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1. 发明申请

US20050004026A1 Methods of treating diseases responsive to induction of Apoptosis and screening assays 失效
标题翻译：治疗对细胞凋亡诱导作用的疾病和筛选试验的方法
公开(公告)号：US20050004026A1
公开(公告)日：2005-01-06
申请号：US10826909
申请日：2004-04-19
申请人： Shailaja Kasibhatla , Sui Cai , Ben Tseng , Katayoun Jessen , Nicole English , Serguei Maliartchouk , Songchun Jiang , Nilantha Sirisoma , Han-Zhong Zhang , Jared Kuemmerle
发明人： Shailaja Kasibhatla , Sui Cai , Ben Tseng , Katayoun Jessen , Nicole English , Serguei Maliartchouk , Songchun Jiang , Nilantha Sirisoma , Han-Zhong Zhang , Jared Kuemmerle
IPC分类号： A61K31/352 , A61K38/17 , A61K49/00 , C07D493/20 , C07D519/00 , C12Q20060101
CPC分类号： A61K49/0052 , A61K31/352 , A61K49/0043 , A61K51/0412 , A61K51/0419 , A61K51/0421 , A61K51/0453 , A61K51/0495
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 one or more Apoptosis Inducing Proteins (AIPs). AIPs include Transferrin Receptor Related Apoptosis Inducing Proteins (TRRAIPs), Clathrin Heavy Chain Related Apoptosis Inducing Proteins (CHCRAIPs), IQ motif containing GTPase Activating Protein Related Apoptosis Inducing Proteins (IQGAPRAIPs), and Heat Shock Protein Related Apoptosis Inducing Proteins (HSPRAIPs). The present invention also relates to screening methods useful for drug discovery of apoptosis inducing compounds. In particular, the screening methodology relates to using AIPs 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 AIPs; or whole cell assays using cells with altered levels of one or more AIPs. The invention also contemplates use of gambogic acid or GA-related compounds which bind AIPs and can accordingly be used to raise antibodies useful for drug discovery. Alternatively, labeled GA 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：本发明涉及一种治疗，预防或改善对动物中胱天蛋白酶级联诱导起反应的疾病的方法，包括向动物施用与一种或多种凋亡诱导蛋白（AIP）特异性结合的化合物。 AIPs包括转铁蛋白受体相关凋亡诱导蛋白（TRRAIP），网格蛋白重链相关凋亡诱导蛋白（CHCRAIPs），包含GTPase激活蛋白相关凋亡诱导蛋白（IQGAPRAIPs）和热休克蛋白相关凋亡诱导蛋白（HSPRAIPs）的IQ基序。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AIP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AIPs进行均一或异源结合测定; 或使用具有改变水平的一种或多种AIP的细胞的全细胞测定。本发明还考虑使用结合AIP的葡萄糖酸或GA相关化合物，因此可以用于产生可用于药物发现的抗体。或者，标记的GA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。

2. 发明申请

US20050004005A1 Methods of treating diseases responsive to Induction of Apoptosis 审中-公开
标题翻译：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。

