Estrogen receptor modulators

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

Reexamination Certificate

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C548S240000, C548S247000

Reexamination Certificate

active

06869969

ABSTRACT:
Isoxazole estrogen receptor agonist and antagonist compounds having unexpected and surprising activity in modulating estrogen receptor activity are described. In addition, methods and compositions for treating or preventing estrogen receptor-mediated disorders are disclosed. The compounds, methods, and compositions of the invention have utility in preventing or treating estrogen receptor-mediated disorders such as osteoporosis, breast and endometrial cancers, atherosclerosis, and Alzheimer's disease.

REFERENCES:
patent: 4112108 (1978-09-01), Nadelson
patent: 4229204 (1980-10-01), Howe
patent: 4268678 (1981-05-01), Diana et al.
patent: 5512564 (1996-04-01), Zilch et al.
patent: 5547967 (1996-08-01), Kehrbach et al.
patent: 5565482 (1996-10-01), Talley et al.
patent: 5859257 (1999-01-01), Talley
patent: 5861359 (1999-01-01), Theodoridis
patent: 6030970 (2000-02-01), Elliot et al.
patent: 6069141 (2000-05-01), Barbachyn et al.
patent: 6114328 (2000-09-01), Wityak et al.
patent: 6114367 (2000-09-01), Cohan et al.
patent: 6187797 (2001-02-01), Pruitt et al.
patent: 6221876 (2001-04-01), Gruber et al.
patent: 6245796 (2001-06-01), Maceno et al.
patent: 6441014 (2002-08-01), Talley et al.
patent: 6495582 (2002-12-01), Hale et al.
patent: 6531498 (2003-03-01), Eggenweiler et al.
patent: 6579880 (2003-06-01), Weidner-Wells et al.
patent: 6583141 (2003-06-01), Freyne et al.
patent: 6613719 (2003-09-01), Kudis et al.
patent: 6624311 (2003-09-01), DiCosimo et al.
patent: DD 295 360 (1983-10-01), None
patent: DD 295 630 (1983-10-01), None
patent: 2 250 343 (1972-10-01), None
patent: 24 41504 (1975-03-01), None
patent: 31 19727 (1982-12-01), None
patent: 38 32 570 (1988-09-01), None
patent: 41 26543 (1993-02-01), None
patent: 4230839 (1993-03-01), None
patent: 0 761 654 (1977-03-01), None
patent: 026928 (1981-04-01), None
patent: 0 405 905 (1991-01-01), None
patent: 0 435 381 (1991-07-01), None
patent: 442448 (1991-08-01), None
patent: 0 456 519 (1991-11-01), None
patent: 0 577 218 (1994-01-01), None
patent: 623603 (1994-11-01), None
patent: 2104932 (1972-04-01), None
patent: 55-83766 (1980-06-01), None
patent: 3-74374 (1991-03-01), None
patent: 3-208044 (1991-09-01), None
patent: 7-215952 (1995-08-01), None
patent: WO 9415920 (1994-07-01), None
patent: WO 9417059 (1994-08-01), None
patent: WO 9418201 (1994-08-01), None
patent: WO 9504049 (1995-02-01), None
patent: WO 9506032 (1995-03-01), None
patent: WO 9513262 (1995-05-01), None
patent: 9625405 (1996-08-01), None
patent: 9701551 (1997-01-01), None
patent: WO 9705115 (1997-02-01), None
patent: WO 9711690 (1997-04-01), None
Shankar et al., “One Pot Solid Phase Synthesis of Isoxazolines”, Tetrahedron Letters, 39 (1998) 2447-2448.
Taylor et al., “Simultaneous On-Line Characterization of Small Organic Modecules Derived from Combinatorial Libraries for Identify, Quantity, and Purity by Reversed-Phase HPLC with Chemiluminescent Nitrogen, UV, and Mass Spectrometric Detection”, AC Research, Anal. Chem., 1998, 70, 3339-3347.
Doyle et al., “Derivatives of 6-Aminopenicillanic Acid. Part VII. Further 3,5-Disubstituted Isoxazole-4-Carboxylic Acid Derivatives”, Journal of The Chemical Society, Dec. 1963, pp. 5845-5854.
Hanson et al., “Derivatives of 6-Aminopenicillanic Acid. Part VIII, Further Analogues of 3-o-Chlorophenyl-5-methyl-4-isoxazolypenicillin”, Journal of the Chemical Society, Nov. 1965, pp. 5976-5983.
Doyle et al., “Derivatives of 6-Aminopenicillanic Acid. Part VI, Penicillins from 3-and 5-Phenylisoxazole-4-carboxylic Acids and their Alkyl and Halogen Derivatives”, Journal of The Chemical Society, Dec. 1963, pp. 5838-5845.
Hamper et al., “Synthesis and Herbicidal Activity of 3-Aryl-5-(haloalkyl)-4isoxazolecarboxamides and Their Derivatives”, J. Agric. Food Chem. 1995, 43, pp. 219-228.
