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1.发明公开3-ARYL-6-ARYL-7H-[1,2,4]TRIAZOLO[3,4-b][1,3,4]THIADIAZINES AND ANALOGS AS ACTIVATORS OF CASPASES AND INDUCERS OF APOPTOSIS AND THE USE THEREOF 审中-公开3-芳基-6-芳基 - 7H- [1,2,4]三唑并[3,4-b] [1,3,4]噻二嗪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：EP2046336A2
公开(公告)日：2009-04-15
申请号：EP07796912.9
申请日：2007-07-18
申请人： Cytovia, Inc.
发明人： CAI, Sui Xiong , DREWE, John A. , ZHANG, Han-Zhong , KASIBHATLA, Shailaja , CLAASSEN, Gisela , SIRISOMA, Nilantha Sudath , KEMNITZER, William Edward
IPC分类号： A61K31/53 , A61K31/542 , A61K31/5365
CPC分类号： A61K31/53 , A61K31/542 , C07D487/04 , C07D513/04
摘要： Disclosed are 3-aryl-6-aryl-7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazines and analogs thereof, represented by the Formula (I), wherein Ar1, Q2, R1, R2, dashed line and X 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.
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公开(公告)号：EP1833482A2
公开(公告)日：2007-09-19
申请号：EP06717281.7
申请日：2006-01-03
发明人： CAI, Sui Xiong , ANDERSON, Mark B. , WILLARDSEN, Adam , SIRISOMA, Nilantha Sudath , ZHANG, Hong , SUZUKI, Kazuyuki
IPC分类号： A61K31/50 , A61K31/519 , A61K31/517 , C07D239/72 , C07D239/00 , C07D241/04 , C07D265/12 , C07D321/00 , C07D401/00 , C07D403/00 , C07D498/00
CPC分类号： C07D239/94 , C07D239/72 , C07D403/12
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.
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3.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亚麻及其类似物的半胱氨酸蛋白酶激活因子和细胞凋亡INDUCTORS
公开(公告)号：EP1578424A4
公开(公告)日：2007-08-08
申请号：EP03813401
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： C07D471/04 , A61K31/4745 , A61K31/496 , A61K31/498 , A61K31/4985 , C07D471/06 , C07D471/14 , C07D487/04 , C07D487/06 , C07D487/12
CPC分类号： C07D471/04 , A61K31/4745 , A61K31/496 , A61K31/4985 , C07D471/14 , C07D487/04
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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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5.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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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：EP1151295A4
公开(公告)日：2005-03-30
申请号：EP00907081
申请日：2000-02-01
申请人： CYTOVIA INC
发明人： WEBER ECKARD , TSENG BEN Y , DREWE JOHN , CAI SUI XIONG , KASIBHATLA SHAILAJA
IPC分类号： A61K31/00 , A61K31/352 , A61K31/4025 , A61K31/4178 , A61K31/4188 , A61K31/4433 , A61K31/453 , A61K31/475 , A61K31/496 , A61K31/5377 , A61K31/5513 , A61K31/675 , C07D493/20 , C07D493/22 , C07D519/00 , C12Q1/37 , G01N33/50
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
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7.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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8.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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9.发明公开NOVEL FLUORESCENCE DYES AND THEIR APPLICATIONS FOR WHOLE CELL FLUORESCENCE SCREENING ASSAYS FOR CASPASES, PEPTIDASES, PROTEASES AND OTHER ENZYMES AND THE USE THEREOF 有权新的荧光染料及其在FLUORESZENSNACHWEISVERFAHREN应用的所有单元格FOR胱天蛋白酶，肽酶，蛋白酶和其他酶及其用途
公开(公告)号：EP1100520A4
公开(公告)日：2002-07-17
申请号：EP99935751
申请日：1999-07-21
申请人： CYTOVIA INC
发明人： ZHANG HAN-ZHONG , CAI SUI XIONG , DREWE JOHN A , YANG WU
IPC分类号： C07D311/82 , C07D493/10 , C07K5/06 , C07K5/08 , C07K5/10 , C07K7/06 , A61K38/00 , A61K38/04 , A61K38/08 , C07D309/00 , C07D311/78 , C12N9/48 , C12N9/50 , C12Q1/37 , G01N33/53
CPC分类号： C07D493/10 , C07D311/82 , C07K5/06191 , C07K5/0827 , C07K5/1027 , C07K7/06 , Y10T436/142222
摘要： The present invention relates to novel fluorescent dyes, novel fluorogenic and fluorescent reporter molecules and new enzymes 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, HIV protease, adenovirus protease, HSV-1 protease, HCMV protease and HCV protease.
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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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