2,19-methyleneoxy and 2,19-methylenethio bridged steroids as aromatase, 19-hydroxylase inhibitors and methods of their use in the treatment of estrogen mediated disorders
AssigneeMerrell Pharmaceuticals Inc.
InventorsNorton P. Peet, J. O'Neal Johnston, Joseph P. Burkhart
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Abstract
The present invention is directed to a method of using a certain compounds which are 2,19-methyleneoxy or 2,19 methylenethio bridged steroids, and related steroidal compounds as inhibitors of the enzyme steroid aromatase, 19-hydroxylase and as treatment for various estrogen dependent/mediated disorders including hormonal dependent breast cancer.
Claims14
A method of treating benign prostatic hyperplasia which comprises administrating to a patient in need thereof an effective aromatase-inhibiting amount of a compound of the formula:
- wherein:
- represents a single or double bond, with the proviso that the compound must contain at least one double bond,
- A is O, S, SO, or SO2,
- R is H, ═CH2, ═O, or —OH,
- R1 is H or C1-4 alkyl,
- R2 is ═O, —OH, or —O—(C1-4 alkanoyl),
- X is ═O, ═CH2, —OH, or —O—(C1-4 alkanoyl), and
- Y is H, —OH, or —O—(C1-4 alkanoyl), and when Y=H, —H, or —O—(C1-4 alkanoyl), X may not include —OH, and R may not include ═O or —OH.
A method of inhibiting intratumoral aromatase of a breast cancer tumor which comprises administrating to a patient in need thereof an effective aromatase-inhibiting amount of a compound of the formula:
- wherein:
- represents a single or double bond, with the proviso that the compound must contain at least one double bond,
- A is O, S, SO, or SO2,
- R is H, ═CH2, ═O, or —OH,
- R1 is H or C1-4 alkyl,
- R2 is ═O, —OH, or —O—(C1-4 alkanoyl),
- X is ═O, ═CH2, —OH, or —O—(C1-4 alkanoyl), and
- Y is H, —OH, or —O—(C1-4 alkanoyl), and when Y═H, —OH, or —O—(C1-4 alkanoyl), X may not include —OH, and R may not include ═O or —OH.
A method of treating a breast cancer tumor which results in growth inhibition or remission comprising administrating to a patient in need thereof an effective aromatase-inhibiting amount of a compound of the formula:
- wherein:
- represents a single or double bond, with the proviso that the compound must contain at least one double bond,
- A is O, S, SO, or SO2,
- R is H, ═CH2, ═O, or —OH,
- R1 is H or C1-4 alkyl,
- R2 is ═O, —OH, or —O—(C1-4 alkanoyl),
- X is ═O, ═CH2, —OH, or —O—(C1-4 alkanoyl), and
- Y is H, —OH, or —O—(C1-4 alkanoyl), and when Y═H, —OH, or —O—(C1-4 alkanoyl), X may not include —OH, and R may not include ═O or —OH.
Dependencies are inferred from the claim text.