Patent ID: 6245745
Filing Date: 2001-06-12
Classification: A61P,C07H

Abstract:
A compound of the formula ##STR7##or a pharmaceutically acceptable salt or solvate thereof wherein:X.sup.1 and X.sup.2 are each independently selected from the group consisting of --CR.sup.6 R.sup.7 --, --S(O).sub.n -- wherein n is 0 to 2, --NR.sup.6 --, and O, except that (a) if either X.sup.1 or X.sup.2 is O, S, or S(O) then the other moiety (X.sup.1 or X.sup.2) is --CR.sup.6 R.sup.7 --; (b) if either X.sup.1 or X.sup.2 is SO.sub.2 then the other moiety (X.sup.1 or X.sup.2) is --NR.sup.6 -- or --CR.sup.6 R.sup.7 --; and (c) if X.sup.1 is --NR.sup.6 --, then X.sup.2 is SO.sub.2 or --C(O)--;R.sup.1 is H or OH;R.sup.2 is H, C.sub.1 -C.sub.6 alkyl, or halo, wherein the foregoing R.sup.2 alkyl group is optionally substituted by 1 or 2 R.sup.4 groups;or where X.sup.2 is --NR.sup.6 --, then R.sup.3 and X.sup.2 may be taken together to form a 5 to 12 membered ring, wherein said ring is saturated or partially unsaturated with up to 3 carbon-carbon double bonds, the carbon atoms of said ring are optionally subsituted by 1 to 3 R.sup.4 groups, and the ring optionally contains up to 2 additional hetero moieties (in addition to the X.sup.2 moiety which is --NR.sup.6 --) selected from O, S(O).sub.j wherein j is an integer from 0 to 2, and --NR.sup.6 --, with the proviso that two O atoms, two S atoms, an O and S atom, an N and O atom, and an N and S atom are not attached directly to each other;each R.sup.3 is independently selected from the group consisting of H, C.sub.1 -C.sub.10 alkyl, --(CR.sup.6 R.sup.7).sub.t (C.sub.6 -C.sub.10 aryl), --(CR.sup.6 R.sup.7).sub.t (4-10 membered heterocyclic), --C(O)(CR.sup.6 R.sup.7).sub.t (C.sub.6 -C.sub.10 aryl), --C(O)(CR.sup.6 R.sup.7).sub.t (4-10 membered heterocyclic), --C(O)NR.sup.6 (CR.sup.6 R.sup.7).sub.t (C.sub.6 -C.sub.10 aryl), and --C(O)NR.sup.6 (CR.sup.6 R.sup.7).sub.t (4-10 membered heterocyclic), wherein t is an integer ranging from 0 to 5, said alkyl group optionally contains 1 or 2 hetero moieties selected from O, --S(O).sub.j -- wherein j is an integer ranging from 0 to 2, and --NR.sup.6 -- with the proviso that two O atoms, two S atoms, an O and S atom, an N and O atom, and an N and S atom are not attached directly to each other; the --(CR.sup.6 R.sup.7).sub.t -- moieties of the foregoing R.sup.3 groups optionally include a carbon-carbon double or triple bond where t is an integer between 2 and 5; and the heterocyclic and aryl moieties of the foregoing R.sup.3 groups are optionally substituted by 1 to 5 R.sup.4 groups;each R.sup.4 is 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, halo, cyano, nitro, trifluoromethyl, trifluoromethoxy, azido, hydroxy, C.sub.1 -C.sub.6 alkoxy, --C(O)R.sup.5, --C(O)OR.sup.5, --NR.sup.6 C(O)OR.sup.8, --OC(O)R.sup.5, --NR.sup.6 SO.sub.2 R.sup.8, --SO.sub.2 NR.sup.5 R.sup.6, --NR.sup.6 C(O)R.sup.5, --C(O)NR.sup.5 R.sup.6, --NR.sup.5 R.sup.6, --S(O).sub.j (CR.sup.6 R.sup.7).sub.m (C.sub.6 -C.sub.10 aryl), --S(O).sub.j (C.sub.1 -C.sub.6 alkyl), --(CR.sup.6 R.sup.7).sub.m (C.sub.6 -C.sub.10 aryl), --O(CR.sup.6 R.sup.7).sub.m (C.sub.6 -C.sub.10 aryl), --NR.sup.6 (CR.sup.6 R.sup.7).sub.m (C.sub.6 -C.sub.10 aryl), --(CR.sup.6 R.sup.7).sub.m (4-10 membered heterocyclic), --C(O)(CR.sup.6 R.sup.7).sub.m (C.sub.6 -C.sub.10 aryl), and --C(O)(CR.sup.6 R.sup.7).sub.m (4-10 membered heterocyclic), wherein m is an integer from 0 to 4; j is an integer from 0 to 2, and said alkyl, alkenyl, alkynyl, aryl and heterocyclic moieties of the foregoing R.sup.4 groups are optionally substituted by 1 to 3 substituents independently selected from the group consisting of halo, cyano, nitro, trifluoromethyl, trifluoromethoxy, azido, --NR.sup.6 SO.sub.2 R.sup.8, --SO.sub.2 NR.sup.5 R.sup.6, --C(O)R.sup.5, --C(O)OR.sup.5, --OC(O)R.sup.5, --NR.sup.6 C(O)OR.sup.8, --NR.sup.6 C(O)R.sup.5, --C(O)NR.sup.5 R.sup.6, --NR.sup.5 R.sup.6, --OR.sup.5, C.sub.1 -C.sub.10 alkyl, --(CR.sup.6 R.sup.7).sub.m (C.sub.6 -C.sub.10 aryl), and --(CR.sup.6 R.sup.7).sub.m (4-10 membered heterocyclic), wherein m is an integer from 0 to 4;each R.sup.5 is independently selected from the group consisting of H, C.sub.1 -C.sub.10 alkyl, --(CR.sup.6 R.sup.7).sub.m (C.sub.6 -C.sub.10 aryl), and --(CR.sup.6 R.sup.7).sub.m (4-10 membered heterocyclic), wherein m is an integer from 0 to 4, and the foregoing R.sup.5 substituents, except H, are optionally substituted by 1 to 3 substituents independently selected from the group consisting of halo, cyano, nitro, trifluoromethyl, trifluoromethoxy, azido, --C(O)R.sup.6, --C(O)OR.sup.6, --OC(O)R.sup.6, --NR.sup.6 C(O)R.sup.7, --C(O)NR.sup.6 R.sup.7, --NR.sup.6 R.sup.7, hydroxy, C.sub.1 -C.sub.6 alkyl, and C.sub.1 -C.sub.6 alkoxy;each R.sup.6 and R.sup.7 is independently H, --C(O)(C.sub.1 -C.sub.6 alkyl), C.sub.1 -C.sub.6 alkyl or fluoro; and,R.sup.8 is selected from the substituents provided in the definition of R.sup.5 except R.sup.8 is not H.