Preparation of substituted bicyclic imidazole derivatives as gamma secretase modulators.

Abstract

The title bicyclic imidazoles I [R0 = H, halo, C1-C4 alkyl; R1 = H, C1-C4 alkyl, halo; R3 = H, C1-C6 alkyl (un)substituted with one or more substitutions each independently selected from OH, halo, morpholinyl, etc.; R4 = H, CN, halo, etc.; X = CR7, N where R7 = H, halo; A1 = CR2, N where R2 = H, halo, C1-C4 alkoxy; A2 = CR8, N where R8 = H, halo; A3, A4 = independently CH, N; Y1 = CH, N; Y2 = CR9, N where R9 = H, halo, C1-C4 alkoxy, etc.; Y3 = CH, N; or its stereoisomer, pharmaceutically acceptable salt, solvate] were prepd. For example, a multistep synthesis of II was given. The compds. I were claimed useful for the treatment or prevention of a disease such as Alzheimer's disease, traumatic brain injury, mild cognitive impairment, etc. as gamma secretase modulators. The pharmaceutical formulations comprising I were disclosed. [on SciFinder(R)]