Recent Advances in the Discovery of Competitive Protein Tyrosine Phosphatase 1B Inhibitors for the Treatment of Diabetes, Obesity, and Cancer

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Van Zandt, M. C.Preparation of Pyridinyl Biphenyl Derivatives Useful in the Treatment of Metabolic Disorders Related to Insulin Resistance, Leptin Resistance, or Hyperglycemia. PCT Int. Appl. WO 2008033455, 2008; 221 pp (The Institutes for Pharmaceutical Discovery, LLC).

Van Zandt, M. C.Preparation of Arylthiazolylalkylsulfanylalkanoic Acids and Analogs Thereof for the Treatment of Syndrome X, Obesity, and Diabetes. PCT Int. Appl. WO 2008033932, 2008; 73 pp (The Institutes for Pharmaceutical Discovery, LLC).

Van Zandt, M. C.Heteroaryl Carboxylic Acid Derivatives as PTB-1B Inhibitors and Their Preparation, Pharmaceutical Compositions and Use in the Treatment of Metabolic Disorders. PCT Int. Appl. WO 2008033934, 2008; 108 pp (The Institutes for Pharmaceutical Discovery, LLC).

Van Zandt, M. C.Preparation of para-Xylylenecarboxylic Acids and Isothiazolones as Inhibitors of Protein Tyrosine Phosphatases (PTP) in Particular PTP-1B. PCT Int. Appl. WO 2008033931, 2008; 90 pp (The Institutes for Pharmaceutical Discovery, LLC).

Van Zandt, M. C.; Fang, H.; Hu, S.; Whitehouse, D.Preparation of Phenyl Substituted Carboxylic Acids as Inhibitors of Protein Tyrosine Phosphatase-1B (PTP-1B). PCT Int. Appl. WO 2006055625, 2006; 179 pp (The Institutes for Pharmaceutical Discovery, LLC).

Van Zandt, M. C.; Whitehouse, D.; Combs, K.; Hu, S.Preparation of Substituted Carboxylic Acids, Including Amino Acid Derivatives, as Inhibitors of Protein Tyrosine Phosphatases for Treatment of Diabetes, Cancer, and Related Conditions. PCT Int. Appl. WO 2004099168, 2004; 96 pp (The Institutes for Pharmaceutical Discovery, LLC).

Whitehouse, D.; Hu, S.; Fang, H.; Van Zandt, M.Preparation of Phenyl Substituted Carboxylates, Including Amino Acid Derivatives, as Inhibitors of Protein Tyrosine Phosphatases for Treatment of Diabetes, Cancer, and Related Conditions. PCT Int. Appl. WO 2004099170, 2004; 121 pp (The Institutes for Pharmaceutical Discovery, LLC).

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Coppola, G. M.; Davies, J. W.; Jewell, C. F., Jr.; Li, Y.C.; Wareing, J. R.; Sperbeck, D. M.; Stams, T. M.; Topiol, S. W.; Vlattas, I.Preparation of Substituted 1,1-Dioxo-1,2,5-thiazolidine-3-ones as Protein Tyrosine Phosphatase 1b and T-Cell Protein Tyrosine Phosphatase Inhibitors to Mitigate Insulin Resistance in the Treatment of Diabetes or Atherosclerosis. PCT Int. Appl. WO 2003082841, 2003; 148 pp (Novartis A.G., Switzerland; Novartis Pharma G.m.b.H.).

Kenny, P. W.; Morley, A. D.; Russell, D. J.; Toader, D.Preparation of 1,2,5-Thiadiazolidin-3-one 1,1-Dioxide Derivatives as Inhibitors of Protein Tyrosine Phosphatase 1B. PCT Int. Appl. WO 2004050646, 2004; 48 pp (Astrazeneca AB, Sweden; Astrazeneca U.K. Ltd.).

Birch, A. M.; Kenny, P. W.; Morley, A. D.; Russell, D. J.; Toader, D.Preparation of 5-(Substituted phenyl)thiadiazolidin-3-ones as Inhibitors of Protein Tyrosine Phosphatase 1B. PCT Int. Appl. WO 2004041799, 2004; 89 pp (Astrazeneca AB, Sweden; Astrazeneca U.K. Ltd.).

Saunders, J. O.; Miknis, G. F.; Blake, J. F.Preparation of Sulfahydantoins as Phosphate Isosteres for Use as Phosphatase Inhibitors in the Treatment of Cancer and Autoimmune Disorders. PCT Int. Appl. WO 2004062664, 2004; 62 pp (Vertex Pharmaceuticals Inc.).

Combs, A. P.; Yue, E. W. T.; Bower, M. J.; Zhu, W.; Crawley, M. L.; Sparks, R. B.; Pruitt, J. R.; Takvorian, A.Inhibitors of Proteins That Bind Phosphorylated Molecules. PCT Int. Appl. WO 2005035551, 2005; 529 pp (Incyte Corp.).

