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公开(公告)号：US09149465B2
公开(公告)日：2015-10-06
申请号：US12782650
申请日：2010-05-18
申请人： Mark L. Behnke , Alfredo C. Castro , Lawrence K. Chan , Catherine A. Evans , Louis Grenier , Michael J. Grogan , Yves Leblanc , Tao Liu , Stephane Peluso , Daniel A. Snyder , Thomas T. Tibbitts
发明人： Mark L. Behnke , Alfredo C. Castro , Lawrence K. Chan , Catherine A. Evans , Louis Grenier , Michael J. Grogan , Yves Leblanc , Tao Liu , Stephane Peluso , Daniel A. Snyder , Thomas T. Tibbitts
IPC分类号： C07D261/04 , A61K31/5377 , A61K31/42 , A61K31/4245 , A61K31/4439 , A61K31/4709 , A61K31/501 , A61K31/506 , C07D413/04 , C07D413/12 , C07D413/14 , C07D471/04
CPC分类号： A61K31/42 , A61K31/4245 , A61K31/4439 , A61K31/4709 , A61K31/501 , A61K31/506 , A61K31/5377 , C07D261/04 , C07D413/04 , C07D413/12 , C07D413/14 , C07D471/04
摘要： The present invention provides isoxazoline FAAH inhibitors of the formula (I): or pharmaceutically acceptable forms thereof, wherein each of G, Ra, Rb, Rc, and Rd are as defined herein. The present invention also provides pharmaceutical compositions comprising a compound of formula (I), or a pharmaceutically acceptable form thereof, and a pharmaceutically acceptable excipient.The present invention also provides methods for treating an FAAH-mediated condition comprising administering a therapeutically effective amount of a compound of formula (I), or pharmaceutically acceptable form thereof, to a subject in need thereof.
摘要翻译： 本发明提供式（I）的异恶唑啉FAAH抑制剂或其药学上可接受的形式，其中G，Ra，Rb，Rc和Rd各自如本文所定义。 本发明还提供包含式（I）化合物或其药学上可接受的形式的药物组合物和药学上可接受的赋形剂。 本发明还提供了治疗FAAH介导的病症的方法，包括向有需要的受试者施用治疗有效量的式（I）化合物或其药学上可接受的形式。
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公开(公告)号：US09056877B2
公开(公告)日：2015-06-16
申请号：US13552473
申请日：2012-07-18
申请人： Alfredo C. Castro , Catherine A. Evans , Andre Lescarbeau , Tao Liu , Daniel A. Snyder , Martin R. Tremblay , Pingda Ren , Yi Liu , Liansheng Li , Katrina Chan
发明人： Alfredo C. Castro , Catherine A. Evans , Andre Lescarbeau , Tao Liu , Daniel A. Snyder , Martin R. Tremblay , Pingda Ren , Yi Liu , Liansheng Li , Katrina Chan
IPC分类号： C07D277/20 , C07D513/04
CPC分类号： C07D513/04 , A61K31/519 , C07D519/00
摘要： Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.
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公开(公告)号：US08765735B2
公开(公告)日：2014-07-01
申请号：US12782658
申请日：2010-05-18
申请人： Mark L. Behnke , Alfredo C. Castro , Lawrence K. Chan , Catherine A. Evans , Louis Grenier , Michael J. Grogan , Yves Leblanc , Tao Liu , Stephane Peluso , Daniel A. Snyder , Thomas T. Tibbitts
发明人： Mark L. Behnke , Alfredo C. Castro , Lawrence K. Chan , Catherine A. Evans , Louis Grenier , Michael J. Grogan , Yves Leblanc , Tao Liu , Stephane Peluso , Daniel A. Snyder , Thomas T. Tibbitts
IPC分类号： A01N43/00 , A61K31/55 , A01N43/42 , A61K31/44 , A01N43/80 , A61K31/42 , C07D261/02 , C07D401/00
CPC分类号： C07D498/10 , A61K31/42 , A61K31/438 , A61K31/55 , C07D261/20 , C07D498/04
摘要： The present invention provides isoxazoline FAAH inhibitors of the formula (I): or pharmaceutically acceptable forms thereof, wherein each of G, Ra, Rb, Rc, and Rd are as defined herein. The present invention also provides pharmaceutical compositions comprising a compound of formula (I), or a pharmaceutically acceptable form thereof, and a pharmaceutically acceptable excipient.The present invention also provides methods for treating an FAAH-mediated condition comprising administering a therapeutically effective amount of a compound of formula (I), or pharmaceutically acceptable form thereof, to a subject in need thereof.
