摘要:
The invention relates to 15,16-methylene-17-hydroxy-19-nor-21-carboxylic acid-steroid γ-lactone derivatives with the general chemical formula I, and R4, R6a, R6b, R7 and Z have the meanings stated in claim 1, and their solvates, hydrates, stereoisomers and salts. The invention further relates to the use of these derivatives for the production of a medicinal product for oral contraception and for the treatment of pre-, peri- and postmenopausal complaints and medicinal products that contain said derivatives. The derivatives according to the invention have a progestational and in preferred cases additionally an antimineralocorticoid and neutral to slightly androgenic action.
摘要:
The 17β-cyano-19-androst-4-ene derivatives of the present invention possess gestagenic activity. They have the general chemical formula 1, in which Z is selected from the group comprising O, two hydrogen atoms, NOR and NNHSO2R, in which R is hydrogen or C1-C4-alkyl, R1, R2 are each independently hydrogen or methyl, or R1 and R2 together form methylene or are omitted with formation of a double bond between C1 and C2, R4 is hydrogen or halogen, furthermore either: R6a, R6b together form methylene or 1,2-ethanediyl or R6a is hydrogen and R6b is selected from the group comprising hydrogen, methyl and hydroxymethylene, and R7 is selected from the group comprising hydrogen, C1-C4-alkyl, C2-C3-alkenyl and cyclopropyl, or: R6a hydrogen and R6b and R7 together form methylene or are omitted with formation of a double bond between C6 and C7 or: R6a is methyl and R6b and R7 are omitted with formation of a double bond between C6 and C7, R15, R16 are hydrogen or together form methylene, R17 is selected from the group comprising hydrogen, C1-C4-alkyl and allyl, and moreover comprise their solvates, hydrates, stereoisomers, diastereomers, enantiomers and salts, with the proviso that particular compounds are excluded.
摘要:
The 15α,16α-methylene-17-hydroxy-19-nor-17-pregna-4-en-3-one-21-carboxylic acid γ-lactone derivatives of the present invention possess progestational efficacy. They have the general chemical formula I, in which Z is selected from the group comprising an oxygen atom, two hydrogen atoms, NOR and NNHSO2R, where R is hydrogen, C1-C10-alkyl, aryl or C7-C20-aralkyl, R4 is hydrogen or halogen, and moreover either: R6a, R6b together form methylene or 1,2-ethanediyl or R6a is hydrogen and R6b is selected from the group comprising hydrogen, C1-C10-alkyl, C2-C10-alkenyl or C2-C10-alkynyl, and R7 is selected from the group comprising hydrogen, C1-C10-alkyl, C3-C6-cycloalkyl, C2-C10-alkenyl or C2-C10-alkynyl, or: R6a is hydrogen and R6b and R7, together, denote a bond, an oxygen or form methylene, R18 represents hydrogen or C1-C3-alkyl and in addition include their solvates, hydrates, stereoisomers and salts.
摘要:
The invention relates to 15,16-methylene-17-(1′-propenyl)-17-3′-oxidoestra-4-en-3-one derivatives with the general chemical formula I, where the Z, R4, R6a, R6b, R7 and R18 have the meanings stated in claim 1, and solvates, hydrates and salts thereof, including all crystal modifications and all stereoisomers of these compounds. The invention also relates to the use of these derivatives for the production of a drug for oral contraception and for the treatment of pre-, peri- and postmenopausal problems and drugs which contain such derivatives, in particular use in the aforesaid indications. The derivatives according to the invention have a progestational and in preferable cases also an antimineralcorticoid and neutral to slight androgenic activity.
