专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明申请

WO2008014381A3 MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY, CRYSTALLINE FORMS AND PROCESS 审中-公开
公开(公告)号：WO2008014381A3
公开(公告)日：2008-01-31
申请号：PCT/US2007/074438
申请日：2007-07-26
申请人： BRISTOL-MYERS SQUIBB COMPANY , YANG, Michael, G. , CHERNEY, Robert, J. , EASTGATE, Martin, G. , MUSLEHIDDINOGLU, Jale , PRASAD, Siva, Josyula , XIAO, Zili
发明人： YANG, Michael, G. , CHERNEY, Robert, J. , EASTGATE, Martin, G. , MUSLEHIDDINOGLU, Jale , PRASAD, Siva, Josyula , XIAO, Zili
IPC分类号： C07D403/12 , C07D207/273 , A61K31/4025 , C07D317/72
摘要： The present invention provides a novel antagonist or partial agonists/antagonists of MCP-1 receptor activity: N-((1R,2S,5R)-5-(isopropyl(methyl)amino)-2-((S)-2-oxo-3-(6-(trifluoromethyl)quinazolin-4-ylamino)pyrrolidin-1-yl)cyclohexyl)acetamide, or a pharmaceutically acceptable salt, solvate or prodrug, thereof, having an unexpected combination of desirable pharmacological characteristics. Crystalline forms of the present invention are also provided. Pharmaceutical compositions containing the same and methods of using the same as agents for the treatment of inflammatory diseases, allergic, autoimmune, metabolic, cancer and/or cardiovascular diseases is also an objective of this invention. The present disclosure also provides a process for preparing compounds of Formula (I), including N-((1R,2S,5R)-5-(isopropyl(methyl)amino)-2-((S)-2-oxo-3-(6-(trifluoromethyl)quinazolin-4-ylamino)pyrrolidin-1-yl)cyclohexyl)acetamide: wherein R 1 , R 8 , R 9 , R 10 , and structure (a) are as described herein. Compounds that are useful intermediates of the process are also provided herein.

2. 发明申请

WO2008014381A2 MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY, CRYSTALLINE FORMS AND PROCESS 审中-公开
标题翻译：化合物受体活性的调节剂，结晶形式和过程
公开(公告)号：WO2008014381A2
公开(公告)日：2008-01-31
申请号：PCT/US2007074438
申请日：2007-07-26
申请人： SQUIBB BRISTOL MYERS CO , YANG MICHAEL G , CHERNEY ROBERT J , EASTGATE MARTIN G , MUSLEHIDDINOGLU JALE , PRASAD SIVA JOSYULA , XIAO ZILI
发明人： YANG MICHAEL G , CHERNEY ROBERT J , EASTGATE MARTIN G , MUSLEHIDDINOGLU JALE , PRASAD SIVA JOSYULA , XIAO ZILI
IPC分类号： C07D207/273 , A61K31/4025 , C07D403/12
CPC分类号： C07D403/12 , C07D207/273 , C07D317/72 , Y02P20/55
摘要： The present invention provides a novel antagonist or partial agonists/antagonists of MCP-1 receptor activity: N-((1R,2S,5R)-5-(isopropyl(methyl)amino)-2-((S)-2-oxo-3-(6-(trifluoromethyl)quinazolin-4-ylamino)pyrrolidin-1-yl)cyclohexyl)acetamide, or a pharmaceutically acceptable salt, solvate or prodrug, thereof, having an unexpected combination of desirable pharmacological characteristics. Crystalline forms of the present invention are also provided. Pharmaceutical compositions containing the same and methods of using the same as agents for the treatment of inflammatory diseases, allergic, autoimmune, metabolic, cancer and/or cardiovascular diseases is also an objective of this invention. The present disclosure also provides a process for preparing compounds of Formula (I), including N-((1R,2S,5R)-5-(isopropyl(methyl)amino)-2-((S)-2-oxo-3-(6-(trifluoromethyl)quinazolin-4-ylamino)pyrrolidin-1-yl)cyclohexyl)acetamide: wherein R 1 , R 8 , R 9 , R 10 , and structure (a) are as described herein. Compounds that are useful intermediates of the process are also provided herein.
摘要翻译：本发明提供MCP-1受体活性的新型拮抗剂或部分激动剂/拮抗剂：N - （（1R，2S，5R）-5-（异丙基（甲基）氨基）-2 - （（S） -3-（6-（三氟甲基）喹唑啉-4-基氨基）吡咯烷-1-基）环己基）乙酰胺或其药学上可接受的盐，溶剂合物或前药，具有期望的药理学特征的意想不到的组合。还提供了本发明的结晶形式。含有该组合物的药物组合物以及使用其作为治疗炎性疾病，过敏性，自身免疫性，代谢性，癌症和/或心血管疾病的药剂的方法也是本发明的目的。本公开还提供制备式（I）化合物的方法，包括N - （（1R，2S，5R）-5-（异丙基（甲基）氨基）-2 - （（S）-2-氧代-3 - （6-（三氟甲基）喹唑啉-4-基氨基）吡咯烷-1-基）环己基）乙酰胺其中R 1，R 8，R 9， / SUP>，R 10和结构（a）如本文所述。本文还提供了该方法有用中间体的化合物。

3. 发明申请

WO2007124332A1 PROCESS FOR THE PREPARATION OF [(1R), 2S]-2-AMINOPROPIONIC ACID 2-[4-(4-FLUORO-2-METHYL-1H-INDOL-5-YLOXY)-5-METHYLPYRROLO[2,1-f][1,2,4]TRIAZIN-6-YLOXY]-1-METHYLETHYL ESTER 审中-公开
标题翻译：制备[（1R），2S] -2-氨基丙酸2- [4-（4-氟-2-甲基-1H-吲哚-5-基）-5-甲基吡咯并[2,1-f] [1,2,4]三嗪-6-基锂] -1-甲基乙基酯
公开(公告)号：WO2007124332A1
公开(公告)日：2007-11-01
申请号：PCT/US2007/066911
申请日：2007-04-19
申请人： BRISTOL-MYERS SQUIBB COMPANY , CRISPINO, Gerard A. , HAMEDI, Mourad , LAPORTE, Thomas L. , THORNTON, John E. , PESTI, Jaan A. , XU, Zhongmin , LOBBEN, Paul C. , LEAHY, David K. , MUSLEHIDDINOGLU, Jale , LAI, Chiajen , SPANGLER, Lori Ann , DISCORDIA, Robert P.
发明人： CRISPINO, Gerard A. , HAMEDI, Mourad , LAPORTE, Thomas L. , THORNTON, John E. , PESTI, Jaan A. , XU, Zhongmin , LOBBEN, Paul C. , LEAHY, David K. , MUSLEHIDDINOGLU, Jale , LAI, Chiajen , SPANGLER, Lori Ann , DISCORDIA, Robert P.
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： The invention relates to an improved process for preparing [(1R), 2 S ]-2-aminopropionic acid 2-[4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy]-1-methylethyl ester of the formula: (I). Compound (I) has been shown to be useful for the treatment of certain types of cancer.
摘要翻译：本发明涉及制备[（1R），2S] -2-氨基丙酸2- [4-（4-氟-2-甲基-1H-吲哚-5-基氧基）-5-甲基吡咯并[2， 1-f] [1,2,4]三嗪-6-基氧基] -1-甲基乙基酯。化合物（I）已被证明可用于治疗某些类型的癌症。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式