摘要:
There are provided 13-alkyl-11beta-phenyl-gonanes of formula I ##STR1## wherein Z is an oxygen atom or N--OH;R.sup.2 is alpha- or beta-position methyl or ethyl;R.sup.1 is selected from heteroaryl radicals, cycloalkyl radicals, cycloalkenyl radicals, aryl radicals, alkenyl radicals, and alkyl radicals where R.sup.2 is in the alpha-position and an ethyl radical where R.sup.2 is in the beta-position; andR.sup.3 and R.sup.4 are selected from one of two different groups of substituent pairs, the group from which the selection is made being determined by the position of R.sup.2.
摘要翻译:提供式I的13-烷基-11β-苯基 - 正膦(I)其中Z是氧原子或N-OH; R2是α-或β-位甲基或乙基; R 1选自杂芳基,环烷基,环烯基,芳基,烯基和其中R2为α-位的烷基和R2为β-位的乙基; 并且R3和R4选自两个不同取代基组之一,进行选择的基团由R2的位置确定。
摘要:
New 11.beta. phenyl-4,9,15-estratrienes of formula I ##STR1## are described, where X implies an oxygen atom or a hydroxyimino grouping N.about.OH,R.sup.1 stands for a hydrogen atom or a methyl group,R.sup.2 implies a hydrogen atom, an alkyl radical or an acyl radical with in each case 1 to 10 carbon atoms,R.sup.3 stands for a hydrogen atom, a cyanomethyl group, --(CH.sub.2).sub.n CH.sub.2 Z where n implies the numbers 0, 1, 2, 3, 4 or 5, Z=--H or --OR.sup.5 with R.sup.5 having the significance of a hydrogen atom or an alkyl or acyl group with in each case 1 to 10 carbon atoms, or for --(CH.sub.2).sub.m --C.tbd.C--Y where m=0-2 and Y implies a hydrogen, chlorine, fluorine, iodine or bromine atom, an alkyl, hydroxyalkyl, alkoxyalkyl or acyloxyalkyl group with in each case 1 to 10 carbon atoms,R.sup.4 represents a straight-chain or branched-chain, saturated or unsaturated hydrocarbon radical with up to 8 carbon atoms which contains the grouping ##STR2## with X having the above significance. The compounds have antigestagenic and antiglucocorticoid activity.
摘要:
There are provided 13-alkyl-11beta-phenyl-gonanes of formula I ##STR1## wherein Z is an oxygen atom or N--OH;R.sup.2 is alpha- or beta-position methyl or ethyl;R.sup.1 is selected from heteroaryl radicals, cycloalkyl radicals, cycloalkenyl radicals, aryl radicals, alkenyl radicals, and alkyl radicals where R.sup.2 is in the alpha-position and an ethyl radical where R.sup.2 is in the beta-position; andR.sup.3 and R.sup.4 are selected from one of two different groups of substituent pairs, the group from which the selection is made being determined by the position of R.sup.2.
摘要翻译:提供式I的13-烷基-11β-苯基 - 正膦(I)其中Z是氧原子或N-OH; R2是α-或β-位甲基或乙基; R 1选自杂芳基,环烷基,环烯基,芳基,烯基和其中R2为α-位的烷基和R2为β-位的乙基; 并且R3和R4选自两个不同取代基组之一,进行选择的基团由R2的位置确定。
摘要:
New 11.beta.-phenyl-14.beta.H-steroids of general formula (I), where Z is an oxygen atom or the hydroxyimino-grouping N.about.OH, and M and N are either jointly a second compound or L is a hydrogen atom and M is an .alpha.-permanent hydroxy group and either A and B together are a second compound and D is a hydrogen atom, where R.sup.1 is a five or six-part heteroalkyl residue or a cycloalkyl, cycloalkenyl or aryl residue or A is a hydrogen atom and B and D together are a methylene bridge, where R.sup.1 besides the aforementioned residues may be a possibly substituted hydrocarbon residue with up to 10 C atoms, a possibly substituted amino group, a hydroxy or C.sub.1-8 alkoxy, mercapto or thioalkyl group, R.sup.2 is a methyl or ethyl residue, and R.sup.3 /R.sup.4 represents the usual combination of substituents on the C17 atom in steroid chemistry, having antigestagenic and other properties.
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:
A pharmaceutical agent contains a progesterone synthesis inhibitor (ProI) of the trilostane or epostane type and an antigestagen (AG). It can be used for inducing delivery at term in humans and animals, for terminating normal or pathological pregnancies therein or for treatment of hormone-dependent tumors, endometriosis or dysmenorrhea.
摘要:
An agent containing at least one compound having antiprogestational activity and at least one compound having anti-estrogenic activity is disclosed. The agent is suitable for the induction of labor, termination of preganancy, as well as for the treatment of gynecological disorders.