Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Reexamination Certificate
2005-08-09
2005-08-09
Stockton, Laura L. (Department: 1626)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
C514S367000, C514S539000, C514S602000, C514S603000, C514S604000, C514S605000, C514S445000, C549S065000, C546S234000, C548S167000, C560S012000, C564S089000, C564S097000, C564S086000, C564S088000, C564S091000, C564S087000, C564S099000, C562S098000
Reexamination Certificate
active
06927224
ABSTRACT:
The present invention provides, inter alia, triphenylethylene derivatives, such as, 3-{4-[6-(3-Methoxy-phenyl)-8,9-dihydro-7H-benzocyclohepten-5-yl]-phenyl}-acrylic acid, as selective estrogen receptor modulators. Also provided are methods for the treatment and/or prevention of estrogen stimulated diseases in mammals including breast, uterine, ovarian, prostrate and colon cancer, osteoporosis, cardiovascular disease, and benign proliferative disorders, as well as pharmaceutical compositions of the compounds of the present invention.
REFERENCES:
patent: 5681835 (1997-10-01), Willson
patent: 6005003 (1999-12-01), Nique
patent: WO 99/08682 (1999-02-01), None
patent: WO 01/26651 (2001-04-01), None
patent: WO 01/77055 (2001-10-01), None
patent: WO 01/77057 (2001-10-01), None
Willson, T.M. et al., “3-[4-(1,2-Diphenylbut-1-enyl)phenyl]acrylic Acid: A Non-Steroidal Estrogen with Functional Selectivity for Bone over Uterus in Rats”, J. Med. Chem., vol. 37, pp. 1550-1552 (1994).
Weatherman, R.V. et al., “Differential SERM activation of the estrogen receptors (ERα and ERβ) at AP-1 sites”, Chemistry & Biology, vol. 8, pp. 427-436 (2001).
Database CAPLUS [Online] Chemical Abstracts Service, Columbus, Ohio, U.S., Database accession No. 121:34956 XP0022222761 *RNs: 155701-59-0, 155701-64-4, 155701-70-5, 155701-71-6* abstract (1994).
Eaker, E.D. et al., “Cardiovascular Disease in Women”, Circulation, vol. 88, No. 4, Part 1, pp. 1999-2009 (1993).
Evans, R.M., “The Steroid and Thyroid Hormone Receptor Superfamily”, Science, vol. 240, pp. 889-895 (1988).
Jordan, V.C. et al., “Endocrine Pharmacology of Antiestrogens as Antitumor Agents”, Endocrine Reviews, vol. 11, No. 4, pp. 578-610 (1990).
Kedar, R.P. et al., “Effects of tamoxifen on uterus and ovaries of postmenopausal women in a randomised breast cancer prevention trial”, Lancet, vol. 343, pp. 1318-1321 (1994).
Love, R.R. et al., “Effects of Tamoxifen on Bone Mineral Density in Postmenopausal Women with Breast Cancer”, The New England Journal of Medicine, vol. 326, No. 13, pp. 852-856 (1992).
Love, R.R. et al., “Effects of Tamoxifen on Cardiovascular Risk Factors in Postmenopausal Women”, Annals of Internal Medicine, vol. 115, pp. 860-864 (1991).
McCague, R. et al., “Synthesis and Estrogen Receptor Binding of 6,7-Dihydro-8-phenyl-9-[4-[2-(dimethylamino)ethoxy]phenyl]-5H-benzocycloheptene, a Nonisomerizable Analogue of Tamoxifen. X-ray Crystallographic Studies”, J. Med. Chem. vol. 29, pp. 2053-2059 (1986).
McDonnell, D.P. et al., “Analysis of Estrogen Receptor Function in Vitro Reveals Three Distinct Classes of Antiestrogens”, Molecular Endocrinology, vol. 9, No. 6, pp. 659-669 (1995).
Parker, M.G., “Action of ‘pure’ antiestrogens in inhibiting estrogen receptor action”, Breast Cancer Research and Treatment, vol. 26, pp. 131-137 (1993).
Tasset, D. et al., “Distinct Classes of Transcriptional Activating Domains Function by Different Mechanisms”, Cell, vol. 62, pp. 1177-1187 (1990).
Tonetti, D.A. et al., “Possible mechanisms in the emergence of tamoxifen-resistant breast cancer”, Anti-Cancer Drugs, vol. 6, pp. 498-507 (1995).
Tora, L. et al., “The Human Estrogen Receptor Has Two Independent Nonacidic Transcriptional Activation Functions”, Cell, vol. 59, pp. 477-487 (1989).
Tzukerman, M.T. et al., “Human Estrogen Receptor Transactivational Capacity is Determined by both Cellular and Promoter Context and Mediated by Two Functionally Distinct Intramolecular Regions”, Molecular Endocrinology, vol. 8, No. 1, pp. 21-30 (1994).
Wagner, B.L. et al., “16α-substituted analogs of the antiprogestin RU486 induce a unique conformation in the human progesterone receptor resulting in mixed agonist activity”, Proc. Natl. Acad. Sci. USA, vol. 93, pp. 8739-8744 (1996).
Beekman, J.M. et al., “Transcriptional Activation by the Estrogen Receptor Requires a Conformational Change in the Ligand Binding Domain”, Molecular Endocrinology, vol. 7, No. 10, pp. 1266-1274 (1993).
Black, L.J. et al., “Raloxifene (LY139481 HCl) Prevents Bone Loss and Reduces Serum Cholesterol without Causing Uterine Hypertrophy in Ovariectomized Rats”, J. Clin. Invest., vol. 93, pp. 63-69 (1994).
Chow, J. et al., “Estrogen Maintains Trabecular Bone Volume in Rats Not Only by Suppression of Bone Resorption but Also by Stimulation of Bone Formation”, J. Clin. Invest., vol. 89, pp. 74-78 (1992).
Scanlan, Thomas S., “Differential SERM activation of the estrogen receptors (ERα and ERβ ) at AP-1 sites”, Chemistry & Biology, vol. 8, No. 5, pp. 427-436 (2001) (XP002220838).
PCT International Search Report mailed Feb. 26, 2003.
Kaltenbach Robert F.
Robinson Simon P.
Trainor George L.
Bristol Myers Squibb Company
Cohen Jacqueline M.
Korsen Elliott
Stockton Laura L.
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