凋亡诱导剂及其用途
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。

8. 发明申请

US20180177872A1 Combination of PD-1 antagonist with an EGFR inhibitor 审中-公开
公开(公告)号：US20180177872A1
公开(公告)日：2018-06-28
申请号：US15877436
申请日：2016-07-27
申请人： Yong Jia , Shailaja Kasibhatla , Sanela Bilic , John Cameron , Danny Howard, JR.
发明人： Yong Jia , Shailaja Kasibhatla , Sanela Bilic , John Cameron , Danny Howard, JR.
IPC分类号： A61K39/395 , A61K47/68 , C07K16/28 , A61P35/00
摘要： The present invention relates to a pharmaceutical composition comprising PD-1 antagonist and an EGFR Inhibitor. The present combination can be administered independently or separately, in a quantity which is jointly therapeutically effective for the treatment of cancer. The invention also provides the use of such a combination for the manufacture of a medicament; the use of such a combination as a medicine; a kit of part comprising such a combination; and a method of treatment of such a combination.

9. 发明授权

US07968595B2 Substituted 4-aryl-chromene as activator of caspases and inducer of apoptosis and as antivascular agent and the use thereof 有权
标题翻译：取代的4-芳基 - 色烯作为胱天蛋白酶的活化剂和细胞凋亡诱导剂和抗血管剂及其用途
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。

10. 发明申请

US20080085328A1 Substituted 4-aryl-chromene as activator of caspases and inducer of apoptosis and as antivascular agent and the use thereof 有权
标题翻译：取代的4-芳基 - 色烯作为胱天蛋白酶的活化剂和细胞凋亡诱导剂和抗血管剂及其用途
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。

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