Neurogen Corporation

Novartis Ag

Cadent Therapeutics, Inc.

Exithera Pharmaceuticals, Inc.

Exlthera Pharmaceuticals, Inc.

Yuelian Xu

Bingsong Han

Linghong Xie

Robert A Volkmann

George D Maynard

Bertrand Leo Chenard

David R Anderson

Christopher Fanger

Frank S Menniti

Yang Gao

Frans L Stassen

Neil J Hayward

Zhiyao Teng

Kenneth Shaw

John M Peterson

Ping Ge

Timothy M Caldwell

Robert Ohliger

Joseph W Ochterski

Disclosed herein, in part, are heteroaromatic compounds and methods of use in treating neuropsychiatric disorders, e.g., schizophrenia and major depressive disorder. Pharmaceutical compositions and methods of making heteroaromatic compounds are provided. The compounds are contemplated to modulate the NMDA receptor.

NMDA receptor modulators and uses thereof

The present invention provides compounds that inhibit Factor XIa or kallikrein and pharmaceutically acceptable salts thereof and compositions thereof. The present invention also provides methods of using these compounds and compositions.

Therapeutic compounds and compositions

Dipiperazinyl ketones and related analogues are provided, as are methods for their preparation and use. Such compounds may generally be used to modulate ligand binding to histamine H3 receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of disorders in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and therapeutic methods are provided, as are methods for using such ligands for detecting histamine H3 receptors (e.g., receptor localization studies).

Dipiperazinyl ketones and related analogues

The invention provides compounds of Formula (I) that bind to GABAreceptors. In the above formula, variables are defined herein. Such compounds may be used to modulate ligand binding to GABAreceptors in vivo or in vitro, and are particularly useful in the treatment of a variety of central nervous system (CNS) disorders in humans, domesticated companion animals, and livestock animals. Compounds provided herein may be administered alone or in combination with one or more other CNS agents to potentiate the effects of the other CNS agent(s). Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting GABAreceptors (e.g., receptor localization studies) 

Aryl acid pyrimidinyl methyl amides, pyridazinyl methyl amides and related compounds

Compounds of Formula I are provided, as are methods for their preparation. The variables Z, Z, Z, R, R, R, R, Rand Ar in the above formula are defined herein. Such compounds may be used to modulate ligand binding to GABAreceptors in vivo or in vitro, and are particularly useful in the treatment of a variety of central nervous system (CNS) disorders in humans, domesticated companion animals and livestock animals. Compounds provided herein may be administered alone or in combination with one or more other CNS agents to potentiate the effects of the other CNS agent(s). Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting GABAreceptors (e.g., receptor localization studies).

Imidazo-pyrimidines and triazolo-pyrimidines: benzodiazepine receptor ligands

The invention provides imidazol-1-ylmethyl pyridazine derivatives of the formula: that bind to GABAreceptors. In the above formula, R, RR, R, R, Rand Ar are defined herein. Such compounds may be used to modulate ligand binding to GABAreceptors in vivo or in vitro, and are particularly useful in the treatment of a variety of central nervous system (CNS) disorders in humans, domesticated companion animals, and livestock animals. Compounds provided herein may be administered alone or in combination with one or more other CNS agents to potentiate the effects of the other CNS agent(s). Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting GABAreceptors (e.g., receptor localization studies).

Imidazol-1-ylmethyl pyridazine derivatives

The invention provides 4-imidazol-1-ylmethyl pyrimidine of the formulathat bind to GABAreceptors. In the above formula, R, RR, R, R, Rand Ar are defined herein. Such compounds may be used to modulate ligand binding to GABAreceptors in vivo or in vitro, and are particularly useful in the treatment of a variety of central nervous system (CNS) disorders in humans, domesticated companion animals, and livestock animals. Compounds provided herein may be administered alone or in combination with one or more other CNS agents to potentiate the effects of the other CNS agent(s). Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting GABAreceptors (e.g., receptor localization studies).

4-imidazol-1-ylmethyl-pyrimidine derivatives

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East Haven, CT, United States of America

Yuelian Xu