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    N-aryl-thienopyrimidin-4-amines and analogs as activators of caspases and inducers of apoptosis and the use thereof
    2.
    发明申请
    N-aryl-thienopyrimidin-4-amines and analogs as activators of caspases and inducers of apoptosis and the use thereof 审中-公开
    N-芳基 - 噻吩并嘧啶-4-胺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：US20070099877A1

    公开(公告)日：2007-05-03

    申请号：US11591532

    申请日：2006-11-02

    申请人： Sui Cai ,  William Kemnitzer ,  Nilantha Sirisoma ,  Han-Zhong Zhang

    发明人： Sui Cai ,  William Kemnitzer ,  Nilantha Sirisoma ,  Han-Zhong Zhang

    IPC分类号： A61K31/655 ,  A61K31/519 ,  C07D498/02

    CPC分类号： C07D495/04 ,  A61K31/519 ,  A61K31/655

    摘要： Disclosed are N-aryl-thienopyrimidin-4-amines and analogs thereof, represented by the Formulae I-II: wherein Ar and R1-R4 are defined herein. The present invention relates to the discovery that compounds having Formulae I-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： 公开了由式I-II表示的N-芳基 - 噻吩并嘧啶-4-胺及其类似物：其中Ar和R 1 -R 4定义在本文中。 本发明涉及具有式I-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。

    Methods of treating diseases responsive to Induction of Apoptosis
    3.
    发明申请
    Methods of treating diseases responsive to Induction of Apoptosis 审中-公开
    治疗响应诱导凋亡的疾病的方法

    公开(公告)号：US20050004005A1

    公开(公告)日：2005-01-06

    申请号：US10826923

    申请日：2004-04-19

    申请人： Shailaja Kasibhatla ,  Sui Cai ,  Ben Tseng ,  Katayoun Jessen ,  Serguei Maliartchouk ,  Nicole English ,  Jared Kuemmerle ,  William Kemnitzer ,  Han-Zhong Zhang

    发明人： Shailaja Kasibhatla ,  Sui Cai ,  Ben Tseng ,  Katayoun Jessen ,  Serguei Maliartchouk ,  Nicole English ,  Jared Kuemmerle ,  William Kemnitzer ,  Han-Zhong Zhang

    IPC分类号： A61K31/47 ,  A61K38/00 ,  C12Q20060101

    CPC分类号： G01N33/5011 ,  A61K31/729

    摘要： The present invention pertains to a method of treating, preventing or ameliorating a disease responsive to induction of the caspase cascade in an animal, comprising administering to the animal a compound which binds specifically to a Tail Interacting Protein Related Apoptosis Inducing Protein (TIPRAIP). The present invention also relates to screening methods useful for drug discovery of apoptosis inducing compounds. In particular, the screening methodology relates to using TIPRAIP as a target for the discovery of apoptosis activators useful as anticancer agents. The screening methods of the present invention can employ homogenous or heterogenous binding assays using purified or partially purified TIPRAIP; or whole cell assays using cells with altered levels of TIPRAIP. The invention also contemplates use of 3-(4-azidophenyl)-5-(3-chloro-thiophen-2-yl)-[1,2,4]-oxadiazole or a substituted 3-aryl-5-aryl-[1,2,4]-oxadiazole which bind TIPRAIP and can accordingly be used to raise antibodies useful for drug discovery. Alternatively, labeled 3-(4-azidophenyl)-5-(3-chloro-thiophen-2-yl)-[1,2,4]-oxadiazole (or a labeled substituted 3-aryl-5-aryl-[1,2,4]-oxadiazole) is used for competitive binding assays for drug discovery. Such assays afford high throughput screening of chemical libraries for apoptosis activators.

    摘要翻译： 本发明涉及治疗，预防或改善对动物中胱天蛋白酶级联诱导有反应的疾病的方法，包括向动物施用与尾部相互作用蛋白相关的细胞凋亡诱导蛋白（TIPRAIP）特异性结合的化合物。 本发明还涉及可用于药物发现凋亡诱导化合物的筛选方法。 特别地，筛选方法涉及使用TIPRAIP作为发现用作抗癌剂的凋亡激活剂的靶标。 本发明的筛选方法可以使用纯化或部分纯化的TIPRAIP的均质或异源结合测定; 或使用具有改变水平的TIPRAIP的细胞的全细胞测定。 本发明还考虑使用3-（4-叠氮基苯基）-5-（3-氯 - 噻吩-2-基） - [1,2,4] - 恶二唑或取代的3-芳基-5-芳基 - [1 ，2,4] - 恶二唑，其结合TIPRAIP，因此可用于引发可用于药物发现的抗体。 或者，将标记的3-（4-叠氮基苯基）-5-（3-氯 - 噻吩-2-基） - [1,2,4] - 恶二唑（或标记的取代的3-芳基-5-芳基 - 2,4] - 恶二唑）用于药物发现的竞争性结合测定。 这样的测定提供用于凋亡激活剂的化学文库的高通量筛选。

