Patent ID: 6194438
Filing Date: 2001-02-27
Classification: A61P,C07F

Abstract:
A compound of the formula ##STR14##or a pharmaceutically acceptable salt thereof, wherein:R.sup.1 and R.sup.2 are each independently selected from the group consisting of C.sub.1 -C.sub.10 alkyl, C.sub.2 -C.sub.10 alkenyl, C.sub.2 -C.sub.10 alkynyl, --(CH.sub.2).sub.p (C.sub.6 -C.sub.10 aryl), and --(CH.sub.2).sub.p (4-10 membered unsaturated heterocyclyl), wherein p is an integer from 0 through 3, or R.sup.1 and R.sup.2 form a C.sub.3 -C.sub.6 cycloalkyl ring, and wherein any of said R.sup.1 and R.sup.2 groups are optionally substituted with 1 to 3 R.sup.6 groups, provided that when R.sup.1 and R.sup.2 form a C.sub.3 -C.sub.6 cycloalkyl ring, said C.sub.3 -C.sub.6 cycloalkyl ring is substituted with at least one R.sup.6 selected from C.sub.2 -C.sub.10 alkenyl, C.sub.2 -C.sub.10 alkynyl, and --(CH.sub.2).sub.t (C.sub.6 -C.sub.10) aryl wherein t is an integer from 1 to 3;and wherein one or both of R.sup.1 and R.sup.2 is --(CH.sub.2).sub.p (6 membered unsaturated heterocyclyl containing one or more nitrogen atoms);R.sup.3 is --(CH.sub.2).sub.m (4-10 membered heterocyclyl) optionally substituted with 1 to 5 R.sup.6 groups;m in the aforementioned R.sup.3 groups is independently an integer from 0 through 6; and R.sup.4 is C.sub.6 -C.sub.10 aryl, 4-10 membered heterocyclyl, or C.sub.1 -C.sub.6 alkyl, each of said R.sup.4 groups being optionally substituted by 1 to 3 R.sup.6 groups;each R.sup.5 is independently selected from halo, C.sub.1 -C.sub.6 alkyl substituted by 1 to 3 halo, nitro, cyano, --OR.sup.9, --C(O)R.sup.9, --SR.sup.9, --SO.sub.2 R.sup.9, --SO.sub.3 H, --S(O)R.sup.7, --NR.sup.7 R.sup.8, --C(O)OR.sup.9, --OC(O)R.sup.9, --SO.sub.2 NR.sup.9 R.sup.8, --C(O)NR.sup.9 R.sup.8, --NR.sup.8 C(O)R.sup.9, --OC(O)NR.sup.9 R.sup.8, --C(O)ONR.sup.7 R.sup.9, --NR.sup.8 C(O)NR.sup.9 R.sup.8, --NR.sup.8 C(O)O(C.sub.1 -C.sub.4 alkyl), --C(NR.sup.8)NR.sup.9 R.sup.8, --C(NCN)NR.sup.9 R.sup.8, --C(NCN)S(C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 haloalkyl), --NR.sup.8 C(NCN)S(C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 haloalkyl), --NR.sup.8 C(NCN)NR.sup.7 R.sup.8, --NR.sup.8 SO.sub.2 (C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 haloalkyl), --NR.sup.8 C(O)C(O)R.sup.8, --NR.sup.8 C(O)C(O)NR.sup.9 R.sup.8, --P(O)(OR.sup.7).sub.2, and --(CH.sub.2).sub.q (4-10 membered heterocyclyl), q is an integer from 0 through 3, and the alkyl and heterocyclyl moieties of the foregoing R.sup.5 groups are optionally substituted by 1 to 3 R.sup.10 groups;each R.sup.6 is independently selected from R.sup.5, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.10 alkenyl, C.sub.2 -C.sub.10 alkynyl and --CH.sub.2).sub.t (C.sub.6 -C.sub.10 aryl) optionally substituted with1 to 3 R.sup.10 groups, t being an integer from 0 through 3;each R.sup.7 is independently hydrogen or C.sub.1 -C.sub.4 alkyl optionally substituted by 1 to 3 halo;each R.sup.8 is independently R.sup.7 or --OR.sup.7 ;each R.sup.9 is independently selected from hydrogen, C.sub.1 -C.sub.6 alkyl, --(CH.sub.2).sub.q (C.sub.6 -C.sub.10 aryl), and --(CH.sub.2 ).sub.q (4-10 membered heterocyclyl), said R.sup.9 groups, except H, are optionally substituted with 1 to 3 R.sup.10 groups, and each q is independently an integer from 0 through 3; and,each R.sup.10 is independently selected from halo, nitro, cyano, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 haloalkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 haloalkoxy, --C(O)O(C.sub.1 -C.sub.6 alkyl), and C.sub.6 -C.sub.10 aryl; with the proviso that R.sup.1 and R.sup.2 are not both simultaneously C.sub.1 -C.sub.10 alkyl.