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21. 发明申请

WO2011094708A2 SMALL MOLECULES FOR THE MODULATION OF MCL-1 AND METHODS OF MODULATIING CELL DEATH, CELL DIVISION, CELL DIFFERENTIATION AND METHODS OF TREATING DISORDERS 审中-公开
标题翻译：用于调节MCL-1的小分子和调节细胞死亡，细胞分裂，细胞分化和治疗疾病的方法的方法
公开(公告)号：WO2011094708A2
公开(公告)日：2011-08-04
申请号：PCT/US2011/023220
申请日：2011-01-31
申请人： DANA-FARBER CANCER INSTITUTE, INC , WALENSKY, Loren, D. , STEWART, Michelle, L. , COHEN, Nicole
发明人： WALENSKY, Loren, D. , STEWART, Michelle, L. , COHEN, Nicole
IPC分类号： C07C251/20 , C07D215/16 , C07D249/08 , A61K31/41 , A61P35/00
CPC分类号： C07D513/04 , C07C251/20 , C07C251/84 , C07C311/20 , C07C335/16 , C07C337/08 , C07C2602/10 , C07D239/60 , C07D249/12 , C07D277/34 , C07D279/06 , C07D307/54 , C07D327/04 , C07D401/12 , C07D403/04 , C07D403/06 , C07D403/08 , C07D405/12 , C07D405/14 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/06 , C07D413/14 , C07D417/04 , C07D417/14
摘要： This invention relates to compounds which selectively bind to the survival protein MCL-1 with high affinity and selectivity, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for modulating MCL-1 activity and for treating hyperproliferative disorders, angiogenesis disorders, cell cycle regulation disorders, autophagy regulation disorders, inflammatory disorders, and/or infectious disorders and/or for enhancing cellular engraftment and/or wound repair, as a sole agent or in combination with other active ingredients.
摘要翻译：本发明涉及以高亲和性和选择性选择性结合生存蛋白MCL-1的化合物，含有这些化合物的药物组合物以及用于调节MCL-1活性和用于治疗过度增殖性疾病，血管生成障碍，细胞的这些化合物或组合物的用途循环调节障碍，自噬调节障碍，炎性疾病和/或感染性疾病和/或用于增强细胞移植和/或伤口修复，作为唯一的试剂或与其它活性成分组合。

22. 发明申请

WO2010042225A3 CHEMICAL MODULATORS OF PRO-APOPTOTIC BAX AND BCL-2 POLYPEPTIDES 审中-公开
标题翻译：化学调节剂的PRO-APOPTOTIC BAX和BCL-2多肽
公开(公告)号：WO2010042225A3
公开(公告)日：2010-10-07
申请号：PCT/US2009005568
申请日：2009-10-09
申请人： DANA FARBER CANCER INST INC , WALENSKY LOREN D , GAVATHIOTIS EVRIPIDIS
发明人： WALENSKY LOREN D , GAVATHIOTIS EVRIPIDIS
IPC分类号： G01N33/68 , A61K38/17 , A61P35/00 , C07K14/435
CPC分类号： G06F19/12 , A61K38/00 , C07K14/4747 , C40B30/02
摘要： The invention provides a method for identifying a compound which modulates the activity of a BCL-2 family polypeptide, the method comprising: a) contacting said BCL-2 family polypeptide with a compound under conditions suitable for modulation of the activity of said BCL-2 family polypeptide; and b) detecting modulation of the activity of said BCL-2 family polypeptide by the compound, wherein the compound interacts with a binding site comprising one or more of an al helix, a2 helix, a loop between al-a2, a.6 helix, and select residues of a4, a.5, and a.8 helices in said BCL-2 family polypeptide; wherein the interaction of the compound with the binding site occurs at a horizontal hydrophobic groove with or without a perimeter of charged and hydrophilic residues, a superior juxta-loop, an inferior juxta-loop, or combination thereof.
摘要翻译：本发明提供了鉴定调节BCL-2家族多肽活性的化合物的方法，所述方法包括：a）在适于调节所述BCL-2活性的条件下使所述BCL-2家族多肽与化合物接触家族多肽; 和b）检测所述化合物对所述BCL-2家族多肽的活性的调节，其中所述化合物与包含α1螺旋，α2螺旋，α1-α2，α6螺旋之间的环中的一个或多个的结合位点相互作用，并选择所述BCL-2家族多肽中a4，a.5和a.8螺旋的残基; 其中所述化合物与所述结合位点的相互作用发生在具有或不具有带电和亲水残基的周界，上级并置环，下级并置环或其组合的水平疏水性凹槽处。

