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31.发明授权STEREOISOMERICALLY ENRICHED 3-AMINOCARBONYL BICYCLOHEPTENE PYRIMIDINEDIAMINE COMPOUNDS AND THEIR USES 有权富含立体异构体-3-氨基羰基 - 二环嘧啶化合物及其用途
公开(公告)号：EP1824489B1
公开(公告)日：2011-01-05
申请号：EP05844183.3
申请日：2005-11-15
发明人： ARGADE, Ankush , SINGH, Rajinder , LI, Hui
IPC分类号： C07D239/48 , C07D413/12
CPC分类号： C07D239/48 , A61K31/495 , C07D413/12
摘要： The present invention provides stereoisomers and stereoisomeric mixtures of 3-aminocarbonyl-bicycloheptene-2,4-pyrimidinediamine compounds having antiproliferative activity, compositions comprising the compounds and methods of using the compounds to inhibit cellular proliferation and to treat proliferate diseases such as tumorigenic cancers.
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公开(公告)号：EP1573026A4
公开(公告)日：2010-09-08
申请号：EP02791559
申请日：2002-07-31
发明人： DEMO SUSAN , HITOSHI YASUMICHI , JENKINS YONCHU
IPC分类号： C12Q1/34 , G01N33/50 , G01N33/573 , C12Q1/68 , A61K38/43 , A61K48/00 , C12N5/00 , C12N9/00 , C12N9/22
CPC分类号： C12Q1/34 , G01N33/5011 , G01N33/573 , G01N2333/922 , G01N2500/02
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33.发明公开
公开(公告)号：EP2183225A1
公开(公告)日：2010-05-12
申请号：EP08782014.8
申请日：2008-07-17
发明人： SINGH, Rajinder , LI, Hui , ZHAO, Haoran , PAYAN, Donald G. , KOLLURI, Rao , TSO, Kin , RAMPHAL, John , GU, Shihai
IPC分类号： C07D239/48 , C07D401/12 , C07D401/14 , C07D407/14 , C07D413/14 , C07D417/14 , C07D498/04 , A61K31/506 , A61P35/00
CPC分类号： C07D401/12 , C07D239/48 , C07D401/14 , C07D407/14 , C07D413/14 , C07D417/14 , C07D498/04
摘要： The invention encompasses Pyrimidine compounds and the compositions and methods using these compounds in the treatment of conditions in which inhibition of PKC and PKD is therapeutically useful.
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公开(公告)号：EP2079736A1
公开(公告)日：2009-07-22
申请号：EP07866124.6
申请日：2007-12-28
发明人： GOFF, Dane , ZHANG, Jing , SYLVAIN, Catherine , SINGH, Rajinder , HOLLAND, Sacha , YU, Jiaxin , HECKRODT, Thilo , DING, Pingyu
IPC分类号： C07D471/04 , C07D495/04 , C07D487/04 , A61K31/4196 , A61P19/00 , C07D249/14 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D417/04 , C07D417/14 , C07D491/04
CPC分类号： A61K31/4196 , A61K31/428 , A61K31/4355 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/497 , A61K31/498 , A61K31/501 , A61K31/502 , A61K31/506 , A61K31/517 , A61K31/519 , A61K31/5377 , A61K31/635 , C07D249/14 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D417/04 , C07D417/14 , C07D471/04 , C07D487/04 , C07D491/04 , C07D491/048 , C07D495/04
摘要： Substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.
摘要翻译： 公开了含有这些化合物的取代的三唑和药物组合物可用于抑制受体蛋白酪氨酸激酶Ax1的活性。 还公开了使用该化合物治疗与Axl活性相关的疾病或病症的方法。
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35.发明公开2,4-PYRIMIDINEDIAMINE COMPOUNDS FOR TREATING OR PREVENTING AUTOIMMUNE DISEASES 有权2.4 PYRIMIDINDIAMINVERBINDUNGEN用于治疗或 预防自身免疫性疾病
公开(公告)号：EP1984357A2
公开(公告)日：2008-10-29
申请号：EP07778258.9
申请日：2007-02-16
发明人： CLOUGH, Jeffrey Wayne , BHAMIDIPATI, Somasekhar , SINGH, Rajinder , MASUDA, Esteban , ZHAO, Haoran
IPC分类号： C07D403/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D498/04 , A61K31/506 , A61P29/00
CPC分类号： C07D417/12 , C07D401/12 , C07D403/12 , C07D413/12 , C07D413/14 , C07D498/04
摘要： The present invention provides 3-hydroxyphenyl-2,4-pyrimidinediamine compounds of formula (I), as well as related compositions and methods for treating a variety of autoimmune diseases.
