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公开(公告)号：EP1177168B1
公开(公告)日：2007-05-30
申请号：EP00921874.4
申请日：2000-04-07
申请人： Cytovia, Inc.
IPC分类号： C07C229/00 , C07C205/00 , C07C61/08 , C07C237/22 , C07C271/22 , C07C311/19 , C07D295/20 , C07D311/16 , C07D311/66
CPC分类号： C07D295/205 , C07C237/22 , C07C271/22 , C07C311/19 , C07C2601/08 , C07C2601/14 , C07D311/16 , C07D311/66
摘要： The present invention is directed to novel dipeptide thereof, represented by general formula (I): where R1-R3, X and Y are defined herein. The present invention also relates to the discovery that compounds having Formula (I) are potent inhibitors of caspases and apoptotic cell death. Therefore, the inhibitors of this invention can retard or block cell death in a variety of clinical conditions in which the loss of cells, tissues or entire organs occurs.
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2.发明公开SUBSTITUTED 1-BENZOYL-3-CYANO-PYRROLO 1,2-A] QUINOLINES AND ANALOGS AS ACTIVATORS OF CASPASES AND INDUCERS OF APOPTOSIS 审中-公开SUBSTITUIERTE1苯甲酰基-3-CYANOPYRROLO¬1,2-A CHINO亚麻及其类似物作为胱天蛋白酶的活化剂和细胞凋亡INDUCTORS
公开(公告)号：EP1578424A2
公开(公告)日：2005-09-28
申请号：EP03813401.1
申请日：2003-12-12
申请人： Cytovia, Inc.
发明人： CAI, Sui, Xiong , DREWE, John, A. , JIANG, Sungchun , KASIBHATLA, Shailaja , KUEMMERLE, Jared, Daniel , SIRISOMA, Nilantha, Sudath , ZHANG, Han-Zhong
IPC分类号： A61K31/4745 , A61K31/498 , A61K31/4985 , C07D471/12 , C07D471/06 , C07D487/06 , C07D487/12
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 as defined herein. The present invention also relates to the discovery that compounds of the 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.
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3.发明公开SUBSTITUTED 3-ARYL-5-ARYL- 1,2,4]-OXADIAZOLES AND ANALOGS AS ACTIVATORS OF CASPASES AND INDUCERS OF APOPTOSIS AND THE USE THEREOF 审中-公开取代的3-芳基-5-芳基-1,2,4-恶二唑及其类似物作为与细胞凋亡胱天蛋白酶的活化剂的电感器和它们的用途
公开(公告)号：EP1406632A2
公开(公告)日：2004-04-14
申请号：EP02753336.3
申请日：2002-06-10
申请人： Cytovia, Inc.
发明人： CAI, Sui, Xiong , ZHANG, Han-Zhong , DREWE, John, A. , REDDY, P., Sanjeeva , KASIBHATLA, Shailaja , KUEMMERLE, Jared, Daniel , OLLIS, Kristin, P.
IPC分类号： A61K31/54 , A61K31/415 , A61K31/424 , A61K31/495 , A61K31/541 , A61K31/4166 , A61K31/5377 , A61K31/538 , A61K31/5415
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-[1,2,3]-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.
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4.发明公开SUBSTITUTED 1,4-THIAZEPINE AND ANALOGS AS ACTIVATORS OF CASPASES AND INDUCERS OF APOPTOSIS AND THE USE THEREOF 审中-公开取代的1,4-硫氮杂类似物和它们作为半胱氨酸蛋白酶激活剂
公开(公告)号：EP1324993A2
公开(公告)日：2003-07-09
申请号：EP01969044.5
申请日：2001-04-18
发明人： CAI, Sui, Xiong , DREWE, John, A. , SHELTON, Emma, Jane , LITVAK, Joane , SPERANDIO, David , SPENCER, Jeffrey, R.
IPC分类号： C07D281/06 , C07D281/10 , C07D417/04 , C07D417/14 , C07D513/04 , C07D513/14 , C07D405/04 , A61K31/55 , A61P35/00
CPC分类号： C07D417/14 , C07D281/06 , C07D281/10 , C07D405/04 , C07D417/04 , C07D513/04 , C07D513/14
摘要： The present invention is directed to substituted 1,4-thiazepine and analogs thereof, represented by the general Formula (I): wherein the dashed lines, A?1, A2, A3, X1 and R1¿ are defined herein. The present invention also relates to the discovery that compounds having Formula I are activators of capases and inducers of apoptosis. Therefore, the activators of caspases and inducers 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.
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公开(公告)号：EP1076563A1
公开(公告)日：2001-02-21
申请号：EP99912579.2
申请日：1999-03-16
申请人： Cytovia, Inc.
发明人： CAI, Sui, Xiong , DREWE, John , WANG, Yan , WEBER, Eckard
摘要： The present invention is directed to novel dipeptides thereof, represented by general Formula (I): where R1-R2 and AA are defined herein. The present invention relates to the discovery that compounds having Formula (I) are potent inhibitors of caspases and apoptotic cell death. Therefore, the inhibitors of this invention can retard or block cell death in a variety of clinical conditions in which the loss of cells, tissues or entire organs occurs.
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6.发明公开SUBSTITUTED 4-ARYL-CHROMENE AS ACTIVATOR OF CASPASES AND INDUCER OF APOPTOSIS AND AS ANTIVASCULAR AGENT AND THE USE THEREOF 审中-公开取代的4-芳基 - 色烯ALS胱天蛋白酶激活剂，细胞凋亡INDUCTOR和抗血管AGENTS AND USE
公开(公告)号：EP2049101A2
公开(公告)日：2009-04-22
申请号：EP07810283.7
申请日：2007-07-06
申请人： Cytovia, Inc.