23. 发明申请

WO2009042237A2 METHODS AND COMPOSITIONS FOR MODULATING BCL-2 FAMILY POLYPEPTIDES 审中-公开
标题翻译：调节BCL-2家族多肽的方法和组合物
公开(公告)号：WO2009042237A2
公开(公告)日：2009-04-02
申请号：PCT/US2008/011500
申请日：2008-09-26
申请人： DANA FARBER CANCER INSTITUTE , NATIONAL INSTITUTES OF HEALTH , WALENSKY, Loren, D. , TJANDRA, Nico , GAVATHIOTIS, Evripidis , SUZUKI, Motoshi , BIRD, Gregory, H.
发明人： WALENSKY, Loren, D. , TJANDRA, Nico , GAVATHIOTIS, Evripidis , SUZUKI, Motoshi , BIRD, Gregory, H.
IPC分类号： G01N33/574
CPC分类号： G01N33/5079 , C07K14/4747 , G01N33/5011 , G01N33/5035 , G01N2510/00
摘要： The present invention is based, at least in part, on the identification of a novel active site on BCL-2 family polypeptide such as BAX, which when bound by a compound, modifies the activity of the BCL-2 family polypeptide.
摘要翻译：本发明至少部分基于BCL-2家族多肽如BAX上的新活性位点的鉴定，其在被化合物结合时修饰BCL-2的活性 -2家族多肽。

24. 发明申请

WO2008137633A3 METHODS OF MODULATING CELLULAR HOMEOSTATIC PATHWAYS AND CELLULAR SURVIVAL 审中-公开
公开(公告)号：WO2008137633A3
公开(公告)日：2008-11-13
申请号：PCT/US2008/062345
申请日：2008-05-02
申请人： DANA-FARBER CANCER INSTITUTE, INC. , KORSMEYER, Susan, R. , DANIAL, Nika, N. , WALENSKY, Loren, D. , BIRD, Gregory
发明人： DANIAL, Nika, N. , WALENSKY, Loren, D. , BIRD, Gregory
IPC分类号： A61K38/17 , A61P3/10
摘要： The invention provides composition and therapeutic, methods for modulating homeostatic pathways that are useful in treatment, and prevention of diabetes, diabetes associated disorders, metabolic disorders and cancer.

25. 发明申请

WO2008095063A1 STABILIZED P53 PEPTIDES AND USES THEREOF 审中-公开
标题翻译：稳定的P53肽及其用途
公开(公告)号：WO2008095063A1
公开(公告)日：2008-08-07
申请号：PCT/US2008/052580
申请日：2008-01-31
申请人： DANA-FARBER CANCER INSTITUTE, INC. , HARVARD UNIVERSITY , BERNAL, Federico , WALENSKY, Loren D. , VERDINE, Gregory L.
发明人： BERNAL, Federico , WALENSKY, Loren D. , VERDINE, Gregory L.
IPC分类号： C07K7/54
CPC分类号： C07K14/4746 , A61K38/00 , C07K1/113
摘要： Cross-linked peptides related to human p53 and bind to HMD2 or a family member of HDM2 useful for promoting apoptosis, e.g., in the treatment of and identifying therapeutic agents that binding to HMD2 or a family member of HDM2.
摘要翻译：与人p53相关并与HMD2或HDM2家族成员相关的交联肽可用于促进凋亡，例如用于治疗和鉴定与HMD2或HDM2家族成员结合的治疗剂。

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