Patent ID: 6242439
Filing Date: 2001-06-05
Classification: A61P,C07D

Abstract:
A compound of formula (1) ##STR41##wherein R.sup.1 is hydrogen, methyl, ethyl, methoxy or methylthio;R.sup.2 and R.sup.3 each independently is hydrogen or lower alkyl;R.sup.4 is hydrogen or lower alkyl;R.sup.5 is lower alkyl, lower cycloalkyl, CH.sub.2 C(O)OR.sup.6wherein R.sup.6 is methyl, ethyl or phenylmethyl; phenyl, phenyl monosubstituted, disubstituted or trisubstituted with a substituent selected independently from the group consisting of lower alkyl, lower alkoxy, lower alkylthio, halo, hydroxy and amino; phenyl(lower alkyl), phenyl(lower alkyl) monosubstituted or disubstituted on the phenyl portion thereof with a substituent selected independently from the group consisting of lower alkyl, lower alkoxy, lower alkylthio, halo, hydroxy, nitro, amino, lower alkyl amino, di(lower alkyl)amino, lower alkyl-C(O)NH--, di(lower alkyl)aminocarbonyl, cyano, trifluoromethyl, (trifluoromethyl)thio, (trifluoromethyl)sulfinyl, (trifluoromethyl)sulfonyl and C(O)OR.sup.7 wherein R.sup.7 is methyl, ethyl or phenylmethyl;Het or Het(lower alkyl) wherein Het is 2-furyl, 2-methyl-3-furyl, 2-thienyl, 2-pyridinyl, 3-pyridinyl, 4-pyridinyl, 3-methyl-2-pyrrolyl, 2-thiazolyl, 4-thiazolyl, 2-isoxazolyl, 2-pyrimidinyl, 4-methyl-2-pyrimidinyl, 4,6-dimethyl-2-pyrimidinyl, 4-pyrimidinyl, 2,6-dimethyl-2-pyrimidinyl or 4-methyltetrazolyl;(5-benzo[1,3]dioxolyl)methyl, 1(R)-(1-naphthalenyl)ethyl, 2-benzothiazolyl or 2-thiazolo[4,5-b]pyridinyl; orR.sup.4 and R.sup.5 together with the nitrogen atom to which they are attached form a pyrrolidino, piperidino, morpholino, N-methylpiperazino, 1-(3,4-dihydro-1H-isoquinolinyl) or 2-(3,4-dihydro-1H-isoquinolinyl);and Z is lower alkyl, phenyl, phenyl monosubstituted or disubsituted with a substituent selected independently from lower alkyl, lower alkoxy, halo, hydroxy and amino; phenylmethyl, phenylmethyl monosubstituted or disubstituted on the phenyl portion thereof with a substituent selected from the group consisting of lower alkyl, lower alkoxy, halo, hydroxy and amino; or (CH.sub.2).sub.p -(Het) wherein p is the integer 0 or 1 and Het is a monovalent five or six membered saturated or unsaturated heterocycle containing from one to four heteroatoms selected from N, O or S, said Het being optionally mono- or di-substituted with N-oxido, lower alkyl, phenyl-(C.sub.1-3) alkyl, lower alkoxy, halo or amino, and said Het being optionally fused to a phenyl ring; with the proviso that when Z is (CH.sub.2).sub.p -(Het) as defined herein then R.sup.2 and R.sup.3 each is hydrogen.