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    Branched chain and cycloaliphatic esters of the androstane and oestrane series and pharmaceutical compositions containing same
    1.
    发明授权
    Branched chain and cycloaliphatic esters of the androstane and oestrane series and pharmaceutical compositions containing same 失效
    雄甾烷和雌二醇系的支链和脂环族酯以及含有它们的药物组合物

    公开(公告)号：US4329296A

    公开(公告)日：1982-05-11

    申请号：US120608

    申请日：1980-02-12

    申请人： Lambert J. W. M. Tax

    发明人： Lambert J. W. M. Tax

    IPC分类号： A61K31/565 ,  C07J1/00 ,  A61K31/56

    CPC分类号： C07J1/0074 ,  C07J1/0025 ,  Y10S514/874

    摘要： There are disclosed branched chain and cycloaliphatic esters of steroids having the formula: ##STR1## or the 5.alpha.H analog thereof, where R is H or CH.sub.3 ;R.sub.1 is H or CH.sub.3 ;R.sub.2 is H or CH.sub.3 ;R.sub.3 is H, OH, CH.sub.3 or Cl;R.sub.4 is H or C.sub.1 to C.sub.4 alkyl;R.sub.5 is H, C.sub.1 to C.sub.4 alkyl or CF.sub.3 ;R.sub.6 is H, C.sub.1 to C.sub.4 alkyl, C.sub.1 to C.sub.4 alkoxy,halogen or .beta.--OH providing that when R.sub.6 is .beta.--OH, the steroid also contains 9.alpha.--F.The steroid esters have androgenic, anabolic, oestrogenic or anti-oestrogenic properties depending upon the ring configurations and the substituent(s). Pharmaceutical compositions containing the steroid esters are also disclosed.

    摘要翻译： 公开了具有下式的类固醇的支链和脂环族酯：其中R是H或CH 3; R1是H或CH3; R2是H或CH3; R3是H，OH，CH3或Cl; R4是H或C1-C4烷基; R5是H，C1-C4烷基或CF3; R6为H，C1至C4烷基，C1至C4烷氧基，卤素或β-OH，条件是当R6为β-OH时，类固醇也含有9个α-F。 甾族酯具有取决于环构型和取代基的雄激素，合成代谢，雌激素或抗雌激素特性。 还公开了含有类固醇酯的药物组合物。

    Branched chain and cycloaliphatic esters of the androstane and destrane series and pharmaceutical compositions containing same
    2.
    发明授权
    Branched chain and cycloaliphatic esters of the androstane and destrane series and pharmaceutical compositions containing same 失效
    雄甾烷和脱水系列的支链和脂环族酯以及含有它们的药物组合物

    公开(公告)号：US4307086A

    公开(公告)日：1981-12-22

    申请号：US120607

    申请日：1980-02-12

    申请人： Lambert J. W. M. Tax

    发明人： Lambert J. W. M. Tax

    IPC分类号： A61K31/565 ,  C07J1/00 ,  A01N45/00

    CPC分类号： C07J1/0074 ,  C07J1/0025 ,  Y10S514/874

    摘要： There are disclosed branched chain and cycloaliphatic esters of steroids having the formula: ##STR1## where R is H or CH.sub.3 ;R.sub.1 is H or CH.sub.3 ;R.sub.2 is H or CH.sub.3 ;R.sub.3 is H, OH, CH.sub.3 or Cl;R.sub.4 is H or C.sub.1 to C.sub.4 alkyl;R.sub.5 is H, C.sub.1 to C.sub.4 alkyl or CF.sub.3 ;R.sub.6 is H, C.sub.1 to C.sub.4 alkyl, C.sub.1 to C.sub.4 alkoxy, halogen or .beta.-OH providing that when R.sub.6 is .beta.-OH, the steroid also contains 9.alpha.-F and further providing that R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 represent at least 4 and at most 5 hydrogen atoms, except in the case of a .DELTA..sup.1,4 -steroid, in which case R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are all hydrogen;R.sub.7 is H or CH.sub.3 ;R.sub.8 is ##STR2## providing the R.sub.8 is --OH or ##STR3## when the steroid has an aromatic ring A and the 3-position is substituted by ##STR4## R.sub.9 is ##STR5## where n is 0, 1 or 2;R.sub.10 is C.sub.1 to C.sub.10 alkyl;R.sub.11 is H or C.sub.1 to C.sub.10 alkyl;R.sub.12 is an aliphatic group with 1 to 18 carbon atoms, or R.sub.10 and R.sub.12 taken together with the carbon atom to which they are attached form a C.sub.7 to C.sub.12 cycloaliphatic group providing the total carbon atom content in the carboxylic acid residue is 8 to 20;ring A is either saturated or has one of the following types of unsaturation: .DELTA..sup.1 ; .DELTA..sup.4 ; .DELTA..sup.1,4 ; .DELTA..sup.5(10) ; .DELTA..sup.1,3,5(10), andX is .dbd.O, --OH or ##STR6## providing that X is OH or ##STR7## when the steroid has an aromatic ring A, The steroid esters have androgenic, anabolic, oestrogenic or anti-oestrogenic properties depending upon the ring configurations and the substituent(s). Pharmaceutical compositions containing the steroid esters are also disclosed.

