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    • 10. 发明授权
    • Depot steroid esters
    • 酯类固醇酯
    • US4119626A
    • 1978-10-10
    • US74841176
    • 1976-12-08
    • SCHERING AG
    • SCHULZE PAUL-EBERHARDSPECK ULRICHBITTLER DIETERWIECHERT RUDOLFACKSTEINER BERNARD
    • A61K31/565A61K31/567A61K31/57C07J1/00C07J3/00C07J5/00C07J7/00C07J11/00C07J21/00C07J31/00C07J53/00
    • C07J1/0048C07J1/0096C07J5/0053C07J11/00C07J21/006C07J31/006C07J53/005C07J53/008
    • Steroid esters of the Formula I I wherein the A, B, C, and D rings can be substituted in the usual manner, R10 is hydrogen or methyl; R13 is alkyl of 1-3 carbon atoms; R17 is 17 alpha -alkynyl or alkadiinyl of up to 4 carbon atoms or 17 beta -acetyl, Z is X-OH, Y-CO-OH, X-O-CO-Y-CO-OH, X-O-CO-R, Y-CO-OR, X-O-CO-Y-CO-OR, or X-O-SO2-R; X is a straight-chain or branched alkylene of 1-6 carbon atoms, optionally interrupted by O or S atoms, wherein the chain or branches can be substituted by -OH, -O-CO-R, or -O-SO2-R; Y is a direct bond, a straight-chain or branched carbon chain of 1-3 atoms, optionally interrupted by an O or S atom if Y is linked to the steroid residue via -O-CO-; of 1-16 atoms if Y is linked to X via -O-CO; or 1,4-phenylene, 1,4-cyclohexylene, or 1,3-cyclopentylene optionally substituted by alkyl of 1-2 carbon atoms, or groups analogously 1,2- and 1,3-disubstituted, respectively; and R is an optionally substituted alkyl of up to 22 carbon atoms, have longer acting activity than the corresponding unesterified steroids and higher activity than the corresponding long chain esters.
    • 式I的类固醇,其中A,B,C和D环可以通常的方式被取代,R 10是氢或甲基; R13是1-3个碳原子的烷基; R 17为17个α-炔基或至多4个碳原子的烷基亚烷基或17个β-乙酰基,Z为X-OH,Y-CO-OH,XO-CO-Y-CO-OH,XO-CO-R, CO-OR,XO-CO-Y-CO-OR或XO-SO2-R; X是1-6个碳原子的直链或支链亚烷基,任选被O或S原子中断,其中链或支链可以被-OH,-O-CO-R或-O-SO2-R ; Y是直接键,1-3个原子的直链或支链碳链,如果Y通过-O-CO-连接到类固醇残基,任选被O或S原子中断; 如果Y通过-O-CO与X连接,则为1-16个原子; 或1,4-亚苯基,1,4-亚环己基或任选被1-2个碳原子的烷基取代的1,3-亚环戊基,或分别为1,2-和1,3-二取代的基团; 并且R是任选取代的至多22个碳原子的烷基,具有比相应的未酯化的类固醇更长的作用活性和比相应的长链酯更高的活性。