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1. 发明授权

US07226927B2 Substituted 2-aryl-4-arylaminopyrimidines and analogs as activators of caspases and inducers of apoptosis and the use thereof 失效
标题翻译：取代的2-芳基-4-芳基氨基嘧啶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：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。

2. 发明授权

US06716851B2 Substituted 2-aryl-4-arylaminopyrimidines and analogs as activators or caspases and inducers of apoptosis and the use thereof 失效
标题翻译：取代的2-芳基-4-芳基氨基嘧啶和类似物作为活化剂或胱天蛋白酶和凋亡诱导剂及其用途
公开(公告)号：US06716851B2
公开(公告)日：2004-04-06
申请号：US10012444
申请日：2001-12-12
申请人： Sui Xiong Cai , John A. Drewe , Bao Nguyen , Azra Pervin
发明人： Sui Xiong Cai , John A. Drewe , Bao Nguyen , Azra Pervin
IPC分类号： A61K31505
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，R 1和R 3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。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。

3. 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。

4. 发明授权

US07618975B2 4-arylamino-quinazolines and analogs as activators of caspases and inducers of apoptosis and the use thereof 有权
标题翻译： 4-芳基氨基 - 喹唑啉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：US07618975B2
公开(公告)日：2009-11-17
申请号：US10885903
申请日：2004-07-06
申请人： Sui Xiong Cai , Nilantha Sudath Sirisoma , Azra Pervin , John A. Drewe , Shailaja Kasibhatla , Songchun Jiang , Hong Zhang , Chris Pleiman
发明人： Sui Xiong Cai , Nilantha Sudath Sirisoma , Azra Pervin , John A. Drewe , Shailaja Kasibhatla , Songchun Jiang , Hong Zhang , Chris Pleiman
IPC分类号： A01N43/90 , A01N43/54 , A61K31/519 , A61K31/517 , C07D413/00 , C07D473/00 , C07D401/00 , C07D403/00 , C07D417/00 , C07D419/00 , C07D239/72
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.
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。

5. 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.

6. 发明申请

US20070043076A1 Substituted 2-arylmethylene-n-aryl-n'aryl-malonamides and analogs as activators of caspases and inducers of apoptosis 审中-公开
标题翻译：取代的2-芳基亚甲基 - 芳基 - 芳基 - 丙二酰胺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：US20070043076A1
公开(公告)日：2007-02-22
申请号：US10572910
申请日：2004-10-05
申请人： Sui Cai , Azra Pervin , Shailaja Kasibhatla , Bao Nguyen
发明人： Sui Cai , Azra Pervin , Shailaja Kasibhatla , Bao Nguyen
IPC分类号： A61K31/4709 , A61K31/444 , A61K31/416 , A61K31/4178 , A61K31/405 , A61K31/381 , A61K31/4025 , A61K31/165
CPC分类号： A61K31/16 , A61K31/165 , A61K31/381 , A61K31/4025 , A61K31/405 , A61K31/416 , A61K31/4178 , A61K31/444 , A61K31/4709 , A61K45/06 , A61K2300/00
摘要： The present invention is directed to substituted 2-arylmethylene-N-aryl-N′-aryl-malonamides and analogs thereof. The present invention also relates to the discovery that the compounds are activators of caspases and inducers of apoptosis. Therefore, the activators os 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：本发明涉及取代的2-芳基亚甲基-N-芳基-N'-芳基 - 丙二酰胺及其类似物。本发明还涉及这些化合物是胱天蛋白酶的激活剂和凋亡诱导剂的发现。因此，本发明的活化剂os半胱天冬酶和细胞凋亡诱导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。

7. 发明申请

US20050137213A1 Compounds and therapeutical use thereof 有权
标题翻译：化合物及其治疗用途
公开(公告)号：US20050137213A1
公开(公告)日：2005-06-23
申请号：US10885903
申请日：2004-07-06
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 , A61K31/519 , C07D239/94 , C07D239/95 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/12 , C07D471/04 , C07D473/34 , C07D487/04
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.
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。

8. 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。

9. 发明申请

US20080039479A1 COMPOUNDS AND THERAPEUTICAL USE THEREOF 审中-公开
公开(公告)号：US20080039479A1
公开(公告)日：2008-02-14
申请号：US11781660
申请日：2007-07-23
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 , A61P35/00 , C07D239/72
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.

10. 发明授权

US06433134B1 Peptide nucleic acid precursors and methods of preparing same 失效
标题翻译：肽核酸前体及其制备方法
公开(公告)号：US06433134B1
公开(公告)日：2002-08-13
申请号：US09479320
申请日：2000-01-05
申请人： Andrew P. Patron , Azra Pervin
发明人： Andrew P. Patron , Azra Pervin
IPC分类号： C07K700
CPC分类号： C07K14/003 , C07K1/047
摘要： Novel and efficient syntheses create novel piperazinone intermediates which facilitate the production and use of PNAs. Such syntheses and the products enhance the feasibility of a system which permits the rapid identification of PNA oligomers useful as therapeutics, diagnostics and/or gene characterization tools. A first component of the system is a universal PNA library that most preferably incorporates one or more universal nucleotide bases into carefully selected positions within each oligomer species thereby providing the library with the screening ability of a much larger library. The second component of the system is a high throughput screening system that includes a number of assays designed to provide information on the binding activities of the different PNAs to a target nucleotide sequence (generally, a DNA or RNA sequence). The third component is a software system especially designed to provide rapid analysis of the data collected from the high throughput screening system and to determine therefrom the sequence base identities and sequence lengths of PNA oligomers most likely to bind to and appropriately affect the target molecule.
摘要翻译：新型和高效的合成产生促进PNA生产和使用的新型哌嗪酮中间体。这样的合成和产物增强了可以快速鉴定可用作治疗剂，诊断和/或基因表征工具的PNA寡聚体的系统的可行性。该系统的第一组分是通用的PNA文库，其最优选地将一个或多个通用核苷酸碱基引入每个低聚物种类内精心选择的位置，从而为文库提供更大的文库的筛选能力。该系统的第二部分是高通量筛选系统，其包括许多测定，其设计用于提供关于不同PNA与目标核苷酸序列（通常为DNA或RNA序列）的结合活性的信息。第三个组件是一个软件系统，特别设计用于快速分析从高通量筛选系统收集的数据，并从中确定最可能结合并适当影响靶分子的PNA寡聚体的序列基本标识和序列长度。

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