11.beta.-phenyl-4,9,15-estratrienes, their manufacture and
pharmaceutical preparations containing same
    2.
    发明授权
    11.beta.-phenyl-4,9,15-estratrienes, their manufacture and pharmaceutical preparations containing same 失效
    11(BETA)-PHENYL-4,9,15-ESTRATRIENES,其制造和含有其的药物制剂

    公开(公告)号:US5132299A

    公开(公告)日:1992-07-21

    申请号:US458668

    申请日:1990-01-16

    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.

    摘要翻译: PCT No.PCT / DE88 / 00447 Sec。 371日期1990年1月16日 102(e)日期1990年1月16日PCT提交1988年7月15日PCT公布。 出版物WO89 / 00578 日本1月26日,1989年。新的11β型苯基-4,9,15-雌三醇,其中X表示氧原子或羟基亚氨基,N代表OH,R1代表氢 原子或甲基,R2表示氢原子,烷基或酰基,在每种情况下为1-10个碳原子,R3表示氢原子,氰基甲基, - (CH2)nCH2Z其中n表示数字 0,1,2,3,4或5,Z = -H或-OR 5,其中R 5具有氢原子或烷基或酰基的含义,在每种情况下为1-10个碳原子,或 - (CH 2) mC 3BOND CY,其中m = 0-2,Y表示氢,氯,氟,碘或溴原子,烷基,羟基烷基,烷氧基烷基或酰氧基烷基,在每种情况下为1-10个碳原子,R4表示直链或 含有至多8个碳原子的支链,饱和或不饱和烃基,其含有具有上述意义的X的分组。 这些化合物具有抗前列腺素和抗糖皮质激素活性。

    11.beta.-phenyl-14.beta.H steroids
    4.
    发明授权
    11.beta.-phenyl-14.beta.H steroids 失效
    11(BETA)-PHENYL-14(BETA)H STEROIDS

    公开(公告)号:US5244886A

    公开(公告)日:1993-09-14

    申请号:US663819

    申请日:1991-03-20

    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.

    摘要翻译: PCT No.PCT / EP89 / 01090 371日期1991年3月20日 102(e)1991年3月20日PCT PCT 1989年9月20日PCT公布。 出版物WO90 / 03385 日本1994年4月5日。通式(I)的新的11β-苯基-14βH-类固醇,其中Z是氧原子或羟基亚氨基基团N差异OH,M和N或者是共同的第二化合物 或L是氢原子,M是α-永久性羟基,A和B一起是第二化合物,D是氢原子,其中R 1是五或六部分杂烷基残基或环烷基,环烯基或芳基 残基或A是氢原子,B和D一起是亚甲基桥,其中除了上述残基之外,R 1可以是具有至多10个C原子的可能取代的烃残基,可能被取代的氨基,羟基或C 1-8烷氧基 ,巯基或硫代烷基,R2是甲基或乙基残基,R3 / R4代表类固醇化学中C17原子上取代基的通常组合,具有抗原原性和其他性质。

    11 Beta-N,N-dimethylaminophenyl-estradienes, their manufacture and
pharmaceutical preparations containing them
    6.
    发明授权
    11 Beta-N,N-dimethylaminophenyl-estradienes, their manufacture and pharmaceutical preparations containing them 失效
    11β-N,N-二甲基氨基苯基 - 雌二醇,其制备和含有它们的药物制剂

    公开(公告)号:US4829060A

    公开(公告)日:1989-05-09

    申请号:US832604

    申请日:1986-02-24

    IPC分类号: A61K31/565 A61P5/38 C07J41/00

    CPC分类号: C07J41/0083

    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.

    摘要翻译: 给出了通式I(I)的11个β-芳基 - 雌二醇的描述,其中X表示氧原子或羟基亚氨基N差异OH,其中羟基可以在顺式或反位,R1表示 甲基或乙基R2表示-C3OND C-CH = CH2,-CH2-(CH2)nY-R3或-CH = CH-(CH2)mY-R3基团,Y表示氧或硫原子, n为0或1,m为1,2或3,R3为氢原子,分别为具有1至4个碳原子的烷基或酰基,条件是当m表示1时,Y表示氧 原子,R3表示具有1至4个碳原子的烷基。 新的11β-芳基 - 雌二醇具有抗前列腺素和抗糖皮质激素作用。