发明名称 Androgen glycosides and androgenic activity thereof
摘要 A compound having the Formula (III) where; the dotted line represents a single or double bond; the rings P and Q are independently, saturated or partially unsaturated; R is hydrogen or a straight or branched chain glycosidic residue containing 1-20 glycosidic units per residue, or R is an orthoester glycoside moiety of the formula (IV). Regarding formula (IV): the semi-dotted ring indicated at "C" is a glycofuranosyl or glycopyranosyl ring; R8- is hydrogen, c1-4 alkyl, C7-10 aralkyl, phenyl, phenyl substituted by chloro, fluoro, bromo, iodo, C1-4 alkyl, or C1-4 alkoxy, or is napthyl; R9 is hydrogen or a straight or branched chain glycosidic residue containing 1-20 glycoside units; R1 is hydrogen, C1-4 alkyl, C2-4 alkenyl, C2-4 alkynyl, C1-4 alkanoyl or R1 and R' together with the atoms to which they are attached, form a carbonyl group; R2 is hydrogen or C-1-4 alkyl; R3 is hydrogen or hydroxy; R4 where present is hydrogen or a halogen atom; R5 is absent or is hydrogen or C1-4 alkyl; R6 is hydrogen or C1-4; R14 is hydrogen or C1-4 alkyl; A is oxygen, =CH, .C=CHOH, or is the group >CHR13, where R13 is hydrogen or a C1-4 alkyl group, or A and B together form an optionally substituted pyrazole or isoxazole ring; B is a carbonyl group, =CH, >CH2, .CHOR7 or =C(OR7), where R7 hydrogen or a straight or branched chain glycosidic residue containing 1-20 glycoside units, or R7 is an orthoester glycoside moiety of the Formula (V). Regarding formula (V) where; the semi-dotted ring indicated at "D" represents a glycofurnosyl or glycopyranosyl ring; R10 is hydrogen, C1-4 alkyl, C7-10 aralkyl, phenyl, phenyl substituted by chloro, fluoro, bromo, iodo, C1-4 alkyl or C1-4 alkoxy, or is napthyl, and R11 is hydrogen or a straight or branched chain glycosidic residue containing 1-20 glycoside units, and esters thereof; Provided that when R is hydrogen, the B is .CHOR7 or =C(OR7)-, and R7 is a glycosidic residue or orthoester glycoside moiety, and provided that the compound is not: - testosterone glucoside, 17Beta-oestradiol-17-glucoside, 17Beta-)(Beta-D-glucopyranosyloxy)-5Alpha-androstan-3-one, an unsubstituted glycoside of epiandrosterone, a glucopyranoside of androstenediol or an ester thereof or a 17-glucopyranosyloxy derivative of the 3-oxo, 4-deshydro, 6-hydro analogue of dehydroepiandrosterone.
申请公布号 NZ515134(A) 申请公布日期 2004.01.30
申请号 NZ20000515134 申请日期 2000.05.04
申请人 STRAKAN LIMITED 发明人 HOLICK, MICHAEL FRANCIS;KANIS, JOHN ANTONY
分类号 A61K31/7028;A61P3/00;A61P5/26;A61P15/10;A61P15/16;A61P19/10;A61P31/18;C07J17/00;C07J71/00;(IPC1-7):C07J17/00;A61K31/58 主分类号 A61K31/7028
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