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公开(公告)号：EP1560829B1
公开(公告)日：2008-02-20
申请号：EP03758072.7
申请日：2003-10-27
IPC分类号： C07D487/04 , A61K31/519 , A61P35/00
CPC分类号： C07D487/04 , G01N2800/52
摘要： Disclosed are novel pyrimido compounds of the formula (I) wherein R1 to R9 are as defined in the specification, that are selective inhibitors of the Src family of tyrosine kinases. These compounds and their pharmaceutically acceptable salts are anti-proliferative agents useful in the treatment or control of solid tumors, in particular breast, colon, hepatic and pancreatic tumors. Also disclosed are pharmaceutical compositions containing these compounds and the use for treating cancer.
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2.发明公开4- AND 5-ALKYNYLOXINDOLES AND 4- AND 5-ALKENYLOXINDOLES 有权图4和5 ALKYNYLOXINDOLE和4以及5 ALKENYLOXINDOLE
公开(公告)号：EP1149092A2
公开(公告)日：2001-10-31
申请号：EP99957341.3
申请日：1999-12-07
IPC分类号： C07D403/00
CPC分类号： C07D401/14 , C07D403/06 , C07D403/14 , C07D405/14 , C07D409/14
摘要： 4- and 5-alkynyloxindoles as well as 4- and 5-alkenyloxindoles having formula (I) and (II), wherein R?1, R2, R3, R11, R12¿, X and z have the meaning indicated in the specification, inhibit or modulate protein kinases, in particular JNK protein kinases and are useful as anti-inflammatory agents, particularly in the treatment of rheumatoid arthritis.
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3.发明授权
公开(公告)号：EP1565475B1
公开(公告)日：2009-04-08
申请号：EP03775346.4
申请日：2003-11-12
发明人： CHEN, Jian, Jeffrey , LUK, Kin-Chun
IPC分类号： C07D498/04 , A61K31/519 , A61K31/5395 , A61P19/02 , A61P29/00 , A61P11/00 , A61P25/28 , A61P35/00
CPC分类号： C07D498/04
摘要： The present invention provides a compound of the formula: (I) ;or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, X1, X2, and Ar1 are as defined herein. The present invention also provides a process for producing the same, compositions comprising the same, and methods for using the same.
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4.发明授权DISUBSTITUTED PYRAZOLOBENZODIAZEPINES USEFUL AS INHIBITORS FOR CDK2 AND ANGIOGESIS, AND FOR THE TREATMENT OF BREAST, COLON, LUNG AND PROSTATE CANCER 有权AS CDK2和血管生成抑制剂和用于乳腺癌，结肠癌，肺癌和前列腺SUITABLE二取代PYRAZOLOBENZODIAZEPINE于治疗
公开(公告)号：EP1802625B1
公开(公告)日：2008-06-18
申请号：EP05792946.5
申请日：2005-10-04
发明人： LIU, Jin-Jun , LUK, Kin-Chun , PIZZOLATO, Giacomo , REN, Yi , THAKKAR, Kshitij Chhabilbhai , WOVKULICH, Peter, Michael , ZHANG, Zhuming
IPC分类号： C07D487/04 , A61K31/5517 , A61P35/00
CPC分类号： C07D487/04
摘要： The present invention provides compounds of the formula (I) wherein R1, R2, R3 and R4 are described herein. The invention also provides syntheses for preparation of such compounds and pharmaceutical compositions containing them. The invention further provides methods for inhibiting kinases, in particular CDK2, for inhibiting angiogenesis, and for treating cancers, in particular breast, colon, prostate, and lung cancer.
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公开(公告)号：EP1896412A2
公开(公告)日：2008-03-12
申请号：EP06777423.2
申请日：2006-06-22
发明人： LUK, Kin-Chun , SO, Sung-Sau , ZHANG, Jing , ZHANG, Zhuming
IPC分类号： C07D209/34 , C07D401/04 , C07D401/14 , C07D403/04 , A61K31/4155 , A61K31/4439 , A61P35/00
CPC分类号： C07D401/14 , C07D209/34 , C07D401/04 , C07D403/04
摘要： The invention describes compounds of the general formula (I-A) or the pharmaceutically acceptable salts thereof, wherein R1, R2, R4 and R5 are herein described, a process for their manufacture, medicaments containing them as well as the use of these compounds as pharmaceutically active agents. The compounds show activity as antiproliferative agents and may be especially useful for the treatment of cancer.