    摘要翻译： 公开了具有下式的类固醇的支链和脂环族酯：其中R是H或CH 3; R1是H或CH3; R2是H或CH3; R3是H，OH，CH3或Cl; R4是H或C1-C4烷基; R5是H，C1-C4烷基或CF3; R6为H，C1至C4烷基，C1至C4烷氧基，卤素或β-OH，条件是当R6为β-OH时，类固醇还含有9个α-F，并进一步提供R1，R2，R3，R4，R5和 R6代表至少4个和至多5个氢原子，除了在DELTA1,4-甾类的情况下，其中R1，R2，R3，R4，R5和R6都是氢; R7是H或CH3; R8是，当类固醇具有芳环A且3位被 R9取代时，R8是-OH或，其中n是0,1或2; R10为C1〜C10烷基; R11为H或C1〜C10烷基; R12是具有1至18个碳原子的脂族基团，或者R10和R12与它们所连接的碳原子一起形成C7至C12脂环族基团，其中羧酸残基中的总碳原子含量为8至20; 环A饱和或具有以下不饱和度之一：DELTA 1; DELTA 4; DELTA 1,4; DELTA 5（10）; DELTA 1,3,5（10），X为= O，-OH或，当类固醇具有芳环A时，X为OH或。类固醇酯具有雄激素，合成代谢，雌激素或 取决于环构型和取代基的抗雌激素特性。 还公开了含有类固醇酯的药物组合物。

    Branched chain and cycloaliphatic esters of the androstane and oestrane series and pharmaceutical compositions containing same
    4.
    发明授权
    Branched chain and cycloaliphatic esters of the androstane and oestrane series and pharmaceutical compositions containing same 失效
    雄甾烷和雌二醇系的支链和脂环族酯以及含有它们的药物组合物

    公开(公告)号：US4212864A

    公开(公告)日：1980-07-15

    申请号：US852326

    申请日：1977-11-17

    申请人： Lambert J. W. M. Tax

    发明人： Lambert J. W. M. Tax

    IPC分类号： A61K31/565 ,  C07J1/00 ,  C07J43/00

    CPC分类号： C07J1/0074 ,  C07J1/0025 ,  Y10S514/874

    摘要： There are disclosed branched chain and cycloaliphatic esters of steroids having the formula: ##STR1## or the 5.alpha.H analog thereof, where R is H or CH.sub.3 ;R.sub.1 is H or CH.sub.3 ;R.sub.2 is H or CH.sub.3 ;R.sub.3 is H, OH, CH.sub.3 or Cl;R.sub.4 is H or C.sub.1 to C.sub.4 alkyl;R.sub.5 is H, C.sub.1 to C.sub.4 alkyl or CF.sub.3 ;R.sub.6 is H, C.sub.1 to C.sub.4 alkyl, C.sub.1 to C.sub.4 alkoxy, halogen or .beta.-OH providing that when R.sub.6 is .beta.-OH, the steroid also contains 9.alpha.-F and further providing that R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 represent at least 4 and at most 5 hydrogen atoms, except in the case of a .DELTA..sup.1,4 -steroid, in which case R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are all hydrogen;R.sub.7 is H or CH.sub.3 ; ##STR2## providing the R.sub.8 is --OH or ##STR3## when the steroid has an aromatic ring A and the 3-position is substituted by ##STR4## R.sub.9 is ##STR5## where n is 0, 1 or 2;R.sub.10 is C.sub.1 to C.sub.10 alkyl;R.sub.11 is H or C.sub.1 to C.sub.10 alkyl;R.sub.12 is an aliphatic group with 1 to 18 carbon atoms, or R.sub.10 and R.sub.12 taken together with the carbon atom to which they are attached form a C.sub.7 to C.sub.12 cycloaliphatic group providing the total carbon atom content in the carboxylic acid residue is 8 to 20;ring A is either saturated or has one of the following types of unsaturation: .DELTA..sup.1 ; .DELTA..sup.4 ; .DELTA..sup.1,4 ; .DELTA..sup.5(10) ; .DELTA..sup.1,3,5(10), andX is .dbd.O, --OH or ##STR6## providing that X is OH or ##STR7## when the steroid has an aromatic ring A. The steroid esters have androgenic, anabolic, oestrogenic or anti-oestrogenic properties depending upon the ring configurations and the substituent(s). Pharmaceutical compositions containing the steroid esters are also disclosed.

