10-(1,2-Propadienyl) steroids as irreversible aromatase inhibito

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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424241, 424243, 26023955R, 26023955C, 2603973, 2603975, 2603974, A61K 3156, A61K 3158

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042897629

ABSTRACT:
Irreversible aromatase inhibitors are provided having the formulae ##STR1## wherein represents a single or a double bond; R.sup.1 is CH.sub.3 or C.sub.2 H.sub.5 ; R.sup.2 is (H) (OR.sup.8) or 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.sub.2, O or (H) (C.sub.1-3 alkyl); R.sup.6 and R.sup.7 are each independently H or C.sub.1-3 alkyl; and R.sup.8 is H or C.sub.1-4 alkanoyl. Intermediates useful in preparing the foregoing aromatase inhibitors, methods of using them and a pharmaceutical composition containing them are also provided.

REFERENCES:
patent: 3939264 (1976-02-01), Lachnit-Fixson
patent: 4052421 (1977-10-01), Biollaz et al.

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