摘要:
1-Alkyl androsta-1,4-diene-3,17-diones of the formula ##STR1## wherein R.sub.1 is a methyl, ethyl, hydroxymethyl, C.sub.1 -C.sub.3 -alkoxymethyl, or C.sub.1 -C.sub.4 -alkanoyloxymethyl group, R.sub.6 is a hydrogen atom or a methyl group, and R.sub.7 is a hydrogen atom or a methyl group in the 7.alpha.- or 7.beta.-position, are useful for fertility control and for the treatment of estrogen-triggered diseases.
摘要:
Compounds of the formula I ##STR1## wherein R.sub.1 is ##STR2## wherein R.sup.I and R.sup.II each independently is alkyl of 1-4 carbon atoms, or R.sup.I and R.sup.II together with the connecting N-atom form a 5- or 6-membered heterocyclic ring whose remaining atoms are all C-atoms, or which also includes and additional N-atom, an additional O or S atom or a combination thereof; ##STR3## wherein R.sup.I and R.sup.II are as defined above; --SR.sup.III, wherein R.sup.III is methyl, ethyl or phenyl; or--OR.sup.IV, wherein R.sup.IV is methyl, ethyl, propyl, methoxymethyl, allyl, or .beta.-dimethylaminoethyl;R.sub.2 is hydrogen, methyl, or ethyl; ##STR4## wherein the wavy lines mean that the substituent is in the .alpha.- or .beta.-position, and ##STR5## M is Na, K or Li; and R.sup.V, R.sup.VI, R.sup.VII and R.sup.VIII each independently is alkyl of 1-4 carbon atoms, have valuable pharmacological properties, e.g., a combination of antiprogestational and antimineralocorticordal effects.
摘要:
C-homoestratrienes of the formula ##STR1## wherein ##STR2## R.sub.1 and R.sub.2 are the same or different, and each is hydrogen, acyl, alkyl, cycloalkyl or tetrahydropyranyl; andR.sub.3 is hydrogen, ethynyl or chloroethynyl; possess very good estrogenic properties.
摘要:
This invention describes the new 7&agr;-(5-methylaminopentyl)-estratrienes of general formula I in which R2 stands for a hydrogen or fluorine atom, R17 stands for a hydrogen atom, a methyl or ethinyl group, n stands for 2, 3 or 4, and x stands for 0, 1 or 2. The new compounds are strong, pure antiestrogens and can be used for the production of pharmaceutical agents for treatment of estrogen-dependent diseases, for example, breast cancer, endometrial carcinoma, prostatic hyperplasia, anovulatory infertility and melanoma.
摘要:
This invention describes new, substituted 7&agr;-(&egr;-aminoalkyl)-estratrienes of general formula I in which side chain SK is a radical of partial formula The new compounds represent compounds with very strong antiestrogenic action. The compounds according to the invention are, on the one hand, pure antiestrogens, or, on the other hand, antiestrogens with estrogenic partial action. Based on this spectrum of action, the new compounds are highly suitable for the production of pharmaceutical agents for tumor therapy and hormone replacement treatment.
摘要:
This invention describes the new 11&bgr;-halogen-7&agr;-substituted estratrienes of general formula I in which R11 is a fluorine or chlorine atom, and the other substituents have the meanings that are explained in more detail in the description. The compounds have antiestrogenic properties or tissue-selective estrogenic properties and are suitable for the production of pharmaceutical agents.
摘要:
This invention describes new, substituted 7.alpha.-(.xi.-aminoalkyl)-estratrienes of general formula I ##STR1## in which side chain SK is a radical of partial formula ##STR2## as well as their physiologically compatible addition salts with organic and inorganic acids.The new compounds represent compounds with very strong antiestrogenic action.The compounds according to the invention are, on the one hand, pure antiestrogens, or, on the other hand, antiestrogens with estrogenic partial action. Based on this spectrum of action, the new compounds are highly suitable for the production of pharmaceutical agents for tumor therapy and hormone replacement treatment.
摘要:
This invention describes new, substituted 7.alpha.-(.xi.-aminoalkyl)-estratrienes of general formula I ##STR1## in which side chain SK is a radical of partial formula ##STR2## as well as their physiologically compatible addition salts with organic and inorganic acids.The new compounds represent compounds with very strong antiestrogenic action.The compounds according to the invention are, on the one hand, pure antiestrogens, or, on the other hand, antiestrogens with estrogenic partial action. Based on this spectrum of action, the new compounds are highly suitable for the production of pharmaceutical agents for tumor therapy and hormone replacement treatment.
摘要:
Bicycloalkane derivatives of the formula ##STR1## wherein n is 1 or 2, R.sub.1 is lower alkyl, Acyl is alkanoyl, and Y is --S--R.sub.2, --SO.sub.m --R.sub.2, or ##STR2## wherein m is 1 or 2, R.sub.2 is alkyl, R.sub.3 is hydrogen or lower alkyl, R.sub.4 is acyl or phenyl optionally substituted with lower alkoxy, benzyloxy or alkanoyloxy; and Z is nitro, lower alkoxycarbonyl, lower alkanoyl, lower alkylsulfinyl, or lower alkylsulfonyl are useful intermediates in the total synthesis of steroids. The compounds are prepared by reacting a corresponding compound lacking the CH.sub.2 Y substituent with formaldehyde and a mercaptan or sulfinic acid, followed if desired by oxidation and optional salt condensation.
摘要:
Benzopyran derivatives of the formula ##STR1## wherein R.sub.1 and R.sub.3 each are lower alkyl; n is the integer 1 or 2; --A--B-- is >CH--CH.sub.2 - or >CH=CH-; X is a free, esterified or etherified hydroxy group; and Y is H or X and Y collectively are =O; and W is --(CH.sub.2).sub.3 --Z--R.sub.4 ##STR2## --(CH.sub.2).sub.3 --COOR.sub.6 or --(CH.sub.2).sub.3 CN, wherein V is halogen, Z is a ketalized carbonyl group or a free, esterified or etherified hydroxymethylene group; R.sub.4 and R.sub.5 each are lower alkyl and R.sub.6 is alkyl, aryl or aralkyl, are valuable intermediates in the synthesis of steroids.