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11. 发明申请

WO2008057402A2 N-ARYL-ISOXAZOLOPYRIMIDIN-4-AMINES AND RELATED COMPOUNDS AS ACTIVATORS OF CASPASES AND INDUCERS OF APOPTOSIS AND THE USE THEREOF 审中-公开
标题翻译： N-ARYL-ISOXAZOLOPYRIMIDIN-4-AMINES和相关化合物作为病毒和杀虫剂的激活剂及其用途
公开(公告)号：WO2008057402A2
公开(公告)日：2008-05-15
申请号：PCT/US2007/023109
申请日：2007-11-02
申请人： CYTOVIA, INC. , CAI, Sui, Xiong , KEMNITZER, William, E. , SIRISOMA, Nilantha, Sudath , ZHANG, Han-Zhong
发明人： CAI, Sui, Xiong , KEMNITZER, William, E. , SIRISOMA, Nilantha, Sudath , ZHANG, Han-Zhong
IPC分类号： A61K31/519
CPC分类号： A61K31/519
摘要： Disclosed are N-aryl-isoxazolopyrimidin-4-amines and related compounds thereof, represented by the Formula (I): wherein Ar, R 1 -R 5 , A, B, D, E, F and H 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 - 异恶唑并嘧啶-4-胺及其相关化合物：其中Ar，R 1〜R 5，A，B ，D，E，F和H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。

12. 发明申请

WO2007056215A3 N-ARYL-THIENOPYRIMIDIN-4-AMINES AND THE USE THEREOF 审中-公开
公开(公告)号：WO2007056215A3
公开(公告)日：2007-05-18
申请号：PCT/US2006/043087
申请日：2006-11-02
申请人： CYTOVIA, INC. , CAI, Sui, Xiong , KEMNITZER, William, E. , SIRISOMA, Nilantha, Sudath , ZHANG, Han-zhong
发明人： CAI, Sui, Xiong , KEMNITZER, William, E. , SIRISOMA, Nilantha, Sudath , ZHANG, Han-zhong
IPC分类号： A01N43/04 , C09B29/52
摘要： Disclosed are N -aryl-thienopyrimidin-4-amines and analogs thereof, represented by the Formulae I-II: wherein Ar and R 1 -R 4 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.

13. 发明申请

WO2002092076A1 SUBSTITUTED COUMARINS AND QUINOLINES AS CASPASES ACTIVATORS 审中-公开
标题翻译：作为CASPASES ACTIVATORS的取代的COUMARINS和QUINOLINES
公开(公告)号：WO2002092076A1
公开(公告)日：2002-11-21
申请号：PCT/US2002/015401
申请日：2002-05-16
申请人： CYTOVIA, INC. , SHIRE BIOCHEM, INC. , CAI, Sui, Xiong , ZHANG, Hong , KEMMITZER, William, E. , JIANG, Songchum , DREWE, John, A. , STORER, Richard
发明人： CAI, Sui, Xiong , ZHANG, Hong , KEMMITZER, William, E. , JIANG, Songchum , DREWE, John, A. , STORER, Richard
IPC分类号： A61K31/35
CPC分类号： C07D335/06 , A61K31/35 , A61K31/385 , A61K31/47 , C07D215/54 , C07D221/10 , C07D311/16 , C07D311/58 , C07D409/04 , C07D471/04 , C07D491/04 , C07D493/04 , C07D495/04 , C07D513/04
摘要： 5 The present invention is directed to substituted coumarins and quinolines and analogs thereof, represented by the general Formula I: A (I) 10 wherein A, B, X, Y, and Z 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：A（I）10表示的取代香豆素和喹啉及其类似物，其中A，B，X，Y和Z如本文所定义。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。

14. 发明申请

WO2003090680A3 NOVEL PHENYL DERIVATIVES AS INDUCERS OF APOPTOSIS 审中-公开
公开(公告)号：WO2003090680A3
公开(公告)日：2003-11-06
申请号：PCT/US2003/012604
申请日：2003-04-23
申请人： AXYS PHARMACEUTICALS, INC. , CYTOVIA, INC. , CAI, Sui, Xiong , CEBON, Ben , LITVAK, Joane , PARARAJASINGHAM, Keith , SHELTON, Emma, J. , SPENCER, Jeffrey, R. , SPERANDIO, David , SPRENGELER, Paul, A. , TAI, Vincent, W.-F. , YEE, Robert, M.
发明人： CAI, Sui, Xiong , CEBON, Ben , LITVAK, Joane , PARARAJASINGHAM, Keith , SHELTON, Emma, J. , SPENCER, Jeffrey, R. , SPERANDIO, David , SPRENGELER, Paul, A. , TAI, Vincent, W.-F. , YEE, Robert, M.
IPC分类号： C07D263/34
摘要： The present invention related to certain phenyl derivatives that are activators of caspases and inducers of apoptosis, pharmaceutical composition comprising these compounds and method of treating cancer utilizing these compounds.

