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1.发明授权Compounds and methods for inhibiting the interaction of BCL proteins with binding partners 有权抑制BCL蛋白与结合配偶体相互作用的化合物和方法公开(公告)号：US07851637B2
公开(公告)日：2010-12-14
申请号：US11156364
申请日：2005-06-17
申请人： Alfredo C. Castro , Wei Deng , Kristopher M. Depew , Michael A. Foley , Christian C. Fritz , Asimina T. Georges Evangelinos , Michael J. Grogan , Nafeeza Hafeez , Edward B. Holson , Brian T. Hopkins , Nii O. Koney , Tao Liu , David A. Mann , Lisa A. Marcaurelle , Daniel A. Snyder , Dennis J. Underwood , Andrew A. Wylie , Lin-Chen Yu , Linping Zhang
发明人： Alfredo C. Castro , Wei Deng , Kristopher M. Depew , Michael A. Foley , Christian C. Fritz , Asimina T. Georges Evangelinos , Michael J. Grogan , Nafeeza Hafeez , Edward B. Holson , Brian T. Hopkins , Nii O. Koney , Tao Liu , David A. Mann , Lisa A. Marcaurelle , Daniel A. Snyder , Dennis J. Underwood , Andrew A. Wylie , Lin-Chen Yu , Linping Zhang
IPC分类号： C07D261/02 , A61K31/42
CPC分类号： C07D261/02 , C07D261/18 , C07D413/10 , C07D413/12 , C07D417/12 , C07D498/04
摘要： One aspect of the present invention relates to heterocyclic compounds that bind to bcl proteins and inhibit Bcl function. Another aspect of the present invention relates to compositions comprising a heterocyclic compound of the invention. The present invention provides methods for treating and modulating disorders associated with hyperproliferation, such as cancer.
摘要翻译： 本发明的一个方面涉及结合bcl蛋白并抑制Bcl功能的杂环化合物。 本发明的另一方面涉及包含本发明的杂环化合物的组合物。 本发明提供了治疗和调节与过度增生相关的疾病如癌症的方法。
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公开(公告)号：US20110166353A1
公开(公告)日：2011-07-07
申请号：US12969024
申请日：2010-12-15
申请人： Julian Adams , Alfredo C. Castro , Michael A. Foley , Somarajan Nair Janardanan Nair , Marta Nevalainen , James R. Porter , Martin R. Tremblay
发明人： Julian Adams , Alfredo C. Castro , Michael A. Foley , Somarajan Nair Janardanan Nair , Marta Nevalainen , James R. Porter , Martin R. Tremblay
IPC分类号： C07D221/20
CPC分类号： C07D491/04
摘要： The present invention provides compositions and methods for modulating smoothened-dependent pathway activation. The present invention provides analogs of cyclopamine that can be used to counteract the phenotypic effects of unwanted activation of a hedgehog pathway, such as resulting from hedgehog gain-of-function, Ptc loss-of-function or smoothened gain-of-function mutations. The compounds of the present invention are particularly useful in treating cancers.
摘要翻译： 本发明提供用于调节平滑依赖性途径激活的组合物和方法。 本发明提供环巴胺的类似物，其可用于抵消刺猬蛋白途径的不期望的活化的表型效应，例如由刺猬蛋白获得功能，Ptc功能丧失或平滑获得功能突变引起的表型效应。 本发明的化合物特别可用于治疗癌症。
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公开(公告)号：US07875628B2
公开(公告)日：2011-01-25
申请号：US12171208
申请日：2008-07-10
申请人： Julian Adams , Alfredo C. Castro , Michael A. Foley , Somarajannair Janardanannair , Marta Nevalainen , James R. Porter , Martin R. Tremblay
发明人： Julian Adams , Alfredo C. Castro , Michael A. Foley , Somarajannair Janardanannair , Marta Nevalainen , James R. Porter , Martin R. Tremblay
IPC分类号： A61K31/4355 , C12N9/99
CPC分类号： C07D491/04
摘要： The present invention provides compositions and methods for modulating smoothened-dependent pathway activation. The present invention provides analogs of cyclopamine that can be used to counteract the phenotypic effects of unwanted activation of a hedgehog pathway, such as resulting from hedgehog gain-of-function, Ptc loss-of-function or smoothened gain-of-function mutations. The compounds of the present invention are particularly useful in treating cancers.