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Sparks R. B., 2007, Bioorg. Med. Chem. Lett., 17, 736, 10.1016/j.bmcl.2006.10.079

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Barnes, D.; Bebernitz, G. R.; Coppola, G. M.; Nakajima, K.; Stams, T.; Topiol, S. W.; Vedananda, T. R.; Wareing, J. R.Thiadiazolidinone Compounds as Protein Tyrosine Phosphatase Inhibitors and Their Preparation, Pharmaceutical Compositions and Use in the Treatment of Diseases. PCT Int. Appl. WO 2007067615, 2007; 136 pp (Novartis A.G., Switzerland; Novartis Pharma G.m.b.H.).

Barnes, D.; Bebernitz, G. R.; Coppola, G. M.; Stams, T.; Topiol, S. W.; Vedananda, T. R.; Wareing, J. R.1,2,5-Thiadiazolidine Derivatives Useful for Treating Conditions Mediated by Protein Tyrosine Phosphatases (PTPASE) and Their Preparation and Pharmaceutical Compositions. PCT Int. Appl. WO 2007067613, 2007; 108 pp (Novartis A.G., Switzerland; Novartis Pharma G.m.b.H.).

Barnes, D.; Coppola, G. M.; Damon, R. E.; Nakajima, K.; Raudenbush, B. C.; Stams, T.; Topiol, S. W.; Vedananda, T. R.1,1,3-Trioxo-1,2,5-thiadiazolidines as PTPases Inhibitors and Their Preparation, Pharmaceutical Compositions and Use in the Treatment of Disease. PCT Int. Appl. WO 2007067614, 2007; 94 pp (Novartis A.G., Switzerland; Novartis Pharma G.m.b.H.).

Barnes, D.; Coppola, G. M.; Stams, T.; Topiol, S. W.1-Orthofluorophenyl-Substituted 1,2,5-Thiadiazolidinone Derivatives as PTPase Inhibitors and Their Preparation, Pharmaceutical Compositions and Use in the Treatment of Diseases. PCT Int. Appl. WO 2007067612, 2007; 129 pp (Novartis A.G., Switzerland; Novartis Pharma G.m.b.H.).

Neubert, A.; Barnes, D.; Kwak, Y.S.; Nakajima, K.; Bebernitz, G. R.; Coppola, G. M.; Kirman, L.; Serrano-Wu, M. H.; Stams, T.; Topiol, S. W.; Vedananda, T. R.; Wareing, J. R.Organic Arylthiadiazolidinetrione Compounds as Protein Tyrosine Phosphatase Inhibitors and Their Preparation, Pharmaceutical Compositions and Use in the Treatment of Diseases. PCT Int. Appl. WO 2007115058, 2007; 331 pp (Novartis A.G., Switzerland; Novartis Pharma G.m.b.H.).

Barnes, D.; Coppola, G. M.; Stams, T.; Topiol, S. W.; Wareing, J. R.Preparation of Thiadiazole Derivatives as Antidiabetic Agents. PCT Int. Appl. WO 2008148744, 2008; 36 pp (Novartis A.G., Switzerland; Novartis Pharma G.m.b.H.).

Paul, A. C.; Halse, R.; Duttaroy, A.; Holton, L. E.; Kemp, D.; Glass, D. J.; Barnes, D. W.PTP Inhibitors for Treatment of Muscle Atrophy and Related Disorders. PCT Int. Appl. WO 2008067527, 2008; 154 pp (Novartis A.G., Switzerland; Novartis Pharma G.m.b.H.).

Mjalli, A. M. M.; Andrews, R. C.; Yarragunta, R. R.; Xie, R.; Subramanian, G.; Quada, J. C., Jr.; Arimilli, M. N.; Polisetti, D. R.Preparation of Substituted Imidazoles as Protein Tyrosine Phosphatase Inhibitors for Treatment of Diabetes and Other PTPase Mediated Conditions. PCT Int. Appl. WO 2004071448, 2004; 281 pp (Transtech Pharma, Inc.).

Mjalli, A. M. M.; Polisetti, D. R.; Quada, J. C.; Yarragunta, R. R.; Andrews, R. C.; Xie, R.; Subramanian, G.Preparation of 1,2,5-Thiadiazolidin-3-one 1,1-Dioxides and Related Compounds Containing Imidazole Moiety as PTPase (Protein Tyrosine Phosphatase) Inhibitors. PCT Int. Appl. WO 2007089857, 2007; 192 pp (Transtech Pharma, Inc.).

Mjalli, A. M. M.; Shahbaz, K. G. J.Preparation of Bis-Heteroaryl Alkanes as Protein Tyrosine Phosphatase 1B Inhibitors. PCT Int. Appl. WO 2003032982, 2003; 58 pp (Transtech Pharma, Inc.).

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Gray, J. L.Preparation of Thiazoles as Human Protein Tyrosine Phosphatase Inhibitors for Use in Treating Conditions That Benefit from Angiogenesis Regulation. PCT Int. Appl. WO 2008002570, 2008; 166 pp (The Procter & Gamble Company).

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