Selective estrogen receptor modulators

Details Selective estrogen receptor modulators Selective estrogen receptor modulators

2008-01-29

2008-01-29

Stockton, Laura L. (Department: 1626)

Organic compounds -- part of the class 532-570 series

Organic compounds

Carboxylic acid esters

C514S577000

Reexamination Certificate

active

11152891

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 treating estrogen stimulated diseases in mammals including, but not limited to, for example, breast, uterine, ovarian, prostate and colon cancer; osteoporosis; endometriosis; uterine fibroid; Alzheimer's disease; macular degeneration; urinary incontinence; and type II diabetes, as well as, pharmaceutical compositions comprising at least one compound 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
Merchenthaler et al., Drug Development Research, 66, pp. 172-181 (2006).
Diaz Brinton, Journal of Alzheimer's Disease, 6, (2004), pp. S27-S35.
Dhandapani et al., Biology of Reproduction, 67, pp. 1379-1385, (2002).
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 HCI) 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).
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)ethox]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).
PCT International Search Report mailed Feb. 26, 2003, PCT/US02/25394.
Scanlan, Thomas S., “Differential SERM activation of the estrogen receptors (ERalpha and ERbeta) at AP-1 sites”, Chemistry & Biology, vol. 8, No. 5, pp. 427-436 (2001) (XP002220838).
Tasset, D. et al., “Distinct Classes of Trancriptional Activating Domains Function by Different Mechanism”, 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).
Tzukeman, 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., “16-α-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).
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 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, 155701-61-4, 155701-70-5, 155701-71-6* abstract (1994).

Affiliated with

Also associated with

Rating

Selective estrogen receptor modulators does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Selective estrogen receptor modulators, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Selective estrogen receptor modulators will most certainly appreciate the feedback.

Rate now

Comments { 0 }

Profile ID: LFUS-PAI-O-3929784