• 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 steroids, in particular, a process for the preparation of steroid derivatives of the general formula c (x) (... Y) -g., -Sn, -cH4: (RO-CHi: -CH C-CH-CH. -CH, - rH -...- C (CbCRA) -CH7- -CHi-C (0) -CH, where Ri C, -Se-a / alkyl (it can be substituted by a hydroxy group); K, - X and Y mean radio - cal - O - C (0) ... with pharmacological properties that can be used in medicine. The goal is to create new pharmaceutical active compounds of the specified class. Synthesis of target substances is carried out by the reaction of compounds of general formula C (O) -CE7 -CNg-GH-C (RO-SNg-CH ... C h: n-sn7-cn, -c (... oH) -c (CECRi b. -CTtg-CH 7-CK-CHi, where R and R are higher, and the existing hydroxy groups are protected, K is a ketal protective group for the ketone function, with a reagent of the general formula CH CH-CH -0-P (0) (Alk) 5 ,, where Alk Ci-Cz-alkyl , in the presence of a strong organic base, followed by acid treatment. New compounds have antihypertensive activity, as they alter the membrane permeability of the vascular walls to Na and K®, thereby reducing their contractility. The toxicity of compounds jo jo 400 mg / kg. 1 tab. (Y) 4:
    公开号:SU1470198A3
    申请号:SU3952445
    申请日:1985-08-23
    公开日:1989-03-30
    发明作者:Торелли Весперто；Неделек Люсьен；Могилевский Мартин；Мура Анн-Мари
    申请人:Руссель-Юклаф (Фирма)；
    IPC主号:
    专利说明:

    where R-, - C1-С j-al kil, possibly substituted by a hydroxy group;
    . Where A1K - C, -C-Alksh1, in the presence of a strong organic base, followed by acid treatment.
    Products
    The product according to example 1
    The product according to example 5
    The product X (10 / i-α-ethynyl-21-hydroxy-19-nor-pregna-4.9 (11) -die-3,20-dione)
    Efflux in vitro Na at a concentration of 10 M,% inhibition. Antagonistic effect
    passive
    100 28
    100 60
    权利要求:
    Claims (1)
    [1]
    Claim
    A method of obtaining derivatives of steroids of the general formula where R, - C, -Calkyl, possibly substituted by a hydroxy group;
    where R and R 2 have the indicated meanings, 20 and the existing hydroxy groups are protected;
    K is the ketal protecting group for the ketone j function,>.
    / is treated with a reagent of the general formula (ΑΙΚ) ζ Ν χ θ. . / P - ° -CH 2 -CH-CH , zo (A1K) 2 K / 2. where A1K is C, -C 3 -alkyl, in the presence of a strong organic base, followed by treatment with acid.
    Products
    Efflux in vitro 1l Na at a concentration of 10 ' 8 M,% inhibition. Antagonistic effect
    passive j pump Product according toRU 1Product according to 100 1.00 RU 5 28 60 Product X (10 ^ -ethynyl-21-hydroxy-1 9-nor-pregna-4.9 (11) -dina-3,20-dion) 0 0
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    同族专利:
    公开号 | 公开日
    EP0176399A1|1986-04-02|
    FI853254A0|1985-08-23|
    AU580086B2|1988-12-22|
    EP0313960A1|1989-05-03|
    EP0313960B1|1992-07-29|
    DK382185A|1986-02-25|
    DK382185D0|1985-08-23|
    FI82699C|1991-04-10|
    FI853254L|1986-02-25|
    IE852075L|1986-02-24|
    GR852037B|1985-12-18|
    MX159930A|1989-10-06|
    DK168538B1|1994-04-18|
    AT42561T|1989-05-15|
    ES546372A0|1986-03-01|
    KR940008596B1|1994-09-24|
    JPS6176499A|1986-04-18|
    DE3569739D1|1989-06-01|
    CA1260459A|1989-09-26|
    FR2569408A1|1986-02-28|
    AT78826T|1992-08-15|
    FR2569408B1|1986-10-03|
