Preparation of pyrazole derivatives having orexin receptor antagonistic activity.

Abstract

Title compds. I [X = N, CH; Y1 or Y2 = N; the other = CH; R1 = H, halo, C1-6 alkyl, C1-6 alkoxy; R2 = H, (un)substituted C1-6 alkyl, etc.; R3 = triazolyl, pyridyl, pyrimidyl (optionally substituted with halo); R4, R5 = H, halo, or C1-6 alkyl (optionally substituted with halo)] and their pharmaceutically acceptable salts, are provided for the treatment and prevention of sleep disorder, depression, anxiety disorder, panic disorder, schizophrenia, drug dependence, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, headaches, migraine, pain, digestive system diseases, epilepsy, inflammation, immune-related diseases, endocrine-related diseases, and hypertension. Thus, I, prepd. by several steps, showed antagonistic activities against human orexin receptors 1 and 2 with IC50 values of 0.5-1037.3 and 1.3-2387.5 nM, resp. [on SciFinder(R)]