Shanker et al., Synthesis and Cleavage Reactions of Benzothiazepinyl Chromone Derivatives, Phosphoros, Sulfur, and Silicon, 1989, vol. 44, pp. 143-147.
Amme et al., “Synthesis, Binding Affinities and Uterotrophic Activity of Some 2-Substituted Estradiol and Ring-A-Fused Pyrone Derivatives”Eur. J. Med. Chem. 29:25-32, 1994.
Duncan et al., “The Preparation of N-Carboalkoxypyrazoles and N-Phenylpyrazoles from C(α)-Dianions of Carboalkoxyhydrazones and Phenylhydrazones”J. Heterocyclic Chem. 24:555, 1987.
Fink et al., “Novel Structural Templates for Estrogen-Receptor Ligands and Prospects for Combinatorial Synthesis of Estrogens”Chemistry and Biology 6:205-219, Apr., 1999.
Sun et al., “Novel Ligands that Function as Selective Estrogens or Antiestrogens for Estrogen Receptor-α or Estrogen Receptor-β”Endrocrinology 140(2):800-804, 1999.
Wachter et al., “Tetrahydronaphthalenes: Influence of Heterocyclic Substituents on Inhibition of Steroidogenic Enzymes P450 arom and P450 17”J. Med. Chem. 39:834-841, 1996.
Meisenheimer et al., “Uber Triaryl-Isoxazole”Chemische Berichte3195-3206, 1921.
Krishna et al., “Synthesis and Physiological Activity of 3-Hydrxy-Pheny-5-Aryl Isoxazoles”Chemical Abstracts 79(13):487, 1973.
Yamawaki et al., “Synthesis and Biological Activity of the Metabolites of [3, 4-Bis(4-Methoxyphenyl)-5-Isoxazolyl] Acetic Acid”Chemical and Pharmaceutical Bulletin 36(8):3142-3146, 1988.
Kim et al., “Reactions of 5-Substituted 3-Alkyl- and 3-Aryl-Isoxaozoles with Tetrasulfur Tetranitride Antimony Pentachloride Complex (S4N4SbCl5): Complete Regioselective Formation of 4-Substituted 3-Acyl- and 3-Aroyl-1, 2,5-Thiadiozoles and Their Mechanism of Formation”J. Chemical Society 14:2175-2180, 1998.
Mohan et al., “Search for Physiologically Active Compounds XIV Synthesis of Some 3,5-Disubstituted Isoxazoles and Their Physiological Activity”Chemical Abstracts 69(11):4107, 1968.
Wrobel et al., “Conversion of 1-(O-Nitroaryl) Alkyl P-Tolysulfones into Isoxazoles”Heterocycles 40(1):187-190, 1995.
Kasturi et al., “Reaction of Spironaphthalenones with Hydroxylamine Hydrochloride: Part IV”Tetrahedron 51(10):3051-3060, 1995.
Bass, R.G., Polymer Preprints (American Chemical Society) 32(2):160-161, 1991.
Sulfonyl pyrazoles and isoxazoles: cycloaddition of nitrile imines and nitrile oxides to aryl styryl sulfones. Padmavathi, et al., Department of Chemistry, Sri Venkateswara University, Indian Journal of Chemistry, Section B: Organic Chemistry Including Medicinal Chemistry (1998), 37B(12), 1286-1289. (abstract).
Reactions of 5-substituted 3-alkyl- and 3-aryl-isoxazoles with tetrasulfur tetranitride antimony pentachloride complex (S4N4.SbCI5): complete regioselective formation of 4-substituted 3-acyl- and 3-aroyl-1,2,5-thiadiazoles and their mechanism of formation. [Erratum to document cited in CA129:175594]. Kim, et al., Department of Chemistry, Journal of the Chemical Society, Perkin Transactions 1: Organic and Bio-Organic Chemistry (1998), (18). 3121. (abstract).
Intermolecular cycloaddition of nitrile imines and nitrile oxides to 1,3-diarylprop-2-en-1 -ones. Padmavathi, et al., Department of Chemistry, Heterocyclic Communications (1998), 4(2), 163-168. (abstract).
Reactions of 5-substituted 3-alkyl- and 3-arylisoxazoles with tetrasulfur tetranitride antimony pentachloride complex (S4N4.SbCI5): complete regioselective formation of 4-substituted 3-acyl- and 3-aroyl-1,2,5-thiadiazoles and their mechanism of formation. Kim, et al., Department of Chemistry, Seoul National University, Seoul, S. Korea. Journal of the Chemical Society, Perkin Transactions 1: Organic and Bio-Organic Chemistry (1998), (14), 2175-2180. (abstract).
Some reactions of I-phenyl-3-(4,6-dimethoxy- or 4,6,7-trimethoxy-5-benzofuranyl)-1,3-propanedione. Saleh, Nadia M. Faculty of Science, Chemistry Department, AI-Azhar University, (for girls), Nasr City, Egypt. Al-Azhar Bulletin of Science (1996), 7(1, Pt. 1), 19-27. (abstract).
1,3-diphenylpropane-1, 3-diamines. Part VIII. Reactions of lithiated oximes and oxime ethers with C:N-electrophiles. Kaise

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