摘要翻译:本发明涉及具有一般化学式I的15,16-亚甲基-17-(1'-丙烯基)-17-3'-氧代雌-4-烯-3-酮衍生物,其中Z,R4,R6a,R6b R 7和R 18具有权利要求1所述的含义,并溶剂合物,其水合物和盐,包括这些化合物的所有晶体改性和所有立体异构体。 本发明还涉及这些衍生物用于生产口服避孕药物和用于治疗绝经前,绝经期和绝经后问题的药物以及含有此类衍生物的药物,特别是在上述适应症中使用。 根据本发明的衍生物具有促孕作用,并且在优选情况下还具有抗铁皮质激素和中性至轻度雄激素活性。
摘要:
The invention relates to 17-(1′-propenyl)-17-3′-oxidoestra-4-en-3-one derivatives with the general chemical formula I, where the residues Z, R4, R6a, R6b, R7, R15, R16a, R16b and R18 have the meanings stated in Claim 1, and their solvates, hydrates and salts, including all stereoisomers of these compounds. The invention further relates to the use of these derivatives for the production of a medicinal product for oral contraception and for the treatment of pre-, peri- and postmenopausal complaints and medicinal products that contain said derivatives, and in particular application in the aforementioned indications. The derivatives according to the invention have a progestational and in preferred cases additionally an antimineralocorticoid and neutral to slightly androgenic action.
摘要:
The invention relates to 17-(1′-propenyl)-17-3′-oxidoestra-4-en-3-one derivatives with the general chemical formula I, where the residues Z, R4, R6a, R6b, R7, R15, R16a, R16b and R18 have the meanings stated in Claim 1, and their solvates, hydrates and salts, including all stereoisomers of these compounds. The invention further relates to the use of these derivatives for the production of a medicinal product for oral contraception and for the treatment of pre-, peri- and postmenopausal complaints and medicinal products that contain said derivatives, and in particular application in the aforementioned indications. The derivatives according to the invention have a progestational and in preferred cases additionally an antimineralocorticoid and neutral to slightly androgenic action.
摘要:
The invention relates to 17-hydroxy-19-nor-21-carboxylic acid-steroid γ-lactone derivatives with the chemical formula I, where R4, R6a, R6b, R7, R15, R16a, R16b, R18 and Z have the meanings stated in claim 1, and their solvates, hydrates, stereoisomers and salts. The invention further relates to the use of these derivatives for the production of a medicinal product for oral contraception and for the treatment of pre-, peri- and postmenopausal complaints and medicinal products that contain said derivatives. The derivatives according to the invention have a progestational and in preferred cases additionally an antimineralocorticoid and neutral to slightly androgenic action.
摘要:
The invention relates to novel 18-methyl-19-nor-17-pregn-4-en-21,17-carbolactones of general formula (I), where Z=O, H2, ═NOR or ═NNHSO2R, where R=H, a straight- or branched-chain 1-4 or 3-4 C alkyl group, R4=H, halogen, methyl or trifluoromethyl, R6 and/or R7 can be α- or β-positioned and independently=branched- or straight-chain 1-4 or 3-4 alkyl, or R6=H and R7=a- or β-positioned, straight- or branched-chain 1-4 or 3-4 C alkyl, or R6 and R7=H, or R6 and R7 together=a- or β-positioned methylene or an additional bond. The novel compounds have gestagenic and antimineralocorticoid activity and are suitable for the production of pharmaceutical preparations, for example, for oral contraception and the treatment of pre-, peri- and post-menopausal pain.
摘要:
The present invention describes non-steroidal compounds of the general formula (I) in which A is in which X1 means one or more groups on the phenyl ring and represents independently of one another a halogen, OH, (C1-C4)alkyl, (C1-C4)alkyl-O, (C3-C6)cycloalkyl-O, (C1-C14)acyl-O, (C1-C4)alkenyl, (C1-C4)alkynyl, perfluoro(C1-C4)alkyl radical, —CHO or CN, and X2 means one or more groups on the phenyl ring and represents independently of one another an H, halogen, OH, (C1-C4)alkyl, (C1-C4)alkyl-O, (C1-C4)alkenyl, (C1-C4)alkynyl, perfluoro-(C1-C4)alkyl radical, —CHO or CN, as Estrogens.
摘要:
The present invention relates to acyltryptophanols of the general formula I, in which R1, R2, R3, Q and X have the meaning as defined in the description.The compounds according to the invention are effective FSH antagonists and can be used for example for fertility control in men or in women, or for the prevention and/or treatment of osteoporosis.