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1.发明公开
公开(公告)号：EP2046779A2
公开(公告)日：2009-04-15
申请号：EP07813363.4
申请日：2007-07-26
发明人： CARTER, Percy, H. , DUNCIA, John, V. , MUDRYK, Boguslaw, M. , RANDAZZO, Michael, E. , XIAO, Zili , YANG, Michael, G. , ZHAO, Rulin
IPC分类号： C07D403/12 , C07D207/273 , A61K31/4025
CPC分类号： C07D403/12 , C07D207/273 , C07D317/72
摘要： The present invention provides a novel antagonist or partial agonists/antagonist of MCP-I receptor activity: N-((lR,2S,5R)-5-(tert-butylamino)-2- ((S)-2-oxo-3-(6-(trifluoromethyl)quinazolin-4-ylamino)pyrrolidin-l- 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-((lR,2S,5R)-5-(tert-butylamino)-2-((S)-2-oxo-3-(6- (trifluoromethyl)quinazolin-4-ylamino)pyrrolidin-l-yl)cyclohexyl)acetamide: wherein R1, R8, R9, R10, and 'HET' are as described herein. Compounds that are useful intermediates of the process are also provided herein.
摘要翻译： N - （（1R，2S，5R）-5-（叔丁基氨基）-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，或其药学上可接受的盐，溶剂化物或前药，其具有理想药理学特性的意想不到的组合。 还提供了本发明的晶体形式。 含有其的药物组合物及其作为治疗炎性疾病，变应性疾病，自身免疫疾病，代谢疾病，癌症和/或心血管疾病的药物的方法也是本发明的目的。 本发明还提供了制备式（I）化合物的方法，其包括N - （（1R，2S，5R）-5-（叔丁基氨基）-2 - （（S）-2-氧代-3- （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，R 10和'HET'如本文所述。 本文还提供了作为该方法的有用中间体的化合物。
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2.发明授权
公开(公告)号：EP2046779B1
公开(公告)日：2011-05-18
申请号：EP07813363.4
申请日：2007-07-26
发明人： CARTER, Percy, H. , DUNCIA, John, V. , MUDRYK, Boguslaw, M. , RANDAZZO, Michael, E. , XIAO, Zili , YANG, Michael, G. , ZHAO, Rulin
IPC分类号： C07D403/12 , C07D207/273 , A61K31/4025
CPC分类号： C07D403/12 , C07D207/273 , C07D317/72
摘要： The present invention provides a novel antagonist or partial agonists/antagonist of MCP-I receptor activity: N-((lR,2S,5R)-5-(tert-butylamino)-2- ((S)-2-oxo-3-(6-(trifluoromethyl)quinazolin-4-ylamino)pyrrolidin-l- 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-((lR,2S,5R)-5-(tert-butylamino)-2-((S)-2-oxo-3-(6- (trifluoromethyl)quinazolin-4-ylamino)pyrrolidin-l-yl)cyclohexyl)acetamide: wherein R1, R8, R9, R10, and 'HET' are as described herein. Compounds that are useful intermediates of the process are also provided herein.
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公开(公告)号：EP1581543A2
公开(公告)日：2005-10-05
申请号：EP03800231.7
申请日：2003-12-23
发明人： DESHPANDE, Prashant, P. , ELLSWORTH, Bruce, A. , SINGH, Janak , LAI, Chiajen , CRISPINO, Gerard , RANDAZZO, Michael, E. , GOUGOUTAS, Jack, Z. , DENZEL, Theodor, W.
CPC分类号： C07H23/00 , C07H5/04 , C07H5/06 , C07H7/00 , C07H15/207
摘要： Method for the production of C-aryl glucoside SGLT2 inhibitors useful for the treatment of diabetes and related diseases. and intermediates thereof. The C-aryl glucosides may be complexed with amino acid complex forming reagents.
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公开(公告)号：EP1324975B1
公开(公告)日：2005-11-16
申请号：EP01971317.1
申请日：2001-09-24
发明人： VENIT, John, J. , MADDING, Gary, D. , ROSSO, Victor, W. , OKUNIEWICZ, Francis, J. , DISCORDIA, Robert, P. , KIAU, Susanne , KOTNIS, Atul, S. , RANDAZZO, Michael, E. , HENNINGS, David, D. , ZHU, Jingyang , CHEN, Jason, G.
