-
1.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.
-
2.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.
-
3.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.
-
4.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.
-
5.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.
-
6.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.
-
7.发明授权GAMBOGIC ACID DERIVATIVES AS ACTIVATORS OF CASPASES AND INDUCERS OF APOPTOSIS 有权GAMBOGISCHE酸衍生物CASPASENAKTIVATOREN和凋亡的归纳
公开(公告)号：EP1180991B1
公开(公告)日：2010-05-19
申请号：EP00905839.7
申请日：2000-02-01
申请人： Cytovia, Inc.
发明人： CAI, Sui, Xiong , ZHANG, Han-Zhong , WANG, Yan , TSENG, Ben , KASIBHATLA, Shailaja , DREWE, John, A.
IPC分类号： A61K31/352 , A61P35/00 , A61P35/02 , A61P29/00 , A61P37/06 , A61P17/00 , C07D493/20
CPC分类号： C07D493/20 , A61K31/352 , A61K31/4025 , A61K31/4178 , A61K31/4188 , A61K31/4433 , A61K31/453 , A61K31/496 , A61K31/497 , A61K31/5377 , A61K31/5513 , C07D493/22 , C07D519/00
-
8.发明公开DERIVATIVES OF GAMBOGIC ACID AND ANALOGS AS ACTIVATORS OF CASPASES AND INDUCERS OF APOPTOSIS 审中-公开藤黄酸和半胱氨酸蛋白酶的类似物作为资产盖茨衍生物和手段释放细胞凋亡
公开(公告)号：EP1562598A2
公开(公告)日：2005-08-17
申请号：EP03748924.2
申请日：2003-07-01
申请人： Cytovia, Inc.
发明人： TSENG, Ben , SIRISOMA, Nilantha, Sudath , CAI, Sui, Xiong , ZHANG, Han-Zhong , KASIBHATLA, Shailaja , OLLIS, Kristin, P. , DREWE, John, A.
IPC分类号： A61K31/45 , A61K31/497
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.
-
公开(公告)号：EP1392283A1
公开(公告)日：2004-03-03
申请号：EP02731803.9
申请日：2002-05-16
申请人： Cytovia, Inc. , Shire Biochem Inc.
发明人： CAI, Sui, Xiong , ZHANG, Hong , KEMNITZER, William, E. , JIANG, Songchun , DREWE, John, A. , STORER, Richard
IPC分类号： A61K31/35 , A61K31/385 , A61K31/47 , C07D215/16 , C07D215/20 , C07D311/04 , C07D335/04
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表示的取代的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细胞凋亡诱导剂。 因此，本发明的半胱天冬酶的活化剂和细胞凋亡诱导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条件下诱导细胞死亡。
-
10.发明授权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：EP1230232B1
公开(公告)日：2004-02-25
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
-
-
-
-
-
-
-
-
-
搜索结果
18 条记录 (耗时 0.021 秒)
