Patent ID: 6114372
Filing Date: 2000-09-05
Classification: A61P,C07C,C07D

Abstract:
A compound of general formula (I) ##STR13## wherein: X is N;R.sup.1 is selected from the group consisting of C.sub.1-6 alkyl, C.sub.2-6 alkenyl, aryl, C.sub.1-6 alkyl-aryl, heteroaryl, C.sub.1-6 alkylheteroaryl, cyclo(C.sub.3-6)alkyl, C.sub.1-6 alkyl-cyclo(C.sub.3-6)alkyl, heterocyclo(C.sub.4-6)alkyl, C.sub.1-6 alkyl-heterocyclo(C.sub.4-6)alkyl, C.sub.1-6 alkyl-COR.sup.2, and C.sub.1-6 alkyl-AR.sup.3 group where A is selected from the group consisting of O, NR.sup.3 and S(O).sub.n where n=0-2 and R.sup.3 is selected from the group consisting of H, C.sub.1-4 alkyl, aryl, heteroaryl, C.sub.1-4 alkyl-aryl and C.sub.1-4 alkyl-heteroaryl; if A=NR.sup.3 the groups R.sup.3 may be the same or different;R.sup.2 is OR.sup.4 or N(R.sup.4).sub.2 where each R.sup.4 may be the same or different;R.sup.4 is H or C.sub.1-4 alkyl;R.sup.5 is selected from the group consisting of aryl (optionally substituted with R.sup.6), heteroaryl (optionally substituted with R.sup.6), C.sub.1-4 alkyl-aryl (optionally substituted with R.sup.6), C.sub.1-4 alkyl-heteroaryl (optionally substituted with R.sup.6), C.sub.1-4 alkyl (optionally substituted with R.sup.6), cyclo(C.sub.3-6) alkyl (optionally substituted with R.sup.6), C.sub.1-4 alkyl-cyclo(C.sub.3-6)alkyl (optionally substituted with R.sup.6), heterocyclo(C.sub.4-6)alkyl (optionally substituted with R.sup.6) and C.sub.1-4 alkyl-heterocyclo(C.sub.4-6)alkyl (optionally substituted with R.sup.6);R.sup.6 is selected from the group consisting of halogen, C.sub.1-6 alkyl, aryl, heteroaryl, AR.sup.3, NR.sup.3 R.sup.7, COR.sup.9, SO.sub.2 N(R.sup.3).sub.2 where each R.sup.3 may be the same or different, CO.sub.2 R.sup.4, CON(R.sup.3).sub.2 where each R.sup.3 may be the same or different, amidine and guanidine;R.sup.7 is selected from the group consisting of COR.sup.20, CO.sub.2 R.sup.19, SO.sub.2 R.sup.9, and CO(NR.sup.3).sub.2 where each R.sup.3 may be the same or different;R.sup.8 is H or COR.sup.9 ;R.sup.9 is selected from the group consisting of C.sub.1-4 alkyl, aryl, heteroaryl, C.sub.1-4 alkyl-aryl and C.sub.1-4 alkyl-heteroaryl;R.sup.10 and R.sup.11 are the same or different and are each selected from the group consisting of H, C.sub.1-6 alkyl (optionally substituted with R.sup.12), aryl (optionally substituted with R.sup.12), C.sub.1-6 alkyl-aryl (optionally substituted with R.sup.12), heteroaryl (optionally substituted with R.sup.12), C.sub.1-6 alkyl-heteroaryl (optionally substituted with R.sup.12), cyclo(C.sub.3-6) alkyl (optionally substituted with R.sup.12), C.sub.1-6 alkyl-cyclo(C.sub.3-6)alkyl (optionally substituted with R.sup.12), heterocyclo(C.sub.4-6)alkyl (optionally substituted with R.sup.12) and C.sub.1-4 alkyl-heterocyclo(C.sub.4-6)alkyl (optionally substituted with R.sup.12);R.sup.12 is selected from the group consisting of SO.sub.2 R.sup.9, SO.sub.2 N(R.sup.3).sub.2 where each R.sup.3 may be the same or different, SR.sup.8, COR.sup.13, N(R.sup.3).sub.2 where each R.sup.3 may be the same or different, NR.sup.3 R.sup.14, OR.sup.3, phthalimido and the groups: ##STR14## p and q are each 0 or 1 and may be the same or different; R and S are each CH or N and may be the same or different;W is O, S(O).sub.n where n=0-2, or NR.sup.15 ;Z is H or C.sub.0-4 alkyl-R.sup.18 and may be attached to any available position on the ring;R.sup.13 is selected from the group consisting of OR.sup.20, N(R.sup.3).sub.2 where each R.sup.3 may be the same or different, C.sub.1-4 alkyl, aryl, C.sub.1-4 alkyl-aryl, heteroaryl and C.sub.1-4 alkyl-heteroaryl;R.sup.14 may be any group defined in R.sup.7 or COR.sup.16 ;R.sup.15 is selected from the group consisting of H, C.sub.1-4 alkyl, COR.sup.9, CO.sub.2 R.sup.19, CON(R.sup.3).sub.2 where each R.sup.3 may be the same or different and SO.sub.2 R.sup.9 ;R.sup.16 is C.sub.1-4 alkyl-R.sup.17 ;R.sup.17 is selected from the group consisting of CO.sub.2 R.sup.4, CON(R.sup.3).sub.2 where each R.sup.3 may be the same or different, N(R.sup.3).sub.2 where each R.sup.3 may be the same or different, SO.sub.2 R.sup.9 and the groups: ##STR15## R.sup.18 is selected from the group consisting of CO.sub.2 R.sup.3, CON(R.sup.3).sub.2 where each R.sup.3 may be the same or different, N(R.sup.3).sub.2 where each R.sup.3 may be the same or different, NHCO.sub.2 R.sup.19, NHSO.sub.2 R.sup.9 and NHCOR.sup.9 ;R.sup.19 is selected from the group consisting of C.sub.1-4 alkyl, C.sub.1-4 alkyl-aryl, and C.sub.1-4 alkyl-heteroaryl;R.sup.20 is selected from the group consisting of H, C.sub.1-4 alkyl, C.sub.1-4 alkyl-aryl and C.sub.1-4 alkyl-heteroaryl;and the salts, solvates and hydrates thereof.