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11.发明申请Compounds and Methods for Inhibiting the Interaction of BCL Proteins with Binding Partners 有权抑制BCL蛋白与结合伙伴相互作用的化合物和方法公开(公告)号：US20080114167A1
公开(公告)日：2008-05-15
申请号：US11842581
申请日：2007-08-21
申请人： Alfredo CASTRO , Kristopher DEPEW , Michael GROGAN , Charles JOHANNES , Edward HOLSON , Brian HOPKINS , Gregg KEANEY , Nii KONEY , Tao LIU , David MANN , Marta NEVALAINEN , Stephane PELUSO , Lawrence PEREZ , Daniel SNYDER , Thomas TIBBITTS
发明人： Alfredo CASTRO , Kristopher DEPEW , Michael GROGAN , Charles JOHANNES , Edward HOLSON , Brian HOPKINS , Gregg KEANEY , Nii KONEY , Tao LIU , David MANN , Marta NEVALAINEN , Stephane PELUSO , Lawrence PEREZ , Daniel SNYDER , Thomas TIBBITTS
IPC分类号： C07D261/02 , C07D277/24 , C07D413/10 , C07D413/12
CPC分类号： C07D261/02 , A61K31/42 , A61K31/422 , A61K31/427 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/5377 , A61K45/06 , C07D413/10 , C07D413/12 , C07D417/12
摘要： The invention relates to isoxazolidine containing compounds that bind to bcl proteins and inhibit Bcl function. The compounds may be used for treating and modulating disorders associated with hyperproliferation, such as cancer.
摘要翻译： 本发明涉及与bcl蛋白结合并抑制Bcl功能的含异唑烷的化合物。 该化合物可用于治疗和调节与过度增生相关的疾病，例如癌症。
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公开(公告)号：US20060074030A1
公开(公告)日：2006-04-06
申请号：US11213534
申请日：2005-08-26
申请人： Julian Adams , Alfredo Castro , Michael Foley , Somarajan Janardanan Nair , Marta Nevalainen , James Porter , Martin Tremblay
发明人： Julian Adams , Alfredo Castro , Michael Foley , Somarajan Janardanan Nair , Marta Nevalainen , James Porter , Martin Tremblay
IPC分类号： A61K31/7052 , A61K31/4747 , C07D491/10
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：US07727985B2
公开(公告)日：2010-06-01
申请号：US10821545
申请日：2004-04-09
申请人： Michael E. Hepperle , Julie Fields Liu , Francois Soucy , Yingchun Ye , Robert S. Murray , Raman Prakash , Jeremy D. Little , Alfredo Castro , Hormoz Mazdiyasni , Paul E. Fleming , Dominic Reynolds
发明人： Michael E. Hepperle , Julie Fields Liu , Francois Soucy , Yingchun Ye , Robert S. Murray , Raman Prakash , Jeremy D. Little , Alfredo Castro , Hormoz Mazdiyasni , Paul E. Fleming , Dominic Reynolds
IPC分类号： A61K31/5377 , C07D413/14 , C07D413/02
CPC分类号： C07D265/30 , C07D471/04
摘要： This invention provides beta-carboline compounds of formula I: wherein Ring A is a substituted pyridinyl, pyrimidinyl, morpholinyl, piperidinyl, piperazinyl, pyrrolidinyl, pyranyl, tetrahydrofuranyl, cyclohexyl, cyclopentyl or thiomorpholinyl ring and R1, R2 and R3 are as described in the specification. The compounds are IKK-2 inhibitors that are useful for treating IKK-2-mediated diseases such as inflammatory diseases and cancer.
摘要翻译： 本发明提供式I的β-咔啉化合物：其中环A是取代的吡啶基，嘧啶基，吗啉基，哌啶基，哌嗪基，吡咯烷基，吡喃基，四氢呋喃基，环己基，环戊基或硫代吗啉基，R1，R2和R3如 规范。 这些化合物是可用于治疗IKK-2介导的疾病如炎性疾病和癌症的IKK-2抑制剂。
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公开(公告)号：US20080287420A1
公开(公告)日：2008-11-20
申请号：US12044878
申请日：2008-03-07
IPC分类号： A61K31/4375 , C07D491/147 , A61K31/55 , A61P35/00
CPC分类号： C07D491/20 , C07D215/06
摘要： The present invention relates to steroidal alkaloids useful in the treatment of hedgehog pathway related disorders, particularly cancer.
