Patent ID: 6329526
Filing Date: 2001-12-11
Classification: A61P,C07D

Abstract:
A compound of the Formula ##STR27##whereinR.sub.1 is 4-pyridyl ring, which ring is substituted with a C.sub.1-4 alkoxy group, and is additionally unsubstituted or substituted independently by C.sub.1-4 alkyl, halogen, hydroxyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, C.sub.1-4 alkylsulfinyl, CH.sub.2 OR.sub.12, amino, mono and di-C.sub.1-6 alkyl substituted amino, N(R.sub.10)C(O)R.sub.c, an N-heterocyclyl ring which ring has from 5 to 7 members, or an N-heterocyclyl ring which ring has from 5 to 7 members and contains an additional heteroatom selected from oxygen, sulfur or NR.sub.15 ;R.sub.4 is phenyl, naphth-1-yl or naphth-2-yl, or a heteroaryl, which is unsubstituted or substituted by one or two substituents, each of which is independently selected, and which, for a 4-phenyl, 4-naphth-1-yl, 5-naphth-2-yl or 6-naphth-2-yl substituent, is halogen, cyano, nitro, --C(Z)NR.sub.7 R.sub.17, --C(Z)OR.sub.16, --(CR.sub.10 R.sub.20).sub.v COR.sub.12, --SR.sub.5, --SOR.sub.5, --OR.sub.12, halo-substituted-C.sub.1-4 alkyl, C.sub.1-4 alkyl, --ZC(Z)R.sub.12, --NR.sub.10 C(Z)R.sub.16, or --(CR.sub.10 R.sub.20).sub.v NR.sub.10 R.sub.20 and which, for other positions of substitution, is halogen, cyano, --C(Z)NR.sub.13 R.sub.14, --C(Z)OR.sub.3, --CR.sub.10 R.sub.20).sub.m"" COR.sub.3, --S(O).sub.m R.sub.3, --OR.sub.3, halosubstituted-C.sub.1-4 alkyl, --C.sub.1-4 alkyl, --(CR.sub.10 R.sub.20).sub.m"" NR.sub.10 C(Z)R.sub.3, --NR.sub.10 S(O).sub.m' R.sub.8, --NR.sub.10 S(O).sub.m' NR.sub.7 R.sub.17, --ZC(Z)R.sub.3 or --(CR.sub.10 R.sub.20).sub.m"" NR.sub.13 R.sub.14 ;v is 0, or an integer having a value of 1 or 2;m is 0, or the integer 1 or 2;m' is an integer having a value of 1 or 2;m"" is 0, or an integer having a value of 1 to 5;R.sub.c is hydrogen, C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, aryl, arylC.sub.1-4 alkyl, heteroaryl, heteroarylC.sub.1-4 alkyl, heterocyclyl, or heterocyclylC.sub.1-4 alkyl C.sub.1-4 alkylR.sub.2 is an unsubstituted or substituted cyclohexyl or cyclohexyl C.sub.1-10 alkyl;R.sub.3 is heterocyclyl, heterocyclylC.sub.1-10 alkyl or R.sub.8 ;R.sub.5 is hydrogen, C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.2-4 alkynyl or NR.sub.7 R.sub.17, excluding the moieties --SR.sub.5 being --SNR.sub.7 R.sub.17 and --SOR.sub.5 being --SOH;R.sub.7 and R.sub.17 is each independently selected from hydrogen or C.sub.1-4 alkyl or R.sub.7 and R.sub.17 together with the nitrogen to which they are attached form a heterocyclic ring of 5 to 7 members, or R.sub.7 and R.sub.17 together with the nitrogen to which they are attached form a heterocyclic ring of 5 to 7 members which ring contains an additional heteroatom selected from oxygen, sulfur or NR.sub.15 ;R.sub.8 is C.sub.1-10 alkyl, halo-substituted C.sub.1-10 alkyl, C.sub.2-10 alkenyl, C.sub.2-10 alkynyl, C.sub.3-7 cycloalkyl, C.sub.5-7 cycloalkenyl, aryl, arylC.sub.1-10 alkyl, heteroaryl, heteroarylC.sub.1-10 alkyl, (CR.sub.10 R.sub.20).sub.n OR.sub.11, (CR.sub.10 R.sub.20).sub.n S(O).sub.m R.sub.18, (CR.sub.10 R.sub.20).sub.n NHS(O).sub.2 R.sub.18, (CR.sub.10 R.sub.20).sub.n NR.sub.13 R.sub.14 ; wherein the aryl, arylalkyl, heteroaryl, heteroaryl alkyl may be unsubstituted or substituted;n is an integer having a value of 1 to 10;R.sub.9 is hydrogen, --C(Z)R.sub.11 or unsubstituted or substituted C.sub.1-10 alkyl, S(O).sub.2 R.sub.18, unsubstituted or substituted aryl or unsubstituted or substituted aryl-C.sub.1-4 alkyl;R.sub.10 and R.sub.20 is each independently selected from hydrogen or C.sub.1-4 alkyl;R.sub.11 is hydrogen, or R.sub.18 ;R.sub.12 is hydrogen or R.sub.16 ;R.sub.13 and R.sub.14 is each independently selected from hydrogen or unsubstituted or substituted C.sub.1-4 alkyl, unsubstituted or substituted aryl or unsubstituted or substituted aryl-C.sub.1-4 alkyl, or together with the nitrogen which they are attached form a heterocyclic ring of 5 to 7 members, or together with the nitrogen which they are attached form a heterocyclic ring of 5 to 7 members, which ring contains an additional heteroatom selected from oxygen, sulfur or NR.sub.9 ;R.sub.15 is hydrogen, C.sub.1-4 alkyl or C(Z)--C.sub.1-4 alkyl;R.sub.16 is C.sub.1-4 alkyl, halo-substituted-C.sub.1-4 alkyl, or C.sub.3-7 cycloalkyl;R.sub.18 is C.sub.1-10 alkyl, C.sub.3-7 cycloalkyl, heterocyclyl, aryl, arylC.sub.1-10 alkyl, heterocyclyl, heterocyclyl-C.sub.1-10 alkyl, heteroaryl or heteroarylalkyl; andZ is oxygen or sulfur;or a pharmaceutically acceptable salt thereof.