    FI82699B|1990-12-31|
    DE3586427D1|1992-09-03|
    PT81020A|1985-09-01|
    ES8604988A1|1986-03-01|
    IL76096A|1989-09-10|
    DE3586427T2|1993-01-07|
    US4701449A|1987-10-20|
    PT81020B|1987-12-30|
    AU4662585A|1986-02-27|
    ZA856427B|1986-10-29|
    HU194276B|1988-01-28|
    HUT39461A|1986-09-29|
    EP0176399B1|1989-04-26|
    CN85106995A|1987-04-01|
    CN1029683C|1995-09-06|
    JPH0649717B2|1994-06-29|
    KR860001824A|1986-03-22|
    IL76096D0|1985-12-31|
    IE64675B1|1995-08-23|
    引用文献:
    公开号 | 申请日 | 公开日 | 申请人 | 专利标题
    US3102127A|1962-06-12|1963-08-27|Syntex Corp|19-methylene-androstane derivatives|
    US3218316A|1963-08-26|1965-11-16|Syntex Corp|10beta-ethynyl-19-norandrostane derivatives|
    US3275622A|1963-12-18|1966-09-27|Syntex Corp|19-alkylidene-delta4-3, 20-keto pregnanes|
    FR1519387A|1966-04-20|1968-03-29|Hoffmann La Roche|Process for the preparation of 19-alkenyl steroids|
    FR2344286B1|1976-03-16|1978-11-17|Roussel Uclaf|
    FR2462445B1|1979-07-31|1982-02-12|Roussel Uclaf|
    HU179980B|1979-12-28|1983-01-28|Gyogyszerkutato Intezet|Process for preparing substituted steroid-spiro-oxazolidinone derivatives|
    US4322416A|1980-06-27|1982-03-30|Merrell Dow Pharmaceuticals Inc.|10-Alkynyl steroids|FR2576025B1|1985-01-14|1987-01-23|Roussel Uclaf|NOVEL SUBSTITUTED STEROIDS IN POSITION 10, THEIR PROCESS AND THE PREPARATION INTERMEDIATES, THEIR APPLICATION AS MEDICAMENTS, THE PHARMACEUTICAL COMPOSITIONS CONTAINING THEM|
    FR2594829B1|1986-02-24|1988-06-03|Roussel Uclaf|NEW STEROIDS 9SATURES SUBSTITUTED IN POSITION 10 BY A RADICAL COMPRISING A TRIPLE LINK, THEIR PREPARATION METHOD, THEIR APPLICATION AS MEDICAMENTS, THE PHARMACEUTICAL COMPOSITIONS CONTAINING THEM|
    WO1990002781A1|1988-09-16|1990-03-22|Lithium Corporation Of America|Thermally stable, reactive organometallic compositions containing copper|
    US5100575A|1989-09-08|1992-03-31|Fmc Corporation|Thermally stable, reactive organometallic compositions containing copper|
    WO1999061055A1|1998-05-22|1999-12-02|The Board Of Trustees Of The Leland Stanford Junior University|Bifunctional molecules and therapies based thereon|
    JP2008539047A|2005-04-28|2008-11-13|プロテウスバイオメディカルインコーポレイテッド|Pharma Informatics System|
    WO2007035716A2|2005-09-16|2007-03-29|Raptor Pharmaceutical Inc.|Compositions comprising receptor-associated proteinvariants specific for cr-containing proteins and uses thereof|
    FR2917975B1|2007-06-26|2009-10-16|Ceva Sante Animale Sa|COMPOSITIONS AND TREATMENT OF CARDIAC INSUFFICIENCY IN NON-HUMAN MAMMAL ANIMALS|
    US20090270356A1|2008-04-28|2009-10-29|Ceva Sante Animale Sa|Compositions and treatments of heart failure in non-human mammal animals|
    CN104208718B|2009-02-20|2017-12-29|2-Bbb医疗股份有限公司|drug delivery system based on glutathione|
    CN103145785B|2013-03-19|2016-03-02|浙江仙居仙乐药业有限公司|A kind of synthetic method of cyproterone acetate dehydrogen substance|
    法律状态:
    2005-05-10| REG| Reference to a code of a succession state|Ref country code: RU Ref legal event code: MM4A Effective date: 20030824 |
    优先权:
    申请号 | 申请日 | 专利标题
    FR8413189A|FR2569408B1|1984-08-24|1984-08-24|NOVEL STEROIDS SUBSTITUTED IN POSITION 10 BY A RADICAL HAVING A DOUBLE OR TRIPLE LINK, THEIR PREPARATION METHOD, THEIR APPLICATION AS MEDICAMENTS, THE PHARMACEUTICAL COMPOSITIONS CONTAINING THEM|
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