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公开(公告)号：WO2019103952A1
公开(公告)日：2019-05-31
申请号：PCT/US2018/061726
申请日：2018-11-19
发明人： LIU, Chunjian , YANG, Michael G. , XIAO, Zili , CHEN, Ling , MOSLIN, Ryan M. , TOKARSKI, John S. , WEINSTEIN, David S.
IPC分类号： C07D401/14 , A61K31/501 , C07D401/12 , C07D487/04 , A61P29/00 , A61P37/00
摘要： Compounds having the following formula (I), or a stereoisomer or pharmaceutically-acceptable salt thereof, where R 1 , R 2 , R 3 , R 4 , and R 5 are as defined herein, are useful in the modulation of IL-12, IL-23 and/or IFNα, by acting on Tyk-2 to cause signal transduction inhibition.
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公开(公告)号：WO2016028959A1
公开(公告)日：2016-02-25
申请号：PCT/US2015/046005
申请日：2015-08-20
发明人： XIAO, Hai-Yun , DYCKMAN, Alaric J. , XIAO, Zili , YANG, Michael G. , DHAR, T.G. Murali , GILMORE, John L. , MARCOUX, David
IPC分类号： C07D309/06 , A61K31/133 , A61K31/135 , A61K31/353 , A61K31/36 , A61K31/47 , C07D309/12 , C07D215/14 , C07D311/58 , C07D311/76 , C07D217/24 , C07D319/20 , C07D231/12 , C07D333/16 , C07D239/26 , C07C317/32 , C07C217/52 , C07C219/24 , C07C219/26 , C07D241/04 , C07C323/29 , C07D277/24 , C07C251/38 , C07C251/40 , C07C251/42 , C07C251/44 , C07C251/54 , C07D209/46 , C07D213/32 , C07D213/38 , C07D213/69 , A61P9/00 , A61P35/00 , A61P37/00
CPC分类号： A61K31/695 , A61K31/135 , A61K31/137 , A61K31/15 , A61K31/165 , A61K31/166 , A61K31/17 , A61K31/222 , A61K31/24 , A61K31/27 , A61K31/337 , A61K31/351 , A61K31/352 , A61K31/381 , A61K31/415 , A61K31/4174 , A61K31/426 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/47 , A61K31/4965 , A61K31/505 , A61K31/661 , C07B2200/05 , C07C215/42 , C07C217/52 , C07C217/58 , C07C217/74 , C07C219/24 , C07C233/41 , C07C233/65 , C07C235/46 , C07C251/38 , C07C251/42 , C07C251/44 , C07C251/50 , C07C251/52 , C07C251/54 , C07C271/34 , C07C275/26 , C07C317/28 , C07C317/32 , C07C321/16 , C07C321/22 , C07C321/28 , C07C323/25 , C07C323/29 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2602/10 , C07C2603/74 , C07D209/46 , C07D213/32 , C07D213/38 , C07D213/69 , C07D213/70 , C07D215/12 , C07D215/14 , C07D217/24 , C07D231/12 , C07D231/20 , C07D239/26 , C07D241/04 , C07D241/12 , C07D277/24 , C07D305/08 , C07D309/06 , C07D309/12 , C07D311/58 , C07D311/76 , C07D319/20 , C07D333/16 , C07F7/0818 , C07F9/091 , C07F9/117 , C07F9/5442 , C07F9/5728 , C07F9/62 , C07F9/65031 , C07F9/650952 , C07F9/65522 , C07F9/655345
摘要： Disclosed are compounds of Formulas (I), (II), (III), (IV), and (V) and/or a salt thereof, wherein R1 is OH or OP(O)(OH)2, and X1, X2, X3, R2, R2a, Ra, Rb, and Rc are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
摘要翻译： 公开了式（I），（II），（III），（IV）和（V）和/或其盐的化合物，其中R1是OH或OP（O）（OH）2，X1，X2 ，X3，R2，R2a，Ra，Rb和Rc在本文中定义。 还公开了使用这些化合物作为G蛋白偶联受体S1P1的选择性激动剂的方法和包含这些化合物的药物组合物。 这些化合物可用于治疗，预防或减缓各种治疗领域如自身免疫性疾病和血管疾病中的疾病或病症的发展。
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公开(公告)号：WO2008014360A3
公开(公告)日：2008-01-31
申请号：PCT/US2007/074377
申请日：2007-07-26
申请人： BRISTOL-MYERS SQUIBB COMPANY , CARTER, Percy, H. , DUNCIA, John, V. , MUDRYK, Boguslaw, M. , RANDAZZO, Michael, E. , XIAO, Zili , YANG, Michael, G. , ZHAO, Rulin
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 , 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 R 1 , R 8 , R 9 , R 10 , 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：WO2022086828A1
公开(公告)日：2022-04-28
申请号：PCT/US2021/055340
申请日：2021-10-18
发明人： LUO, Guanglin , CHEN, Jie , DZIERBA, Carolyn Diane , FRENNESSON, David B. , GUO, Junqing , HART, Amy C. , HU, Xirui , MERTZMAN, Michael E. , PATTON, Matthew Reiser , SHI, Jianliang , SPERGEL, Steven H. , VENABLES, Brian Lee , WU, Yong-Jin , XIAO, Zili , YANG, Michael G.
