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公开(公告)号：EP3331889B1
公开(公告)日：2020-09-23
申请号：EP16748045.8
申请日：2016-08-02
发明人： XIAO, Hai-Yun , DHAR, Murali T.G. , JIANG, Bin , DUAN, Jingwu
IPC分类号： C07D487/14 , A61K31/4184 , A61K31/4188 , C07D487/04 , A61P37/00
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公开(公告)号：EP3271361B1
公开(公告)日：2020-04-22
申请号：EP16712646.5
申请日：2016-03-17
发明人： WROBLESKI, Stephen T. , BROWN, Gregory D. , LIN, Shuqun , DUAN, Jingwu , LU, Zhonghui , DHAR, T.G. Murali , XIAO, Hai-Yun , TEBBEN, Andrew J.
IPC分类号： C07D487/06 , A61K31/4353 , A61P1/00 , A61P11/06 , A61P17/00 , A61P17/06 , A61P19/02 , A61P19/06 , A61P25/00 , A61P37/00
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公开(公告)号：EP3271360B1
公开(公告)日：2020-04-22
申请号：EP16712645.7
申请日：2016-03-17
IPC分类号： C07D487/06 , A61K31/4353 , A61P11/06 , A61P17/00 , A61P17/06 , A61P19/06 , A61P25/00 , A61P37/00
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公开(公告)号：EP3271361A1
公开(公告)日：2018-01-24
申请号：EP16712646.5
申请日：2016-03-17
发明人： WROBLESKI, Stephen T. , BROWN, Gregory D. , LIN, Shuqun , DUAN, Jingwu , LU, Zhonghui , DHAR, T.G. Murali , XIAO, Hai-Yun , TEBBEN, Andrew J.
IPC分类号： C07D487/06 , A61K31/4353 , A61P1/00 , A61P11/06 , A61P17/00 , A61P17/06 , A61P19/02 , A61P19/06 , A61P25/00 , A61P37/00
摘要： Disclosed are compounds of Formula (I) or a salt thereof, wherein: X is N; W is: —(CR3R3)2-5-, —(CR3R3)x-Y—(CR3R3)y-, —Y—(CR3R3)2-3-Y—, —CR3R3-Y—(CR3R3)2-Y—, —Y—(CR3R3)2-Y—CR3R3-; and Y, R1, R2, R3, R5, R6, R8, x, and y are define herein. Also disclosed are methods of using such compounds as modulators of TNFα, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating inflammatory and autoimmune diseases.
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公开(公告)号：EP3271360A1
公开(公告)日：2018-01-24
申请号：EP16712645.7
申请日：2016-03-17
IPC分类号： C07D487/06 , A61K31/4353 , A61P11/06 , A61P17/00 , A61P17/06 , A61P19/06 , A61P25/00 , A61P37/00
摘要： Disclosed are compounds of Formula (I) or a salt thereof, wherein: X is N; W is: (i) —(CR3R3)1-4—; (ii) —(CR3R3)x—Y—(CR3R3)y—; Or (iii) —Y—(CR3R3)2—Y—; and Y, R1, R2, R3, R5, R6, R8, x, and y are defined herein. Also disclosed are methods of using such compounds as modulators of TNFα, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating inflammatory and autoimmune diseases.
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公开(公告)号：EP1303514B9
公开(公告)日：2006-11-08
申请号：EP01932879.8
申请日：2001-05-02
发明人： CHEN, Bang-Chi , KIM, Kyoung, S. , KIMBALL, S., David , MISRA, Raj, N. , SALVATI, Mark, E. , SUNDEEN, Joseph, E. , XIAO, Hai-Yun , ZHAO, Rulin
IPC分类号： C07D417/14 , C07D487/18 , C07D263/32 , C07D251/00
CPC分类号： C07D417/12 , A61K31/427 , A61K31/454 , C07D231/12 , C07D233/56 , C07D249/08 , C07D417/14
摘要： The present invention relates to new, efficient processes for the preparation of 5-(2-oxazolylalkylthio)-2-azacycloalkanoylaminothiazole compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein R, R?1, R2, R3, R4, R5, R6, R7, R8¿, m and n are as defined in the specification. The compounds formula (I) are potent inhibitors of cyclin dependent kinases (cdks). The present invention further concerns new key intermediate compounds, a quaternary ammonium salt of formula (III') and a 2-oxazolylalkyl derivative of formula (IX).
