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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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2.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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公开(公告)号：EP1076563B1
公开(公告)日：2005-05-11
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
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4.发明公开SUBSTITUTED 4-ARYL-3-(3-ARYL-1-OXO-2-PROPENYL)-2(1H)-QUINOLINONES AND ANALOGS AS ACTIVATORS OF CASPASES AND INDUCERS OF APOPTOSIS AND THE USE THEREOF 审中-公开取代的4-芳基-3-（3-芳基-1-氧代-2-丙烯基）-2（1H）-quinolinones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：EP1404329A1
公开(公告)日：2004-04-07
申请号：EP02741817.7
申请日：2002-06-04
申请人： Cytovia, Inc.
IPC分类号： A61K31/47
CPC分类号： C07D215/227 , A61K31/4704 , A61K31/4709 , A61K45/06 , C07D405/04 , A61K2300/00
摘要： The present invention is directed to substituted 4-aryl-3-(3-aryl-1-oxo-2-propenyl)-2(1H)-quinolinones and analogs thereof, represented by the general Formula I: wherein ar1, Ar2, R1-R6 are defined herein. The present invention also relates to the discovery that compounds having Formula I are activators of caspases and inducers of apoptosis. The compounds of this invention may be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of anormal cells occurs.
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5.发明公开SUBSTITUTED N'-(ARYLCARBONYL)-BENZHYDRAZIDES, N'-(ARYLCARBONYL)-BENZYLIDENE-HYDRAZIDES AND ANALOGS AS ACTIVATORS OF CASPASES AND INDUCERS OF APOTOSIS AND THE USE THEREOF 审中-公开取代的N“ - （芳基羰基）-BENZHYDRAZIDE，N” - （芳基羰基）苯亚甲基 - 酰肼和类似物作为胱天蛋白酶的活化剂和凋亡及其应用的诱导
公开(公告)号：EP1392219A2
公开(公告)日：2004-03-03
申请号：EP02731739.5
申请日：2002-05-10
申请人： Cytovia, Inc.
IPC分类号： A61K6/00
CPC分类号： A61K31/165 , A61K31/44 , C07D213/87 , C07D213/89 , C07D401/14
摘要： The present invention is directed to substituted N'-(arylcarbonyl)- benzhydrazides, N'-(arylcarbonyl)-benzylidene-hydrazides and analogs thereof, represented by the Formulae (I) and (II) wherein Ar1, Ar2, and R1-R2 are defined herein. The present invention also relates to the discovery that compounds having Formulae (I) and (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.
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6.发明公开METHODS OF IDENTIFYING THERAPEUTICALLY EFFECTIVE ANTINEOPLASTIC AGENTS WITH CULTURED CELLS HAVING INTACT CELL MEMBRANES AND CORRESPONDING PRODUCTS 审中-公开一种用于识别治疗物质通过完整细胞膜及相关产品实施有效的抗肿瘤细胞培养
公开(公告)号：EP1151295A1
公开(公告)日：2001-11-07
申请号：EP00907081.4
申请日：2000-02-01
申请人： Cytovia, Inc.
CPC分类号： C07D493/20 , A61K31/00 , A61K31/352 , A61K31/4025 , A61K31/4178 , A61K31/4188 , A61K31/4433 , A61K31/453 , A61K31/475 , A61K31/496 , A61K31/5377 , A61K31/5513 , A61K31/675 , C07D493/22 , C07D519/00 , C12Q1/37 , G01N33/5011 , G01N2500/10
摘要： A method for identifying potentially therapeutically effective antineoplastic compounds comprising determining the ability of test compounds to act as activators of the caspase cascade in viable cultured eukaryotic cells having an intact cell membrane and expressing a cancer phenotype, wherein a test compound that enhances caspase cascade activity is determined to have potential therapeutic efficacy. The method specifically differentiates activators of the caspase cascade from non-specific cell poisons. A therapeutic method useful to modulate in vivo apoptosis or in vivo neoplastic disease, comprising administering to a subject an effective amount of a compound identified as a caspase cascade activator is provided. Compounds, pharmaceutical compositions and a kit for performing the therapeutic method are further provided.
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