Patent ID: 6239138
Filing Date: 2001-05-29
Classification: A61P,C07C,C07D

Abstract:
A compound according to formula (1): ##STR19##wherein:R.sup.1 is R.sup.7, or A-C.sub.0-4 alkyl, A-C.sub.2-4 alkenyl, A-C.sub.2-4 alkynyl, A-C.sub.3-4 oxoalkenyl, A-C.sub.3-4 oxoalkynyl, A-C.sub.1-4 aminoalkyl, A-C.sub.3-4 aminoalkenyl, A-C.sub.3-4 aminoalkynyl, optionally substituted by any accessible combination of one or more of R.sup.10 or R.sup.7 ;X is O, C(O)NR', or NR'C(O);A is H, C.sub.3-6 cycloalkyl, Het or Ar;R.sup.7 is --COR.sup.8, --COCR'.sub.2 R.sup.9, --C(S)R.sup.8, --S(O).sub.m OR', --S(O).sub.m NR'R"", --PO(OR'), --PO(OR).sub.2, --B(OR).sub.2, --NO.sub.2, or tetrazolyl;each R.sup.8 independently is --OR', --NRR"", --NR'SO.sub.2 R', --NR'OR', or --OCR'.sub.2 CO(O)R';R.sup.9 is --OR', --CN, --S(O).sub.r R', --S(O).sub.m NR'.sub.2, --C(O)R', C(O)NR'.sub.2, or --CO.sub.2 R';R.sup.10 is H, halo, --OR.sup.11, --CN, --NR'R.sup.11, --NO.sub.2, --CF.sub.3, CF.sub.3 S(O).sub.r --, --CO.sub.2 R', --CONR'.sub.2, A-C.sub.0-6 alkyl-, A-C.sub.1-6 oxoalkyl-, A-C.sub.2-6 alkenyl-, A-C.sub.2-6 alkynyl-, A-C.sub.0-6 alkyloxy-, A-C.sub.0-6 alkylamino- or A-C.sub.0-6 alkyl-S(O).sub.r -;R.sup.11 is R', --C(O)R', --C(O)NR'.sub.2, --C(O)OR', --S(O).sub.m R', or --S(O).sub.m NR'.sub.2 ;R.sup.2 is ##STR20##W is --(CHR.sup.g).sub.a --U--(CHR.sup.g).sub.b --;U is absent or CO, CR.sup.g.sub.2, C(.dbd.CR.sup.g.sub.2), S(O).sub.k, O, NR.sup.g, CR.sup.g OR.sup.g, CR.sup.g (OR.sup.k)CR.sup.g.sub.2, CR.sup.g.sub.2 CR.sup.g (OR.sup.k), C(O)CR.sup.g.sub.2, CR.sup.g.sub.2 C(O), C(O)NR.sup.i, NR.sup.i C(O), OC(O), C(O)O, C(S)O, OC(S), C(S)NR.sup.g, NR.sup.g C(S), S(O).sub.2 NR.sup.g, NR.sup.g S(O).sub.2 N.dbd.N, NR.sup.g NR.sup.g, NR.sup.g CR.sup.g.sub.2, NR.sup.g CR.sup.g.sub.2, CR.sup.g.sub.2 O, OCR.sup.g.sub.2, C.tbd.C or CR.sup.g.dbd.CR.sup.g ;G is NR.sup.e, S or O,R.sub.g is H, C.sub.1-6 alkyl, Het-C.sub.0-6 alkyl, C.sub.3-7 cycloalkyl-C.sub.0-6 alkyl or Ar-C.sub.0-6 alkyl;R.sup.k is R.sup.g, --C(O)R.sup.g, or --C(O)OR.sup.f ;R.sup.i is is H, C.sub.1-6 alkyl, Het-C.sub.0-6 alkyl, C.sub.3-7 cycloalkyl-C.sub.0-6 alkyl, Ar-C.sub.0-6 alkyl, or C.sub.1-6 alkyl substituted by one to three groups chosen from halogen, CN, NR.sup.g.sub.2, OR.sup.g, SR.sup.g, CO.sub.2 R.sup.g, and CON(R.sup.g).sub.2 ;R.sup.f is H, C.sub.1-6 alkyl or Ar-C.sub.1-6 alkyl;R.sup.e is H, C.sub.1-6 alkyl, Ar-C.sub.1-6 alkyl, Het-C.sub.1-6 alkyl, C.sup.3-7 cycloalkyl-C.sub.1-6 alkyl, or (CH.sub.2).sub.k CO.sub.2 R.sup.g ;R.sup.b and R.sup.c are independently selected from H, C.sub.1-6 alkyl, Ar-C.sub.0-6 alkyl, Het-C.sub.0-6 alkyl, or C.sub.3-6 cycloalkyl-C.sub.0-6 alkyl, halogen, CF.sub.3, OR.sup.f, S(O).sub.k R.sup.f, COR.sup.f, NO.sub.2, N(R.sup.f).sub.2, CO(NR.sup.f).sub.2, CH.sub.2 N(R.sup.f).sub.2, or R.sup.b and R.sup.c are joined together to form a five or six membered aromatic or non-aromatic carbocyclic or heterocyclic ring, optionally substituted by up to three substituents chosen from halogen, CF.sub.3, C.sub.1-4 alkyl, OR.sup.f, S(O).sub.k R.sup.f, COR.sup.f, CO.sub.2 R.sup.f, OH, NO.sub.2, N(R.sup.f).sub.2, CO(NR.sup.f).sub.2, and CH.sub.2 N(R.sup.f).sub.2 ; or methylenedioxy;Q.sup.1, Q.sup.2, Q.sup.3 and Q.sup.4 are independently N or C--R.sup.y, provided that no more than one of Q.sup.1, Q.sup.2, Q.sup.3 and Q.sup.4 is N;R' is H, C.sub.1-6 alkyl, Ar-C.sub.0-6 alkyl or C.sub.3-6 cycloalkyl-C.sub.0-6 alkyl;R"" is R', --C(O)R' or --C(O)OR';R'"" is H, C.sub.1-6 alkyl, Ar-C.sub.0-6 alkyl, Het-C.sub.0-6 alkyl, or C.sub.3-6 cycloalkyl-C.sub.0-6 alkyl, halogen, CF.sub.3, OR.sup.f, S(O).sub.k R.sup.f, COR.sup.f, NO.sub.2, N(R.sup.f).sub.2, CO(NR.sup.f).sub.2, CH.sub.2 N(R.sup.f).sub.2 ;R.sup.y is H, halo, --OR.sup.g, --SR.sup.g, --CN, --NR.sup.g R.sup.k, --NO.sub.2, --CF.sub.3, CF.sub.3 S(O).sub.r --, --CO.sub.2 R.sup.g, --COR.sup.g or --CONR.sup.g.sub.2, or C.sub.1-6 alkyl optionally substituted by halo, --OR.sup.g, --SR.sup.g, --CN, --NR.sup.g R"", --NO.sub.2, --CF.sub.3, R'S(O).sub.r --, --CO.sub.2 R.sup.g, --COR.sup.g or --CONR.sup.9.sub.2 ;a is 0, 1 or 2;b is 0, 1 or 2;k is 0, 1 or 2;m is 1 or 2;r is 0, 1 or 2;s is 0, 1 or 2;u is 0 or 1;andv is 0 or 1;or a pharmaceutically acceptable salt thereof.