Substituted tetralins as selective estrogen receptor-beta agonists
AssigneeEli Lilly and Company
InventorsVenkatesh Krishnan, Julian Stanley Kroin, Bryan Hurst Norman, Elizabeth Marie Thomas
Life of this patent
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Abstract
The present invention relates to novel tetralin ER-β agonist compounds, pharmaceutical compositions thereof, and use of these compounds to treat a ER-β mediated disease such as nocturia, obstructive uropathy, benign prostatic hypertrophy, obesity, dementia, hypertension, incontinence, colon cancer, prostate cancer, infertility, depression, leukemia, inflammatory bowel disease, and arthritis.
Claims37
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A pharmaceutical composition comprising a therapeutically effective amount of a compound, or a pharmaceutically acceptable salt thereof, of claim 37 together with a pharmaceutically acceptable carrier, diluent or excipient.
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A compound selected from the group consisting of:
- 9-(4-Hydroxy-phenyl)-4b,5,6,7,8,8a,9,10-octahydro-phenanthren-3-ol;
- 4-(4-Hydroxy-phenyl)-2,3,3a,4,5,9b-hexahydro-1H-cyclopenta[a]naphthalen-8-ol;
- 9-(4-Hydroxy-phenyl)-4b,5,6,7,8,8a,9,10-octahydro-phenanthrene-1,3-diol;
- 9-(4-Hydroxy-phenyl-1-methoxymethyl-4b,5,6,7,8,8a,9,10-octahydro-phenanthren-3-ol;
- 1-Hydroxymethyl-9-(4-hydroxy-phenyl)-4b,5,6,7,8,8a,9,10-octahydro-phenanthren-3-ol;
- [3-Hydroxy-9-(4-hydroxy-phenyl)-4b,5,6,7,8,8a,9,10-octahydro-phenanthren-1-yl]-acetonitrile;
- 3-Hydroxy-9-(4-hydroxy-phenyl)-4b,5,6,7,8,8a,9,10-octahydro-phenanthrene-1-carbonitrile;
- 9-(4-Hydroxy-phenyl)-4b,5,6,7,8,8a,9,10-octahydro-phenanthrene-2,3-diol;
- 9-(4-Hydroxy-phenyl)-2-methoxy-4b,5,6,7,8,8a,9,10-octahydro-phenanthren-3-ol;
- 9-(4-Hydroxy-phenyl)-2-methoxymethyl-4b,5,6,7,8,8a,9,10-octahydro-phenanthren-3-ol;
- [6-Hydroxy-10-(4-hydroxy-phenyl)-1,2,3,4,4a,9,10,10a-octahydro-phenanthrene-9-yl]-acetonitrile;
- or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.