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1.发明授权PYRIDO 2,3-D PYRIMIDINES AND 4-AMINOPYRIMIDINES AS INHIBITORS OF CELLULAR PROLIFERATION 失效吡啶并（2,3-D）嘧啶和4-氨基PRIMIDINE AS细胞增殖的抑制剂的
公开(公告)号：EP0964864B1
公开(公告)日：2008-04-09
申请号：EP98908442.1
申请日：1998-01-26
发明人： BOSCHELLI, Diane, Harris , DOBRUSIN, Ellen, Myra , DOHERTY, Annette, Marian , FATTAEY, Ali , FRY, David, W. , BARVIAN, Mark, R. , TRUMPP-KALLMEYER, Susanne, A , WU, Zhipei
IPC分类号： C07D471/00
CPC分类号： C07D239/47 , C07D239/48 , C07D471/04
摘要： This invention provides pyridopyrimidines and 4-aminopyrimidines that are useful for treating cell proliferative disorders, such as cancer and restenosis. We have now discovered a group of 7,8-dihydro-2-(amino and thio)pyrido[2,3-d]pyrimidines and 4-aminopyrimidines that are potent inhibitors of cyclin-dependent kinases (cdks) and growth factor-mediated kinases. The compounds are readily synthesized and can be administered by a variety of routes, including orally, and have sufficient bioavailability. This invention provides compounds of Formula (I) and Formula (II), where W is NH, S, SO, or SO2, R1 includes phenyl and substituted phenyl, R2 includes alkyl and cycloalkyl, R3 includes alkyl and hydrogen, R?8 and R9¿ include hydrogen and alkyl, and Z is carboxy. This invention also provides pharmaceutical formulations comprising a compound of Formula (I or II) together with a pharmaceutically acceptable carrier, diluent, or excipient therefor.
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2.发明授权BENZOTHIOPHENE, BENZOFURAN AND INDOLETHIAZEPINONES, OXAZEPINONES AND DIAZEPINONES AS INHIBITORS OF CELL ADHESION AND AS INHIBITORS OF HIV 失效苯并噻吩，苯并呋喃和吲哚THIAZEPINONE，OXAZEPINONE和二氮杂酮细胞粘附和艾滋病毒抑制剂
公开(公告)号：EP0749434B1
公开(公告)日：1999-12-15
申请号：EP95908760.2
申请日：1995-01-30
发明人： BOSCHELLI, Diane, Harris , CONNOR, David, Thomas , KRAMER, James, Bernard , UNANGST, Paul, Charles
IPC分类号： C07D495/04 , C07D498/04 , C07D513/04 , A61K31/55
CPC分类号： C07D495/04 , A61K31/551 , A61K31/553 , A61K31/554 , C07D513/04
摘要： Benzothiophene, benzofuran and indolethiazepinones, oxazepinones and diazepinones of formula (I) as well as methods of preparation thereof are described as agents which inhibit leukocyte adherence to vascular endothelium and, as such, are effective therapeutic agents for treating inflammatory diseases; these compounds also inhibit the activation of human immunodeficiency virus (HIV).
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3.发明授权PYRIDO[2,3-d]PYRIMIDINES FOR INHIBITING PROTEIN TYROSINE KINASE MEDIATED CELLULAR PROLIFERATION 失效吡啶并[2,3-D]蛋白介导的细胞传播的嘧啶类酪氨酸激酶作为抑制剂
公开(公告)号：EP0823908B1
公开(公告)日：2006-11-02
申请号：EP96913175.4
申请日：1996-04-26
发明人： BLANKLEY, Clifton, John , BOSCHELLI, Diane, Harris , DOHERTY, Annette, Marian , HAMBY, James, Marino , KLUTCHKO, Sylvester , PANEK, Robert, Lee
IPC分类号： C07D471/04 , A61K31/505
CPC分类号： C07D471/04
摘要： 6-Aryl pyrido[2,3-d]pyrimidine 7-imines, 7-ones, and 7-thiones o f formula (I) are inhibitors of protein tyrosine kinases, and are thus useful in treating cellular proliferation mediated thereby. The compounds are especially useful in treating cancer, atherosclerosis, restenosis, and psoriasis.
