15,15-dialkyl-substituted derivatives of estradiol

Details 15,15-dialkyl-substituted derivatives of estradiol 15,15-dialkyl-substituted derivatives of estradiol

1995-06-07

1997-08-12

Jordan, Charles T.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Cyclopentanohydrophenanthrene ring system doai

514170, 552629, A61K 3156

Patent

active

056566220

ABSTRACT:
New 15,15-dialkyl-substituted derivatives of the estradiol of general formula I ##STR1## in which R.sup.1 and R.sup.2, independently of one another, are each a hydrogen atom or a straight-chain alkanoyl group with 1 to 10 carbon atoms, a branched-chain alkanoyl group with 3-10 carbon atoms, an alkanoyl group of 3-10 carbon atoms containing a cycloaliphatic structure of 3-6 carbon ring atoms or a benzoyl group, and
R.sup.3 and R.sup.4, independently of one another, are each a straight-chain alkyl group with 1 to 10 carbon atoms or a branched-chain alkyl group with 3 to 10 carbon atoms,
are described, a process for their production and initial products for this process. The new compounds have--also after oral administration--high estrogenic effectiveness and are suitable for the production of pharmaceutical agents.

REFERENCES:
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patent: 3766224 (1973-10-01), Coombs
patent: 4789671 (1988-12-01), Bull et al.
patent: 5587496 (1996-12-01), Bull et al.
Groen et al., "Biomimetric Total Synthesis of Steroids IV. Stereoselective Synthesis of 15.alpha.-methyl-19-norsteroids," J. of the Royal Netherlands Chem. Soc., 94(4): 239-242 (Apr. 1979).
Tetrahedron, 47(37):7751-7766 (Sep. 9, 1991) Poirer et al. Synthesis of 17.beta.-Estradiol Derivatives with N-Butyl, N-Methyl Alkylauide Side Chain at Position 15.

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