摘要翻译： 本发明提供用于调节平滑依赖性途径激活的组合物和方法。 本发明提供环巴胺的类似物，其可用于抵消刺猬蛋白途径的不期望的活化的表型效应，例如由刺猬蛋白获得功能，Ptc功能丧失或平滑获得功能突变引起的表型效应。 本发明的化合物特别可用于治疗癌症。
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公开(公告)号：US07407967B2
公开(公告)日：2008-08-05
申请号：US11737035
申请日：2007-04-18
申请人： Julian Adams , Alfredo C. Castro , Michael A. Foley , Somarajan Nair Janardanan Nair , Marta Nevalainen , James R. Porter , Martin R. Tremblay
发明人： Julian Adams , Alfredo C. Castro , Michael A. Foley , Somarajan Nair Janardanan Nair , Marta Nevalainen , James R. Porter , Martin R. Tremblay
IPC分类号： A61K31/4355 , C07D491/048
CPC分类号： C07D491/04
摘要： The present invention provides compositions and methods for modulating smoothened-dependent pathway activation. The present invention provides analogs of cyclopamine that can be used to counteract the phenotypic effects of unwanted activation of a hedgehog pathway, such as resulting from hedgehog gain-of-function, Ptc loss-of-function or smoothened gain-of-function mutations. The compounds of the present invention are particularly useful in treating cancers.
摘要翻译： 本发明提供用于调节平滑依赖性途径激活的组合物和方法。 本发明提供环巴胺的类似物，其可用于抵消刺猬蛋白途径的不期望的活化的表型效应，例如由刺猬蛋白获得功能，Ptc功能丧失或平滑获得功能突变引起的表型效应。 本发明的化合物特别可用于治疗癌症。
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公开(公告)号：US20080269272A1
公开(公告)日：2008-10-30
申请号：US12171208
申请日：2008-07-10
申请人： Julian Adams , Alfredo C. Castro , Michael A. Foley , Somarajan Nair Janardanan Nair , Marta Nevalainen , James R. Porter , Martin R. Tremblay
发明人： Julian Adams , Alfredo C. Castro , Michael A. Foley , Somarajan Nair Janardanan Nair , Marta Nevalainen , James R. Porter , Martin R. Tremblay
IPC分类号： A61K31/438 , C12N5/02 , A61P35/04
CPC分类号： C07D491/04
摘要： The present invention provides compositions and methods for modulating smoothened-dependent pathway activation. The present invention provides analogs of cyclopamine that can be used to counteract the phenotypic effects of unwanted activation of a hedgehog pathway, such as resulting from hedgehog gain-of-function, Ptc loss-of-function or smoothened gain-of-function mutations. The compounds of the present invention are particularly useful in treating cancers.
摘要翻译： 本发明提供用于调节平滑依赖性途径激活的组合物和方法。 本发明提供环巴胺的类似物，其可用于抵消刺猬蛋白途径的不期望的活化的表型效应，例如由刺猬蛋白获得功能，Ptc功能丧失或平滑获得功能突变引起的表型效应。 本发明的化合物特别可用于治疗癌症。
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公开(公告)号：US08236956B2
公开(公告)日：2012-08-07
申请号：US12969024
申请日：2010-12-15
申请人： Julian Adams , Alfredo C. Castro , Michael A. Foley , Somarajan Nair Janardanan Nair , Marta Nevalainen , James R. Porter , Martin R. Tremblay
发明人： Julian Adams , Alfredo C. Castro , Michael A. Foley , Somarajan Nair Janardanan Nair , Marta Nevalainen , James R. Porter , Martin R. Tremblay
IPC分类号： C07D491/048 , C07D491/04
CPC分类号： C07D491/04
摘要： The present invention provides compositions and methods for modulating smoothened-dependent pathway activation. The present invention provides analogs of cyclopamine that can be used to counteract the phenotypic effects of unwanted activation of a hedgehog pathway, such as resulting from hedgehog gain-of-function, Ptc loss-of-function or smoothened gain-of-function mutations. The compounds of the present invention are particularly useful in treating cancers.
摘要翻译： 本发明提供用于调节平滑依赖性途径激活的组合物和方法。 本发明提供环巴胺的类似物，其可用于抵消刺猬蛋白途径的不期望的活化的表型效应，例如由刺猬蛋白获得功能，Ptc功能丧失或平滑获得功能突变引起的表型效应。 本发明的化合物特别可用于治疗癌症。
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公开(公告)号：US07230004B2
公开(公告)日：2007-06-12
申请号：US11213534
申请日：2005-08-26
申请人： Julian Adams , Alfredo C. Castro , Michael A. Foley , Somarajan Nair Janardanan Nair , Marta Nevalainen , James R. Porter , Martin R. Tremblay
发明人： Julian Adams , Alfredo C. Castro , Michael A. Foley , Somarajan Nair Janardanan Nair , Marta Nevalainen , James R. Porter , Martin R. Tremblay
IPC分类号： A61K31/438 , A61K31/4355 , C07D491/10 , C07D491/048
CPC分类号： C07D491/04
摘要： The present invention provides compositions and methods for modulating smoothened-dependent pathway activation. The present invention provides analogs of cyclopamine that can be used to counteract the phenotypic effects of unwanted activation of a hedgehog pathway, such as resulting from hedgehog gain-of-function, Ptc loss-of-function or smoothened gain-of-function mutations. The compounds of the present invention are particularly useful in treating cancers.
