• 专利附录
  • 专利说明
  • 权利要求
  • 类似技术
  • 同族专利
  • 引用文献
  • 法律状态
  • 优先权
    • 专利摘要:
    The present invention relates to new 6-substituted 1,2 beta -methylen-androst-4-ene-3, 17-diones of the following general formula: <CHEM> wherein one of R1 and R2 is hydrogen and the other is halogen, amino or azido, or R1 and R2, taken together, form a = CH2 or = 0 group, and, when one of R1 and R2 is amino, the pharmaceutically acceptable salts thereof. The compounds of the invention are useful in therapy, in particular as anti-cancer agents.
    公开号:SU1537141A3
    申请号:SU874202750
    申请日:1987-06-19
    公开日:1990-01-15
    发明作者:Буццетти Франко；Ди Салле Энрико；Ломбарди Паоло
    申请人:Фармиталиа Карло Эрба С.П.А. (Фирма)；
    IPC主号:
    专利说明:

    Inhibition of aromatase of human placenta i
    Compound
    in vitro
    ICgo Relative Strength
    NM
    4-Hydroxyandrost-4-en-3,17-Dion 1,2 y-Methylene-6-methylenandrost-en 3,17-Dion (FGE 25026) 1,2 p-Methylenandrost - - en-3,17 dion
    1.00 2.64
    2.11
    权利要求:
    Claims (1)
    [1]
    Claims characterized in that the compound of the formula
    The method of obtaining 6-methylene-1,2β-methyleneandrost-4-en-Z, 17-dione of the formula
    5 · Methylated with 'formaldehyde diethyl acetal in op medium ! a chemical solvent at reflux temperature in the presence of a condensing agent.
    , • Inhibitory1 human placenta aromatase in vitro Compound Icso 'nm Relative strength
    4-hydroxyandrost- -4-en-z, 17-dione 44 ‘1.00 1,2p-Methylene-6-methyleneandrost-4-ene 17 2.64 3.17-dion(FGE 25026)1,2β-Methyleneandrost-4-en-3,17-dione 21 2.11
    类似技术:
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    同族专利:
    公开号 | 公开日
    DK315387D0|1987-06-19|
    HU196431B|1988-11-28|
    GB8615092D0|1986-07-23|
    FI872659A0|1987-06-16|
    IL82894D0|1987-12-20|
    ZA874402B|1987-12-21|
    PT85121A|1987-07-01|
    KR880000461A|1988-03-26|
    JPS635096A|1988-01-11|
    NZ220744A|1989-07-27|
    AU7429087A|1987-12-24|
    HUT44036A|1988-01-28|
    EP0250262A1|1987-12-23|
    AU592878B2|1990-01-25|
    DK315387A|1987-12-21|
    FI872659A|1987-12-21|
    US4840943A|1989-06-20|
    引用文献:
    公开号 | 申请日 | 公开日 | 申请人 | 专利标题
    GB929985A|
    US2744120A|1953-01-14|1956-05-01|Olin Mathieson|1-dehydrotestololactone|
    GB1042291A|1961-11-08|1966-09-14|Organon Labor Ltd|í¸-6ª‡-amino steroids and the preparation thereof|
    DE1250436B|1964-03-26|
    DK120154B|1968-02-29|1971-04-19|Schering Ag|Process for the preparation of N-substituted 4-amino-3-oxosteroid-4,6-dienes of the androstane or pregnane series or their ammonium salts.|
    US4235893A|1978-05-08|1980-11-25|Brodie Angela M|Ester derivatives of 4-hydroxy-4-androstene-3,17-dione and a method for inhibiting estrogen biosynthesis|
    DE3422187A1|1984-06-12|1985-12-12|Schering AG, 1000 Berlin und 4709 Bergkamen|1,2SS-METHYLENE-4-ANDROSTEN AND 4,6-ANDROSTADIEN-3,17-DIONE|
    GB8519398D0|1985-08-01|1985-09-04|Erba Farmitalia|Steroidic aromatase inhibitors|
    GB8615093D0|1986-06-20|1986-07-23|Erba Farmitalia|Methylene derivatives of androst-4-ene-1317-diones|CH683151A5|1991-04-24|1994-01-31|Ciba Geigy Ag|Contraception in female primates without affecting the menstrual cycle.|
    FI941359A0|1993-12-03|1994-03-24|Snow Brand Milk Prod Co Ltd|Foerfarande Foer undersoekning av hormonoberoende tumoerer|
    DE4435368A1|1994-09-22|1996-03-28|Schering Ag|Use of aromatase inhibitors for the manufacture of a medicament for the treatment of a relative androgen deficiency in men|
    US6028064A|1996-09-13|2000-02-22|New Life Pharmaceuticals Inc.|Prevention of ovarian cancer by administration of progestin products|
    US6034074A|1996-09-13|2000-03-07|New Life Pharmaceuticals Inc.|Prevention of ovarian cancer by administration of a Vitamin D compound|
    US6511970B1|1996-09-13|2003-01-28|New Life Pharmaceuticals Inc.|Prevention of ovarian cancer by administration of products that induce transforming growth factor-beta and/or apoptosis in the ovarian epithelium|
    US6407082B1|1996-09-13|2002-06-18|New Life Pharmaceuticals Inc.|Prevention of ovarian cancer by administration of a vitamin D compound|
    US6765002B2|2000-03-21|2004-07-20|Gustavo Rodriguez|Prevention of ovarian cancer by administration of products that induce transforming growth factor-β and/or apoptosis in the ovarian epithelium|
    US20010044431A1|2000-03-21|2001-11-22|Rodriguez Gustavo C.|Prevention of ovarian cancer by administration of products that induce biologic effects in the ovarian epithelium|
    US8168621B2|2005-09-30|2012-05-01|Endece, Llc|6-substituted estradiol derivatives and methods of use|
    US10174070B2|2005-09-30|2019-01-08|Endece Llc|6-substituted estradiol derivatives and methods of use|
    法律状态:
    优先权:
    申请号 | 申请日 | 专利标题
    GB868615092A|GB8615092D0|1986-06-20|1986-06-20|Androst-4-ene-317-diones|
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