10-Alkynyl steroids

Drug – bio-affecting and body treating compositions – Antigen – epitope – or other immunospecific immunoeffector – Bacterium or component thereof or substance produced by said...

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424243, 26023955C, 26023955R, 2603973, 2603974, A61K 3156, C07J 100

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active

043224164

ABSTRACT:
Aromatase inhibitors are provided having the formula ##STR1## wherein represents a single or double bond; R is hydrogen or C.sub.1-4 alkyl; R.sup.1 is methyl or ethyl; R.sup.2 is (H) (OR.sup.8) or .dbd.O; R.sup.3 is H or C.sub.1-3 alkyl; R.sup.4 is H or OR.sup.8 ; R.sup.5 is H, C.sub.1-3 alkyl or, when the 5,6-bond is saturated, R.sup.5 is divalent .dbd.O; R.sup.6 and R.sup.7 are each H or C.sub.1-3 alkyl; and R.sup.8 is H or C.sub.2-4 alkanoyl. Intermediates useful in preparing the foregoing aromatase inhibitors, and methods of using the aromatase inhibitors of the invention are also provided.

REFERENCES:
patent: 3127427 (1964-03-01), Boller et al.
patent: 3218316 (1965-11-01), Edwards
Tetrahedron Letters No. 23 (1979), pp. 2105-2108, relied on Article by D. F. Covey et al.
J. Biol. Chem., No. 256 (1981), p. 1076, Article by D. F. Covey et al.

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