10-(1,2-Propadienyl) steroids as irreversible aromatase inhibitors
AssigneeMerrell Dow Pharmaceuticals Inc.
InventorsBrian W. Metcalf, J. O'Neal Johnston
Life of this patent
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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.
Claims23
Compounds having the formulae ##STR15## 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.
Compound having the formulae ##STR16## wherein 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.5 is H, or C.sub.1-3 alkyl;
- R.sup.8 is H or C.sub.1-4 alkanoyl;
- R.sup.9 and R.sup.10 together are >O, or R.sup.9 is OH and R.sup.10 is C.sub.1-3 alkyl;
- and R.sup.11 is (H)(OH) or O.
A pharmaceutical composition comprising a compound having the formula ##STR17## 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;
- and a pharmaceutically acceptable carrier.
Dependencies are inferred from the claim text.