4-substituted 6-alkylidenandrosteine-3,17-dione derivatives and

Details 4-substituted 6-alkylidenandrosteine-3,17-dione derivatives and 4-substituted 6-alkylidenandrosteine-3,17-dione derivatives and

1987-08-18

1989-04-18

Sneed, H. M. S.

Chemistry of carbon compounds

Miscellaneous organic carbon compounds

C-metal

2603974, 260349, C07J 100, C07C11700

Patent

active

048225282

ABSTRACT:
The invention relates to 4-substituted 6-alkylidenandrostene-3,17-dione derivatives of the following formula ##STR1## wherein each of R.sub.1, R.sub.2 and R.sub.3 is, independently, hydrogen or C.sub.1 -C.sub.6 alkyl; R.sub.4 is hydrogen of fluorine; (x) represents a single or double bond; and R is, especially, a hydroxy or mercapto or amino group or a functional derivative thereof. The compounds of the invention show aromatase inhibitory activity and may be useful, for instance, in the treatment of hormone-dependent tumors and of prostatic hyperplasia.

REFERENCES:
patent: 2744120 (1956-05-01), Fried et al.
patent: 3341560 (1967-09-01), Campbell et al.
patent: 3953483 (1976-04-01), Hiraga et al.
patent: 4235893 (1980-11-01), Brodie et al.
Bull et al., "An Unusual Acid-Catalyzed Reaction of Steroidal 4,6-Diols with Acetone", J. Chem. Soc.(D), 1971, (13), 717-718.
Brodie, "Overview of Recent . . . ", Cancer Research (Suppl.), 42, 3312s-33143s, Aug. (1982).
Covey et al., "A New Hypothesis Based . . . ", Cancer Reserach (Suppl.), 42 . . . 3327s-3333s, Aug. (1982).
U.S. Pat. No. 4,289,762, Derwent Publication.
U.S. Pat. No. 4,322,416, Derwent Publication.
Metcalf, et al., "Substrate-Induced . . . ", J. Am. Chem. Soc., 1981, 3321-3222.
EP 100,566A, Derwent Publication.
GB 2100-601 Derwent Publication.
100:968489. Chemical Abstracts, vol. 100, 1984.
Marsch, et al., "Aromatase Inhibitors. Synthesis . . . ", J. Med. Chem., 1985, 28, 788-795.
GB 2177-700-A Pharmaceuticals p. 3, Week 8704.
"Aromatase Inhibitors. Synthesis and Biological Activity of Androstenedione Derivatives", David A. Marsh et al., J. Med. Chem., 1985, pp. 788-795.

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