BLANEY, Paul Matthew,NEUHAUS, Roland,KAULFUSS, Stefan,ZIMMERMANN, Katja,BAUSER, Marcus,REHWINKEL, Hartmut,NGUYEN, Duy,SIEBENEICHER, Holger,ANLAUF, Sonja,RING, Sven,PANKNIN, Olaf,SCHWEDE, Wolfgang
申请号：
PE0014652016
公开号：
PE01432017A1
申请日:
2015.02.10
申请国别(地区):
PE
年份:
2017
代理人:
摘要：
Refers to a compound of formula I, where R1 is Halogen, alkyl, cycloalkyl - C1 - C6 C3, C6, R2, R3, among othersR6 and R12 are Hydrogen R4 is Hydrogen or Halogen R5 is r13oc (= o) - C1 - C6 alkyl, r13oc (= o) - alquenilo C2 - C6, among others R4 is Hydrogen, alkyl alkoxy C1 - C6 C1 - C6Among others is C1 - C3 alkyl R8, R9, R10 and R11 are Hydrogen, C1 - C3 alkyl R13 is C1 - C6 Hydrogen, alkyl, cycloalkyl C3 C6, among others.Preferred compounds are: {[1 - (3,3,5,5 - tetrametilciclohexil) - 2 - [4 - (trifluoromethoxy) phenyl] amino} - 1H benzimidazole - 5 - il] oxy) acetate Tert Butyl (2E) (+) - 3 - (2 - ((4 - (trifluoromethoxy) phenyl] amino} - 1 - [(CIS - 3.3)5 - trimetilciclohexil] - 1H benzimidazole - 5 - yl) Methyl acrylate among others. It also relates to a preparation method of a Pharmaceutical Composition and a Pharmaceutical combination.These compounds are inhibitors of the isocitrate dehydrogenase 1 (midh1) being useful in the treatment of autoimmune diseases, inflammatory, tumor, Leukemia, among others.Se refiere a un compuesto de formula I, donde: R1 es halogeno, alquilo C1-C6, cicloalquilo C3-C6, entre otros R2, R3, R7 y R12 son hidrogenos R4 es hidrogeno o halogeno R5 es R13OC(=O)-alquilo C1-C6, R13OC(=O)-alquenilo C2-C6, entre otros R6 es hidrogeno, alquilo C1-C6, alcoxi C1-C6, entre otros R8 es alquilo C1-C3 R9, R10 y R11 son hidrogeno, alquilo C1-C3 R13 es hidrogeno, alquilo C1-C6, cicloalquilo C3-C6, entre otros. Son compuestos preferidos: {[1-(3,3,5,5-tetrametilciclohexil)-2-{[4-(trifluorometoxi)fenil]amino}-1H-bencimidazol-5-il]oxi}acetato de tert-butilo (±) (2E)-3-(2-{[4-(trifluorometoxi)fenil]amino}-1-[(cis)-3,3,5-trimetilciclohexil]-1H-bencimidazol-5-il)acrilato de metilo entre otros. Tambien se refiere a un metodo de preparacion, a una composicion farmaceutica y a una combinacion farmaceutica. Dichos compuestos son inhibidores de la isocitrato deshidrogenasa 1 (MIDH1) siendo utiles en el tratamiento de enfermedades autoinmunes, inflamatorias, t
