VENKATESAN, Hariharan,TANIS, Virginia,GOLDBERG, Steven,FOURIE, Anne M.,XUE, Xiaohua,KINZEL, Olaf,GEGE, Christian,STEENECK, Christoph,KLEYMANN, Gerald,HOFFMANN, Thomas
申请号：
PE2017002473
公开号：
PE20180250A1
申请日:
2015.10.30
申请国别(地区):
PE
年份:
2018
代理人:
摘要：
About the reaction stage of penta - (2,3-dichloro-4 - (1,1,1,1,3,3,3-hexafluoro-2-hydroxypropane-2-il) phenyl-n - (2-hydroxy-2-methylpropyl) - 4 - (r1-1-carbo) thiol-2-amides, including penta - (2,3-dichloro-4 - (1,1,3,3,3), 3-hexafluoro-2-hydroxypropan-2-il) - 2 - ((2-hydroxy-2-methylpropil) carbamoil) has n, n-diisopropilelamine and O - (7-azabenzotriazol-1-il) - N, N, n ',N'tetramethyluroni； R1 is propil methylamina, meth pirrolidina, triflurmetil azetidina, etc. These alternative thiazole compounds are modulators of the rorgamma t-nuclear receiver, a useful tool for the prevention, treatment or improvement of sindrome, flammable disorders or diseases mediated by rogamma t.Referido a un metodo para preparar un 5-(2,3-dicloro-4-(1,1,1,3,3,3-hexafluoro-2-hidroxipropan-2-il)fenil)-N-(2-hidroxi-2-metilpropil)-4-(R1-1-carbonil)tiazol-2-carboxamida que comprende la etapa de reaccionar R1-H con acido 5-(2,3-dicloro-4-(1,1,1,3,3,3-hexafluoro-2-hidroxipropan-2-il)fenil)-2-((2-hidroxi-2-metilpropil)carbamoil)tiazol-4-carboxilico en presencia de N,N-diisopropiletilamina y hexafluorofosfato de O-(7-azabenzotriazol-1-il) -N,N,N´, N´-tetrametiluronio； donde R1 es propil-metilamina, metil-pirrolidina, trifluorometil-azetidina, entre otros. Estos compuestos tiazol sustituidos son moduladores del receptor nuclear RORgamma t, util para prevenir, tratar o mejorar un sindrome, trastorno o enfermedad inflamatoria mediada por RORgamma t.
