摘要:
##STR1## New 14α,17α-ethano-estratrienes of general formula (I) wherein R 1 is a hydrogen atom, an alkyl or acyl group with 1 to 12 carbon atoms, R 2 is a hydrogen atom or a methyl group, R 3 is a hydrogen atom or an acyl group with 1 to 12 carbon atoms and (a) is either (II) or (III), where R 4 is an alkyl residue in the α or β position with 1 to 8 carbon atoms or an α,β-alkenyl residue which may contain several double bonds or an α,β-alkinyl residue, both with 2 to 8 carbon atoms, are described. Also described is a process for producing them. These new compounds have a marked oestrogenic activity.
摘要:
A 14.alpha.,17.alpha.-bridged estratriene of formula I ##STR1## wherein (a) OR.sup.3 is in .alpha.-positionR.sup.1, R.sup.2 and R.sup.3, each independently are (i) hydrogen, (ii) ##STR2## in which R.sup.4 is an organic radical with up to 11 carbon atoms or (iii) --(CH.sub.2).sub.n COOH wherein n=1-4, or (iv) R.sup.1 is a benzyl, C.sub.1 -C.sub.8 alkyl or C.sub.3 -C.sub.5 cycloalkyl, or(b) OR.sup.3 is in .beta.-positionR.sup.1, R.sup.2 and R.sup.3, each independently are (i) hydrogen, (ii) an acyl group with 1 to 12 carbon atoms or (iii) R.sup.1 is C.sub.1 -C.sub.8 alkyl, and in both (a) and (b) A--B is an etheno or ethano bridge.
摘要:
New 19,11.beta.-bridged steroids of the general formula I ##STR1## where R.sup.1 stands for a methyl or ethyl radical,R.sup.2 for a hydrogen or chlorine atom or a C.sub.1 -C.sub.4 -alkyl radical,B and G, which are the same or different, respectively for a hydrogen atom, a C.sub.1 -C.sub.4 -alkyl radical or, together, for a second bond between the carbon atoms 6 and 7,B and R.sup.2 together for a methylene or an ethylene group,Z for the radical of a pentagonal or hexagonal ring, which is possibly substituted and possibly unsaturated,V stands for a possibly substituted carbocyclic or heterocyclic aryl radical,the ring A for ##STR2## M and N together meaning a second bond or M a hydrogen atom and N a hydroxy group,X means an oxygen atom, two hydrogen atoms or a hydroxyimino grouping N.about.OH,R.sup.3 and D, which are the same or different, respectively a hydrogen atom, a nitrile radical or a C.sub.1 -C.sub.4 -alkyl radical or, together, a methylene or ethylene group,E a hydrogen atom or a C.sub.1 -C.sub.4 -alkyl radical,D and E together meaning a second bond between carbon atoms 1 and 2 or together a methylene group ##STR3## with R.sup.11 in the meaning of a hydrogen atom or a C.sub.1 -C.sub.8 -alkyl radical,are described as well as their pharmaceutically tolerated addition salts with acids. The new compounds possess valuable pharmacological properties.
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.-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:
9.alpha.-Hydroxy-19,11.beta.-bridged steroids of general formula I ##STR1## are described. The more detailed meaning of A, B, R.sup.1, R.sup.2, G, Z, R.sup.4 --Y and R.sup.4' --Y' follows from the description. The steroids of general formula I have antigestagen and/or antiglucocorticoidal action and can be used for the production of pharmaceutical agents.
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:
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:
A process of cyclizing compounds of formula II ##STR1## wherein K, V', R.sup.1 and 1 are as herein defined, is described whereby a compound of formula IVa is produced ##STR2## wherein K, V', R.sup.1, Q, S and 1 are as herein defined. The compounds of formula IVa are useful intermediates in the production of compounds of formula I ##STR3## wherein ring A, B, G, V, Z, R.sup.1 and R.sup.2 are as herein defined.
摘要:
10.beta.,11.beta.-bridged steroids of Formula I ##STR1## wherein R.sup.1 is H or methyl;R.sup.2 is H, a cyanide residue, a heteroaryl residue, a straight-chain or branched aliphatic, e.g., alkyl group of up to 20 carbon atoms, optionally exhibiting double or triple bonds and, if desired, being substituted by one or several oxo groups, a C.sub.4-7 cycloalkyl or C.sub.4-7 cycloalkenyl group, an OR.sup.3 --, SR.sup.3 --, --OSO.sub.2 --R.sup.11 -- group wherein R.sup.11 means a perfluroinated C.sub.1 -C.sub.4 -alkyl group or an NR.sup.3 R.sup.4 -group wherein R.sup.3 means an H atom or C.sub.1 -C.sub.8 -alkyl residue, R.sup.4 means R.sup.3, a cyanide or a C.sub.1 -C.sub.10 -acyl residue, or R.sup.3 and R.sup.4 jointly with the inclusion of N means of 5- or 6-membered heterocyclic ring wherein the ring can additionally contain a further hetero atom N, O, or S, or a 4-cyano-, 4-methoxy- or 4-dimethylamino-substituted phenyl group,A and B either mean jointly a further bond between C4 and C5, or A is an .alpha.-hydroxy group and B is H,X is a keto or oxime group, andZ is a pentagonal or hexagonal ring residue which is optionally substituted and optionally unsaturated,or pharmaceutically compatible acid additional salts thereof which possess antigestagen and antiglucocorticoid properties.