Compounds and methods for modulation of estrogen receptors

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...

Reexamination Certificate

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C514S307000, C514S277000, C514S269000, C514S339000, C514S345000, C514S357000, C514S415000

Reexamination Certificate

active

07435729

ABSTRACT:
Compounds that modulate the estrogen receptor (ER) are disclosed, as well as pharmaceutical compositions containing the same. In a specific embodiment, the compounds are selective modulators for ER-β over ER-α. Methods are disclosed for modulating ER-β in cell and/or tissues expressing the same, including cells and/or tissue that preferentially express ER-β. More generally, methods for treating estrogen-related conditions are also disclosed, including conditions such as is breast cancer, testicular cancer, osteoporosis, endometriosis, cardiovascular disease, hypercholesterolemia, prostatic hypertrophy, prostatic carcinomas, obesity, hot flashes, skin effects, mood swings, memory loss, urinary incontinence, hairloss, cataracts, natural hormonal imbalances, and adverse reproductive effects associated with exposure to environmental chemicals.

REFERENCES:
patent: 3234090 (1966-02-01), Huebner et al.
patent: 3274123 (1966-09-01), Lednicer
patent: 3277106 (1966-10-01), Bencze
patent: 5552412 (1996-09-01), Cameron et al.
patent: 6291456 (2001-09-01), Stein et al.
patent: 842 661 (1998-05-01), None
patent: 1 113 007 (2001-04-01), None
patent: 1143833 (1987-11-01), None
patent: WO 92/18498 (1992-10-01), None
patent: WO 96/21656 (1996-07-01), None
patent: WO 00/39120 (2000-07-01), None
patent: WO 00/55137 (2000-09-01), None
Koehler et al. Endocrine Reviews 26(3):465-478 2005.
Brandenberger et al., 1998, “estrogen Receptor Alpha (ER-α) and Estrogen Receptor Beta (ER-β) mRNAs in Normal Ovary, Ovarian Serous Cystandenocarcinoma and Ovarian Cancer Cell Lines: Down-Regulation of ER-β in Neoplastic Tissues”, J. Clin. Endocrinol. Metab. 83:1025-8.
Chang and Prins, 1999, “Estrogen receptor-beta: implications for the prostate gland”, Prostate, 40:115-24.
Clinton and Hua, 1997, “Estrogen action in human ovarian cancer.”Crit Rev Oncol. Hematol. 25:1-9.
Farhat et al., 1996, “The vascular protective effects of estrogen”, FASEB J. 10:615-624.
Hata et al., 1998, “Role of Estrogen and estrogen-related growth factor in the mechanism of hormone dependency of endometrial carcinoma-cells”, Oncology 55 Suppl 1, 35-44.
Iafrati et al., 1997, “Estrogen inhibits the vascular injury response in estrogen receptor alpha-deficient mice”, Nature Med 3(5):545-8.
Korach et al., 1994, “Insights from the study of animals lacking functional estrogen receptor” , Science 266:1524-7.
Krege et al., 1998, “Generation and reproductive phenotypes of mice lacking estrogen receptor beta”, Proc. Natl. Acad. Sci. USA 95:15677-82.
Lednicer et al.,1969, “Mammalian Antifertility Agents. VI. A Novel sequence for the Preparation of 1,2-Disubstituted 3,4-Dehydronaphthalenes,”, J. of Med. Chem. 12:881-885.
Mosselman et al., 1996, “ERβ Idnentification and Characterization of a Novel Human Estrogen Receptor”, FEBS Lett. 392:49-53.
Nilsson et al., 1998, “Erβ : A Novel Estrogen Receptor Offers the Potential for New Drug Development”, TEM 9:387-95.
Ogawa et al., 1997, “Behavioral effects of estrogen receptor gene disruption in male mice”, Proc. Natl. Acad. Sci. USA 94:1476-81.
Rissman et al., 1997, “Estrogen receptor function as revealed by knockout studies: neuroendocrine and behavioral aspects”, Horm. Behavior 31:232-243.
Rissman et al, 1997, “Estrogen receptors are essential for female sexual receptivity”, Endocrinology 138:507-10.
Rohlff et al., 1998, “Prostate cancer cell growth inhibition by tamoxifen is associated with inhibition of protein kinase C and induction of p21 (wafl/cip 1)”, Prostate 37:51-9.
