Organic compounds -- part of the class 532-570 series – Organic compounds – Carboxylic acids and salts thereof
C562S422000, C514S595000, C514S576000
The present invention is related to carboxylic acids of Formula (I) and use thereof for the treatment and/or prevention of obesity and/or metabolic disorders mediated by insulin resistance or hyperglycemia, comprising diabetes type I and/or II, inadequate glucose tolerance, insulin resistance, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, polycystic ovary syndrome (PCOS). In particular, the present invention is related to the use of carboxylic acids of Formula (I) to modulate, notably to inhibit the activity of PTPs.
patent: 4439617 (1984-03-01), Sestanj et al.
patent: 4927831 (1990-05-01), Malamas
patent: 6479524 (2002-11-01), Priepke et al.
patent: WO 98/16503 (1998-04-01), None
patent: WO 00/15213 (2000-03-01), None
patent: 00 35859 (2000-06-01), None
patent: 02 04459 (2002-01-01), None
patent: 03 032999 (2003-04-01), None
patent: 03 064376 (2003-08-01), None
Rexford S. Ahima, et al., “LEPTIN”, Annu. Rev. Physiol., vol. 62, 2000, pp. 413-437.
Jeffery D. Bjorge, et al., “Identification of Protein-tyrosine Phosphatase 1B as the Major Tyrosine Phosphatase Activity Capable of Dephosphorylating and Activating c-Src in Several Human Breast Cancer Cell Lines”, The Journal of Biological Chemistry, vol. 275, No. 52, Dec. 29, 2000, pp. 41439-41446.
Alan Cheng, et al., “Attenuation of Leptin Action and Regulation of Obesity by Protein Tyrosine Phosphatase 1B” Developmental Cell, vol. 2, Apr. 2002, pp. 497-503.
Ralph A. Defronzo, et al., “Insulin Resistance A Multifaceted Syndrome Responsible for NIDDM, Obesity, Hypertension, Dyslipidemia, and Atherosclerotic Cardiovascular Disease”, Diabetes Care, vol. 14, No. 3, Mar. 1991, pp. 173-194.
Evanthia Diamanti-Kandarakis, et al., “Therapeutic effects of metformin on insulin resistance and hyperandrogenism in polycystic ovary syndrome”, European Journal of Endocrinology, vol. 138, 1998, pp. 269-274.
Siegfried E. Drewes, et al., “Reaction of Diazomethane with Quaternary Nitrogen Compounds to form Betaines”, J. Chem. Soc. Perkin Trans 1, 1975, pp. 1283-1284.
Andrea Dunaif, “Insulin Resistance and the Polycystic Ovary Syndrome: Mechanism and Implications for Pathogenesis”, Endocrine Reviews, vol. 18, No. 6, 1997, pp. 774-800.
Mounib Elchebly, et al., “Modulation of insulin signaling by protein tyrosine phosphatases”, J Mol Med, vol. 78, 2000, pp. 473-482.
Adrian Folkes, et al., “Synthesis and in Vitro Evaluation of a Series of Diketopiperazine Inhibitors of Plasminogen Activator Inhibitor-1”, Bioorganic & Medicinal Chemistry Letters, vol. 11, 2001, pp. 2589-2592.
R. J. Jarrett, “Cardiovascular Disease and Hypertension in Diabetes Mellitus”, Diabetes/Metabolism Reviews, vol. 5, No. 7, 1989, pp. 547-558.
Brian P. Kennedy, et al., “Protein Tyrosine Phosphatase-1B in Diabetes”, Biochemical Pharmacology, vol. 60, 2000, pp. 877-883.
Lori D. Klaman, et al., “Increased Energy Expenditure, Decreased Adiposity, and Tissue-Specific Insulin Sensitivity in Protein-Tyrosine Phosphatase 1B-Deficient Mice”, Molecular and Cellular Biology, vol. 20, No. 15, pp. 5479-5489, year: 2000.
Jonathan H. Marriott, et al., “Synthesis of the farnesyl ether 2,3,5-trifluoro-6-hydroxy-4-[(E,E)-3,7,11-trimethyldodeca-2,6,10-trien-1-yloxy]nitrobenzene, and related compounds containing a substituted hydroxytrifluorophenyl residue: novel inhibitors of protein farnesyltransferase, geranylgeranyltransferase I and squalene synthase”, J. Chem. Soc., Perkin Trans. 1, 2000, pp. 4265-4278.
N. Soundararajan, et al., “Descriptive Photochemistry of Polyfluorinated Azide Derivatives of Methyl Benzoate”, J. Org. Chem, vol. 55, 1990, pp. 2034-2044.
Mary C. McGuire, et al., “Abnormal Regulation of Protein Tyrosine Phosphatase Activities in Skeletal Muscle of Insulin-Resistant Humans”, Diabetes, vol. 40, Jul. 1991, pp. 939-942.
Joseph Meyerovitch, et al., “Hepatic Phosphotyrosine Phosphatase Activity and Its Alterations in Diabetic Rats”, J. Clin. Invest, vol. 84, Sep. 1989, pp. 976-983.
Niels Peter Hundahl Møller, et al., “Protein tyrosine phosphatases (PTPs) as drug targets: Inhibitors of PTP-1B for the treatment of diabetes”, Current Opinion in Drug Discovery & Development, vol. 3, No. 5, 2000, pp. 527-540.
Purnima Pathre, et al., “PTP1B Regulates Neurite Extension Mediated by Cell-Cell and Cell-Matrix Adhesion Molecules”, Journal of Neuroscience Research, vol. 63, 2001, pp. 143-150.
Gerald M. Reaven, et al., “Nonketotic Diabetes Mellitus: Insulin Deficiency or Insulin Resistance?”, The American Journal of Medicine, vol. 60, Jan. 1976, pp. 80-88.
Lisa P. Shock, et al., “Protein tyrosine phosphatases expressed in developing brain and retinal Müller glia”, Molecular Brain Research, vol. 28, 1995, pp. 110-116.
Janet Sredy, et al., “Insulin Resistance Is Associated With Abnormal Dephosphorylation of a Synthetic Phosphopeptide Corresponding to the Major Autophosphorylation Sites of the Insulin Receptor”, Metabolism, vol. 44, No. 8, Aug. 1995, pp. 1074-1081.
Robert W. Stout, “Overview of the Association Between Insulin and Atherosclerosis”, Metabolism, vol. 34, No. 12, Dec. 1985, pp. 7-12.
Zhong-Yin Zhang, “Protein tyrosine phosphatases: prospects for therapeutics”, Current Opinion in Chemical Biology, vol. 5, 2001, pp. 416-423.
Merck Serono SA
Oblon, Spivak McClelland, Maier & Neustadt, L.L.P.
Sullivan Daniel M
1,1′-(1,2-ethynediyl)bis-benzene derivatives as PTP... does not yet have a rating. At this time, there are no reviews or comments for this patent.If you have personal experience with 1,1′-(1,2-ethynediyl)bis-benzene derivatives as PTP..., we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and 1,1′-(1,2-ethynediyl)bis-benzene derivatives as PTP... will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-2679960