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公开(公告)号：EP1463501A1
公开(公告)日：2004-10-06
申请号：EP02796582.1
申请日：2002-12-09
发明人： KONG, Norman , LIU, Emily, Aijun , VU, Binh, Thanh
IPC分类号： A61K31/4164 , A61K31/4178 , C07D233/22 , C07D233/26 , C07D233/20 , C07D403/10 , C07D405/04 , A61P35/00
CPC分类号： C07D405/04 , C07D233/20 , C07D233/22 , C07D233/26
摘要： The present invention provides compounds according to formula I and formula II and pharmaceutically acceptable salts and esters thereof, having the designations provided herein and which inhibit the interaction of MDM2 protein with a p53-like peptide and have antiproliferative activity (I) (II).
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公开(公告)号：EP1791837B1
公开(公告)日：2009-08-19
申请号：EP05784418.5
申请日：2005-09-15
发明人： GOODNOW, Robert, Alan, Jr. , HUBY, Nicholas, John, Silvester , KONG, Norman , MCDERMOTT, Lee, Apostle , MOLITERNI, John, Anthony , ZHANG, Zhuming
IPC分类号： C07D417/12 , C07D417/14 , A61K31/427 , A61P35/00
CPC分类号： C07D417/14 , C07D417/12
摘要： The present invention relates to compounds of the formula (I) which are useful in treating diseases characterized by the hyperactivity of MEK. Accordingly the compounds are useful in the treatment of diseases, such as, cancer, cognative and CNS disorders and inflammatory/autoimmune diseases.
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公开(公告)号：EP1242409A2
公开(公告)日：2002-09-25
申请号：EP00991984.6
申请日：2000-12-21
发明人： FOTOUHI, Nader , KONG, Norman , LOVEY, Allen, John
IPC分类号： C07D403/14
CPC分类号： C07D403/14 , C07D405/14 , C07D409/14 , C07D417/14
摘要： Disclosed are substituted pyrroles having formula (I), wherein R?1, R2, R1' and R2'¿ are as defined in the claims and in the description. These compounds and their pharmaceutically acceptable salts are useful in the treatment and/or control of cell proliferative disorders, in particular cancer. Also disclosed are pharmaceutical compositions containing the foregoing compounds.
摘要翻译： 公开了具有式（I）的取代的吡咯，其中R 1，R 2，R 1'和R 2''如权利要求书和说明书中所定义。 这些化合物及其药学上可接受的盐可用于治疗和/或控制细胞增殖性病症，特别是癌症。 还公开了含有前述化合物的药物组合物。
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4.发明授权2,4,5-TRIPHENYL IMIDAZOLINE DERIVATIVES AS INHIBITORS OF THE INTERACTION BETWEEN P53 AND MDM2 PROTEINS FOR USE AS ANTICANCER AGENTS 有权2,4,5- TRIPHENYLIMIDAZOLINDERIVATE之间。如P53和MDM2蛋白的相互作用以用作抗癌剂抑制剂
公开(公告)号：EP1960368B1
公开(公告)日：2015-05-06
申请号：EP06819663.3
申请日：2006-11-22
发明人： DING, Qingjie , GRAVES, Bradford James , KONG, Norman , LIU, Jin-Jun , LOVEY, Allen John , PIZZOLATO, Giacomo , ROBERTS, John Lawson , SO, Sung-Sau , VU, Binh Thanh , WOVKULICH, Peter Michael
IPC分类号： C07D233/22 , C07D233/26 , C07D401/06 , C07D403/06 , C07D407/12 , C07D409/12 , C07D471/04 , C07D487/04 , A61K31/4164 , A61K31/496 , A61P35/00
CPC分类号： C07D233/22 , C07D233/26 , C07D401/06 , C07D401/12 , C07D403/06 , C07D405/06 , C07D407/12 , C07D409/12 , C07D417/12 , C07D471/04 , C07D487/04
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公开(公告)号：EP2234982A1
公开(公告)日：2010-10-06
申请号：EP08864818.3
申请日：2008-12-10
发明人： CHEN, Shaoqing , HUBY, Nicholas, John, Silvester , KONG, Norman , MOLITERNI, John, Anthony , MORALES, Omar, Jose
IPC分类号： C07D233/74 , C07D233/78 , C07D417/14 , A61K31/4166 , A61P35/00
CPC分类号： C07D233/74 , C07D233/78 , C07D417/14
摘要： The present invention relates to compounds of the formula (I) methods for the preparation thereof, and methods for their use. The compounds are useful in treating diseases characterized by the hyperactivity of MEK. Accordingly the compounds are useful in the treatment of diseases, such as cancer, cognitive and CNS disorders, and inflammatory/autoimmune diseases.
