Substituted benzopyrans as selective estrogen receptor-beta...

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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C549S385000, C549S390000

Reexamination Certificate

active

10493092

ABSTRACT:
The present invention relates to substituted benzopyran derivatives, stereoisomers, and pharmaceutical acceptable salts thereof and processes for the preparation of the same. The compounds of the present invention are useful as Estrogen Receptor β agonists. Such agonists are useful for the treating Estrogen Receptor β mediated diseases such as prostate cancer.

REFERENCES:
patent: 3901926 (1975-08-01), Winn et al.
patent: 6436923 (2002-08-01), Bhagwat et al.
patent: 6518301 (2003-02-01), Barlaam et al.
patent: 6593322 (2003-07-01), Bhagwat et al.
patent: 6630508 (2003-10-01), Dodge et al.
patent: 6794403 (2004-09-01), Malamas et al.
patent: 2 361 642 (2000-10-01), None
patent: WO 97/09348 (1996-09-01), None
patent: WO 99 02512 (1999-01-01), None
patent: WO 01/49673 (2001-07-01), None
patent: WO 01 64665 (2001-09-01), None
patent: WO 01/72713 (2001-10-01), None
patent: WO 03/051805 (2003-06-01), None
Shrestha KS et al, ‘Facil synthesis of the fused 6-6-5ring system containing chroman ring form 2-(1-1hydroxy-5-alkenyl)phenyl derivatives via intramolecular inverse-electron-demand diels-alder reaction’ CA 130:196557 (1999).
Anderson WK et al , ‘Snythesis of 6,9-bisnormethyl-8-methoxy-12, 13-epoxy-6,8, 10-trichothecatriene’ CA 86:121542 (1977).
Oude-Alink, BAM et al, ‘Photolysis of 2-keto-2,3-dihydrobenzofurans, o-hydroxystyrenes and 1-(o-hydroxyphenyl)-1,5-hexadienes’ CA 79:17767 (1973).
Weihua et al, Estrogen receptor beta in the prostate, Molecular and Cellular Endocrinology 193 (2002) 1-5.
Balfe et al, Estrogen receptor beta and breast cancer, PMID:1552549.
Speirs, Oestrogen receptor in breast cancer: good, bad or still too early to tell?, J. Pathol 2002, 197:143-147.
K SH. Shrestha, et al.: “Facile Synthesis of the Fused 6,6,5 Ring System Containing Chroman Ring from 2-(1-Hydroxy-5-alkenyl)phenol Derivatives via Intromolecular Inverse-Election-Demand Diels-Alder Reaction”: Bull. Chem. Soc. Japan, vol. 72, No. 1, (1999), pp. 73-83.
K.W. Anderson, et al.: “Synthesis of 6,9-bisnormethyl-8-methoxy-12, 13-epoxy-6,8, 10-trichothecatriene”: Journal of Organic Chemistry, vol. 42, No. 6, (1977), pp. 1045-1050.
B.A. M. Oude-Alink, et al.: “Photolysis of 2-keto-2, 3-dihydrobenzofurans, o-hydroxystyrenes and 1-o-hydroxyphenyl)-1, 5-hexadienes”: Journal of Organic Chemistry, vol. 38, No. 11, (1973), pp. 1993-2001.
Welhua, Zhang, et al.: “ARole for Estrogen Receptor β in the Regulation of Growth of the Ventral Prostate”; PNAS; vol. 98, No. 11, (2001), pp. 6330-6335.
Mortensen, Deborah S., et al.: “Synthesis and Biological Evaluation of a Novel Series of Furans: Ligands Selectie for Estrogen Receptor α”; Journal of Medicinal Chemistry; A-K, (May 11, 2001), PAGE EST: 10:8.
Meyers, Marvin J., et al.: “Estrogen Receptor-β Potency-Selective Ligands: Structure-Activity Relationship Studies of Diarylpropionitriles and Their Acetylene and Polar Analogues”; Journal of Medicinal Chemistry, A-V, (Jun. 6, 2001), PAGE EST:21:3.
Kuiper, et al., “Cloning of a novel estrogen receptor expressed in rat prostate of ovary,”Proc. Natl. Acad. Sci. USA,vol. 93, pp. 5925-5930 (1996).
Tremblay, et al., “Cloning, Chromosomal Localization, and Functional Analysis of the Murine Estrogen Receptor β,”Molecular Endocrinology, vol. 11, No. 3, pp. 353-365 (1997).
Weihua, et al., “Estrogen receptor beta in the prostate,”Molecular and Cellular Endocrinology, vol. 193, pp. 1-5 (2002).
Balfe, et al., “Estrogen receptor β and breast cancer,”EJSO, vol. 30, pp. 1043-1050 (2004).
