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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: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: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: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:US20120059000A1
公开(公告)日:2012-03-08
申请号:US13112611
申请日:2011-05-20
申请人: Pingda Ren , Yi Liu , Liansheng Li , Katrina Chan , Alfredo C. Castro , Catherine A. Evans
发明人: Pingda Ren , Yi Liu , Liansheng Li , Katrina Chan , Alfredo C. Castro , Catherine A. Evans
IPC分类号: A61K31/5377 , A61K31/496 , A61K31/52 , A61K31/519 , A61P29/00 , C07D487/04 , C07D401/14 , A61P37/02 , A61P35/00 , A61K31/53 , A61K31/506
CPC分类号: C07D473/34 , A61K31/47 , A61K31/52 , C07D401/14 , C07D473/16 , C07D473/32 , C07D487/04 , Y02A50/414 , Y02A50/463
摘要: Chemical compounds that modulate kinase activity, including PI3 kinase activity, and chemical compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including P13 kinase activity, are described herein.
摘要翻译: 本文描述了调节激酶活性的化合物,包括PI3激酶活性和化学化合物,药物组合物以及治疗与激酶活性(包括P13激酶活性)相关的疾病和病症的方法。
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公开(公告)号:US20120088738A1
公开(公告)日:2012-04-12
申请号:US13263324
申请日:2010-04-07
IPC分类号: A61K31/69 , A61P29/00 , A61P37/00 , A61P19/02 , A61P25/22 , A61P25/00 , A61P9/00 , A61P25/06 , C07F5/02 , A61P25/24
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, R4, 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 an FAAH-mediated disorder 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,R4,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:US06376538B1
公开(公告)日:2002-04-23
申请号:US08875321
申请日:1997-09-19
申请人: Steven P. Adams , Ko-Chung Lin , Wen-Cherng Lee , Alfredo C. Castro , Craig N. Zimmerman , Charles E. Hammond , Yu-Sheng Liao , Julio Hernan Cuervo , Juswinder Singh
发明人: Steven P. Adams , Ko-Chung Lin , Wen-Cherng Lee , Alfredo C. Castro , Craig N. Zimmerman , Charles E. Hammond , Yu-Sheng Liao , Julio Hernan Cuervo , Juswinder Singh
IPC分类号: A61K31357
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.
摘要翻译: 本发明涉及可用于抑制和预防细胞粘附和细胞粘附介导的病理学的新型化合物。 本发明还涉及包含这些化合物的药物制剂及其用于抑制和预防细胞粘附和细胞粘附介导的病理学的方法。 本发明的化合物和药物组合物可用作治疗剂或预防剂。 它们特别适用于治疗许多炎性和自身免疫性疾病。
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公开(公告)号:US06875743B1
公开(公告)日:2005-04-05
申请号:US09724139
申请日:2000-11-28
申请人: Ko-Chung Lin , Steven P. Adams , Alfredo C. Castro , Craig N. Zimmerman , Julio Hernan Cuervo , Wen-Cherng Lee , Charles E. Hammond , Mary Beth Carter , Ronald G. Almquist
发明人: Ko-Chung Lin , Steven P. Adams , Alfredo C. Castro , Craig N. Zimmerman , Julio Hernan Cuervo , Wen-Cherng Lee , Charles E. Hammond , Mary Beth Carter , Ronald G. Almquist
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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