摘要:
11 .beta.-(4-isopropenylphenyl)-estra-4,9-dienes of general Formula I ##STR1## wherein X is an oxygen atom or a hydroxyimino grouping N OH,R.sup.1 is a hydrogen atom or a methyl group,R.sup.2 is a hydrogen atom or an acyl residue of 1-10 carbon atoms,R.sup.3 is a hydrogen atom, the cyanomethyl group, --(CH.sub.2).sub.n --, CH.sub.2 Z, --CH.dbd.CH--(CH.sub.2).sub.m Z or --C.tbd.C--Y wherein n=0 to 5 and m=1 to 4, Z meaning a hydrogen atom or the OR.sup.4 group with R.sup.4 meaning a hydrogen atom, an alkyl or alkanoyl group each of 1-4 carbon atoms, and Y meaning a hydrogen, chlorine, fluorine, iodine or bromine atom, an alkyl, hydroxyalkyl, alkoxyalkyl or acyloxyalkyl group each of 1-4 carbon atoms in the alkyl or acyl residue, possess antiprogestational activity.
摘要:
11 .beta.-(4-isopropenylphenyl)-estra-4,9-dienes of general Formula I ##STR1## wherein X is an oxygen atom or a hydroxyimino grouping ##STR2## R.sup.1 is a hydrogen atom or a methyl group, R.sup.2 is a hydrogen atom or an acyl residue of 1-10 carbon atoms,R.sup.3 is a hydrogen atom, the cyanomethyl group, --(CH.sub.2).sub.n --, CH.sub.2 Z, --CH.dbd.CH--(CH.sub.2).sub.m Z or --C.dbd.CC--Y wherein n=0 to 5 and m=1 to 4, Z meaning a hydrogen atom or the OR.sup.4 group with R.sup.4 meaning a hydrogen atom, an alkyl or alkanoyl group each of 1-4 carbon atoms, and Y meaning a hydrogen, chlorine, fluorine, iodine or bromine atom, an alkyl, hydroxyalkyl, alkoxyalkyl or acyloxyalkyl group each of 1-4 carbon atoms in the alkyl or acyl residue, possess antiprogestational activity, e.g., for treating hormonal dependent tumors, and also antiglucocorticoidal activity.
摘要:
11.beta.-substituted steroids of the formula ##STR1## wherein A and B together represent a second bond between the 6-position and 7-position carbon atoms, or, respectively, are each H;X is O, two H atoms or hydroximino;Z is the residue of a pentagonal or hexagonal ring which is optionally substituted and optionally saturated;R.sup.1 is vinyl, C.sub.3-7 -cyclo-1-alkenyl, phenyl, naphthyl or 5- or 6-membered heterocyclic aromatic having at least one N, O or S atom, each being unsubstituted or substituted by 1-3 halogen atoms, 1-3 C.sub.1-4 -alkyl, C.sub.1-4 -alkoxy, C.sub.1-4 -acyl, C.sub.2-10 -alkenyl, C.sub.1-4 -acyloxy, phenyl, nitro, hydroxy, carboxy, cyanide, COOR.sup.4 or amino optionally substituted by 1-2 C.sub.1-4 -alkyl;R.sup.2 is methyl or ethyl,R.sup.3 is H, Cl or methyl; andR.sup.4 is C.sub.1-4 -alkyl optionally substituted by phenyl which itself is optionally substituted by C.sub.1-4 -alkyl, C.sub.1-4 -alkoxy, halogen or phenylhave valuable pharmacological properties.
摘要:
Descriptions are given of 11.beta.-aryl-estradienes of general formula I ##STR1## where X means an oxygen atom or a hydroxyimino group N.about.OH, where the hydroxy group may be in the syn or anti position,R.sup.1 means a methyl or ethyl groupR.sup.2 means a --C.tbd.C--CH.dbd.CH.sub.2, a --CH.sub.2 --(CH.sub.2).sub.n --Y--R.sup.3 or a --CH.dbd.CH--(CH.sub.2).sub.m --Y--R.sup.3 group,Y standing for an oxygen or sulfur atom, n for numbers 0 or 1, m for numbers 1, 2 or 3 and R.sup.3 for a hydrogen atom, for an alkyl or acyl radical with 1 to 4 carbon atoms respectively,with the proviso that when m stands for 1 and Y for an oxygen atom, R.sup.3 means an alkyl radical with 1 to 4 carbon atoms.The new 11.beta.-aryl-estradienes possess antigestagenic and antiglucocorticoid effects.
摘要:
11.beta.-Arylestradienes of general Formula I are disclosed ##STR1## wherein R.sup.2 is a hydrogen atom, a methyl group, or an ethyl group,R.sup.3 is a hydrogen atom or an acyl group,R.sup.1 and A-B have various meanings,which possess antigestagen and antimineralocorticoid activity.
摘要:
13.alpha.-alkylgonanes of formula I ##STR1## where R is an acyl radical with as many as 10 C-atoms, andX is an oxygen atom or the grouping N--OH,have a strong antigestagenic effect and can be used for postcoital fertility control.
摘要:
13-alkyl-11.beta.-phenyl-gonanes of general formula I ##STR1## wherein A and B together stand for an oxygen atom, a CH.sub.2 group or a second bond between carbon atoms 9 and 10,X is an oxygen atom or the hydroxyimino grouping N.about.OH,R.sub.1 is a straight-chained or branched, saturated or unsaturated alkyl radical with up to 8 carbon atoms, which contains the grouping ##STR2## with X as described above, R.sub.2 is a methyl or ethyl radical in the .alpha. or .beta. position,R.sub.9, R.sub.10, R.sub.11 and R.sub.12 each stand for a hydrogen atom, a hydroxy, alkyl, alkoxy or acyloxy group with 1 to 4 carbon atoms respectively or a halogen atom and R.sub.3 and R.sub.4 have a variety of meanings, have antigestagenic and antiglucocorticoid effects.
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:
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:
Disclosed are novel 14,17.alpha.-etheno- and -ethanoestratrienes according to general Formula I ##STR1## wherein X is a --CH.sub.2 --CH.sub.2 or ##STR2## R.sup.1 is a hydrogen atom, a C.sub.1 - to C.sub.15 -acyl, benzoyl, C.sub.1 - to C.sub.15 -alkyl, C.sub.3 - to C.sub.9 -cycloalkyl or alkylcycloalkyl group, andR.sup.2 is the grouping ##STR3## wherein R.sup.3 and R.sup.4 independently of each other mean a hydrogen atom or a straight-chain or branched, optionally partially or completely fluorinated C.sub.1 -C.sub.8 -alkyl group,a process for their preparation, pharmaceutical preparations containing these compounds, as well as their use for the production of medicinal agents.The novel compounds exhibit strong antiestrogenic efficacy.