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公开(公告)号：EP1904457A2
公开(公告)日：2008-04-02
申请号：EP06784727.7
申请日：2006-06-08
发明人： LI, Hui , THOTA, Sambaiah , CARROLL, David , ARGADE, Ankush , TSO, Kin , SRAN, Arvinder , CLOUGH, Jeffrey , KEIM, Holger , BHAMIDIPATI, Somasekhar , TAYLOR, Vanessa , COOPER, Robin , SINGH, Rajinder , WONG, Brian
IPC分类号： C07D239/48 , A61K31/505
CPC分类号： C07D413/12 , A61K31/343 , A61K31/436 , A61K31/505 , A61K31/506 , A61K31/5377 , A61K31/538 , A61K31/5383 , A61K31/541 , A61K31/695 , A61K38/13 , A61K39/3955 , A61K45/06 , C07D239/42 , C07D239/48 , C07D285/22 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D413/14 , C07D417/12 , C07D498/04 , C07F7/0812 , C07F7/10
摘要： The invention encompasses compounds having formula (I-V) and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK3, may be therapeutically useful.
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37.发明公开Methods of assaying for modulators of the inflammatory process using components of the ubiquitin ligation cascade 审中-公开一种用于炎症过程的调节剂，Ubiquitinbindungskaskade的组件的测试方法
公开(公告)号：EP1867731A3
公开(公告)日：2008-03-12
申请号：EP07016552.7
申请日：2003-08-29
发明人： Masuda, Esteban , Wong, Brian
CPC分类号： C12Q1/25 , G01N2333/9015 , G01N2500/04
摘要： The present invention relates to regulation of inflammation. More particularly, the present invention is directed to nucleic acids encoding components of the ubiquitin ligation pathway, e.g., ubiquitin and ubiquitin-like molecules, E1, E2, and E3 proteins and their substrates, which are involved in modulation of the inflammatory process. The invention further relates to methods for identifying and using agents, including small molecule chemical compositions, antibodies, peptides, cyclic peptides, nucleic acids, RNAi, antisense nucleic acids, and ribozymes, that modulate the inflammatory process via modulation of the ubiquitin ligation pathway; as well as to the use of expression profiles and compositions in diagnosis and therapy related to regulation of inflammation and modulation of cytokine signaling involved in inflammation, e.g., for treatment of infection, autoimmune disease and other diseases related to the inflammatory process.
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公开(公告)号：EP1883302A2
公开(公告)日：2008-02-06
申请号：EP06824733.7
申请日：2006-05-02
发明人： WONG, Brian
IPC分类号： A01N57/00 , A61K31/675 , C07D413/00
CPC分类号： A61K31/506 , A61K31/505 , A61K45/06 , A61K2300/00
摘要： The present disclosure provides 2,4-pyrimidinediamine compounds that selectively inhibit JAK kinase as compared to Syk kinase and various methods of using the JAK-selective compounds.
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39.发明公开METHODS OF IDENTIFYING COMPOUNDS THAT MODULATE IL-4 RECEPTOR-MEDIATED IGE SYNTHESIS UTILIZING AN ADENOSINE KINASE 审中-公开一种用于识别THROUGH IGE调节性化合物的IL-4受体介导的合成USING A腺苷激酶
公开(公告)号：EP1578931A4
公开(公告)日：2007-09-12
申请号：EP03764608
申请日：2003-07-15
发明人： MASUDA ESTEBAN , KINSELLA TODD M , WARNER JUSTIN E , KINOSHITA TAISEI , BENNETT MARK K , ANDERSON DAVID C
IPC分类号： A61K31/00 , A61K31/7076 , C12N9/12 , A61K45/00 , A61K38/00 , C07K5/00 , G01N33/566 , G01N33/567
CPC分类号： C12N9/1205 , A61K31/00 , A61K31/7076
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40.发明公开PROCESS FOR THE PREPARATION OF AN OPTICALLY ACITIVE N-CARBAMATE PROTECTED BETA-LACTAM BY OPTICAL RESOLUTION EMPLOYING A CANDIDA ANTARCTICA LIPASE 有权用于生产光学活性的N-氨基甲酸酯PROTECTEDβ-内酰胺类进行旋光拆分USING A南极假丝酵母脂肪酶
公开(公告)号：EP1812581A2
公开(公告)日：2007-08-01
申请号：EP05826088.6
申请日：2005-11-15
发明人： ARGADE, Ankush
CPC分类号： C12P17/10 , C12P13/04 , C12P41/006
摘要： The present disclosure provides enzymatic methods for generating stereoisomerically pure products by resolving a racemic mixture of N-protected β-lactams with a lipase from Candida antarctica with high stereospecificity. The presence of a carbamate protecting group, such as the tert-butoxycarbonyl group protecting group, on the (3-lactam enhances enzyme catalysis and stereoselectivity.
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