15. 发明申请

WO2010008558A1 COMPOUNDS AND METHODS OF INDUCING APOPTOSIS VIA INTERACTION WITH CHAPERONIN CCT 审中-公开
标题翻译：通过与CHAPERONIN CCT相互作用诱导疫苗的化合物和方法
公开(公告)号：WO2010008558A1
公开(公告)日：2010-01-21
申请号：PCT/US2009/004106
申请日：2009-07-16
申请人： CYTOVIA, INC. , CAI, Sui, Xiong , VAILLANCOURT, Mei, Ting , CLAASSEN, Gisela
发明人： CAI, Sui, Xiong , VAILLANCOURT, Mei, Ting , CLAASSEN, Gisela
IPC分类号： C07K14/47 , C07D513/04 , G01N33/566 , A61K31/542 , G01N33/53 , G01N33/58 , A61P35/00 , G01N33/542 , G01N33/60
CPC分类号： C07K14/4747 , A61K31/542 , C07D513/04 , G01N33/68 , G01N2500/04
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 to CCT. The present invention also relates to screening methods useful for drug discovery of apoptosis inducing compounds. In particular, the screening methodology relates to using CCT 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 CCT; or whole cell assays using cells with altered levels of CCT. The invention also contemplates use of 6-aryl-3-aryl-7 H - [1,2,4]triazolo[3,4-&][1,3,4]thiadiazine or derivative which bind CCT and can accordingly be used to raise antibodies useful for drug discovery. Alternatively, labeled 6-aryl-3-aryl-7H-[1,2,4]triazolo[3,4-&][1,3,4]thiadiazine or derivative 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，包括向动物施用结合CCT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CCT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CCT进行均一或异源结合测定; 或使用具有改变的CCT水平的细胞的全细胞测定。本发明还考虑使用结合CCT的6-芳基-3-芳基-7H- [1,2,4]三唑并[3,4-] [1,3,4]噻二嗪或衍生物，因此可用于提出可用于药物发现的抗体。或者，将标记的6-芳基-3-芳基-7H- [1,2,4]三唑并[3,4-d] [1,3,4]噻二嗪或衍生物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。

16. 发明申请

WO2003097806A3 SUBSTITUTED 4-ARYL-4H-PYRROLO[2,3-H]CHROMENES AND ANALOGS AS ACTIVATORS OF CASPASES AND INDUCERS OF APOPTOSIS AND THE USE THEREOF 审中-公开
公开(公告)号：WO2003097806A3
公开(公告)日：2003-11-27
申请号：PCT/US2003/015427
申请日：2003-05-16
申请人： CYTOVIA, INC. , SHIRE BIOCHEM, INC. , CAI, Sui, Xiong , JIANG, Songchun , KEMNITZER, William, E. , ZHANG, Hong , ATTARDO, Giorgio , DENIS, Real
发明人： CAI, Sui, Xiong , JIANG, Songchun , KEMNITZER, William, E. , ZHANG, Hong , ATTARDO, Giorgio , DENIS, Real
IPC分类号： C07D401/00
摘要： The present invention is directed to substituted 4 H -chromenes and analogs thereof, represented by the Formula (I): wherein R 1 , R 3 -R 5 , A, D, Y and Z 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.

17. 发明申请

WO2003090680A2 NOVEL PHENYL DERIVATIVES AS INDUCERS OF APOPTOSIS 审中-公开
标题翻译：作为疫苗诱导剂的新型苯乙烯衍生物
公开(公告)号：WO2003090680A2
公开(公告)日：2003-11-06
申请号：PCT/US2003/012604
申请日：2003-04-23
申请人： AXYS PHARMACEUTICALS, INC. , CYTOVIA, INC. , CAI, Sui, Xiong , CEBON, Ben , LITVAK, Joane , PARARAJASINGHAM, Keith , SHELTON, Emma, J. , SPENCER, Jeffrey, R. , SPERANDIO, David , SPRENGELER, Paul, A. , TAI, Vincent, W.-F. , YEE, Robert, M.
发明人： CAI, Sui, Xiong , CEBON, Ben , LITVAK, Joane , PARARAJASINGHAM, Keith , SHELTON, Emma, J. , SPENCER, Jeffrey, R. , SPERANDIO, David , SPRENGELER, Paul, A. , TAI, Vincent, W.-F. , YEE, Robert, M.
IPC分类号： A61K
CPC分类号： C07D263/34 , C07D231/14 , C07D271/06 , C07D277/56 , C07D401/06 , C07D403/06 , C07D409/12 , C07D409/14 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/06 , C07D417/12 , C07D453/06 , C07D471/08 , C07D491/04 , C07D491/10
摘要： The present invention related to certain phenyl derivatives that are activators of caspases and inducers of apoptosis, pharmaceutical composition comprising these compounds and method of treating cancer utilizing these compounds.
摘要翻译：本发明涉及作为胱天蛋白酶的活化剂和凋亡诱导剂的某些苯基衍生物，包含这些化合物的药物组合物和利用这些化合物治疗癌症的方法。