IPC分类号： C07C213/08 , C07C51/41 , C07C51/43 , C07C213/10 , C07D233/78 , C07K5/06
CPC分类号： C07D233/78 , C07C51/412 , C07C51/43 , C07C213/08 , C07C213/10 , C07D233/74 , C07C57/58
摘要： Provided is a dynamic resolution method of enriching a desired isomer of an alpha-substituted carboxylic acid relative to an undesired isomer, the method comprising: (a) in a solvent, contacting the alpha-substituted carboxylic acid, wherein the alpha substitution is with a leaving group and wherein the alpha carbon is chiral, with a homochiral amine to form a salt that is partially insoluble under selected reaction conditions, wherein the homochiral amine is selected so that the solubility of the amine salt of the undesired alpha-substituted carboxylic acid is greater than that of the amine salt of the desired alpha-substituted carboxylic acid under the selected reaction conditions; (b) reacting under the selected reaction conditions the salt with a nucleophile, wherein the reacting is effective in producing a net increase in the less soluble amine salt of the alpha-substituted carboxylic acid, and wherein the selected conditions are selected to (i) promote nucleophilic substitution of the nucleophile and the leaving group or (ii) to produce the increase in the less soluble amine salt in the absence of a strong base; and (c) maintaining the reaction for a period of time effective to increase the amount of the desired alpha-substituted carboxylic acid isomer.
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公开(公告)号：EP1089973B1
公开(公告)日：2005-11-09
申请号：EP99930402.5
申请日：1999-06-18
发明人： BISACCHI, Gregory , SLUSARCHYK, William, A. , TREUNER, Uwe , SUTTON, James, C. , ZAHLER, Robert , SEILER, Steven , KRONENTHAL, David, R. , RANDAZZO, Michael, E. , XU, Zhongmin , SHI, Zhongping , SCHWINDEN, Mark, D.
IPC分类号： C07D205/08 , C07D205/09 , C07D403/12 , C07D401/06 , C07D403/06 , A61K31/395
CPC分类号： C07D403/12 , C07D205/08
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公开(公告)号：EP1324975A2
公开(公告)日：2003-07-09
申请号：EP01971317.1
申请日：2001-09-24
发明人： VENIT, John, J. , MADDING, Gary, D. , ROSSO, Victor, W. , OKUNIEWICZ, Francis, J. , DISCORDIA, Robert, P. , KIAU, Susanne , KOTNIS, Atul, S. , RANDAZZO, Michael, E. , HENNINGS, David, D. , ZHU, Jingyang , CHEN, Jason, G.
IPC分类号： C07C213/08 , C07C51/41 , C07C51/43 , C07C213/10 , C07D233/78 , C07K5/06
CPC分类号： C07D233/78 , C07C51/412 , C07C51/43 , C07C213/08 , C07C213/10 , C07D233/74 , C07C57/58
摘要： Provided is a dynamic resolution method of enriching a desired isomer of an alpha-substituted carboxylic acid relative to an undesired isomer, the method comprising: (a) in a solvent, contacting the alpha-substituted carboxylic acid, wherein the alpha substitution is with a leaving group and wherein the alpha carbon is chiral, with a homochiral amine to form a salt that is partially insoluble under selected reaction conditions, wherein the homochiral amine is selected so that the solubility of the amine salt of the undesired alpha-substituted carboxylic acid is greater than that of the amine salt of the desired alpha-substituted carboxylic acid under the selected reaction conditions; (b) reacting under the selected reaction conditions the salt with a nucleophile, wherein the reacting is effective in producing a net increase in the less soluble amine salt of the alpha-substituted carboxylic acid, and wherein the selected conditions are selected to (i) promote nucleophilic substitution of the nucleophile and the leaving group or (ii) to produce the increase in the less soluble amine salt in the absence of a strong base; and (c) maintaining the reaction for a period of time effective to increase the amount of the desired alpha-substituted carboxylic acid isomer.
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公开(公告)号：EP1089973A1
公开(公告)日：2001-04-11
申请号：EP99930402.5
申请日：1999-06-18
发明人： BISACCHI, Gregory , SLUSARCHYK, William, A. , TREUNER, Uwe , SUTTON, James, C. , ZAHLER, Robert , SEILER, Steven , KRONENTHAL, David, R. , RANDAZZO, Michael, E. , XU, Zhongmin , SHI, Zhongping , SCHWINDEN, Mark, D.
IPC分类号： C07D205/08 , C07D205/09
CPC分类号： C07D403/12 , C07D205/08
摘要： Compounds of formulae (I), (II), (III).
摘要翻译： 式（I），（II），（III）的化合物。
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