• 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:
    6-Substituted 10 beta -alkynylestrene derivatives of formula (I): …<CHEM>… wherein… X is hydrogen, C1-C4 alkyl or halogen;… n is zero, 1 or 2;… Y is an oxo group or a methylene group;… the symbol @ indicates a single bond or a double bond;… R1 is halogen, azido or a group …<CHEM>… wherein each of R3 and R4 is, independently, hydrogen or C1-C4 alkyl, or R1 may be divalent and is a C1-C6 alkylidene group; and R2 is hydrogen or, when R1 is halogen, R2 may also be the same halogen as R1,… and the pharmaceutically acceptable salts thereof; are aromatase inhibitors and can be used, e.g., in the treatment of hormone-dependent tumors and prostatic hyperplasia.
    公开号:SU1577701A3
    申请号:SU864028669
    申请日:1986-12-22
    公开日:1990-07-07
    发明作者:Фаустини Франко；Ди Салле Энрико；Вилла Витториа；Ломбарди Паоло
    申请人:Фармиталиа Карло Эрба С.П.А. (Фирма)；
    IPC主号:
    专利说明:

    10- (2-propinyl) estr-4-en-3, 1 7
    dione (comparative) 31
    Aminogluttimid (comparative1750
    10 B- (2-Propinyl-6-methylene-4-ene-3, 17-dione19
    (FCE 24716)
    10 ft - (2-Propinyl) -6-methylenestra-1, 4-diene-3,17-dione17
    权利要求:
    Claims (1)
    [1]
    Claim
    10 p-alkynylesthetic general formula
    The method of obtaining reno derivatives symbol. G, --- single or double carbon-carbon bond;
    R / is an alkylidene group C 4 ~ C 3 , distinct a. that the compound of the general formula
    40 where η has the indicated value, is reacted with a Vilsmeier reagent carrying the remainder. R ^, and a compound of formula (I) is obtained, where η has the indicated value, d5 is a single bond, and, if necessary, the compound of formula (I) is subjected to dehydrogenation with obtaining the corresponding compound, where the carbon-carbon double bond.
    Compound | 1 C 50 , nm 10- (2-Propynyl) estr-4-en-Z, 17 dion (comparative) 31 ‘ Aminogluttimide (comparative 1750 10 β- (2-Propinyl) -6 ~ methylene- estra-4-en-3,1 7-dione 19 (FCE 24716) 10 p - (2-propynyl) -6-methylene- estra-1, 4-diene-3,1 7-dion . 17
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    引用文献:
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    US4322416A|1980-06-27|1982-03-30|Merrell Dow Pharmaceuticals Inc.|10-Alkynyl steroids|
    US4289762A|1980-06-27|1981-09-15|Merrell Dow Pharmaceuticals Inc.|10- steroids as irreversible aromatase inhibitors|
    DE3121153C2|1981-05-22|1991-06-20|Schering Ag|
    US4446071A|1982-09-09|1984-05-01|E. R. Squibb & Sons, Inc.|Intermediates useful in the preparation of 17,17-bis androstenes|
    US4546098A|1984-04-13|1985-10-08|The Rockefeller University|Estrogen synthesis inhibitors|US4534722A|1984-04-16|1985-08-13|Gold Bond Ice Cream, Inc.|Forming and conveying of baked confection shells|
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    法律状态:
    优先权:
    申请号 | 申请日 | 专利标题
    GB858531747A|GB8531747D0|1985-12-24|1985-12-24|10beta-alkynylestrene derivatives|
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