Patent ID: 6288228
Filing Date: 2001-09-11
Classification: A61P,C07D

Abstract:
A compound having Formula I, ##STR13##or pharmaceutically acceptable salts or prodrugs thereof, whereinR.sub.1, R.sub.2, R.sub.3, and R.sub.4 are independently selected from the group consisting of hydrogen, C.sub.1 -C.sub.20 -alkyl, and C.sub.1 -C.sub.20 -alkanoyl; orR.sub.1 and R.sub.2 together with the nitrogen atom to which they are attached form a ring independently selected from the group consisting of morpholine, piperidine, piperazine, and pyrrolidine; orR.sub.3 and R.sub.4 together with the nitrogen atom to which they are attached form a ring independently selected from the group consisting of morpholine, piperidine, piperazine, and pyrrolidine;B is selected from the group consisting of phenyl, C.sub.3 -C.sub.10 -cycloalkyl, C.sub.4 -C.sub.10 -cycloalkenyl, azetidinyl, pyrrolidinyl, piperidinyl, pyrrolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, furanyl, thienyl, pyridyl, pyridazinyl, pyrimidinyl, and pyrazinyl;Y is selected from the group consisting of phenyl, C.sub.3 -C.sub.10 -cycloalkyl, C.sub.4 -C.sub.10 -cycloalkenyl, pyrrolidinyl, piperidinyl, morpholinyl, thiomorpholinyl, pyrrolyl, oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, furanyl, thienyl, pyridyl, pyridazinyl, pyrimidinyl, and pyrazinyl;wherein the groups defining B and Y are attached through substitutable carbon atoms or nitrogen atoms in the ring; andwherein the groups defining B and Y can be optionally substituted with 1-3 substituents independently selected from the group consisting of C.sub.1 -C.sub.20 -alkyl, C.sub.1 -C.sub.20 -alkoxy, amino, unsubstituted phenyl, azido, cyano, halo, C.sub.1 -C.sub.20 -haloalkyl, and nitro;L is selected from the group consisting of a covalent bond, --C(.dbd.W)--, C.sub.1 -C.sub.20 -alkylene, --NR.sub.5 --, --NR.sub.6 C(X)NR.sub.7 --, C.sub.2 -C.sub.20 -alkynylene, C.sub.2 -C.sub.20 -alkenylene, --O--, --S(O).sub.t --, --NR.sub.6 C(X)--, --C(X)NR.sub.6 --, --NR.sub.6 SO.sub.2 NR.sub.7 --, --NR.sub.6 SO.sub.2 --, --SO.sub.2 NR.sub.6 --, --OC(R.sub.100)(R.sub.200)--, and --C(H)(R.sub.300)--;wherein each group defined by L is shown with its left end attached to B and its right end attached to YR.sub.5 is selected from the group consisting of hydrogen, C.sub.1 -C.sub.20 -alkyl, C.sub.1 -C.sub.20 -alkanoyl, and aryl-C.sub.1 -C.sub.20 -alkyl;R.sub.6 and R.sub.7 are independently selected from the group consisting of hydrogen, C.sub.1 -C.sub.20 -alkyl, and aryl-C.sub.1 -C.sub.20 -alkyl;R.sub.100 and R.sub.200 are selected from the group consisting of hydrogen, C.sub.1 -C.sub.20 -alkyl, and C.sub.1 -C.sub.20 -alkanoyl;R.sub.300 is selected from the group consisting of hydroxy and phenyl;W is selected from the group consisting of O, S, and (.dbd.N--O--R.sub.6);X is selected from the group consisting of O and S; andt is 0-2;all of the foregoing with the proviso that the following combinations are excluded therefrom:one of B or Y is phenyl or pyridyl, and the other is phenyl or pyridyl;B is phenyl; Y is cycloalkyl; and L is --O--; andR.sub.1, R.sub.2, R.sub.3, and R.sub.4 are hydrogen; B is C.sub.3 -cycloalkyl; Y is phenyl; and L is a covalent bond.