摘要翻译： 本发明涉及用于治疗刺猬蛋白通路相关疾病，特别是癌症的类固醇生物碱。
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15.发明申请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：US20070161690A1
公开(公告)日：2007-07-12
申请号：US11600332
申请日：2006-11-15
申请人： Alfredo Castro , Edward Holson , Brian Hopkins , Nii Koney , Daniel Snyder , Thomas Tibbitts
发明人： Alfredo Castro , Edward Holson , Brian Hopkins , Nii Koney , Daniel Snyder , Thomas Tibbitts
IPC分类号： A61K31/42 , C07D413/02 , C07D261/02
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：US20060166978A1
公开(公告)日：2006-07-27
申请号：US11390287
申请日：2006-03-28
申请人： Olaf Ritzeler , Alfredo Castro , Louis Grenier , Francois Soucy , Wayne Hancock , Hormoz Mazdiyasni , Vito Palombella , Julian Adams
发明人： Olaf Ritzeler , Alfredo Castro , Louis Grenier , Francois Soucy , Wayne Hancock , Hormoz Mazdiyasni , Vito Palombella , Julian Adams
IPC分类号： A61K31/541 , A61K31/5377 , A61K31/519 , A61K31/496 , A61K31/4745 , C07D487/14 , C07D471/14
CPC分类号： A61K31/437 , C07D471/04 , Y02A50/411
摘要： The subject matter of the present invention is directed to novel substituted beta-carbolines, and specifically compounds of the formula I, which are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in whose course an increased activity of IκB kinase is involved.
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公开(公告)号：US20060166866A1
公开(公告)日：2006-07-27
申请号：US10679478
申请日：2003-10-07
申请人： Steven Adams , Ko-Chung Lin , Wen-Cherng Lee , Alfredo Castro , Craig Zimmerman , Charles Hammond , Yu-Sheng Liao , Julio Cuervo , Juswinder Singh
发明人： Steven Adams , Ko-Chung Lin , Wen-Cherng Lee , Alfredo Castro , Craig Zimmerman , Charles Hammond , Yu-Sheng Liao , Julio Cuervo , Juswinder Singh
CPC分类号： C07D213/75 , A61K38/00 , C07C237/22 , C07C255/19 , C07C271/22 , C07C275/28 , C07C275/42 , C07C275/54 , C07C311/06 , C07C311/21 , C07C317/50 , C07C323/60 , C07C2601/02 , C07C2601/14 , C07D209/42 , C07D213/55 , C07D215/48 , C07D277/48 , C07D317/60 , C07D405/12 , C07K7/06
摘要： The present invention relates to novel compounds that are useful for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. This invention also relates to pharmaceutical formulations comprising these compounds and methods of using them for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. The compounds and pharmaceutical compositions of this invention can be used as therapeutic or prophylactic agents. They are particularly well-suited for treatment of many inflammatory and autoimmune diseases.
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公开(公告)号：US06627637B2
公开(公告)日：2003-09-30
申请号：US09812785
申请日：2001-03-15
申请人： Olaf Ritzeler , Alfredo Castro , Louis Grenier , Francois Soucy , Wayne W. Hancock , Hormoz Mazdiyashi , Vito Palombella , Julian Adams
发明人： Olaf Ritzeler , Alfredo Castro , Louis Grenier , Francois Soucy , Wayne W. Hancock , Hormoz Mazdiyashi , Vito Palombella , Julian Adams
IPC分类号： C07D47102
CPC分类号： A61K31/437 , C07D471/04 , Y02A50/411
摘要： The subject matter of the present invention is directed to novel substituted beta-carbolines, and specifically compounds of the formula I, which are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in whose course an increased activity of I&kgr;B kinase is involved.
摘要翻译： 本发明的主题涉及新的取代的β-咔啉，特别是式I化合物，其适用于生产用于预防和治疗IkappaB激酶活性增加的病症的药物 。
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公开(公告)号：US09012603B2
公开(公告)日：2015-04-21
申请号：US12641844
申请日：2009-12-18
IPC分类号： C07K14/705 , A61K38/00 , C07K14/74 , C07K7/06 , C07K7/08 , C07K14/00 , C07K14/735
CPC分类号： C07K14/70539 , A61K38/00 , C07K7/06 , C07K7/08 , C07K14/00 , C07K14/70535 , G01N2333/70535
摘要： The invention relates to peptides which bind to human FcRn and inhibit binding of the Fc portion of an IgG to an FcRn, thereby modulating serum IgG levels. The disclosed compositions and methods may be used for example, in treating autoimmune diseases and inflammatory disorders. The invention also relates to methods of using and methods of making the peptides of the invention.
摘要翻译： 本发明涉及结合人FcRn并抑制IgG的Fc部分与FcRn的结合的肽，从而调节血清IgG水平。 所公开的组合物和方法可用于例如治疗自身免疫性疾病和炎症性疾病。 本发明还涉及制备本发明的肽的方法和制备方法。
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公开(公告)号：US20120083484A1
公开(公告)日：2012-04-05
申请号：US13250080
申请日：2011-09-30
IPC分类号： A61K31/55 , A61P35/00 , A61P35/02 , C07D491/20
CPC分类号： C07D491/20 , C07D215/06
摘要： The present invention relates to steroidal alkaloids useful in the treatment of hedgehog pathway related disorders, particularly cancer.
摘要翻译： 本发明涉及可用于治疗刺猬蛋白通路相关疾病，特别是癌症的类固醇生物碱。
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