PPAR-activating compound and pharmaceutical composition...

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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Details

C548S222000

Reexamination Certificate

active

07109226

ABSTRACT:
A compound represented by the following formula (1):Or a salt thereof; and therapeutic durgs containing the compound. The compound selectively activates PPARα.

REFERENCES:
patent: 6653334 (2003-11-01), Yamazaki et al.
patent: WO 97/28149 (1997-08-01), None
patent: WO 02/46176 (2002-06-01), None
Isabelle Issemann et al., “Activation of a member of the steroid hormone receptor superfamily by peroxisome proliferators”.NATURE, vol. 347, pp. 645-650., Oct. 18, 1990.
Christine Dreyer, et al., “Control of the Peroxisomal β-Oxidation Pathway by a Novel Family of Nuclear Hormone Receptors”,CELL, vol. 68, pp. 879-887, Mar. 6, 1992.
Letter to the Editor, “A Unified Nomenclature System for the Nucleur Receptor Superfamily”,Cell, vol. 97, pp. 161-163, Apr. 16, 1999.
Kristina Schoonjans, et al., “The peroxisome proliferator activated receptors (PPARs) and their effects on lipid metabolism and adipocyte differentiation”,Biochimica Et Biophysica Acta, vol. 1302, pp. 93-109. (1996).
Timothy M. Willson, et al., “The PPARs: From Orphan Receptors to Drug Discovery”,Journal of Medicinal Chemistry, vol. 43, No. 4, pp. 527-550. Feb. 24, 2000.
Mauricio Reginato, et al., “Mechanisms by which Thiazolidinediones Enhance Insulin Action”,TEM, vol. 10, No. 1, pp. 9-13. (1999).
Akira Okuno, et al., “Troglitazone Increases the Number of Small Adipocytes Without the Change of White Adipose Tissue Mass in Obese Zucker Rats”,J. Clin Invest., vol. 101, No. 6, pp. 1354-1361, Mar. 1998.
Jennifer L. Oberfield, et al., “A peroxisome proliferator-activated receptor y ligand inhibits adipocyte differentiation”,Proc. Natl. Acad. Sci USA, vol. 96, pp. 6102-6106, May 1999.
Harold M. Wright et al., “A Synthetic Antagonist for the Peroxisome Proliferator-activated Receptor y Inhibits Adipocyte Differentiation”,The Journal of Biological Chemistry, vol. 275, No. 3, pp. 1873-1877. (2000).
Toshimasa Yamauchi, et al., “Inhibitin of RXR and PPARy ameliorates diet-induced obesity and type 2 diabetes”,The Journal of Clinical Investigation, vol. 108, No. 7, pp. 1001-1013, Oct. 2001.
Didier Auboeuf, et al., “Tissue Distribution and Quantification of the Expression of mRNAs of Peroxisome Proliferator-Activated Receptors and Liver X Receptor-α in Humans, No Alteration in Adipose Tissue of Obese and NIDDM Patients”,Diabetes, vol. 46, pp. 1319-1327, Aug. 1997.
William R. Oliver, Jr., et al., “A selective peroxisome proliferator-activated receptor δ agonist promotes reverse cholesterol transport”,PNAS, vol. 98, No. 9, pp. 5306-5311, Apr. 24, 2001.
Yong-Xu Wang, et al., “Peroxisome-Proliferator-Activated Receptor δ Activates Fat Metabolism to Prevent Obesity”,Cell, vol. 113, pp. 159-170, Apr. 18, 2003.
Isabelle Issemann et al., “Activation of a member of the steroid hormone receptor superfamily by peroxisome proliferators”,Nature, vol. 347, pp. 645-650., Oct. 18, 1990.
Christine Dreyer, et al., “Control of the Peroxisomal β-Oxidation Pathway by a Novel Family of Nuclear Hormone Receptors”,CELL, vol. 68, pp. 879-887, Mar. 6, 1992.
Letter to the Editor, “A Unified Nomenclature System for the Nucleur Receptor Superfamily”,Cell, vol. 97, pp. 161-163, Apr. 16, 1999.
Kristina Schoonjans, et al., “The peroxisome proliferator activated receptors (PPARs) and their effects on lipid metabolism and adipocyte differentiation”,Biochimica Et Biophysica Acta, vol. 1302, pp. 93-109. (1996).
Timothy M. Willson, et al., “The PPARs: From Orphan Receptors to Drug Discovery”,Journal of Medicinal Chemistry, vol. 43, No. 4, pp. 527-550. Feb. 24, 2000.
