Patent ID: 6150336
Filing Date: 2000-11-21
Classification: C07J,Y10S

Abstract:
A steroidal glycoside compound of Formula I ##STR10## and the pharmaceutically-acceptable salts and hydrates thereof wherein: R.sup.1, R.sup.2 and R.sup.3 are each independently hydrogen, hydroxy, halo, amino, azido, (C.sub.1 -C.sub.6)alkoxy(C.sub.1 -C.sub.6)alkoxy or --Z--R.sup.5 ;Z for each occurrence is independently selected from the group consisting of --NH--C(.dbd.O)--, --O--C(.dbd.O)--, --O--C(.dbd.O)--N(R.sup.6)--, --NH--C(.dbd.O)--N(R.sup.6)--, --O--C(.dbd.S)--N(R.sup.6)-- and --O--C(.dbd.O)--N--(R.sup.6)--; ##STR11## wherein: - - - - - - is optionally a double bond;Q.sup.2 is --C(.dbd.O)--, --CH.sub.2 --, --C(N.dbd.OR.sup.9)-- or --CH(CH(CH.sub.3)--CH.sub.2 --CH.sub.2 --C(.dbd.O)(OR.sup.9))--; ##STR12## Q.sup.3 is --C(.dbd.O)--, --CH.sub.2 -- or Q.sup.4 is --CH.sub.2 -- or --C(.dbd.O)--; andQ.sup.5 is --CH.sub.2 -- or --C(.dbd.O)--;R.sup.5 for each occurrence is independently aryl, aryl(C.sub.1 -C.sub.6)alkyl, (C.sub.2 -C.sub.4)alkenyl, (C.sub.1 -C.sub.6)alkyl, (C.sub.3 -C.sub.7)cycloalkyl or (C.sub.3 -C.sub.7)cycloalkyl(C.sub.1 -C.sub.6)alkyl, and each R.sup.5 may be optionally mono-, di, or tri-substituted independently with halo, (C.sub.1 -C.sub.4)alkyl, hydroxy, phenoxy, trifluoromethyl, nitro, (C.sub.1 -C.sub.4)alkoxy, methylenedioxy, oxo, (C.sub.1 -C.sub.4)alkylsulfanyl, (C.sub.1 -C.sub.4)alkylsulfinyl, (C.sub.1 -C.sub.4)alkylsulfonyl, dimethylamino, mono- or di-(C.sub.1 -C.sub.4)alkylaminocarbonyl, (C.sub.1 -C.sub.4)alkylcarbonyl, (C.sub.1 -C.sub.4)alkoxycarbonyl or pyrrolidinylcarbonyl;R.sup.6 for each occurrence is independently hydrogen or (C.sub.1 -C.sub.4)alkyl, or R.sup.6 is taken together with the nitrogen to which it is attached and with R.sup.5, wherein R.sup.5 is a covalent bond, to form pyrrolidinyl, piperidinyl, N-methylpiperazinyl, indolinyl or morpholinyl, and such cyclic group may be mono-substituted on a carbon atom with (C.sub.1 -C.sub.4)alkoxycarbonyl;R.sup.9 is (C.sub.1 -C.sub.4)alkyl or aryl(C.sub.1 -C.sub.6)alkyl;m is 2, 3 or 4;wherein aryl is carbon-linked and is phenyl, furyl, thienyl, pyrrolyl, oxazolyl, isoxazolyl, oxadiazolyl, thiazolyl, isothiazolyl, benzothiazolyl, thiadiazolyl, pyrazolyl, imidazolyl or pyridyl;provided that where Q.sup.2 is --C(.dbd.N--OR.sup.9)--, Q.sup.3 is not --C(.dbd.O)--.