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61.发明授权公开(公告)号：US07842815B2
公开(公告)日：2010-11-30
申请号：US11600332
申请日：2006-11-15
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： 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.
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公开(公告)号：US20120122838A1
公开(公告)日：2012-05-17
申请号：US13293828
申请日：2011-11-10
申请人： Pingda Ren , Yi Liu , Liansheng Li , Katrina Chan , Troy Edward Wilson , Alfredo C. Castro , Catherine A. Evans , Daniel A. Snyder
发明人： Pingda Ren , Yi Liu , Liansheng Li , Katrina Chan , Troy Edward Wilson , Alfredo C. Castro , Catherine A. Evans , Daniel A. Snyder
IPC分类号： A61K31/52 , C07D473/34 , A61K31/5377 , C07D498/08 , A61K31/5386 , C07D513/04 , C07D413/14 , C07D471/04 , A61K31/519 , C07D487/04 , A61K31/5025 , A61P29/00 , A61P37/06 , A61K31/553 , C12N9/99
CPC分类号： C07D473/34 , C07D401/12 , C07D413/14 , C07D471/04 , C07D487/04 , C07D513/04 , 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.
摘要翻译： 本文描述了调节激酶活性（包括PI3激酶活性）的化合物和药物组合物，以及化合物，药物组合物和治疗与激酶活性（包括PI3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：US08604032B2
公开(公告)日：2013-12-10
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： A01N43/64 , A01N43/90 , A01N43/54 , A61K31/53 , A61K31/52 , A61K31/519 , A61K31/505 , C07D487/00 , C07D239/00 , C07D239/70 , C07D471/00 , C07D473/00 , C07D401/00 , C07D403/00 , C07D405/00 , C07D409/00 , C07D411/00 , C07D413/00 , C07D417/00 , C07D419/00 , C07D215/00
CPC分类号： C07D473/34 , A61K31/47 , A61K31/52 , C07D401/14 , C07D473/16 , C07D473/32 , C07D487/04 , Y02A50/414 , Y02A50/463
摘要： Provided herein are compounds of formula (I), pharmaceutical compositions comprising the compounds, and methods of use thereof The compounds provided herein modulate kinase activity, including PI3 kinase activity, and are useful for treating diseases and conditions associated with kinase activity, including diseases and conditions associated with PI3 kinase activity.
摘要翻译： 本文提供了式（I）化合物，包含该化合物的药物组合物及其使用方法本文提供的化合物调节激酶活性，包括PI3激酶活性，并且可用于治疗与激酶活性相关的疾病和病症，包括疾病和 与PI3激酶活性相关的病症。
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66.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：US08461191B2
公开(公告)日：2013-06-11
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： A61K31/422 , 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：US20110274655A1
公开(公告)日：2011-11-10
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 , C07D417/10 , C07D403/10 , C07D401/06 , C07D401/12 , C07D413/12 , C07D417/06 , A61K31/433 , A61K31/454 , A61K31/4439 , A61K31/496 , A61K31/5377 , A61K31/5415 , A61K31/55 , A61K38/21 , A61K31/7056 , A61P33/02 , A61P33/06 , A61P33/00 , A61P31/10 , A61P31/04 , A61P31/12 , A61P31/16 , A61P29/00 , A61P3/04 , A61P3/10 , A61P1/16 , C07D257/04
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：US20110274654A1
公开(公告)日：2011-11-10
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： A61K38/21 , C07D249/04 , A61K31/4709 , A61K31/454 , A61K31/4192 , A61K31/7056 , A61P31/04 , A61P31/10 , A61P31/06 , A61P33/00 , A61P33/02 , A61P33/12 , A61P33/10 , A61P33/04 , A61P33/06 , C07D401/06
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：US07001921B1
公开(公告)日：2006-02-21
申请号：US10625626
申请日：2003-07-24
申请人： Steven P. Adams , Ko-Chung Lin , Wen-Cherng Lee , Alfredo C. Castro , Craig N. Zimmerman , Charles E. Hammond , Yu-Sheng Liao
发明人： Steven P. Adams , Ko-Chung Lin , Wen-Cherng Lee , Alfredo C. Castro , Craig N. Zimmerman , Charles E. Hammond , Yu-Sheng Liao
IPC分类号： A61K31/195 , C07C233/00
CPC分类号： A61K31/195
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：US06596687B1
公开(公告)日：2003-07-22
申请号：US09482296
申请日：2000-01-13
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
IPC分类号： A61K3803
CPC分类号： C07K5/0821 , A61K38/00 , C07K5/0202 , C07K5/021 , C07K5/06034 , C07K5/06113 , C07K5/0806 , C07K5/0808 , C07K5/0815 , C07K5/0819 , C07K5/101 , C07K5/1013 , C07K5/1016 , C07K5/1024 , C07K14/78 , Y10S514/825 , Y10S514/826 , Y10S514/863 , Y10S514/866 , Y10S514/885 , Y10S514/903 , Y10S530/868
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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