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6.发明授权
公开(公告)号：EP1149105B1
公开(公告)日：2008-02-27
申请号：EP99963496.7
申请日：1999-12-11
发明人： LUK, Kin-Chun , MICHOUD, Christophe
IPC分类号： C07D487/04 , A61K31/50 , A61K31/41 , A61P29/00
CPC分类号： C07D487/04
摘要： 4,5-pyrazinoxindoles having formula (I), inhibit or modulate protein kinases, in particular JNK protein kinases and are useful as anti-inflammatory agents, particularly in the treatment of rheumatoid arthritis.
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7.发明公开NAPHTHOSTYRIL DERIVATIVES AND THEIR USE AS INHIBITORS OF CYCLIN-DEPENDENT KINASES 有权NAPHTHOSTYRIL衍生物及其作为抑制剂细胞周期蛋白依赖性激酶
公开(公告)号：EP1358180A2
公开(公告)日：2003-11-05
申请号：EP02706711.5
申请日：2002-01-16
发明人： CHEN, Yi , DERMATAKIS, Apostolos , KONZELMANN, Frederick, Martin , LIU, Jin-Jun , LUK, Kin-Chun
IPC分类号： C07D403/04 , A61K31/40 , A61P43/00 , C07D403/06 , C07D403/14 , C07D401/14
CPC分类号： C07D401/14 , C07D403/04 , C07D403/06 , C07D403/14
摘要： Disclosed are novel naphthostyrils of formula I. These compounds inhibit cyclin-dependent kinases (CDKs), in particular CDK2. These compounds and their pharmaceutically acceptable salts and esters are anti-proliferative agents useful in the treatment or control of cell proliferative disorders, in particular cancer. Also disclosed are pharmaceutical compositions containing such compounds, methods for the treatment and/or prevention of cancer using such composition, and intermediates useful in the preparation of the compounds of formula I.
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公开(公告)号：EP1149106B1
公开(公告)日：2003-03-19
申请号：EP99964543.5
申请日：1999-12-10
IPC分类号： C07D487/04 , A61K31/4188 , A61K31/424 , A61K31/425
CPC分类号： C07D403/06 , C07D487/04 , C07D513/04 , C09B23/04
摘要： Novel 4,5-azolo-oxindoles having formula (I), wherein R1, R2, Y, Z and a have the meaning indicated in the specification, inhibit cyclin-dependent kinases (CDKs), in particular CDK2 and are useful in the treatment or control of cell proliferative disorders, in particular cancer.
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9.发明授权PYRIDINO¬2,3-D PYRIMIDINE DERIVATIVES AS SELECTIIVE KDR AND FGFR INHIBITORS 有权PYRIDINO¬2,3-D嘧啶衍生物作为选择性KDR和FGFR抑制剂
公开(公告)号：EP1581531B1
公开(公告)日：2008-02-27
申请号：EP03785789.3
申请日：2003-12-11
发明人： LIU, Jin-Jun , LUK, Kin-Chun
IPC分类号： C07D471/04 , A61K31/505 , A61P35/00
CPC分类号： C07D471/04
摘要： Disclosed are novel dihydropridinone compounds of the formula (I) wherein Ar, Ar' and R1 are as defined in the description, that are selective inhibitors of both KDR and FGFR kinases. These compounds and their pharmaceutically acceptable salts are anti-proliferative agents useful in the treatment or control of solid tumors, in particular breast, colon lung and prostate tumors. Also, disclosed are pharmaceutical compositions containing these compounds and their preparation.
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10.发明授权PYRIMIDO 4,5-D PYRIMIDINE DERIVATIVES WITH ANTICANCER ACTIVITY 有权嘧啶并4,5-D PYRIMIDINDERIVATE MITANTIKREBSWIRKUNG
公开(公告)号：EP1560832B1
公开(公告)日：2008-01-23
申请号：EP03810410.5
申请日：2003-10-27
发明人： McDermott, Lee Apostle , KABAT, Marek, Michal , LUK, Kin-Chun , ROSSMAN, Pamela, Loreen , SO, Sung-Sau
IPC分类号： C07D487/04 , A61K31/519 , A61P35/00
CPC分类号： C07D487/04 , G01N2800/52
摘要： Disclosed are novel pyrimido compounds of the formula (I) wherein R1 to R9 are as defined in the specification, that are selective inhibitors of both KDR an FGFR kinases and are selective against LCK. These compounds and their pharmaceutically acceptable salts are anti-proliferative agents useful in the treatment or control of solid tumors, in particular breast, colon, lung and prostate tumors. Also disclosed are pharmaceutical compositions containing these compounds and the use for 10 treating cancer.
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