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公开(公告)号：US20160326104A1
公开(公告)日：2016-11-10
申请号：US15109733
申请日：2015-01-05
发明人： Jingwu DUAN , T.G.Murali DHAR , Bin JIANG , Ananta KARMAKAR , Arun Kumar GUPTA , Zhonghui LU , Carolyn A. WEIGELT
IPC分类号： C07C317/20 , C07C317/24 , C07D213/81 , C07D295/096 , C07C317/30 , C07D231/54 , C07D277/82 , C07D213/30 , C07D213/75 , C07D205/04 , C07D207/277 , C07D211/62 , C07D211/78 , C07D309/08 , C07D213/56 , C07D231/14 , C07D295/195 , C07D207/27 , C07D237/24 , C07D239/28 , C07D241/24 , C07D401/06 , C07D405/04 , C07D401/04 , C07D295/16 , C07D471/04 , C07D249/06 , C07D403/04 , C07D401/12 , C07D237/22 , C07D237/08 , C07D211/46 , C07D335/02 , C07C317/46
CPC分类号： C07C317/20 , C07C317/24 , C07C317/30 , C07C317/46 , C07C2601/02 , C07C2601/14 , C07D205/04 , C07D207/27 , C07D207/277 , C07D211/46 , C07D211/48 , C07D211/62 , C07D211/78 , C07D213/30 , C07D213/40 , C07D213/56 , C07D213/71 , C07D213/75 , C07D213/81 , C07D213/82 , C07D231/12 , C07D231/14 , C07D231/54 , C07D231/56 , C07D237/08 , C07D237/20 , C07D237/22 , C07D237/24 , C07D239/28 , C07D241/24 , C07D249/04 , C07D249/06 , C07D277/60 , C07D277/82 , C07D295/096 , C07D295/16 , C07D295/185 , C07D295/195 , C07D295/205 , C07D309/04 , C07D309/08 , C07D335/02 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D405/04 , C07D471/04
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RORY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的RORYY活性的方法和用于治疗患有疾病或病症的受试者的治疗受益于RORYY活性例如自身免疫和/或炎症性疾病的治疗益处的受试者的方法。
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公开(公告)号：US20180111937A1
公开(公告)日：2018-04-26
申请号：US15558708
申请日：2016-03-17
发明人： Stephen T. WROBLESKI , Gregory D. BROWN , Shuqun LIN , Jingwu DUAN , Zhonghui LU , Murali T.G. DHAR , Hai-Yun XIAO , Andrew J. TEBBEN
IPC分类号： C07D471/14 , A61P29/00 , A61P37/00 , C07D491/147
CPC分类号： C07D471/14 , A61P29/00 , A61P37/00 , C07D487/06 , C07D491/147
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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3.发明申请公开(公告)号：US20160326108A1
公开(公告)日：2016-11-10
申请号：US15109719
申请日：2015-01-05
发明人： Jingwu DUAN , T.G.Murali DHAR , Bin JIANG , Zhonghui LU , Hai-Yun XIAO
IPC分类号： C07D207/12 , C07D403/04 , C07D405/06 , C07D403/06 , C07D401/14 , C07D417/06 , C07D413/06 , C07D417/14 , C07D403/12 , C07D405/12 , C07D413/12 , C07D401/12 , C07D493/08 , C07D409/12 , C07D493/04 , C07D471/08 , C07D401/06
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.
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公开(公告)号：US20200024257A1
公开(公告)日：2020-01-23
申请号：US16348195
申请日：2017-11-08
发明人： Jingwu DUAN , Bin Jiang , T.G. Murali Dhar , Zhonghui LU , Arun Kumar Gupta , Ananta Karmakar
IPC分类号： C07D401/14 , C07D207/16 , C07D207/06 , C07D207/12 , C07D401/06 , C07D403/04 , C07D413/06 , C07D405/12
摘要： There are described 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.
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公开(公告)号：US20190241588A1
公开(公告)日：2019-08-08
申请号：US16295378
申请日：2019-03-07
IPC分类号： C07F9/6574 , C07D209/30 , C07D209/60 , C07D409/04 , C07D215/36 , C07D495/08 , C07D209/70 , C07D221/10 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/06 , C07D409/06 , C07D413/06 , C07D413/10 , C07D413/12 , C07D417/06 , C07D417/12 , C07D417/14 , C07D471/04 , C07D491/052 , C07D491/107 , C07D493/08 , C07D495/04 , C07D417/04
摘要： There are described RORγ modulators of the formula (I), and formula (II) 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.
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公开(公告)号：US20180111936A1
公开(公告)日：2018-04-26
申请号：US15558692
申请日：2016-03-17
发明人： Hai-Yun XIAO , Murali T.G. DHAR , Jingwu DUAN , Bin JIANG , Andrew J. TEBBEN
IPC分类号： C07D471/14 , A61P37/00 , A61P29/00
CPC分类号： C07D471/14 , A61P29/00 , A61P37/00 , C07D487/06
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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