Patent ID: 6316429
Filing Date: 2001-11-13
Classification: A61P,C07D

Abstract:
A compound having the chemical structure: ##STR207##or a physiologically acceptable salt thereof wherein:A and D are nitrogen and B and E are carbon or B and E are nitrogen and A and D are carbon, it being understood that when A, B, D, or E is nitrogen, R.sup.3, R.sup.4, R.sup.5 or R.sup.6, respectively, does not exist;R.sup.1 is selected from the group consisting of hydrogen, (C.sub.1 -C.sub.4)alkyl, (C.sub.3 -C.sub.7)cycloalkyl, aryl, hydroxy, (C.sub.1 -C.sub.4)alkoxy, --C(O)OR"", --C(O)NR.sup.10 R.sup.11 and --S(.dbd.O).sub.2 R"";R.sup.2 is selected from the group consisting of hydrogen and unsubstituted (C.sub.1 -C.sub.4)alkyl;R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are independently selected from the group consisting of hydrogen, (C.sub.1 -C.sub.4)alkyl optionally substituted with a group selected from the group consisting of --C(O)OR"", halo, mompholino, piperazinyl, piperidinyl and pyrrolidinyl, trihalomethyl, (C.sub.3 -C.sub.7)cycloalkyl, (C.sub.2 -C.sub.4)alkenyl, (C.sub.2 -C.sub.4)alkynyl, phenyl optionally substituted with one or more groups independently selected from the group consisting of halo, trihalomethyl, hydroxy, unsubstituted (C.sub.1 -C.sub.4)alkoxy, --C(O)OR"", cyano, nitro, and --NR.sup.10 R.sup.11, a heteroaryl group selected from the group consisting of pyrrole, furan, thiophene, oxazole, thiazole, imidazole, pyridine, pyrimidine, optionally substituted with one or more groups selected from the group consisting of halo, trihalomethyl, hydroxy, unsubstituted (C.sub.1 -C.sub.4)alkyl, unsubstituted (C.sub.1 -C.sub.4)alkoxy, --C(O)OR"", cyano, nitro, and --NR.sup.10 R.sup.11, S(O).sub.2 R"", --S(O).sub.2 NR.sup.10 R.sup.11, --S(O).sub.2 morpholino, --S(O).sub.2 N(4-CF.sub.3 phenyl), --C(O)OR"", --C(O)CH.sub.2 morpholino, cyano, nitro, halo, O-carbamyl, N-carbamyl, amino and --NR.sup.10 R.sup.11 ;R.sup.3 and R.sup.4, R.sup.4 and R.sup.5, or R.sup.4 and R.sup.5 may combine to form a phenyl ring or a heteroaryl ring selected from the group consisting of pyrrole, furan, thiophene, oxazole, thiazole, imidazole, pyridine, pyrimidine, optionally substituted with one or more groups selected from the group consisting of halo, trihalomethyl, hydroxy, unsubstituted (C.sub.1 -C.sub.4)alkyl, unsubstituted (C.sub.1 -C.sub.4)alkoxy, --C(O)OR', cyano, nitro, and --NR.sup.10 R.sup.11 ;Q is a heteroaryl group having the following structure: ##STR208##J is selected from the group consisting of oxygen, nitrogen and sulfur;K, L and M are independently selected from the group consisting of carbon, nitrogen, oxygen and sulfur such that the five-member heteroaryl ring formed is one known in the chemical arts, it being understood that when K, L and M are nitrogen, sulfur or oxygen, R.sup.8 or -(alk.sub.1).sub.n Z cannot be covalently bonded to that atom;when J is nitrogen, R.sup.7 is selected from the group consisting of hydrogen, unsubstituted (C.sub.1 -C.sub.4)alkyl, unsubstituted (C.sub.3 -C.sub.7)cycloalkyl, --C(O)OR"", C(O)R"", --S(O).sub.2 R"", OS(O).sub.2 CF.sub.3 and --S(O).sub.2 (CH.sub.2).sub.2 Si(CH.sub.3).sub.3, it being understood that when J is oxygen or sulfur, R.sup.7 does not exist;R.sup.8 is selected from the group consisting of hydrogen, (C.sub.1 -C.sub.4)alkyl optionally substituted with a group selected from the group consisting of --C(O)OR"", --NHC(O)OR"" and halo, trihalomethyl, unsubstituted (C.sub.3 -C.sub.7)cycloalkyl, (C.sub.2 -C.sub.4)alkenyl optionally substituted with a --C(O)OR"" group, unsubstituted (C.sub.2 -C.sub.4)alkynyl, unsubstituted (C.sub.1 -C.sub.4)alkoxy, --S(O).sub.2 R"", --S(O).sub.2 NR.sup.10 R.sup.11 --C(O)OR"", cyano, nitro, halo, C-amido, N-amido, amino, --NR.sup.10 R.sup.11, --CH.sub.2 CH.sub.2 CH.sub.2 CH.sub.2 -- covalently bonded at two adjacent carbon atoms of the Q ring, --CH.dbd.CHCH.dbd.CH-- covalently bonded at two adjacent carbon atoms of the Q ring, --CH.dbd.CCICH.dbd.CH-- covalently bonded at two adjacent carbon atoms of the Q ring and --CH.dbd.C(O(C.sub.1 -C.sub.4)alkyl)HCH.dbd.CH-- covalently bonded at two adjacent carbon atoms of the Q ring;R.sup.10 and R.sup.11 are independently selected from the group consisting of hydrogen, unsubstituted (C.sub.1 -C.sub.4)alkyl, unsubstituted (C.sub.3 -C.sub.7)cycloalkyl, phenyl, --C(O)R"" and --S(O).sub.2 R"";R"" is selected from the group consisting of hydrogen, (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)cycloalkyl, phenyl optionally substituted with one or more groups selected from the group consisting of (C.sub.1 -C.sub.4)alkyl, halo, amino, --NR.sup.10 R.sup.11, trihalomethy and (C.sub.1 -C.sub.4)alkoxy;alk.sub.1 is a (C.sub.1 -C.sub.4)alkyl group;n is 0 to 10, inclusive; andZ is a polar group selected from the group consisting of hydroxy, --C(O)OR, OC(O)R"", --C(O)NR.sup.10 R.sup.11, --NR.sup.10 R.sup.11, --NHC(O)R"", --NHS(O).sub.2 R"", --OC(O)NR.sup.10 R.sup.11, --NHC(O)NR.sup.10 R.sup.11, --C(O)morpholino and morpholino.