3. 发明授权

US07592143B2 Methods of treating diseases responsive to induction of apoptosis and screening assays 失效
标题翻译：治疗对凋亡诱导作用的疾病的筛选方法和筛选试验
公开(公告)号：US07592143B2
公开(公告)日：2009-09-22
申请号：US10826909
申请日：2004-04-19
申请人： Shailaja Kasibhatla , Sui Xiong Cai , Ben Tseng , Katayoun Alavi Jessen , Nicole Marion English , Serguei Maliartchouk , Songchun Jiang , Nilantha Sudath Sirisoma , Han-Zhong Zhang , Jared Kuemmerle
发明人： Shailaja Kasibhatla , Sui Xiong Cai , Ben Tseng , Katayoun Alavi Jessen , Nicole Marion English , Serguei Maliartchouk , Songchun Jiang , Nilantha Sudath Sirisoma , Han-Zhong Zhang , Jared Kuemmerle
IPC分类号： G01N33/53
CPC分类号： A61K49/0052 , A61K31/352 , A61K49/0043 , A61K51/0412 , A61K51/0419 , A61K51/0421 , A61K51/0453 , A61K51/0495
摘要： The present invention relates to screening methods useful for drug discovery of apoptosis inducing compounds. In particular, the screening methodology relates to using Apoptosis Inducing Proteins (AIPs) as a target for the discovery of apoptosis activators useful as anticancer agents. The screening methods of the present invention can employ homogenous or heterogeneous binding assays using purified or partially purified AIPs; or whole cell assays using cells with altered levels of one or more AIPs. The invention also contemplates use of gambogic acid or GA-related compounds which bind AIPs and can accordingly be used to raise antibodies useful for drug discovery. Alternatively, labeled GA 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，筛选方法涉及使用细胞凋亡诱导蛋白（AIPs）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AIPs进行均一或异质结合测定; 或使用具有改变水平的一种或多种AIP的细胞的全细胞测定。本发明还考虑使用结合AIP的葡萄糖酸或GA相关化合物，因此可以用于产生可用于药物发现的抗体。或者，标记的GA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。

4. 发明申请

US20050014759A1 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：US20050014759A1
公开(公告)日：2005-01-20
申请号：US10733229
申请日：2003-12-12
申请人： Sui Cai , John Drewe , Sungchun Jiang , Shailaja Kasibhatla , Jared Kuemmerle , Nilantha Sirisoma , Han-Zhong Zhang
发明人： Sui Cai , John Drewe , Sungchun Jiang , Shailaja Kasibhatla , Jared Kuemmerle , Nilantha Sirisoma , Han-Zhong Zhang
IPC分类号： A61K31/4745 , A61K31/496 , A61K31/4985 , C07D471/04 , C07D471/14 , C07D487/04 , A61K31/498
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-a]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R1-R8，L，Q，虚线和Ar定义这里。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. 发明申请

US20050154012A1 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：US20050154012A1
公开(公告)日：2005-07-14
申请号：US11074077
申请日：2005-03-08
申请人： Sui Cai , Han-Zhong Zhang , John Drewe , P. Reddy , Shailaja Kasibhatla , Jared Kuemmerle , Kristin Ollis
发明人： Sui Cai , Han-Zhong Zhang , John Drewe , P. Reddy , Shailaja Kasibhatla , Jared Kuemmerle , Kristin Ollis
IPC分类号： C07D487/04 , A61K31/335 , A61K31/38 , A61K31/395 , A61K31/4155 , A61K31/422 , A61K31/4245 , A61K31/427 , A61K31/4439 , A61K31/4709 , A61K31/4725 , A61K31/497 , A61K31/506 , A61K31/519 , A61K31/5377 , A61K31/54 , A61P1/04 , A61P17/00 , A61P17/06 , A61P29/00 , A61P31/12 , A61P35/00 , A61P35/02 , A61P37/06 , A61P43/00 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/14 , C07D471/04
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. 发明申请

US20070112003A1 3,5-disubstituted-[1,2,4]-oxadiazoles and analogs as activators of caspases and inducers of apoptosis and the use of thereof 失效
标题翻译： 3,5-二取代 - [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使用
公开(公告)号：US20070112003A1
公开(公告)日：2007-05-17
申请号：US11593030
申请日：2006-11-06
申请人： Sui Cai , Han-Zhong Zhang , Jared Kuemmerle , Hong Zhang , William Kemnitzer
发明人： Sui Cai , Han-Zhong Zhang , Jared Kuemmerle , Hong Zhang , William Kemnitzer
IPC分类号： A61K31/5377 , A61K31/496 , A61K31/454 , A61K31/4245 , C07D413/14
CPC分类号： A61K31/4245 , A61K31/4439
摘要： Disclosed are 3,5-disubstituted-[1,2,4]-oxadiazoles and analogs thereof, represented by the Formula I: wherein Ar1, R2, A, B and D 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3,5-二取代 - [1,2,4] - 恶二唑及其类似物：其中Ar 1，R 2，A， B和D在本文中定义。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。

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