Patent ID: 6281220
Filing Date: 2001-08-28
Classification: A61P,C07D

Abstract:
A pharmaceutical composition comprising a compound of the formula: ##STR42##or a pharmaceutically acceptable salt thereof together with at least one pharmaceutically acceptable carrier, whereinAr is phenyl, 2-, 3-, or 4-pyridyl, 2- or 3-thienyl, 4- or 5-pyrimidyl, each of which is mono-, di-, or trisubstituted with halogen, hydroxy, lower alkyl, or lower alkoxy, with the proviso that at least one of the ortho positions of the Ar substituent is substituted;X is CH or nitrogen;R.sub.1 is lower alkyl;R.sub.2 is hydrogen, halogen, lower alkyl, lower alkoxy, or thioalkoxy; orR.sub.1 and R.sub.2 taken together represent --(CH.sub.2).sub.n --A--(CH.sub.2).sub.m --,where n is 2, 3 or 4, A is methylene, oxygen, sulfur or NR.sub.6,where R.sub.6 is lower alkyl, andm is 0, 1 or 2;R.sub.3 and R.sub.4 are the same or different and represent hydrogen or lower alkyl;phenyl, 2-, 3-, or 4-pyridyl, 2-, or 3-thienyl, or 2-, 4-, or 5-pyrimidyl, each of which is mono- or disubstituted with halogen, hydroxy, lower alkyl, or lower alkoxy;phenyl lower alkyl, 2-, 3-, or 4-pyridyl lower alkyl, 2- or 3-thienyl lower alkyl, or 2-, 4-, or 5-pyrimidyl lower alkyl;cycloalkyl having 3-8 carbon atoms or cycloalkyl lower alkyl where the cycloalkyl portion has 3-8 carbon atoms;2-hydroxyethyl or 3-hydroxypropyl optionally mono or disubstituted with lower alkyl with the proviso that not both R.sub.3 and R4 are hydrogen; orR.sub.3 and R4 taken together represent --(CH.sub.2).sub.n --A--(CH.sub.2).sub.m --where n is 2, or 3,A is methylene, 1,2 phenylene, oxygen, sulfur or NR.sub.6, wherein R.sub.6 is lower alkyl, phenyl, 2-, 3-, or 4-pyridyl, 2- or 3-thienyl or 2-, 4-, or 5-pyrimidyl, phenyl lower alkyl, 2-, 3-, or 4-pyridyl lower alkyl, 2- or 3-thienyl lower alkyl, or 2-, 4-, or 5-pyrimidyl lower alkyl, andm is 1, 2 or 3;R.sub.5 is hydrogen, halogen, lower alkyl, lower alkoxy, or thioalkoxy.