摘要翻译： 本发明提供用于调节平滑依赖性途径激活的组合物和方法。 本发明提供环巴胺的类似物，其可用于抵消刺猬蛋白途径的不期望的活化的表型效应，例如由刺猬蛋白获得功能，Ptc功能丧失或平滑获得功能突变引起的表型效应。 本发明的化合物特别可用于治疗癌症。
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公开(公告)号：US07915265B2
公开(公告)日：2011-03-29
申请号：US11354552
申请日：2006-02-15
申请人： Curtis Keith , Alexis Borisy , Grant Zimmermann , Edward Roydon Jost-Price , Palaniyandi Manivasakam , Nicole W. Hurst , Michael A. Foley
发明人： Curtis Keith , Alexis Borisy , Grant Zimmermann , Edward Roydon Jost-Price , Palaniyandi Manivasakam , Nicole W. Hurst , Michael A. Foley
IPC分类号： A61K31/517 , A61K31/56
CPC分类号： A61K45/06 , A61K31/519 , A61K31/56 , A61K31/573 , A61K31/675 , A61K2300/00
摘要： The invention features pharmaceutical compositions that include dipyridamole and a corticosteroid.
摘要翻译： 本发明的特征在于药物组合物，其包括双嘧达莫和皮质类固醇。
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9.发明授权Combinations of drugs (e.g., a benzimidazole and pentamidine) for the treatment of neoplastic disorders 失效用于治疗肿瘤性疾病的药物（例如，苯并咪唑和戊脒）的组合公开(公告)号：US06693125B2
公开(公告)日：2004-02-17
申请号：US09768870
申请日：2001-01-24
IPC分类号： A61K31415
CPC分类号： A61K31/415 , A61K31/135 , A61K2300/00
摘要： The invention features a method for treating a patient having a cancer or other neoplasm, by administering to the patient (i) a benzimidazole or a metabolite or analog thereof; and (ii) pentamidine or a metabolite or analog thereof simultaneously or within 14 days of each other in amounts sufficient to inhibit the growth of the neoplasm.
摘要翻译： 本发明的特征在于通过给予患者（i）苯并咪唑或其代谢物或类似物来治疗患有癌症或其他肿瘤的患者的方法; 和（ii）戊脒或其代谢物或类似物同时或彼此之间的14天内以足以抑制肿瘤生长的量。
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公开(公告)号：US07109377B2
公开(公告)日：2006-09-19
申请号：US10185364
申请日：2002-06-27
IPC分类号： C07C233/00
CPC分类号： C07D307/33 , B01J19/0046 , B01J2219/00317 , B01J2219/00364 , B01J2219/00367 , B01J2219/005 , B01J2219/00511 , B01J2219/00531 , B01J2219/00585 , B01J2219/00596 , B01J2219/00605 , B01J2219/0061 , B01J2219/00612 , B01J2219/0065 , B01J2219/00659 , B01J2219/00702 , C07C227/10 , C07C231/12 , C07C235/40 , C07C237/20 , C07C237/24 , C07C247/14 , C07C2601/14 , C07C2601/16 , C07D261/20 , C07D493/04 , C40B40/00 , C40B60/14 , C40B80/00 , G01N33/50 , Y10S435/975 , C07C229/34
摘要： The present invention provides complex compounds reminiscent of natural products and libraries thereof, as well as methods for their production. The inventive compounds and libraries of compounds are reminiscent of natural products in that they contain one or more stereocenters, and a high density and diversity of functionality. In general, the inventive libraries are synthesized from diversifiable scaffold structures, which are synthesized from readily available or easily synthesizable template structures. In certain embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from a shikimic acid based epoxyol template. In other embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from the pyridine-based template isonicotinamide. The present invention also provides a novel ortho-nitrobenzyl photolinker and a method for its synthesis. Furthermore, the present invention provides methods and kits for determining one or more biological activities of members of the inventive libraries. Additionally, the present invention provides pharmaceutical compositions containing one or more library members.
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