摘要翻译： 本发明提供式（I）的异恶唑啉FAAH抑制剂或其药学上可接受的形式，其中G，Ra，Rb，Rc和Rd各自如本文所定义。 本发明还提供包含式（I）化合物或其药学上可接受的形式的药物组合物和药学上可接受的赋形剂。 本发明还提供了治疗FAAH介导的病症的方法，包括向有需要的受试者施用治疗有效量的式（I）化合物或其药学上可接受的形式。
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4.发明授权Compounds and methods for inhibiting the interaction of BCL proteins with binding partners 失效抑制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：US08609706B2
公开(公告)日：2013-12-17
申请号：US13472136
申请日：2012-05-15
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： A61K31/42 , C07D261/02
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：US08450350B2
公开(公告)日：2013-05-28
申请号：US13101970
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 , Thomas T. Tibbitts
发明人： Adilah Bahadoor , Alfredo C. Castro , Lawrence K. Chan , Gregg F. Keaney , Marta Nevalainen , Vesa Nevalainen , Stephane Peluso , Thomas T. Tibbitts
IPC分类号： A61K31/41 , A61K31/4192 , C07D249/00 , C07D249/06
CPC分类号： A61K31/4192 , A61K31/454 , A61K31/4709 , A61K45/06 , C07D249/04 , C07D249/06 , C07D249/18 , C07D401/06 , C07D401/12 , C07D471/04
摘要： Provided herein are triazole FASN inhibitors of the formula (I): or a pharmaceutically acceptable form thereof; wherein the variables RA, X, 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）的三唑FASN抑制剂：或其药学上可接受的形式; 其中变量RA，X，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：US20130029984A1
公开(公告)日：2013-01-31
申请号：US13552473
申请日：2012-07-18
申请人： Alfredo C. Castro , Catherine A. Evans , Andre Lescarbeau , Tao Liu , Daniel A. Snyder , Martin R. Tremblay , Pingda Ren , Yi Liu , Liansheng Li , Katrina Chan
发明人： Alfredo C. Castro , Catherine A. Evans , Andre Lescarbeau , Tao Liu , Daniel A. Snyder , Martin R. Tremblay , Pingda Ren , Yi Liu , Liansheng Li , Katrina Chan
IPC分类号： A61K31/519 , A61K31/5377 , A61K31/4725 , A61P37/06 , C07D495/04 , A61P35/00 , A61P29/00 , C07D513/04 , A61K31/506
CPC分类号： C07D513/04 , A61K31/519 , C07D519/00
摘要： Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.
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7.发明授权Compounds and methods for inhibiting the interaction of BCL proteins with binding partners 失效抑制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：US08304428B2
公开(公告)日：2012-11-06
申请号：US12753319
申请日：2010-04-02
申请人： Alfredo C. Castro , Michael J. Grogan , Edward B. Holson , Brian T. Hopkins , Nii O. Koney , Stephane Peluso , Daniel A. Snyder
发明人： Alfredo C. Castro , Michael J. Grogan , Edward B. Holson , Brian T. Hopkins , Nii O. Koney , Stephane Peluso , Daniel A. Snyder
IPC分类号： A61K31/445
CPC分类号： C07D207/16 , C07D207/08 , C07D207/12 , C07D207/14 , C07D211/60 , C07D233/32 , C07D265/30 , C07D277/04 , C07D277/06 , C07D295/04
摘要： The present invention relates to heterocyclic compounds that bind to Bcl proteins and inhibit Bcl function, compositions comprising such compounds, and methods for treating and modulating disorders associated with hyperproliferation, such as cancer.
摘要翻译： 本发明涉及结合Bcl蛋白并抑制Bcl功能的杂环化合物，包含这些化合物的组合物，以及用于治疗和调节与过度增殖相关的疾病如癌症的方法。
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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：US20120094957A1
公开(公告)日：2012-04-19
申请号：US13263328
申请日：2010-04-07
IPC分类号： A61K31/69 , A61P29/00 , A61P25/24 , A61P25/22 , A61P25/04 , A61P9/00 , A61P25/00 , A61P19/02 , A61P1/00 , A61P25/06 , C07F5/02 , A61P27/06
CPC分类号： C07F5/025
摘要： Provided herein are compounds of formula (I) or pharmaceutically acceptable salts, solvates or prodrugs thereof, or mixtures thereof, wherein Z1, Z2, X1, X2, X3, R1, R2 R3, m and n are defined herein. Also provided are pharmaceutically acceptable compositions that include a compound of formula I and a pharmaceutically acceptable excipient. Also provided are methods for treating FAAH-mediated disorders comprising administering to a subject in need thereof a therapeutically effective amount of a compound or composition of the present invention.
摘要翻译： 本文提供了式（I）化合物或其药学上可接受的盐，溶剂合物或前药或其混合物，其中Z1，Z2，X1，X2，X3，R1，R2，R3，m和n如本文所定义。 还提供了药学上可接受的组合物，其包括式I化合物和药学上可接受的赋形剂。 还提供了用于治疗FAAH介导的病症的方法，包括向有需要的受试者施用治疗有效量的本发明的化合物或组合物。
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公开(公告)号：US20120077834A1
公开(公告)日：2012-03-29
申请号：US13191545
申请日：2011-07-27
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： A61K31/4355 , A61P35/02 , A61P35/00
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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