IPC分类号： C07D471/04 , A61P9/04 , A61P17/06 , A61P25/28 , A61P29/00 , A61K31/437 , A61K31/444
摘要： Compounds having formula (I), and enantiomers, and diastereomers, stereoisomers, pharmaceutically-acceptable salts thereof,Formula (I): are useful as kinase modulators, including RIPK1 modulation. All the variables are as defined herein.
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5.发明申请
公开(公告)号：WO2020180907A1
公开(公告)日：2020-09-10
申请号：PCT/US2020/020856
申请日：2020-03-04
IPC分类号： C07D487/04 , C07D519/00 , A61P29/00 , A61P37/00 , A61K31/5025 , A61K31/5377 , A61K31/55
摘要： Compounds having the following formula I: or a stereoisomer or a pharmaceutically-acceptable salt thereof, wherein all substituents are as defined herein, are useful in the modulation of IL-12, IL-23 and/or IFNα by acting on Tyk-2 to cause signal transduction inhibition.
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公开(公告)号：WO2022241172A1
公开(公告)日：2022-11-17
申请号：PCT/US2022/029105
申请日：2022-05-13
发明人： SPERGEL, Steven, H. , MOSLIN, Ryan, M. , MERTZMAN, Michael, Edward , POSY, Shoshana, L. , LAKKARAJU, Sirish, Kaushik , TINO, Joseph, A. , XIAO, Zili , LIU, Chunjian , LIN, James
IPC分类号： C07D401/12 , C07D401/14 , C07D403/12 , C07D413/12 , C07D417/12 , C07D417/14 , A61P29/00 , A61P37/00 , A61K31/501
摘要： There are disclosed compounds of the following formula (I) or a stereoisomer or pharmaceutically acceptable salt thereof, wherein all substituents are as defined herein, which are useful in the modulation of IL-12, IL-23 and/or IFNα, by acting on Tyk-2 to cause signal transduction inhibition. The compounds of the invention may be useful for treating neurodegenerative diseases or disorders.
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公开(公告)号：WO2020159904A1
公开(公告)日：2020-08-06
申请号：PCT/US2020/015291
申请日：2020-01-28
发明人： SHERWOOD, Trevor C. , YANG, Michael G. , GILMORE, John L. , ZHANG, Yanlei , XIAO, Zili , LIU, Qingjie
IPC分类号： C07D213/82 , C07D237/24 , C07D401/12 , C07D403/12 , C07D405/14 , C07D417/14 , C07D413/12 , C07B59/00 , A61K31/44 , A61K31/50 , A61K31/501
摘要： Compounds having the following formula (I): (Formula (I)) or a stereoisomer or pharmaceutically-acceptable salt thereof, are useful in the modulation of IL-12, IL-23 and/or IFNa, by acting on Tyk-2 to cause signal transduction inhibition.
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8.发明申请
公开(公告)号：WO2018111787A1
公开(公告)日：2018-06-21
申请号：PCT/US2017/065665
申请日：2017-12-12
IPC分类号： C07F9/6509 , C07F9/6558 , C07D401/12 , C07D237/24 , A61K31/50 , A61K31/501
摘要： Compounds having the following formula I: or a stereoisomer or pharmaceutically-acceptable salt thereof, where all substituents are as defined herein, are useful in the modulation of IL-12, IL-23 and/or IFNα, by acting on Tyk-2 to cause signal transduction inhibition.
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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.
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公开(公告)号：WO2008014361A3
公开(公告)日：2008-01-31
申请号：PCT/US2007/074378
申请日：2007-07-26
申请人： BRISTOL-MYERS SQUIBB COMPANY , CARTER, Percy H. , CHERNEY, Robert J. , HYNES, John , KO, Soo S. , SRIVASTAVA, Anurag , XIAO, Zili , YANG, Michael G.
发明人： CARTER, Percy H. , CHERNEY, Robert J. , HYNES, John , KO, Soo S. , SRIVASTAVA, Anurag , XIAO, Zili , YANG, Michael G.
IPC分类号： C07D401/12 , C07D403/12 , C07D487/04 , A61K31/4025
摘要： This invention relates generally to modulators of chemokine receptor activity having unexpected combination of desirable pharmacological properties. Pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and prevention of inflammatory, allergic, autoimmune, metabolic, cancer and/or cardiovascular diseases, particularly diabetes, Crohn's disease, atherosclerosis, and multiple sclerosis, along with methods of preparing compounds and intermediates therefor. Metabolites of active compounds are also provided herein, pharmaceutical compositions and use thereof are also provided.
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