Patent ID: 6117911
Filing Date: 2000-09-12
Classification: A61K,C07D,G01N

Abstract:
A therapeutic method for preventing or treating a condition or symptom associated with Marfan's syndrome, fibrosis, or senile dementia, comprising administering to a mammal in need of such therapy, an effective amount of a compound of formula VI: ##STR20## wherein R.sup.6 is (C.sub.1 -C.sub.6)alkyl, or aryl, optionally substituted by 1, 2, or 3 V;R.sup.7 is phenyl, optionally substituted by 1, 2, or 3 V; or R.sup.7 is (C.sub.1 -C.sub.12)alkyl, halo(C.sub.1 -C.sub.12)alkyl, (C.sub.3 -C.sub.6)cycloalkyl, (C.sub.1 -C.sub.6)alkylcyclo(C.sub.1 -C.sub.6)alkyl, (C.sub.3 -C.sub.6)cycloalkenyl, or (C.sub.1 -C.sub.6)alkyl(C.sub.3 -C.sub.6)cycloalkenyl;R.sup.8 is hydrogen or phenyl, optionally substituted by 1, 2, or 3 V;R.sup.9 is hydrogen, halo, aryl, aryl(C.sub.1 -C.sub.3)alkyl, halo(C.sub.1 -C.sub.12)alkyl, cyano(C.sub.1 -C.sub.12)alkyl, or (C.sub.1 -C.sub.12)alkyl, wherein any aryl may optionally be substituted by 1, 2, or 3, V; or-- is a single bond or is --C(B)(D)--, wherein B and D are each independently hydrogen, (C.sub.1 -C.sub.6)alkyl, or halo;V is OPO.sub.3 H.sub.2, (C.sub.1 -C.sub.6)alkyl, (C.sub.1 -C.sub.6)alkoxy, mercapto, (C.sub.1 -C.sub.4)alkylthio, halo, trifluoromethyl, pentafluoroethyl, nitro, N(R.sub.n)(R.sub.o), cyano, trifluoromethoxy, pentafluoroethoxy, benzoyl, hydroxy, --(CH.sub.2).sub.0-4 C(.dbd.O)(C.sub.1 -C.sub.6)alkyl, --UC(.dbd.O)(C.sub.1 -C.sub.6)alkyl, benzyl, --OSO.sub.2 (CH.sub.2).sub.04 CH.sub.3, --U(CH.sub.2).sub.1-4 COOR.sub.p, --(CH.sub.2).sub.04 COOR.sub.p, --U(CH.sub.2).sub.2-4 OR.sub.p, --(CH.sub.2).sub.0-4 OR.sub.p, --U(CH.sub.2).sub.1-4 C(.dbd.O)R.sub.k, --(CH.sub.2).sub.0-4 C(.dbd.O)R.sub.k, --U(CH.sub.2).sub.1-4 R.sub.k, --(CH.sub.2).sub.0-4 R.sub.k, or --U(CH.sub.2).sub.2-4 OC(.dbd.O)R.sub.p ; wherein U is 0, N(R.sub.m), or S;Z is --(CH.sub.2).sub.1-3 --, --O--, --OCH.sub.2 --, --CH.sub.2 O--, --C(.dbd.O)O--, --N(R.sub.q)-, C.dbd.O, or a covalent bond;R.sub.k is amino, optionally substituted with one or two (C.sub.1 -C.sub.6)alkyl; or an N-heterocyclic ring optionally containing 1 or 2 additional N(R.sub.1), S, or nonperoxide O, wherein R.sub.1 is H (C.sub.1 -C.sub.6)alkyl, phenyl, or benzyl;R.sub.n and R.sub.o are independently hydrogen, (C.sub.1 -C.sub.6)alkyl, phenyl, benzyl, or (C.sub.1 -C.sub.6)alkanoyl; or R.sub.n and R.sub.o together with the nitrogen to which they are attached are a 3, 4, 5, or 6 membered heterocyclic ring;R.sub.p is H or (C.sub.1 -C.sub.6)alkyl; andR.sub.m and R.sub.q are independently hydrogen, (C.sub.1 -C.sub.6)alkyl, phenyl, benzyl, or (C.sub.1 -C.sub.6)alkanoyl;the compound is MER25;or a pharmaceutically acceptable salt thereof.