    N-arylalkyl-thienopyrimidin-4-amines and analogs as activators of caspases and inducers of apoptosis and the use thereof
    4.
    发明申请
    N-arylalkyl-thienopyrimidin-4-amines and analogs as activators of caspases and inducers of apoptosis and the use thereof 审中-公开
    N-芳基烷基 - 噻吩并嘧啶-4-胺及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：US20070099941A1

    公开(公告)日：2007-05-03

    申请号：US11591531

    申请日：2006-11-02

    申请人： Sui Cai ,  John Drewe ,  William Kemnitzer ,  Nilantha Sirisoma

    发明人： Sui Cai ,  John Drewe ,  William Kemnitzer ,  Nilantha Sirisoma

    IPC分类号： A61K31/519 ,  C07D498/02

    CPC分类号： C07D495/04 ,  A61K31/519

    摘要： Disclosed are N-arylalkyl-thienopyrimidin-4-amines and analogs thereof, represented by the Formula I: wherein Ar, R1, R3, R4, R10-R12 and n are defined herein. The present invention 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： 公开了由式I表示的N-芳基烷基 - 噻吩并嘧啶-4-胺及其类似物：其中Ar，R 1，R 3，R 4， R 11，R 12，R 12和R 12是这里定义的。 本发明涉及发现具有式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。

    N-alkyl-N-aryl-thienopyrimidin-4-amines and analogs as activators of caspases and inducers of apoptosis and the use thereof
    6.
    发明申请
    N-alkyl-N-aryl-thienopyrimidin-4-amines and analogs as activators of caspases and inducers of apoptosis and the use thereof 审中-公开
    N-烷基-N-芳基 - 噻吩并嘧啶-4-胺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：US20070213305A1

    公开(公告)日：2007-09-13

    申请号：US11591488

    申请日：2006-11-02

    申请人： Sui Cai ,  William Kemnitzer ,  Nilantha Sirisoma

    发明人： Sui Cai ,  William Kemnitzer ,  Nilantha Sirisoma

    IPC分类号： A61K31/655 ,  A61K31/519

    CPC分类号： A61K31/519 ,  A61K31/655 ,  C07D495/04

    摘要： Disclosed are N-alkyl-N-aryl-thienopyrimidin-4-amines and analogs thereof, represented by the Formulae I-II: wherein Ar, R1-R4 and R10 are defined herein. The present invention relates to the discovery that compounds having Formulae I-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： 公开了由式I-II表示的N-烷基-N-芳基 - 噻吩并嘧啶-4-胺及其类似物：其中Ar，R 1 -R 4和 本文定义R 10。 本发明涉及具有式I-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。

    N-aryl-5,7-dihydrofuro[3,4-d]pyrimidin-4-amines and analogs as activators of caspases and inducers of apoptosis and the use thereof
    7.
    发明申请
    N-aryl-5,7-dihydrofuro[3,4-d]pyrimidin-4-amines and analogs as activators of caspases and inducers of apoptosis and the use thereof 审中-公开
    N-芳基-5,7-二氢呋喃并[3,4-d]嘧啶-4-胺及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：US20080113946A1

    公开(公告)日：2008-05-15

    申请号：US11984179

    申请日：2007-11-14

    申请人： Han-Zhong Zhang ,  Sui Cai ,  William Kemnitzer

    发明人： Han-Zhong Zhang ,  Sui Cai ,  William Kemnitzer

    IPC分类号： A61K31/655 ,  A61K31/519

    CPC分类号： A61K31/519 ,  A61K45/06 ,  A61K2300/00

    摘要： Disclosed are N-aryl-5,7-dihydrofuro[3,4-d]pyrimidin-4-amines and analogs thereof, represented by the Formula I: wherein Ar, A, Q and R1-R6 are defined herein. The present invention 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： 公开了由式I表示的N-芳基-5,7-二氢呋喃并[3,4-d]嘧啶-4-胺及其类似物：其中Ar，A，Q和R 1〜 本文定义R 6。 本发明涉及发现具有式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。