Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Reexamination Certificate
2007-10-09
2007-10-09
Coleman, Brenda (Department: 1624)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
C546S144000
Reexamination Certificate
active
10434341
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 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 ER-β. 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, natureal hormonal imbalances, and adverse reproductive effects associated with exposure to environmental chemicals.
REFERENCES:
patent: 3234090 (1966-02-01), Huebner et al.
patent: 3274213 (1966-09-01), Lednicar
patent: 3277106 (1966-10-01), Bencze
patent: 842 661 (1998-05-01), None
patent: 1 113 007 (2001-04-01), None
patent: 1143833 (1987-11-01), None
patent: WO92/18498 (1992-10-01), None
patent: WO96/21656 (1996-07-01), None
patent: WO 00/39120 (2000-07-01), None
patent: WO 00/55137 (2000-09-01), None
Angier, “New Respect For Estrogen's Influence,”Science Times, The New York Times, Tuesday, Jun. 24, 1997.
Arts 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 Parial Estrogen Agonists/Antagonists,”Molecular Pharmacology 54:105-112, 1998.
Bencze et al., “Synthetic Estrogens, Implantation Inhibitors, and Hypocholesterolemic Agents. I. Tetrahydronaphtalene Series,”Journal of Medicinal Chemistry 10:138-144, 1967.
Brandenberger et al., “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, 1998.
CAS printout for Sainsbury et al.,Tetrahedron 48: 8739-50, 1992.
CAS printout for Battersby et al.,J. Chem. Soc. 18: 1739-44, 1967.
CAS printout for Gibson et al.,J. Chem. Soc. 16: 2234-8, 1970.
CAS printout forTantisewie et al.,J. Nat. Prod. 53: 553-8, 1990.
CAS printout for Shavel et al., U.S. Patent No. 3,438,989, Apr. 15, 1969.
CAS printout for U.S. Patent No. 577,817, Jun. 22, 1984.
CAS printout for Bruneton et al.,J. Org. Chem. 48: 3957-60, 1983.
CAS printout for Hsu et al.,Helv. Chim. Acta 65: 1576-89, 1982.
CAS printout for Hoshino et al.,Tetrahedron; Asymmetry 4: 933-42, 1993.
CAS printout for Guinaudeau et al.,Tetrahedron 40: 1975-82, 1984.
CAS printout for Akasu et al., Japanese Patent No. 1,143,833 (English language abstract for reference AJ), Jun. 1989.
CAS printout for Mandell et al.,Heterocycles 26: 713-720, 1987.
CAS printout for Popp et al.,J. Heterocycl. Chem. 15: 429-32, 1978.
CAS printout for Razdan et al.,J. Org. Chem. 44: 3730-1, 1979.
CAS printout for Weisbach et al.,J. Med. Chem. 11: 752-60, 1968.
CAS printout for Kashdan et al.,J. Org. Chem. 47: 2638-43, 1982.
Chang and Prins,The Prostate 40, 115-124, 1999.
Clinton and Hua,Crit. Rev. Oncol. Hematol. 25, 1-9, 1997.
Cooke et al., 1998, “Mechanism of Estrogen Action: Lessons from the Estrogen Receptor-α Knockout Mouse,”Biology of Reproduction 59:470-475.
Couse et al., 1997, “Tissue Distribution and Quantitative Analysis of Estrogen Receptor-α (ERα) and Estrogen Receptor-β (ERβ) Messenger Ribonucleic Acid in the Wild-Type and ERα-Knockout Mouse,”Endocrinology 138(11):4613-4621.
Das et al., 1997, “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.
Farhat et al., 1996, “The vascular protective effects of estrogen”,FASEB J. 10: 6154-624, 1996.
Gustafsson, 1998, “Therapeutic Potential of Selective Estrogen Receptor Modulators,”Current Opinion in Chemical Biology 2:508-511.
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”, 3(5):545-8.Nature Med. 3, 545-8.
Katzenellenbogen and Korach, 1997, “Editorial: A New Actor in the Estrogen Receptor Drama-Enter ER-β,”Endocrinology 138(3):861-862.
Korach, 1994, “Insights from the study of animals lacking functional estrogen receptor”Science 266, 1524-1527.
Krege et al., 1998, “Generation and reproductive phenotypes of mice lacking estrogen receptor beta”,Proc. Natl. Acad. Sci. USA 95, 15677-82.
Kuiper et al., 1997, “Comparison of the Ligand Binding Specificity and Transcript Tissue Distribution of Estrogen Receptors α and β,”Endocrinology 138(3):863-870.
Kuiper et al., 1998, “Interaction of Estrogenic Chemicals and Phytoestrogens with Estrogen Receptor β,”Endocrinology 139(10):4252-4263.
Kuiper et al., 1996, “Cloning of a Novel Estrogen Receptor Expressed in Rat Prostate and Ovary,”Proc. Natl. Acad. Sci. USA 93:5925-5930.
Laflamme et al., 1998, “Expression and Neuropeptidergic Characterization of Estrogen Receptors (ERα and ERβ) throughout the Rat Brain: Anatomical Evidence of Distinct Roles of Each Subtype,”J. Neurobiol. 36:357-378, 1998.
Lednicer et al., 1969, “Mammalian Antifertility Agents. VI. A Novel Sequence for the Preparation of 1,2-Disubstituted 3,4-Dihydronaphthalenes,”Journal of Medicinal Chemistry 12:881-885.
Mosselman et al., 1996, “ERβ Identification and Characterization of a Novel Human Estrogen Receptor,”FEBS Letters 392:49-53.
Nilsson et al,TEM 9, 387-395, 1998.
Ogawa et al., 1997, “Behavioral effects of estrogen receptor gene disruption in male mice”,Proc. Natl. Acad. Sci. USA 94, 1476-81.
Ogawa et al., 1998, “The Complete Primary Structure of Human Estrogen Receptor β (hERβ) and Its Heterodimerization with ER α in Vivo and in Vitro,”Biochemical and Biophysical Research Communications 243:122-126.
Onoe et al., “Expression of Estrogen Receptor β in Rat Bone,”Endocrinology 138(10):4509-4512, 1997.
Paech et al., “Differential Ligand Activation of Estrogen Receptors ERα and ERβ at AP1 Sites,”Science 277:1508-1510, 1997.
Petersen et al., 1998, “Identification of Estrogen Receptor β2, A Functional Variant of Estrogen Receptor β Expressed in Normal Rat Tissues,”Endocrinology 139(2):1082-1092.
Rissman et al., 1997, “Estrogen receptor function as revealed by knockout studies: neuroendocrine and behavioral aspects.”,Horm Behav. 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(waf1/cip1)”,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, “The distribution of estrogen receptor-beta mRNA in forebrain regions of the estrogen receptor-alpha knockout mouse”,Endocrinology 138, 5649-52.
Shughrue et al.,
Bhagwat Shripad S.
Chao Qi
Gangloff Anthony R.
Gayo-Fung Leah Marie
McKie Jeffrey A.
Coleman Brenda
Jones Day
Signal Pharmaceuticals LLC
LandOfFree
Compounds and methods for modulation of estrogen receptors does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Compounds and methods for modulation of estrogen receptors, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Compounds and methods for modulation of estrogen receptors will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-3847105