Frank J. Gonzalez, et al., “Mechanism of Action of the Nongenotoxic Peroxisome Proliferators: Role of the Peroxisome Proliferator-Activated Receptor α”,Journal of the National Cancer Institute. vol. 90, No. 22, Nov. 18, 1998.
Jean-Charles Fruchart, et al., “Peroxisome proliferator-activated receptor-alpha activators regulate genes governing lipoprotein metabolism, vascular inflammation and atherosclerosis”,Current Opinion in Lipidology, vol. 10, pp. 245-257 (1999).
Johan Auwerx, et al., “Regulation of Triglyceride Metabolism by PPARs: Fibrates and Thiazolidinediones have Distinct Effects”,Journal of Atherosclerosis and Thrombosis, vol. 3, No. 2, pp. 81-89. (1996).
Bart Staels. et al., “Role of PPAR in the Pharmacological Regulation of Lipoprotein Metabolism by Fibrates and Thiazolidinediones”,Current Pharmaceutical Design, vol. 3, pp. 1-14, (1997).
Inés Pineda Torra, et al., “Peroxisome proliferator-activated receptor alpha in metabolic disease, inflammation, atherosclerosis and aging”,Current Opinion in Lipidology, vol. 10, pp. 151-159, (1999).
Joseph Vamecq, et al., “Medical significance of peroxisome proliferator-activated receptors”,THE LANCET, vol. 354, pp. 141-148, Jul. 10, 1999.
Sander J. Robins, “PPARα ligands and clinical trials: cardiovascular risk reduction with fibrates”,Journal of Cardiovascular Risk, vol. 8, pp. 195-201. (2001).
Jürgen M. Lehmann, et al., “An Antidiabetic Thiazolidinedione Is a High Affinity Ligand for Peroxisome Proliferator-activated Receptor y (PPARy)”, The Journal of Biological Chemistry, vol. 270, No. 22, pp. 12953-12956. (1995).
Joel Berger, et al., “Thiazolidinediones Produce a Conformational Change in Peroxisomal Proliferator-Activated Receptor-y: Binding and Activation Correlate with Antidiabetic Actions in db/db Mice”,Endocrinology, vol. 137, No. 10, pp. 4189-4195. (1996).
Mauricio Reginato, et al., “Mechanisms by which Thiazolidinediones Enhance Insulin Action”,TEM, vol. 10, No. 1, pp. 9-13. (1999).
Akira Okuno, et al., “Troglitazone Increases the Number of Small Adipocytes Without the Change of White Adipose Tissue Mass in Obese Zucker Rats”,J. Clin Invest., vol. 101, No. 6, pp. 1354-1361, Mar. 1998.
Naoki Sakane, et al., “Glitazones and NIDDM”,The Lancet, vol. 349, pp. 952, Mar. 29, 1997.
Jennifer L. Oberfield, et al., “A peroxisome proliferator-activated receptor y ligand inhibits adipocyte differentiation”,Proc. Natl. Acad. Sci USA, vol. 96, pp. 6102-6106, May 1999.
Harold M. Wright et al., “A Synthetic Antagonist for the Peroxisome Proliferator-activated Receptor y Inhibits Adipocyte Differentiation”,The Journal of Biological Chemistry, vol. 275, No. 3, pp. 1873-1877. (2000).
Toshimasa Yamauchi, et al., “Inhibition of RXR and PPARy ameliorates diet-induced obesity and type 2 diabetes”,The Journal of Clinical Investigation, vol. 108, No. 7, pp. 1001-1013, Oct. 2001.
Didier Auboeuf, et al., “Tissue Distribution and Quantification of the Expression of mRNAs of Peroxisome Prolifertor-Activated Receptors and Liver X Receptor-α in Humans, No Alteration in Adipose Tissue of Obese and NIDDM Patients”,Diabetes, vol. 46, pp. 1319-1327, Aug. 1997.
William R. Oliver, Jr., et al., “A selective peroxisome proliferator-activated recepter δ agonist promotes reverse cholesterol transport”,PNAS, vol. 98, No. 9, pp. 5306-5311, Apr. 2001.
Yong-Xu Wang, et al., “Peroxisome-Proliferator-Activated Receptor δ Activates Fat Metabolism to Prevent Obesity”,Cell, vol. 113, pp. 159-170, Apr. 18, 2003.
Helen Vosper, et al., “The Peroxisome Proliferator-activated Receptor δ Promotes Lipid Accumulation in Human Macropages”,The Journal of Biological Chemistry, vol. 276, No. 47, pp. 44258-44265. (2001).
Yaacov Barak, et al., “Effects of peroxisome proliferator-activated receptor δ on placentation, adiposity, and colorectal cancer”,PNAS, vol. 99, No. 1, pp. 303-308, Jan. 8, 2002.

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