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process for the production of 17alpha - acetoxy - 11beta - 4 - (n, n - (dimethylamino) phenyl - 2 - methoxy - 19 - norpregna - 4.9 - india - 3.10 - dionintermediates of this process and process for the production of the intermediates
process for the production of 17alpha - acetoxy - 11beta - 4 - (n, n - (dimethylamino) phenyl - 2 - methoxy - 19 - norpregna - 4.9 - india - 3.10 - dionintermediates of this process and process for the production of the intermediates
A compound having general formula (I) in which R1 is a member selected from the group consisting of -OCH3, -SCH3, -N(CH3)2, -NHCH3, -CHO, -COCH3 and -CHOHCH3; R2 is a member selected from the group consisting of halogen, alkyl, acyl, hydroxy, alkoxy, acyloxy, alkyl carbonate, cypionyloxy, S-alkyl and S-acyl; R3 is a member selected from the group consisting of alkyl, hydroxy, alkoxy and acyloxy; R4 is a member selected from the group consisting of hydrogen and alkyl; and X is a member selected from the group consisting of -O and -N-OR5, wherein R5 is a member selected from the group consisting of hydrogen and alkyl. In addition to providing the compounds of formula (I), the present invention provides methods wherein the compounds of formula (I) are advantageously used, inter alia, to antagonize endogenous progesterone; to induce menses; to treat endometriosis; to treat dysmenorrhea; to treat endocrine hormone-dependent tumors; to treat uterine fibroids; to inhibit uterine endometrial proliferation; to induce labor; and for contraception.
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机译:具有通式(I)的化合物,其中R 1是选自-OCH 3,-SCH 3,-N(CH 3)2,-NHCH 3,-CHO,-COCH 3和-CHOHCH 3的成员; R 2是选自卤素,烷基,酰基,羟基,烷氧基,酰氧基,碳酸烷基酯,环酰氧基,S-烷基和S-酰基的成员; R 3是选自烷基,羟基,烷氧基和酰氧基的成员; R 4为选自氢和烷基的成员。 X是选自-O和-N-OR 5的成员,其中R 5是选自氢和烷基的成员。除了提供式(I)的化合物之外,本发明提供了其中式(I)的化合物尤其用于拮抗内源性孕酮的方法。引起月经;治疗子宫内膜异位;治疗痛经;治疗内分泌激素依赖性肿瘤;治疗子宫肌瘤;抑制子宫内膜增生;引诱劳工;和避孕。
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