发明人： CAI, Sui, Xiong , DREWE, John, A. , KASIBHATLA, Shailaja , KEMNITZER, William, E. , TSENG, Ben, Y. , LABRECQUE, Denis , BLAIS, Charles , GOURDEAU, Henriette
IPC分类号： A61K31/353 , C07D311/58
CPC分类号： C07D405/12 , C07D311/58
摘要： The present invention is directed to a substituted 4H-chromene represented by the Formula (1R), substantially free from the corresponding (S)-stereoisomer: The present invention also relates to the discovery that compound 1R, substantially free from the corresponding (S)-stereoisomer, is an activator of caspases and inducer of apoptosis, as well as an antivascular agent. Therefore, compound 1R, substantially free from the corresponding (S)-stereoisomer, can be used to induce cell death in a variety of clinical conditions in which uncontrolled growth, and spread of abnormal cells occurs. Compound 1R, substantially free from the corresponding (S)-stereoisomer, also can be used for the treatment of diseases due to overgrowth of vasculature, such as solid tumors and ocular neovascularization.
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7.发明公开CASPASE INHIBITORS FOR THE TREATMENT OF DISEASES AND CONDITIONS CAUSED BY EXPOSURE TO RADIONUCLIDES, BIOLOGICAL AGENTS, OR CHEMICAL AGENTS 审中-公开蛋白酶抑制剂疾病和条件通过与放射性核素，生物制剂或化学药剂接触处理导致
公开(公告)号：EP1494700A2
公开(公告)日：2005-01-12
申请号：EP03754361.8
申请日：2003-04-07
申请人： Cytovia, Inc.
发明人： CAI, Sui, Xiong , TSENG, Ben, Y.
IPC分类号： A61K38/00 , A61K31/535 , A61K31/44 , A61K31/35 , A61K31/27 , A61K31/19 , A61K31/195
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.
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8.发明公开4-SUBSTITUTED-1-(ARYLMETHYLIDENE)THIOSEMICARBAZIDE, 4-SUBSTITUTED-1-(ARYLCARBONYL)THIOSEMICARBAZIDE AND ANALOGS AS ACTIVATORS OF CASPASES AND INDUCERS OF APOPTOSIS AND THE USE THEREOF 审中-公开4-取代的1-（亚苄基）氨基硫脲，4-取代的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细胞凋亡诱导剂及其用途
公开(公告)号：EP1399159A1
公开(公告)日：2004-03-24
申请号：EP02734605.5
申请日：2002-05-31
申请人： Cytovia, Inc.
发明人： CAI, Sui, Xiong , NGUYEN, Bao Ngoc , DREWE, John , REDDY, P., Sanjeeva , KASIBHATLA, Shailaja , PERVIN, Azra
IPC分类号： A61K31/435
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 o f 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.
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9.发明公开SUBSTITUTED 4H-CHROMENE AND ANALOGS AS ACTIVATORS OF CASPASES AND INDUCERS OF APOPTOSIS AND THE USE THEREOF 有权取代-4H-色和类似化合物AS KASPASIS激活剂和细胞凋亡的电感器和它们的用途
公开(公告)号：EP1230232A2
公开(公告)日：2002-08-14
申请号：EP00976912.6
申请日：2000-11-03
申请人： Cytovia, Inc.
发明人： DREWE, John, A. , CAI, Sui, Xiong , WANG, Yan
IPC分类号： C07D311/58 , C07D491/04 , C07D405/04 , C07D407/04 , C07D409/04 , A61K31/352 , C07D311/92 , A61P35/00
CPC分类号： C07D311/58 , C07D311/92 , C07D405/04 , C07D407/04 , C07D409/04 , C07D491/04
摘要： The present invention is directed to substituted 4H-chromene and analogs thereof, represented by general Formula (I), wherein A, B, X, Y, Z and R5 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.
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10.发明公开NOVEL FLUORESCENT REPORTER MOLECULES AND THEIR APPLICATIONS INCLUDING ASSAYS FOR CASPASES 审中-公开荧光显示MOLOKÜLE和应用，包括CASPASEDOSIERUNG
公开(公告)号：EP1026988A1
公开(公告)日：2000-08-16
申请号：EP98953317.9
申请日：1998-10-09
申请人： Cytovia, Inc.
CPC分类号： C07K5/06026 , C07K5/06052 , C07K5/0806 , C07K5/0808 , C07K5/101 , C07K5/1013 , C07K5/1016 , C07K5/1021 , C12Q1/68 , G01N15/1456 , G01N33/533 , G01N2015/1006 , G01N2015/1488 , Y02P20/55
摘要： The present invention relates to novel fluorescent dyes, novel fluorogenic and fluorescent reporter molecules and new enzyme assay processes that can be used to detect the activity of caspases and other enzymes involved in apoptosis in whole cells, cell lines and tissue samples derived from any living organism or organ. The reporter molecules and assay processes can be used in drug screening procedures to identify compounds which act as inhibitors or inducers of the caspase cascade in whole cells or tissues. The reagents and assays described herein are also useful for determining the chemosensitivity of human cancer cells to treatment with chemotherapeutic drugs. The present invention also relates to novel fluorogenic and fluorescent reporter molecules and new enzyme assay processes that can be used to detect the activity of type 2 methionine aminopeptidase, dipeptidyl peptidase IV, calpain, aminopeptidase, HIV protease, adenovirus protease, HSV-1 protease, HCMV protease and HCV protease.
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