VENKATESAN, Hariharan,TANIS, Virginia,GOLDBERG, Steven,FOURIE, Anne M.,XUE, Xiaohua,KINZEL, Olaf,GEGE, Christian,STEENECK, Christoph,KLEYMANN, Gerald,HOFFMANN, Thomas
申请号：
PE0024732017
公开号：
PE02502018A1
申请日:
2015.10.30
申请国别(地区):
PE
年份:
2018
代理人:
摘要：
Refers to a method for preparing a 5 - (2,3 - Dichloro - 4 - (1,1,1,3,3,3 - 2 - 2 - hidroxipropan hexafluoro - il) phenyl) - N - (2 - hydroxy - 2-methylpropyl) - 4 - (R1 - 1 - 2 - carbonyl) thiazole carboxamide which comprises the step of reacting with H acid R1 - 5 - (4 - (2,3 - Dichloro - 1,1,1,3,3,3 - 2 - 2 - hidroxipropan hexafluoro - il) phenyl) - 2 - ((2 - hydroxy - 2-methylpropyl) Carbamoyl) thiazole - 4 - carboxylic acid in the presence of N, N - and diisopropiletilamina hexafluorophosphate (azabenzotriazol - or - 7 - 1 - il) - n, N, n ,N - tetrametiluronio where R1 is Methyl Propyl - methylamine, pyrrolidine, trifluoromethyl - azetidine, among others.These compounds are substituted thiazole rorgamma T nuclear receptor modulators useful for preventing, treating or improving a disorder or Syndrome, inflammatory disease mediated by rorgamma 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.