    摘要翻译： 公开了具有下式的类固醇的支链和脂环族酯：其中R是H或CH 3; R1是H或CH3; R2是H或CH3; R3是H，OH，CH3或Cl; R4是H或C1-C4烷基; R5是H，C1-C4烷基或CF3; R6为H，C1至C4烷基，C1至C4烷氧基，卤素或β-OH，条件是当R6为β-OH时，类固醇还含有9个α-F，并进一步提供R1，R2，R3，R4，R5和 R6代表至少4个和至多5个氢原子，除了在DELTA1,4-甾类的情况下，其中R1，R2，R3，R4，R5和R6都是氢; R7是H或CH3; 当类固醇具有芳香环A并且3位被 R9取代时，提供R8是-OH或，其中n是0,1或2; R10为C1〜C10烷基; R11为H或C1〜C10烷基; R12是具有1至18个碳原子的脂族基团，或者R10和R12与它们所连接的碳原子一起形成C7至C12脂环族基团，其中羧酸残基中的总碳原子含量为8至20; 环A饱和或具有以下不饱和度之一：DELTA 1; DELTA 4; DELTA 1,4; DELTA 5（10）; DELTA 1,3,5（10），X为= O，-OH或，当类固醇具有芳环A时，X为OH或“IMAGE”。类固醇酯具有雄激素，合成代谢，雌激素或 取决于环构型和取代基的抗雌激素特性。 还公开了含有类固醇酯的药物组合物。

    Branched chain and cycloaliphatic esters of the androstane and oestrane series and pharmaceutical compositions containing same
    6.
    发明授权
    Branched chain and cycloaliphatic esters of the androstane and oestrane series and pharmaceutical compositions containing same 失效
    雄甾烷和雌二醇系的支链和脂环族酯以及含有它们的药物组合物

    公开(公告)号：US4307087A

    公开(公告)日：1981-12-22

    申请号：US120609

    申请日：1980-02-12

    申请人： Lambert J. W. M. Tax

    发明人： Lambert J. W. M. Tax

    IPC分类号： A61K31/565 ,  C07J1/00 ,  A61K31/56

    CPC分类号： C07J1/0074 ,  C07J1/0025 ,  Y10S514/874

    摘要： There are disclosed branched chain and cycloaliphatic esters of steroids having the formula: ##STR1## where R is H or CH.sub.3 ;R.sub.1 is H or CH.sub.3 ;R.sub.2 is H or CH.sub.3 ;R.sub.3 is H, OH, CH.sub.3 or Cl;R.sub.4 is H or C.sub.1 to C.sub.4 alkyl;R.sub.5 is H, C.sub.1 to C.sub.4 alkyl or CF.sub.3 ;R.sub.6 is H, C.sub.1 to C.sub.4 alkyl, C.sub.1 to C.sub.4 alkoxy, halogen or .beta.-OH providing that when R.sub.6 is .beta.-OH, the steroid also contains 9.alpha.-F and further providing that R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 represent at least 4 and at most 5 hydrogen atoms, except in the case of a .DELTA..sup.1,4 -steroid, in which case R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are all hydrogen;R.sub.7 is H or CH.sub.3 ;R.sub.8 is ##STR2## providing the R.sub.8 is --OH or ##STR3## when the steroid has an aromatic ring A.

    摘要翻译： 公开了具有下式的类固醇的支链和脂环族酯：其中R是H或CH 3; R1是H或CH3; R2是H或CH3; R3是H，OH，CH3或Cl; R4是H或C1-C4烷基; R5是H，C1-C4烷基或CF3; R6为H，C1至C4烷基，C1至C4烷氧基，卤素或β-OH，条件是当R6为β-OH时，类固醇还含有9个α-F，并进一步提供R1，R2，R3，R4，R5和 R6代表至少4个和至多5个氢原子，除了在DELTA1,4-甾类的情况下，其中R1，R2，R3，R4，R5和R6都是氢; R7是H或CH3; R8是，提供R8是-OH或