Dart Neuroscience, (cayman) Ltd.

Ortho-mcneil Pharmaceutical Corp.

Incyte San Diego Inc.

Dart Neuroscience, LLC

James Zapf

Alan P Kaplan

Venkataiah Bollu

Mark E Wilson

James Breitenbucher

Robert Huerta Lemus

Troy Vickers

Andrew Lindstrom

Catherine Tachdjian

Magnus Pfahl

Hussien A Al-Shamma

Jianhua Guo

Karine Jakubowicz-Jaillardon

Andrea Fanjul Giachino

Lyle W Spruce

Richard Masten Fine

Michael I Weinhouse

Mohamed Boudjelal

The invention provides a chemical entity of Formula (I), and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies, detection and imaging techniques, and radioactive treatments; and therapies, including inhibiting PDE4, enhancing neuronal plasticity, treating neurological disorders, providing neuroprotection, treating a cognitive impairment associated with a CNS disorder, enhancing the efficiency of cognitive and motor training, providing neurorecovery and neurorehabilitation, enhancing the efficiency of non-human animal training protocols, and treating peripheral disorders, including inflammatory and renal disorders.

Substituted pyridine and pyrazine compounds as PDE4 inhibitors

The invention provides a chemical entity of Formula (I) whereinR, R, R, R, Y and Z have any of the values described herein, and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies, detection and imaging techniques, and radioactive treatments; and therapies, including inhibiting PDE4, enhancing neuronal plasticity, treating neurological disorders, providing neuroprotection, treating a cognitive impairment associated with a CNS disorder, enhancing the efficiency of cognitive and motor training, providing neurorecovery and neurorehabilitation, enhancing the efficiency of non-human animal training protocols, and treating peripheral disorders, including inflammatory and renal disorders.

The invention provides a chemical entity of Formula (I) wherein R, R, R, R, Y and Z have any of the values described herein, and compositions comprising such chemical entities; methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies, detection and imaging techniques, and radioactive treatments; and therapies, including inhibiting PDE4, enhancing neuronal plasticity, treating neurological disorders, providing neuroprotection, treating a cognitive impairment associated with a CNS disorder, enhancing the efficiency of cognitive and motor training, providing neurorecovery and neurorehabilitation, enhancing the efficiency of non-human animal training protocols, and treating peripheral disorders, including inflammatory and renal disorders.

The invention relates to certain bicyclic heterocycles havng the structure shown below which are useful in the treatment of diseases related to lipid and carbohydrate metabolism, such as type 2 diabetes, and atherosclerosis. 

Bicyclic heterocycles for the treatment of diabetes and other diseases

The present invention relates to certain substituted heterocycles of Formula (200), wherein B, H, I, J and K together with the Arform a ring containing at least one amide residue, and W, X, Y and Z together form a 2,4-thiazolidinedione, 2-thioxo-thiazolidine-4-one, 2,4-imidazolidinedione or 2-thioxo-imidazolidine-4-one residue; or a pharmaceutically acceptable salt thereof. The compounds are useful in the treatment of diseases such as type 2 diabetes, and related disorders of lipid and carbohydrate metabolism, including atherosclerosis. The compounds are also useful for treating diseases of uncontrolled proliferation, such as cancers in general, including breast cancer.

Heterocyclic amide derivatives for the treatment of diabetes and other diseases

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San Diego, CA, United States of America

James Zapf