• 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 invention relates to new 17-hydroxy androsta-1,4-diene-3-one derivatives of the following formula <CHEM> wherein each of R and R3, independently, is hydrogen or C1-C6 alkyl; R1 is hydrogen, halogen or C1-C6 alkyl; R2 is hydrogen or C1-C6 alkyl; R4 is hydrogen or fluorine; R5 is a) hydrogen or C1-C6 alkyl; b) phenyl unsubstituted or substituted by one or two substituents independently chosen from C1-C6 alkyl, halogen and amino; c) an acyl group; or d) a hydroxy protecting group; and the pharmaceutically acceptable salts thereof, which are useful in therapy, in particular as anti-cancer agents.
    公开号:SU1750431A3
    申请号:SU884356448
    申请日:1988-09-09
    公开日:1992-07-23
    发明作者:Вилла Витториа；Ди Салле Энрико；Ломбарди Паоло
    申请人:Фармиталиа Карло Эрба С.Р.Л. (Фирма)；
    IPC主号:
    专利说明:

    table 2
     The mean value ± S.О., from three experiments.
    权利要求:
    Claims (1)
    [1]
    Claim
    A method of obtaining 17-substituted derivatives of 6-methylene-androsta-1,4-diene-Zone of the general formula where Ri is hydrogen or Cg-Cb-alkanoyl, characterized in that the compounds of the formula where Ri have the indicated meanings are reacted in high boiling alcohol at 130-137 ° C with a source of formaldehyde and a salt formed by hydrochloric or sulfuric acid, with an amine of the general formula where each of the groups R a . which may be the same or different, is lower alkyl containing 1-5 carbon atoms, and, if necessary, acylate the compound of formula (I). where Ri is hydrogen, to give a compound of formula (I). where Ri is Cr-Sat-alkanoyl.
    Table 1
    Compound % aromatase inhibition at 30 mg / kg, sc Drosta-1,4-dien-17-β-ol-3-one 6-methylene 78% 6-Methyleneandrosta-1,4-diene-Μβ -ol-3-one- 17-propionate 69% 6-Methyl enandrosta-4-en-1 Ίβ -ol-3-one-17-acetate Not active
    table 2
    Compound IKet. nm ’ 6-Methyleneandrosta-1,4-diene-17-β-ol-3-one 8 ± 2 6-Methyleneandrosta-1,4-diene-3.17-dione (analogue) 610 ± 82
    Compiled by I. Fedoseev Editor I. Gornaya Tehred M. Morgenthal Corrector T. Paly
    Order 2607 Subscription Circulation, VNIIIPI of the State Committee for Inventions and Discoveries at the USSR State Committee for Science and Technology
    113035, Moscow. J-35. Raushskaya nab .. 4/5 i
    Production and Publishing Combine Patent, Uzhgorod, 101 Gagarin St.
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    引用文献:
    公开号 | 申请日 | 公开日 | 申请人 | 专利标题
    GB929985A|
    GB8517360D0|1985-07-09|1985-08-14|Erba Farmitalia|Substituted androsta-1,4-diene-3,17-diones|CH683151A5|1991-04-24|1994-01-31|Ciba Geigy Ag|Contraception in female primates without affecting the menstrual cycle.|
    FR2681069B1|1991-09-06|1995-04-28|Roussel Uclaf|NEW PROCESS FOR THE PREPARATION OF HYDROCORTISONE AND NEW INTERMEDIATES.|
    GB9201224D0|1992-01-21|1992-03-11|Erba Carlo Spa|Difluoromethylenandrostenone derivatives and process for their preparation|
    GB9217035D0|1992-08-11|1992-09-23|Erba Carlo Spa|Androst-4-enopyrrole derivatives and process for their preparation|
    CA2118317A1|1993-02-18|1994-09-01|Pharmacia S.P.A.|Fluorinated 4-aminoandrostadienone derivatives and process for their preparation|
    DE10104327A1|2001-01-24|2002-07-25|Schering Ag|New 11beta-halo-testosterone derivatives useful in male hormone replacement therapy and in male fertility control|
    CA2463142A1|2001-10-10|2003-04-24|Pharmacia Italia Spa|Methods for preventing and treating bone loss with steroid compounds|
    US7435757B2|2004-07-02|2008-10-14|Schering Ag|2-substituted D-homo-estra-1,3,5-trienes as inhibitors of 17β-hydroxy steroid dehydrogenase type 1|
    US20060211667A1|2005-03-21|2006-09-21|Eric Marchewitz|Use of pregnane steroid derivatives for enhancing physical performance|
    EP1854465A1|2006-05-12|2007-11-14|Alexander Tobias Teichmann|Use of4,17 beta-dihydroxyandrost-4-ene-3-one for treating cancers|
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    DK2060261T3|2007-11-13|2016-06-13|Athenion Ag|C-19 steroids for cosmetic use|
    法律状态:
    2010-07-20| REG| Reference to a code of a succession state|Ref country code: RU Ref legal event code: MM4A Effective date: 20070910 |
    优先权:
    申请号 | 申请日 | 专利标题
    GB878721384A|GB8721384D0|1987-09-11|1987-09-11|17-substituted andro-sta-1 4-dien-3-one derivatives|
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