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公开(公告)号：EP0892789B2
公开(公告)日：2009-11-18
申请号：EP97920213.2
申请日：1997-04-08
发明人： BRIDGES, Alexander, James , DENNY, William Alexander , DOBRUSIN, Ellen, Myra , DOHERTY, Annette, Marian , FRY, David, W. , McNAMARA, Dennis, Joseph , SHOWALTER, Howard, Daniel, Hollis , SMAILL, Jeffrey B. , ZHOU, Hairong
IPC分类号： C07D239/94 , C07D487/04 , C07D471/04 , C07D495/04
CPC分类号： C07D231/12 , C07D233/56 , C07D239/94 , C07D249/08 , C07D403/04 , C07D471/04 , C07D487/04 , C07D495/04 , C07F9/6561
摘要： The present invention provides compounds that are irreversible inhibitors of tyrosine kinases. Also provided is a method of treating cancer, restenosis, atherosclerosis, endometriosis, and psoriasis and a pharmaceutical composition that comprises a compound that is an irreversible inhibitor of tyrosine kinases.
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公开(公告)号：EP1255739B1
公开(公告)日：2008-06-11
申请号：EP00984246.9
申请日：2000-12-12
发明人： BIRD, Paul , ELLSWORTH, Edmund, Lee , NGUYEN, Dai, Quoc , SANCHEZ, Joseph, Peter , SHOWALTER, Howard, Daniel, Hollis , SINGH, Rajeshwar , STIER, Michael, Andrew , TRAN, Tuan, Phong , WATSON, Brian, Morgan , YIP, Judy
IPC分类号： C07D239/96 , C07D403/04 , C07D471/04 , C07D471/06 , C07D498/06 , C07D403/14 , C07D519/00 , C07D487/04 , C07D487/10 , C07D413/04 , C07D417/04 , C07D409/04 , A61K31/505 , A61P31/04
CPC分类号： C07D401/04 , C07D239/96 , C07D403/04 , C07D403/14 , C07D471/04 , C07D487/04 , C07D487/10
摘要： Antibacterial 3-aminoquinazolin-2,4-diones have formula (I) wherein: R1 and R3 include alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heterocyclic, and heteroaryl; R5, R6, and R8 include H, alkyl, alkoxy, halo, NO2, CN, NH2, alkyl and dialkylamino; R7 includes hydrogen, alkyl, cycloalkyl, heterocyclic, fused heterocyclic, aryl and fused aryl; J and K are C or N; and pharmaceutically acceptable salts thereof.
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3.发明授权NAPHTHYRIDINONES FOR INHIBITING PROTEIN TYROSINE KINASE AND CELL CYCLE KINASE MEDIATED CELLULAR PROLIFERATION 有权，用来抑制蛋白酪氨酸激酶和细胞周期激酶Naphthyridinones引起细胞增殖
公开(公告)号：EP1003745B1
公开(公告)日：2004-12-29
申请号：EP98939941.5
申请日：1998-08-13
发明人： BARVIAN, Mark, Robert , DENNY, William, Alexander , DOBRUSIN, Ellen, Myra , HAMBY, James, Marino , SHOWALTER, Howard, Daniel, Hollis , THOMPSON, Andrew, Mark , WINTERS, Roy, Thomas , WU, Zhipei
IPC分类号： C07D471/04 , A61K31/44
CPC分类号： C07D471/04
摘要： Naphthyridinones of Formula (I) are inhibitors of PTKs and cell cycle kinases, and are useful in treating cellular proliferation. The compounds are especially useful in treating cancer, atherosclerosis, restenosis, and psoriasis.
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4.发明授权BICYCLIC PYRIMIDINES AND BICYCLIC 3,4-DIHYDROPYRIMIDINES AS INHIBITORS OF CELLULAR PROLIFERATION 有权双环嘧啶和双环3,4-二氢作为细胞增殖抑制剂
公开(公告)号：EP1080092B1
公开(公告)日：2008-07-23
申请号：EP99924165.6
申请日：1999-05-10
发明人： DOBRUSIN, Ellen, Myra , HAMBY, James, Marino , KRAMER, James, Bernard , SCHROEDER, Mel, Conrad , SHOWALTER, Howard, Daniel, Hollis , TOOGOOD, Peter , TRUMPP-KALLMEYER, Susanne, A.
IPC分类号： C07D487/04 , C07D471/04 , A61K31/505
CPC分类号： C07D471/04 , C07D487/04
摘要： This invention provides bicyclic heterocycles that are useful for treating cell proliferative disorders, such as cancer and restenosis, as well as angiogenesis and atherosclerosis. We have now discovered a group of bicyclic compounds that are potent inhibitors of cyclin-dependent kinases (cdks), growth factor-mediated kinases, and non-receptor kinases. The compounds are readily synthesized and can be administered by a variety of routes, including orally, and have sufficient bioavailability for clinical use. This invention provides compounds of Formula (I), where Z is N or CH; G is N or CH; 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 the pharmaceutically acceptable salts thereof. This invention also provides pharmaceutical formulations comprising a compound of Formula (I) together with a pharmaceutically acceptable carrier, diluent, or excipient therefor.
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