11 beta-short chain substituted estradiol analogs and their use in the treatment of menopausal symptoms and estrogen sensitive cancer
AssigneeYale University
InventorRichard Hochberg
Life of this patent
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Abstract
The present invention relates to novel 11-β estradiol ester compounds and their use as locally active estrogens in the treatment of the symptomology of menopause and to treat estrogen sensitive cancers, including breast cancer.
Claims29
A method of treating the symptomology of menopause in a patient while reducing the risk that the patient develops an estrogen-sensitive cancer, the method comprising administering to said patient an effective amount of a selective estrogen receptor modulator (SERM) which has the chemical structure:
- Where R is a sidechain group of at least 5 non-hydrogen atoms in length selected from a
- group, a
- group, a
- group, or a —(CH2)nXR4 group,
- R1, R2, R3 and R4 are each independently a C1-C6 linear, branch-chained or cyclo-alkyl group;
- R1 is H, CH3, a vinyl group (—CH═CH2), or an ethynyl group (—C≡CH);
- X is O or S and Y is O;
- and
- n is from 1 to 3, wherein said symptomology is one or more of bone loss associated with osteoporosis, elevated cholesterol or elevated low-density lipoproteins (LDL), wherein said compound is other than compound E11-2,2Rev of Table 1 and FIG. 8 having the chemical structure:
A method of treating a patient suffering from an estrogen-sensitive cancer, the method comprising administering to said patient an effective amount of a selective estrogen receptor modulator (SERM) which has the chemical structure:
- Where R is a sidechain group eat least 5 non-hydrogen atoms in length selected from a
- group, a
- group, a
- group, or a —(CH2)nXR4 group,
- R1, R2, R3 and R4 are each independently a C1-C6 linear, branch-chained or cyclo-alkyl group;
- R1 is H, CH3, a vinyl group (—CH═CH2), or an ethynyl group (—C≡CH);
- X is O or S and Y is O;
- and
- n is from 1 to 3, wherein said compound is other than compound E11-2,2Rev of Table 1 and FIG. 8 having the chemical structure:
A method of treating the symptomology of menopause in a patient suffering from an estrogen-sensitive cancer, the method comprising administering to said patient an effective amount of a selective estrogen receptor modulator (SERM) which has the chemical structure:
- Where R is a sidechain group of at least 5 non-hydrogen atoms in length selected from a
- group, a
- group, a
- group, or a —(CH2)nXR4 group,
- R1, R2, R3 and R4 are each independently a C1-C6 linear, branch-chained or cyclo-alkyl group;
- R1 is H, CH3, a vinyl group (—CH═CH2), or an ethynyl group (—C≡CH);
- X is O or S and Y is O;
- n is from 1 to 3, wherein said symptomology of menopause is one or more of bone loss associated with osteoporosis, elevated cholesterol, or elevated low-density lipoproteins (LDL), and wherein said compound is other than compound E11-2,2Rev of Table 1 and FIG. 8 having the chemical structure:
Dependencies are inferred from the claim text.