18. 发明申请

WO2007056214A2 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
标题翻译： N-烷基-N-亚氨基 - 三亚氨基嘧啶-4-胺和类似物作为杀虫剂和杀虫剂的激活剂及其用途
公开(公告)号：WO2007056214A2
公开(公告)日：2007-05-18
申请号：PCT/US2006/043086
申请日：2006-11-02
申请人： CYTOVIA, INC , CAI, Sui, Xiong , SIRISOMA, Nilantha, Sudath , KEMNITZER, William, E.
发明人： CAI, Sui, Xiong , SIRISOMA, Nilantha, Sudath , KEMNITZER, William, E.
IPC分类号： 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, R 1 -R 4 and R 10 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。本发明涉及发现具有式I-II的化合物是胱天蛋白酶的活化剂和凋亡诱导剂。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。

19. 发明申请

WO2004002401A2 CASPASE INHIBITORS FOR THE TREATMENT OF DISEASES AND CONDITIONS CAUSED BY EXPOSURE TO RADIONUCLIDES, BIOLOGICAL AGENTS, OR CHEMICAL AGENTS 审中-公开
标题翻译：用于治疗由放射性核素，生物制剂或化学试剂接触引起的疾病和病症的CASPASE抑制剂
公开(公告)号：WO2004002401A2
公开(公告)日：2004-01-08
申请号：PCT/US2003/010645
申请日：2003-04-07
申请人： CYTOVIA, INC. , CAI, Sui, Xiong , TSENG, Ben, Y.
发明人： CAI, Sui, Xiong , TSENG, Ben, Y.
IPC分类号： A61K
CPC分类号： A61K31/16 , A61K31/19 , A61K31/195 , A61K31/198 , A61K31/27 , A61K31/35 , A61K31/44 , A61K31/535 , A61K38/05 , A61K38/55 , A61K51/12 , Y02A50/406 , Y02A50/471
摘要： The use of caspase inhibitors for treating cell death induced by radionuclides, biological agents, or chemical agents is disclosed. In particular, treatment of diseases or conditions caused by exposure to radionuclides, biological agents, or chemical agents, spread of radionuclides, biological agents, or chemical agents, explosion of radionuclides, biological agents, or chemical agents by terrorists or accidental exposure to radionuclides, biological agents, or chemical agents from a nuclear power plant, manufacturing or processing plant, research facility, or hospital is disclosed.
摘要翻译：公开了使用半胱天冬酶抑制剂来治疗由放射性核素，生物制剂或化学试剂引起的细胞死亡。特别是治疗暴露于放射性核素，生物制剂或化学药剂，放射性核素，生物制剂或化学药剂的扩散，恐怖分子的爆炸性放射性核素，生物制剂或化学试剂引起的疾病或病症或意外暴露于放射性核素，公开了来自核电站，制造或加工厂，研究设施或医院的生物制剂或化学试剂。

20. 发明申请

WO2002092083A1 7,8-FUSED 4$I(H)-CHROMENE AND ANALOGS AS ACTIVATORS OF CASPASES AND INDUCERS OF APOPTOSIS AND THE USE THEREOF 审中-公开
标题翻译： 7,8-FUSED 4 DOLLAR I（H）-CHROMENE AND ANALOGS AS ACTIVATORS OF CASPASES AND INDUCERS OF APOPTOSIS及其用途
公开(公告)号：WO2002092083A1
公开(公告)日：2002-11-21
申请号：PCT/US2002/015398
申请日：2002-05-16
申请人： CYTOVIA, INC. , CAI, Sui, Xiong , XU, Lifen , STORER, Richard , ATTARDO, Giorgio
发明人： CAI, Sui, Xiong , XU, Lifen , STORER, Richard , ATTARDO, Giorgio
IPC分类号： A61K31/4188
CPC分类号： C07D491/04 , A61K31/4188 , A61K31/4196 , A61K31/424 , A61K31/429 , A61K31/436 , A61K31/4365 , A61K31/4375 , A61K31/4985 , A61K31/5365 , A61K33/24 , A61K45/06 , C07D513/04 , A61K2300/00
摘要： The present invention is directed to substituted 4 H -chromene and analogs thereof, represented by the general formula (I) or pharmaceutically acceptable salts or prodrugs thereof, wherein: A, R 1 , R 2 , R 5 , X, Y, and Z, are defined herein and B is fused thiazole, oxazole, 2-imino-imidazole, 2,1,3-thiadiazo-2-one, thiazol-2-one, oxazol-2-one, imidazol-2-thione, thiazol-2-thione, oxazol-2-thione, imidazoline, oxazoline, thiazoline, triazole, oxazine, oxazine-2,3-dione, or piperazine ring. 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4H-色烯及其类似物或其药学上可接受的盐或前药，其中：A，R 1，R 2，R 5，X，Y和Z在本文中定义 B是稠合噻唑，恶唑，2-亚氨基咪唑，2,1,3-噻二唑-2-酮，噻唑-2-酮，恶唑-2-酮，咪唑-2-硫酮，噻唑-2-硫酮，恶唑-2-硫酮，咪唑啉，恶唑啉，噻唑啉，三唑，恶嗪，恶嗪-2,3-二酮或哌嗪环。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。

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