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Steroid process for preparing the same pharmaceutical composition steroid use and contraception process
Steroid process for preparing the same pharmaceutical composition steroid use and contraception process
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机译:类固醇的制备方法与制备相同药物组合物的类固醇使用及避孕方法
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摘要
A steroid with a 17-spiromethylene lactone group having formula I CHEM wherein R1 is O, (H,H), (H,OR), or NOR, R being selected from H, (1-6C) alkyl and (1-6C) acyl; R2 is H, (1-6C) alkyl optionally substituted by a halogen, (2-6C) alkenyl optionally substituted by a halogen, (2-6C) alkynyl optionally substituted by a halogen, or halogen; R2' is H; or R2' together with R2 is a (1-6C) alkylidene group or a (2-6C) alkenylidene group; or R2' together with R3 is a bond; R3 is H if not together with R2' a bond; R4 is (1-6C) alkyl; one of R5 and R6 is hydrogen and the other is hydrogen or (1-6C) alkyl; X is (CH2)n or (CnH2n-2) wherein n is 2 or 3, which is optionally substituted with hydroxy, halogen, (1-6C) alkyl, (1-6C) acyl, (7-9C) phenylalkyl, the phenyl group of which may be substituted with (1-6C) alkyl, (1-6C) alkoxy, hydroxy or halogen; Y is O or (H,OH); and the dotted lines indicate optional bonds, at least one of bonds 4-5, 5-10, and 9-10 being a double bond. The steroids of the invention have progestational activity and can be used as contraceptives.
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机译:具有式I 的17-螺亚甲基内酯基的甾族化合物,其中R1为O,(H,H),(H,OR)或NOR,R选自H,(1-6C)烷基和(1 -6C)酰基; R 2为H,任选被卤素取代的(1-6C)烷基,任选被卤素取代的(2-6C)烯基,任选被卤素取代的(2-6C)炔基或卤素; R2'为H; R2’与R2一起是(1-6C)亚烷基或(2-6C)亚烯基。或R2'与R3一起为键;如果R3不与R2'成键,则R3为H; R4为(1-6C)烷基; R5和R6之一是氢,另一个是氢或(1-6C)烷基。 X为(CH 2)n或(C n H 2n-2),其中n为2或3,其任选地被羟基,卤素,(1-6C)烷基,(1-6C)酰基,(7-9C)苯基烷基取代,其苯基可以被(1-6C)烷基,(1-6C)烷氧基,羟基或卤素取代; Y为O或(H,OH);虚线表示任选的键,键4-5、5-10和9-10中的至少一个是双键。本发明的类固醇具有孕激素活性,可以用作避孕药。
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