Sar and Welsch, 1999, “Differential expression of estrogen receptor-beta and estrogen receptor-alpha in the rat ovary”, Endocrinology 140:963-71.
Shughrue et al., 1997, “Comparative distribution of estrogen receptor alpha- and beta mRNA in the rat central nervous system”, J. Comp Neurol. 388:507-25.
Shughrue et al., 1997, “The distribution of estrogen receptor beta mRNA in forebrain regions of the estrogen receptor-alpha knockout mouse”, Endocrinology 138:5649-52.
Shughrue et al., 1997, “Responses in the brain of estrogen receptor alpha disrupted mice”, Proc. Natl. Acad. Sci. USA 94:11008-12.
Simpson et al., 1998, Responses in the brain of estrogen receptor alpha disrupted mice, J Steroid Biochem Mol Biol 64:137-45.
Sun et al., 1999, “Novel ligands that function as selective estrogens or antiestrogens for estrogen receptor alpha or estrogen receptor beta”, Endocrinology 140:800-4.
Telleria et al., 1998, “Differential Expression of the Estrogen Receptors α and β in the Rat Corpus Luteum of Pregnancy: Regulation by Prolactin and Placental Lactogens”, Endocrinology 139:2432-2442.
Turner et al., 1998, “Differential Responses of Estrogen Target Tissues in Rats Including Bone toClomiphene, Enclomiphene, and Zuclomiphene”, Endocrinology 139:3712-20.
Yamashita et al., 1998, “Endocrine therapy in pancreatic carcinoma”, Oncology 55 Suppl. 1:17-22.
Bencze et al., “Synthetic Estrogens, Implantation Inhibitors, and Hypocholesterolemic Agents. I. Tetrahydronaphtalene Series,” Journal of Medicinal Chemistry 10:138-144, 1967.
Lednicer et al., “Mammalian Antifertility Agents. VI. A Novel Sequence for the Preparation of 1,2-Disubstituted 3,4-Dihydronaphthalenes,” Journal of Medicinal Chemistry 12:881-885, 1969.
Angier, “New Respect For Estrogen's Influence,” Science Times, The New York Times, Tuesday, Jun. 24, 1997.
Art et al., “Differential Expressions of Estrogen Receptors α and β mRNA During Differentiation of Human Osteoblast SV-HFO Cells,” Endocrinology 138(11):5067-5070, 1997.
Barkhem et al., “Differential Response of Estrogen Receptor α and Estrogen Receptor β to Partial Estrogen Agonists/Antagonists,” Molecular Pharmacology 54:105-112, 1998.
Cooke et al., “Mechanism of Estrogen Action: Lessons from the Estrogen Receptor-α Knockout Mouse,” Biology of Reproduction 59:470-475, 1998.
Couse et al., “Tissue Distribution and Quantitative Analysis of Estrogen Receptor-α (ERα) and Estrogen Receptor-β (ERβ) Messeneger Ribonucleic Acid in the Wild-Type and ERα-Knockout Mouse,” Endocrinology 138(11):4613-4621, 1997.
Cowley et al., “Estrogen Receptors α and β Form Heterodimers on DNA,” The Journal of Biological Chemistry 272(32):19858-19862, 1997.
Das et al., “Estrogenic Responses in Estrogen Receptor-α Deficient Mice Reveal a Distinct Estrogen Signaling Pathway,” Proc. Natl. Acad. Sci. USA 94:12786-12791, 1997.
Enmark et al., “Human Estrogen Receptor β-Gene Structure, Chromosomal Localization, and Expression Pattern,” Journal of Clinical Endocrinology and Metabolism 82(12) 4258-4265, 1997.
Gustafsson, “Therapeutic Potential of Selective Estrogen Receptor Modulators,” Current Opinion in Chemical Biology 2:508-511, 1998.
Katzenellenbogen and Korach, “Editorial: A New Actor in the Estrogen Receptor Drama-Enter ER-β,” Endocrinology 138(3):861-862, 1997.
Kuiper et al., “Cloning of a Novel Estrogen Receptor Expressed in Rat Prostate and Ovary,” Proc. Natl. Acad. Sci. USA 93:5925-5930, 1996.
Kuiper et al., “Comparison of the Ligand Binding Specificity and Transcript Tissue Distribution of Estrogen Receptors α and β,” Endocrinology 138(3):863-870, 1997.
Kuiper et al., “Interaction of Estrogenic Chemicals and Phytoestrogens with Estrogen Receptor β,” Endocrinology 139(10):4252-4263, 1998.
Laflamme et al., “Expression and Neuropeptidergic Characterization of Estrogen Receptors (ERαand ERβ) throughout the Rat Brain: Anatomical Evidence of Distinct Roles of Ea

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