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4.发明公开PYRIDO 2,3-d]PYRIMIDINES FOR INHIBITING PROTEIN TYROSINE KINASE MEDIATED CELLULAR PROLIFERATION 失效吡啶并[2,3-D]蛋白介导的细胞传播的嘧啶类酪氨酸激酶作为抑制剂
公开(公告)号：EP0823908A1
公开(公告)日：1998-02-18
申请号：EP96913175.0
申请日：1996-04-26
发明人： BLANKLEY, Clifton, John , BOSCHELLI, Diane, Harris , DOHERTY, Annette, Marian , HAMBY, James, Marino , KLUTCHKO, Sylvester , PANEK, Robert, Lee
CPC分类号： C07D471/04
摘要： 6-Aryl pyrido[2,3-d]pyrimidine 7-imines, 7-ones, and 7-thiones o f formula (I) are inhibitors of protein tyrosine kinases, and are thus useful in treating cellular proliferation mediated thereby. The compounds are especially useful in treating cancer, atherosclerosis, restenosis, and psoriasis.
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5.发明公开PYRIDO 2,3-D] PYRIMIDINES AND 4-AMINOPYRIMIDINES AS INHIBITORS OF CELLULAR PROLIFERATION 失效吡啶并（2,3-D）嘧啶和4-氨基PRIMIDINE AS细胞增殖的抑制剂的
公开(公告)号：EP0964864A2
公开(公告)日：1999-12-22
申请号：EP98908442.0
申请日：1998-01-26
发明人： BOSCHELLI, Diane, Harris , DOBRUSIN, Ellen, Myra , DOHERTY, Annette, Marian , FATTAEY, Ali , FRY, David, W. , BARVIAN, Mark, R. , TRUMPP-KALLMEYER, Susanne, A , WU, Zhipei
CPC分类号： C07D239/47 , C07D239/48 , C07D471/04
摘要： This invention provides pyridopyrimidines and 4-aminopyrimidines that are useful for treating cell proliferative disorders, such as cancer and restenosis. We have now discovered a group of 7,8-dihydro-2-(amino and thio)pyrido[2,3-d]pyrimidines and 4-aminopyrimidines that are potent inhibitors of cyclin-dependent kinases (cdks) and growth factor-mediated kinases. The compounds are readily synthesized and can be administered by a variety of routes, including orally, and have sufficient bioavailability. This invention provides compounds of Formula (I) and Formula (II), where W is NH, S, SO, or SO2, R1 includes phenyl and substituted phenyl, R2 includes alkyl and cycloalkyl, R3 includes alkyl and hydrogen, R?8 and R9¿ include hydrogen and alkyl, and Z is carboxy. This invention also provides pharmaceutical formulations comprising a compound of Formula (I or II) together with a pharmaceutically acceptable carrier, diluent, or excipient therefor.
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6.发明公开BENZOTHIOPHENE, BENZOFURAN AND INDOLETHIAZEPINONES, OXAZEPINONES AND DIAZEPINONES AS INHIBITORS OF CELL ADHESION AND AS INHIBITORS OF HIV 失效苯并噻吩，苯并呋喃和吲哚THIAZEPINONE，OXAZEPINONE和二氮杂酮细胞粘附和艾滋病毒抑制剂
公开(公告)号：EP0749434A1
公开(公告)日：1996-12-27
申请号：EP95908760.0
申请日：1995-01-30
发明人： BOSCHELLI, Diane, Harris , CONNOR, David, Thomas , KRAMER, James, Bernard , UNANGST, Paul, Charles
CPC分类号： C07D495/04 , A61K31/551 , A61K31/553 , A61K31/554 , C07D513/04
摘要： Benzothiophene, benzofuran and indolethiazepinones, oxazepinones and diazepinones of formula (I) as well as methods of preparation thereof are described as agents which inhibit leukocyte adherence to vascular endothelium and, as such, are effective therapeutic agents for treating inflammatory diseases; these compounds also inhibit the activation of human immunodeficiency virus (HIV).
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