6-alkynyl steroids

Details 6-alkynyl steroids 6-alkynyl steroids

1997-05-08

1999-02-02

Robinson, Allen J.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Cyclopentanohydrophenanthrene ring system doai

514178, 552639, 552640, 552647, A61K 31565, C07J 100

Patent

active

058665587

ABSTRACT:
Compounds of formula I: ##STR1## wherein R, R.sup.1, R.sup.2, R.sup.3, and R.sup.4 have any of the values defined in the specification, and their pharmaceutically acceptable salts, are inhibitors of aromatase, and are useful for treating diseases such as breast cancer, in mammals. Also disclosed are pharmaceutical compositions, processes for preparing compounds of formula (I) and intermediates useful for preparing compounds of formula I.

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Akkani, A., et al., "6B-Propynyl-Substituted Steroids: Mechanism-Based Enzyme-Activated Irreversible Inhibitors of Aromatase", J. Med. Chem., 40, 3263-3270, (1997).
Campbell, J.A., et al., "6-Methyl Steroids in the Androstane Series", J. Am. Chem., LXXX, 4717-4721, (1958).
Kitz, R., et al., "Esters of Methanesulfonic Acid as Irreversible Inhibitors of Acetylcholinesterase", J. of Biol. Chem., 237, No. 10, 3245-323249, (1962).
Ryan, K.J., "Biological Aromatization of Steroids", J. of Biol. Chem., 234, No. 2, 268-272, (1959).
63-045294 Feb. 26, 1988 Japan C07J 1/00 Partial translation of pp. 1237-1238, 1247-1248 and 1253-1254 (6 pages).

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