Patent ID: 6274583
Filing Date: 2001-08-14
Classification: A61P,C07D

Abstract:
A compound of the formula: ##STR41##whereinX is selected from CHOR.sup.5, CHF, CR.sup.5 R.sup.6, CF.sub.2, CHCHF.sup.2, or C.dbd.CF.sup.2 ;Y is selected from oxygen, NR.sup.8 or sulfur;Z is selected from CH, CCO.sub.2 R.sup.5, C(CH.sub.2).sub.1-3 CO.sub.2 R.sup.5, COR.sup.12, CNR.sup.12 R.sup.13 or C(CH.sub.2)qCH.sub.2 N(R.sup.5).sub.2 ;R.sup.1 is selected from unsubstituted, mono- or poly-substituted phenyl where the substituents on the phenyl are independently selected from halogen, cyano, OR.sup.5, or C.sub.1-4 alkyl; provided that when R.sup.1 is mono-substituted phenyl and the substituent is OR.sup.5, the substituent is other than in the 2-position on the phenyl ring;R.sup.3 is selected from hydrogen, cyano, CO.sub.2 R.sup.5, CON(R.sup.5).sub.2, C.sub.1-8 alkyl, C.sub.3-8 cycloalkyl or (CH.sub.2).sub.1-3 CO.sub.2 R.sup.5 ;R.sup.4 is selected from hydrogen, OR.sup.5, C.sub.1-8 alkyl, or halogenR.sup.5 and R.sup.6 are each independently selected from hydrogen, C.sub.1-8 alkyl, C.sub.3-8 cycloalkyl, halogen substituted C.sub.1-4 alkyl and halogen substituted C.sub.3-8 cycloalkyl;R.sup.8 is selected from hydrogen, cyano or SO.sub.2 R.sup.5 ;R.sup.12 and R.sup.13 are each independently selected from hydrogen, C.sub.1-8 alkyl, C.sub.3-8 cycloalkyl, CHO, COR.sup.5, CONR.sup.5 R.sup.6, and (CH.sub.2)qOR.sup.5 ;R.sup.14 is selected from hydrogen, C.sub.1-8 alkyl, C.sub.3-8 cycloalkyl, C.sub.1-4 alkoxy, morpholinyl, piperazinyl, d-valerolactamyl, 2-pyrrolidonyl, thiophenyl, furanyl, pyridinyl, naphthyl or unsubstituted, mono- or poly-substituted phenyl where the substituents on the phenyl are independently selected from C.sub.1-4 alkyl, OR.sup.5 or halogen; m, n and q are each independently an integer of from zero to three, provided that when m and nare both zero, then X is selected from CHF, CR.sup.5 R.sup.6, CF.sub.2, CHCHF.sub.2, or C.dbd.CF.sub.2 ; andp is an integer of from zero to five;and further provided that when Z is CH and R.sup.14 is hydrogen, then R.sup.1 is not unsubstituted phenyl;or a pharmaceutically acceptable salt thereof.