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1. 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。

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. 发明授权

US07176234B2 Derivatives of gambogic acid and analogs as activators of caspases and inducers of apoptosis 失效
标题翻译：葡萄糖酸和类似物的衍生物作为胱天蛋白酶的活化剂和凋亡诱导剂
公开(公告)号：US07176234B2
公开(公告)日：2007-02-13
申请号：US10609670
申请日：2003-07-01
申请人： Sui Xiong Cai , Shailaja Kasibhatla , Kristin P. Ollis , Han-Zhong Zhang , John A. Drewe , Ben Tseng , Nilantha Sudath Sirisoma
发明人： Sui Xiong Cai , Shailaja Kasibhatla , Kristin P. Ollis , Han-Zhong Zhang , John A. Drewe , Ben Tseng , Nilantha Sudath Sirisoma
IPC分类号： A61K31/352 , C07D313/06
CPC分类号： A61K31/00 , C07D493/20
摘要： The present invention is directed to derivatives of gambogic acid and analogs thereof. Exemplary gambogic acid derivatives of the present invention include, among others, derivatives substituted in the C10 and C28 positions of gambogic acid. The present invention also relates to the discovery that certain preferred compounds of the present invention 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：本发明涉及吡啶酸及其类似物的衍生物。本发明的示例性的吡咯烷酸衍生物包括其中取代为吡咯烷酸的C10和C28位置的衍生物。本发明还涉及本发明的某些优选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

US06462041B1 Gambogic acid, analogs and derivatives as activators of caspases and inducers of apoptosis 失效
标题翻译：甘草酸，类似物和衍生物作为胱天蛋白酶的活化剂和凋亡诱导剂
公开(公告)号：US06462041B1
公开(公告)日：2002-10-08
申请号：US09495120
申请日：2000-02-01
申请人： Sui Xiong Cai , Han-Zhong Zhang , Yan Wang , Ben Tseng , Shailaja Kasibhatla , John A. Drewe
发明人： Sui Xiong Cai , Han-Zhong Zhang , Yan Wang , Ben Tseng , Shailaja Kasibhatla , John A. Drewe
IPC分类号： A61K3145
CPC分类号： C07D493/20 , A61K31/352 , A61K31/4025 , A61K31/4178 , A61K31/4188 , A61K31/4433 , A61K31/45 , A61K31/453 , A61K31/496 , A61K31/497 , A61K31/5377 , A61K31/5513 , C07D493/22 , C07D519/00
摘要： The present invention is directed to gambogic acid, analogs and derivatives thereof, represented by the general Formulae I-III: wherein R1-R5 are defined herein. The present invention also relates to the discovery that compounds having Formula I-III 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 cell growth and spread of abnormal cells occurs.
摘要翻译：本发明涉及由通式I-III表示的吡咯烷酸，类似物及其衍生物：其中R1-R5在本文中定义。本发明还涉及发现具有式I-III的化合物是胱天蛋白酶的激活剂和凋亡诱导剂。因此，本发明的胱天蛋白酶和细胞凋亡诱导剂的激活剂可以用于在发生不受控制的细胞生长和异常细胞扩散的各种临床条件下诱导细胞死亡。

6. 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。

7. 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.

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。

10. 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。

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