Speirs, “oestrogen receptor β in breast cancer: good, bad or still too early to tell?”Journal of Pathology, vol. 197, pp. 143-147 (2002).
Muchmore, “Raloxifene: A Selective Estrogen Receptor Modulator (SERM) with Multiple Target System Effects,”The Oncologist, vol. 5, pp. 388-392 (2000).
Katzenellenbogen, et al., “Editorial: A New Actor in the Estrogen Receptor Drama—Enter ER-β,”Endocrinology, vol. 138. No. 3, pp. 861-862 (1997).
Mosselmann, et al., “ERβ: identification and characterization of a novel human estrogen receptor,”FEBS Letters, vol. 392, pp. 49-53 (1996).
Paech, et al., “Differential Ligand Activation of Estrogen Receptors Erα and ERβ at AP1 Sites,”Science, vol. 277, pp. 1508-1510 (1997).
Sun, et al., “Novel Ligands the Function as Selective Estrogens or Antiestrogens for Estrogen Receptor-α or Estrogen Receptor-β*,”Endocrinology, vol. 140, No. 2, pp. 800-804 (1999).
Couse, et al., “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, vol. 138, No. 11, pp. 4613-4621 (1997).
Kuiper, et al., “Comparison of the Ligand Binding specificity and Transcript Tissue Distribution of Estrogen Receptors α and β,”Endocrinology, vol. 138, No. 3, pp. 863-870 (1997).
Brandenberger, et al., “Estrogen Receptor Alpha (ER-α) and Beta (ER-β) mRNAs in Normal Ovary, Ovarian Serous Cystadenocarcinoma and Ovarian Cancer Cell Lines: Down-Regulation of ER-β in Neoplastic Tissues,”Journal of Clinical Endocrinology and Metabolism, vol. 83, No. 3. pp. 1025-1028 (1998).
Enmark, et al., “Human Estrogen Receptor β-Gene Structure, Chromosomal Localization, and Expression Pattern,”Journal of Clinical Endocrinology and Metabolism, vol. 82, No. 12, pp. 4258-4265 (1997).
Laflamme, et al., “Expression and Neuropeptidergic Characterization of Estrogen Receptors (ERα and ERβ) throughout the Rat Brain: Anatomical Evidence of Distinct Roles of Each Subtype,”J. Neurobiol.vol. 36, No. 3, pp. 357-578 (1998).
Sar, et al., “Differential Expression of Estrogen Receptor-β and Estrogen Receptor-α in the Rat Ovary,”Endocrinology, vol. 140, No. 2, pp. 963-971 (1999).
Shughrue, et al., “The Distribution of Estrogen Receptor-β nRNA in Forebrain Regions of the Estrogen Receptor-a Knockout Mouse,”Endocrinology, vol. 138, No. 12, pp. 5649-5652 (1997).
Shughrue, et al., “Comparative Distribution of Estrogen Receptor-α and -β nRNA in the Rat Central Nervous System,”The Journal of Comparative Neurology, vol. 388, No. 4, pp. 507-525 (1997).
Chang, et al., “Estrogen Receptor-β: Implications for the Prostate Gland,”The Prostate, vol. 40, pp. 115-124 (1999).
Korach, “Insights from the Study of Animals Lacking Functional Estrogen Receptor,”Science, vol. 266, pp. 1524-1527 (1994).
Krege, et al., “Generation and reproductive phenotypes of mice lacking estrogen receptor β,”Proc. Natl. Acad. Sci USA, vol. 95, pp. 15677-15682 (1998).
Cooke, et al., “Mechanism of Estrogen Action: Lessons from the Estrogen Receptor-α Knockout Mouse,”Biology of Reproduction, vol. 59, pp. 470-475 (1998).
Das, et al., “Estrogenic responses in estrogen receptor-α deficient mice reveal a distinct estrogen signaling pathway,”Proc. Natl. Acad. Sci. USA, vol. 94, pp. 12786-12791 (1997).
Ogawa, et al., “Behavioral effects of estrogen receptor gene disruption in male mice,”Proc. Natl. Acad. Sci, USA, vol. 94, pp. 1476-1481 (1997).
Rissman et al., “Estrogen Receptors are Essential for Female Sexual Receptivity,”Endocrinology, vol. 138, No. 1, pp. 507-510 (1997).
Rissman, et al., “Estrogen Receptor Function as Revealed by Knockout Studies: Neuroendocrine and Behavioral Aspects,”Hormones and Behavior., vol. 31, pp. 232-243 (1997).
Sughrue, et al., “Responses in the brain of estrogen receptor α-disrupted mice,”Proc. Natl. Acad. Sci. USA, vol. 94, pp. 11008-11012 (1997).
Iafrati, et al., “

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