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公开(公告)号：EP3526218A1
公开(公告)日：2019-08-21
申请号：EP17788067.1
申请日：2017-10-12
发明人： LIU, Qingjie , DHAR, T.G. Murali , QIN, Lan-ying , XIAO, Hai-Yun , LI, Jianqing , CHERNEY, Robert, J. , CORNELIUS, Lyndon A.M.
IPC分类号： C07D471/04 , A61K31/437 , A61P17/06 , A61P11/06
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公开(公告)号：EP3331871A1
公开(公告)日：2018-06-13
申请号：EP16750343.2
申请日：2016-08-02
发明人： XIAO, Hai-Yun , DHAR, T. G. Murali , LI, Ning , DUAN, Jingwu , JIANG, Bin , LU, Zhonghui , NGU, Khehyong , PITTS, William J. , TINO, Joseph
IPC分类号： C07D401/14 , C07D405/14 , C07D413/14 , C07D215/42 , C07D401/04 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D471/04 , A61K31/4706 , A61K31/4709 , A61P29/00
CPC分类号： C07D401/04 , C07D215/42 , C07D215/44 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D471/04
摘要： Disclosed are compounds of Formula (I) or a salt thereof, wherein: A is CR1 or N; B is CR3 or N; D is CR4 or N; L1 is -(CR7R7)m-; L2 is -(CR7R7)n-; and X, Z, R1, R2, R3, R4, R5,and R6 are define herein. Also disclosed are methods of using such compounds as modulators of TNFα, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating inflammatory and autoimmune diseases.
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9.发明公开PYRROLIDINYL SULFONE DERIVATIVES AND THEIR USE AS ROR GAMMA MODULATORS 有权DOREN VERWENDUNG ALS ROR-GAMMA-MODULATOREN中的吡咯烷酮
公开(公告)号：EP3092229A1
公开(公告)日：2016-11-16
申请号：EP15700613.1
申请日：2015-01-05
发明人： DUAN, Jingwu , DHAR, T.G. Murali , JIANG, Bin , LU, Zhonghui , XIAO, Hai-Yun
IPC分类号： C07D403/12 , C07D401/14 , C07D413/14 , C07D401/12 , C07D403/04 , C07D407/12 , C07D407/14 , C07D413/12 , C07D417/14 , C07D471/10 , C07D487/04 , C07D487/10 , C07D207/12 , C07D405/12 , C07D409/12
CPC分类号： C07D207/12 , C07D207/16 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12 , C07D405/06 , C07D405/12 , C07D407/12 , C07D407/14 , C07D409/12 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/06 , C07D417/12 , C07D417/14 , C07D471/08 , C07D471/10 , C07D487/04 , C07D487/10 , C07D493/04 , C07D493/08
摘要： Described are RORγ modulators of the formula (I), or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein all substituents are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for modulating RORγ activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of RORγ activity, for example, autoimmune and/or inflammatory disorders.
摘要翻译： 描述了式（I）的RORγ调节剂或其立体异构体，互变异构体，药学上可接受的盐，溶剂合物或前药，其中所有取代基均在本文中定义。 还提供了包含其的药物组合物。 这样的化合物和组合物可用于调节细胞中RORγ活性的方法和用于治疗受试者治疗受益于RORγ活性例如自身免疫和/或炎性疾病的疾病或障碍的受试者的方法。
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公开(公告)号：EP2958888A2
公开(公告)日：2015-12-30
申请号：EP14709822.2
申请日：2014-02-21
发明人： DHAR, T. G. Murali , XIAO, Hai-Yun , DYCKMAN, Alaric J. , CHAN, Eric J. , DABROS, Marta , ROBERTS, Daniel Richard
IPC分类号： C07C215/42 , A61K31/133 , A61P9/00 , A61P37/00
CPC分类号： C07D207/50 , C07B2200/07 , C07B2200/13 , C07C25/22 , C07C49/67 , C07C215/42 , C07C2601/08 , C07C2602/10 , C07F9/117
摘要： Disclosed are compounds of Formula (I) and/or a salt thereof; wherein R is -OH or -OP(O)(OH)
2 . Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P
1 , 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）化合物和/或其盐; 其中R是-OH或-OP（O）（OH）2。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，以及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中的疾病或病症如自身免疫疾病和血管疾病的进展。
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