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6.发明公开2,4,5-TRIPHENYL IMIDAZOLINE DERIVATIVES AS INHIBITORS OF THE INTERACTION BETWEEN P53 AND MDM2 PROTEINS FOR USE AS ANTICANCER AGENTS 有权2,4,5- TRIPHENYLIMIDAZOLINDERIVATE之间。如P53和MDM2蛋白的相互作用以用作抗癌剂抑制剂
公开(公告)号：EP1960368A1
公开(公告)日：2008-08-27
申请号：EP06819663.3
申请日：2006-11-22
发明人： DING, Qingjie , GRAVES, Bradford James , KONG, Norman , LIU, Jin-Jun , LOVEY, Allen John , PIZZOLATO, Giacomo , ROBERTS, John Lawson , SO, Sung-Sau , VU, Binh Thanh , WOVKULICH, Peter Michael
IPC分类号： C07D233/22 , C07D233/26 , C07D401/06 , C07D403/06 , C07D407/12 , C07D409/12 , C07D471/04 , C07D487/04 , A61K31/4164 , A61K31/496 , A61P35/00
CPC分类号： C07D233/22 , C07D233/26 , C07D401/06 , C07D401/12 , C07D403/06 , C07D405/06 , C07D407/12 , C07D409/12 , C07D417/12 , C07D471/04 , C07D487/04
摘要： There is provided a compound of formula (I) and the pharmaceutically acceptable salts and esters thereof wherein X1 , X2, R1 , R2, R3, R4, R5 and R6 are herein described. The compounds exhibit activity as anticancer agents.
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7.发明授权
公开(公告)号：EP1224181B1
公开(公告)日：2003-12-03
申请号：EP00969381.3
申请日：2000-10-02
发明人： FOTOUHI, Nader , KONG, Norman , LIU, Emily, Aijun , LOVEY, Allen, John , MULLIN, John, Guilfoyle, Jr.
IPC分类号： C07D403/14 , C07D401/14 , A61K31/4015 , A61K31/404 , A61P35/00
CPC分类号： C07D401/14 , C07D403/14
摘要： Disclosed are novel substituted pyrroles having formula (I). These compounds and their pharmaceutically acceptable salts are suitable for administration to patients as continuous infusion solution and are useful in the treatment and/or control of cell proliferative disorders, in particular cancer. Also disclosed are pharmaceutical compositions containing the foregoing compounds and their use for the treatment and/or control of cancer.
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公开(公告)号：EP3080099B1
公开(公告)日：2018-04-11
申请号：EP14809645.6
申请日：2014-12-10
IPC分类号： C07D401/14 , C07D403/06 , C07D403/14 , A61K31/4155 , A61K31/4439 , A61P29/00 , A61P11/06
CPC分类号： C07D403/06 , A61K31/4155 , A61K31/4439 , C07D401/14 , C07D403/14 , C07D487/04
摘要： This application discloses compounds according to generic Formula (I) wherein all variables are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are useful for the treatment of oncological, auto-immune, and inflammatory diseases caused by aberrant B-cell activation. Also disclosed are compositions containing compounds of Formula (I) and at least one carrier, diluent or excipient.
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公开(公告)号：EP3080098B1
公开(公告)日：2017-12-06
申请号：EP14809643.1
申请日：2014-12-10
IPC分类号： C07D401/14 , C07D403/06 , A61K31/4155 , A61K31/4439 , A61P29/00 , A61P11/06
CPC分类号： C07D403/06 , C07D401/14
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公开(公告)号：EP2188276B1
公开(公告)日：2012-03-28
申请号：EP08786933.5
申请日：2008-08-06
发明人： CHEN, Shaoqing , HUBY, Nicholas, John, Silvester , KONG, Norman , MOLITERNI, John, Anthony , MORALES, Omar, Jose
IPC分类号： C07D403/06 , A61K31/4184 , A61P35/00
CPC分类号： C07D403/06
摘要： This invention relates to compounds of formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, and R6 are described in this application. These compounds inhibit the enzymes MEK 1 and MEK 2, protein kinases that are components of the MAP kinase signal transduction pathway. As such the compounds have anti-hyperproliferative cellular activity and are thus useful in the treatment of cell proliferative disorders, such as cancer.
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