NOVEL BENZIMIDAZOLE DERIVATIVES AS EP4 ANTAGONISTS

摘要

The present invention relates to novel benzimidazole derivatives of the general formula (I), processes for their preparation and their use for the production of pharmaceutical compositions for the treatment of diseases and indications that are connected with the receptor EP4.

主权项

1. A compounds of the general formula (I) in which R1a, R1b independently of one another represent H, C1-C5-alkyl, C2-C5-alkenyl, C2-C5-alkynyl, C3-C6-cycloalkyl-(CH2)m, C3-C6-heterocycloalkyl-(CH2)n, C1-C5-alkoxy-C1-C3-alkyl, C3-C6-cycloalkoxy-C1-C3-alkyl, amino-C1-C3-alkyl, C1-C5-alkylamino-C1-C3-alkyl, C1-C5-dialkylamino-C1-C3-alkyl or cyano, where the optionally present heterocyclic unit is preferably selected from the group consisting of oxetane, tetrahydrofuran, tetrahydropyran, 1,4-dioxane, morpholine, azetidine, pyrrolidine, piperazine and piperidine and where optionally present alkyl, cycloalkyl or heterocycloalkyl radicals can be mono- or polysubstituted, identically or differently by halogen, C1-C5-alkyl, hydroxyl, carboxyl, carboxy-C1-C5-alkyl, C1-C5-alkoxycarbonyl-C1-C5-alkyl or C1-C5-alkylsulphonyl, R4 represents H, F, Cl, C1-C2-alkyl, C3-C5-cycloalkyl, C1-C2-alkoxy or C3-C4-cycloalkylmethyl, where the corresponding alkyl or cycloalkyl unit can be mono- or polysubstituted, identically or differently by halogen or hydroxyl, A represents RO—CO(CH2)p, where R represents H or C1-C2-alkyl, m is 0, 1, 2 or 3, n is 0, 1, 2 or 3, p is 0, and B is selected from the following structures, R6 represents H, F, Cl, CH3, CF3 CH3O or CF3O, R7, R8 in each case independently of one another represent H, F, Cl, cyano, SF5, C1-C3-alkyl, C3-C5-cycloalkyl, C1-C2-alkoxy or C3-C4-cycloalkylmethyl, where the corresponding alkyl or cycloalkyl unit can be mono- or polyhalogenated, and R9 represents C1-C5-alkyl, C2-C5-alkenyl, C2-C5-alkynyl, C3-C6-cycloalkyl-(CH2)n, C3-C6-heterocycloalkyl-(CH2)n, or C1-C7-alkoxy-C2-C5-alkyl, where the optionally present heterocyclic unit is selected from the group consisting of oxetane, tetrahydrofuran, tetrahydropyran, morpholine, pyrrolidine and piperidine and where the optionally present alkyl, cycloalkyl or heterocycloalkyl units can be mono- or polysubstituted, identically or differently by halogen, C1-C2-alkyl, C1-C2-alkoxy or carboxyl, or an isomer, diastereomer, enantiomer, solvate, salt or cyclodextrin clathrate thereof.