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SYNTHESIS AND SEPARATION OF OPTICALLY ACTIVE ISOMERS AND CYCLOPROPYL DERIVATIVES OF SPIRONOLACTONE AND THEIR BIOLOGICAL ACTION
SYNTHESIS AND SEPARATION OF OPTICALLY ACTIVE ISOMERS AND CYCLOPROPYL DERIVATIVES OF SPIRONOLACTONE AND THEIR BIOLOGICAL ACTION
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机译:螺内酯的光学活性异构体和环丙基衍生物的合成,分离及其生物学作用
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摘要
Methods for separation and synthesis of the optically active 7-thioester isomers and mono or bis-cyclopropyl derivatives of spironolactone are provided. Preferred stereoisomerically purified 7-thioester isomers and mono or bis-cyclopropyl derivatives of spironolactone have fewer effects mediated by gonadal steroid receptors relative to effects mediated by minteralocorticoid progesterone receptors, compared to the stereoisomerically unpurified form of the compound. These optically active compounds can be useful for obtaining reduction in moderate essential hypertension and in the treatment of congestive heart failure in humans with minimized undesirable side effects such as gynecomastia, tender breast enlargement and menstrual irregularities in women, and loss of libido in
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