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公开(公告)号:US08546432B2
公开(公告)日:2013-10-01
申请号:US13101978
申请日:2011-05-05
申请人: Adilah Bahadoor , Alfredo C. Castro , Lawrence K. Chan , Gregg F. Keaney , Marta Nevalainen , Vesa Nevalainen , Stephane Peluso , Daniel A. Snyder , Thomas T. Tibbitts
发明人: Adilah Bahadoor , Alfredo C. Castro , Lawrence K. Chan , Gregg F. Keaney , Marta Nevalainen , Vesa Nevalainen , Stephane Peluso , Daniel A. Snyder , Thomas T. Tibbitts
IPC分类号: A61K31/41 , C07D249/00
CPC分类号: A61K31/41 , A61K31/4184 , A61K31/428 , A61K31/4439 , A61K31/454 , A61K31/4709 , A61K31/497 , A61K31/5377 , A61K31/5415 , A61K31/55 , A61K31/7056 , A61K38/21 , A61K38/212 , A61K38/217 , A61K45/06 , C07D257/04 , C07D295/185 , C07D295/205 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12 , C07D405/12 , C07D407/12 , C07D413/06 , C07D413/12 , C07D417/04 , C07D417/06 , Y02A50/385 , Y02A50/387 , Y02A50/393 , Y02A50/397 , Y02A50/409 , Y02A50/411 , Y02A50/414 , Y02A50/421 , Y02A50/422 , Y02A50/423 , Y02A50/478 , Y02A50/491 , Y02A50/492
摘要: Provided herein are tetrazolone FASN inhibitors of the formula (I): or a pharmaceutically acceptable form thereof; wherein the variables RA, RB and RC are defined herein. Also provided herein are pharmaceutical compositions of the compounds provided herein as well as methods of their use for the treatment of various disorders such as hyperproliferative disorders, inflammatory disorders, obesity-related disorders and microbial infections.
摘要翻译: 本文提供式(I)的四唑酮FASN抑制剂:或其药学上可接受的形式; 其中变量RA,RB和RC在本文中定义。 本文还提供本文提供的化合物的药物组合物及其用于治疗各种疾病如过度增殖性疾病,炎症性疾病,肥胖相关病症和微生物感染的方法。
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公开(公告)号:US20130108582A1
公开(公告)日:2013-05-02
申请号:US13475352
申请日:2012-05-18
申请人: Alfredo C. Castro , Michael J. Grogan , William Matsui , Karen J. McGovern , Martin R. Tremblay
发明人: Alfredo C. Castro , Michael J. Grogan , William Matsui , Karen J. McGovern , Martin R. Tremblay
IPC分类号: C07D491/107 , A61K31/56 , A61K38/21 , A61K31/704 , A61K31/573 , A61K31/196 , A61K31/519 , A61K31/4745 , A61K31/69 , A61K31/198 , A61K31/17 , A61K31/664 , A61K31/454 , A61K31/7068 , A61K31/7076 , A61K31/4355
CPC分类号: A61K31/4355 , A61K9/0014 , A61K31/17 , A61K31/196 , A61K31/198 , A61K31/454 , A61K31/4745 , A61K31/519 , A61K31/56 , A61K31/573 , A61K31/58 , A61K31/664 , A61K31/69 , A61K31/704 , A61K31/7068 , A61K31/7076 , A61K38/21 , A61K45/06 , A61N5/10 , C07D307/94 , C07D471/04 , C07D471/10 , C07D491/04 , C07D491/048 , C07D491/10 , C07D491/107 , C07J69/00
摘要: The invention provides methods for treating various conditions using derivatives of cyclopamine having the following formula:
摘要翻译: 本发明提供使用具有下式的环巴胺衍生物治疗各种病症的方法:
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公开(公告)号:US08426436B2
公开(公告)日:2013-04-23
申请号:US13168590
申请日:2011-06-24
IPC分类号: A61K31/4355 , C07D491/20
CPC分类号: C07D491/14 , C07D513/14
摘要: The present invention relates to steroidal alkaloids that can be used 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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公开(公告)号:US08293760B2
公开(公告)日:2012-10-23
申请号:US13102395
申请日:2011-05-06
IPC分类号: A61K31/4355 , 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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45.Compounds and methods for inhibiting the interaction of BCL proteins with binding partners 有权
标题翻译: 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:US08178690B2
公开(公告)日:2012-05-15
申请号:US13089530
申请日:2011-04-19
申请人: Alfredo C. Castro , Kristopher M. Depew , Michael J. Grogan , Charles W. Johannes , Edward B. Holson , Brian T. Hopkins , Gregg F. Keaney , Nii O. Koney , Tao Liu , David A. Mann , Marta Nevalainen , Stephane Peluso , Lawrence Blas Perez , Daniel A. Snyder , Thomas T. Tibbitts
发明人: Alfredo C. Castro , Kristopher M. Depew , Michael J. Grogan , Charles W. Johannes , Edward B. Holson , Brian T. Hopkins , Gregg F. Keaney , Nii O. Koney , Tao Liu , David A. Mann , Marta Nevalainen , Stephane Peluso , Lawrence Blas Perez , Daniel A. Snyder , Thomas T. Tibbitts
IPC分类号: C07D261/02 , A61K31/42
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:US20120065218A1
公开(公告)日:2012-03-15
申请号:US13168590
申请日:2011-06-24
IPC分类号: A61K31/4355 , A61P35/00 , A61P35/02 , C07D491/20
CPC分类号: C07D491/14 , C07D513/14
摘要: The present invention relates to steroidal alkaloids that can be used 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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47.Compounds and Methods for Inhibiting the Interaction of BCL Proteins with Binding Partners 有权
标题翻译: 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:US20110213145A1
公开(公告)日:2011-09-01
申请号:US13089530
申请日:2011-04-19
申请人: Alfredo C. Castro , Kristopher M. Depew , Michael J. Grogan , Charles W. Johannes , Edward B. Holson , Brian T. Hopkins , Gregg F. Keaney , Nii O. Koney , Tao Liu , David A. Mann , Marta Nevalainen , Stephane Peluso , Lawrence B. Perez , Daniel A. Snyder , Thomas T. Tibbitts
发明人: Alfredo C. Castro , Kristopher M. Depew , Michael J. Grogan , Charles W. Johannes , Edward B. Holson , Brian T. Hopkins , Gregg F. Keaney , Nii O. Koney , Tao Liu , David A. Mann , Marta Nevalainen , Stephane Peluso , Lawrence B. Perez , Daniel A. Snyder , Thomas T. Tibbitts
IPC分类号: C07D413/12 , C07D413/10 , C07D261/02 , C07D498/04
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: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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49.Compounds and Methods for Inhibiting the Interaction of BCL Proteins with Binding Partners 失效
标题翻译: 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:US20110160259A1
公开(公告)日:2011-06-30
申请号:US12956969
申请日:2010-11-30
申请人: Alfredo C. Castro , Edward B. Holson , Brian T. Hopkins , Nii O. Koney , Daniel A. Snyder , Thomas T. Tibbitts
发明人: Alfredo C. Castro , Edward B. Holson , Brian T. Hopkins , Nii O. Koney , Daniel A. Snyder , Thomas T. Tibbitts
IPC分类号: A61K31/42 , A61K31/422 , A61P35/00 , A61P35/02 , A61P35/04
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: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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