Allergan, Inc.

Exonhit Therapeutics, Sa

Chiron Corporation

Novartis Vaccines & Diagnostics, Gmbh

Eric Beausoleil

Bertrand Leblond

John E Donello

Thierry Taverne

Rong Yang

Matthew P Pando

Anne-Sophie Casagrande

Ronald N Zuckermann

Laurent Desire

Cedric Chauvignac

Cédric Chauvignac

Deborah H Charych

Christoph Reinhard

Anne B Jefferson

Fabien (Jacques) Schweighoffer

Laurent Désiré

Matthew Wachowicz

Srinivas Kothakota

The invention relates to compounds of the formula or a pharmaceutically acceptable salt thereof, wherein R', Rthrough Rand Ar are as defined herein. These compounds are useful as inhibitors of phosphodiesterase 10 (PDE10A) which are useful in treating central nervous system diseases such as psychosis and also in treating, for example, obesity, type II diabetes, metabolic syndrome, glucose intolerance, pain and ophthalmic diseases.

Substituted 6, 7-dialkoxy-3-isoquinoline derivatives as inhibitors of phosphodiesterase 10 (PDE 10A)

The invention relates to compounds of the formula wherein R', Rthrough Rand Ar are as defined herein. These compounds are useful as inhibitors of phosphodiesterase 10 (PDE10A) which are useful in treating central nervous system diseases such as psychosis and also in treating, for example, obesity, type II diabetes, metabolic syndrome, glucose intolerance, pain and ophthalmic diseases.

Substituted 6,7-dialkoxy-3-isoquinolinol derivatives as inhibitors of phosphodiesterase 10 (PDE 10A)

The compounds shown by the structural formulas below have analgesic effect and are used in compositions and methods for treating mammal in need of such treatment. 

Methods of using as analgesics 1-benzyl-1-hydroxy-2, 3-diamino-propyl amines, 3-benzyl-3-hydroxy-2-amino-propionic acid amides and related compounds

3-aryl-3-hydroxy-2-amino-propionic acid amides, 3-heteroaryl-3-hydroxy-2-aminopropionic acid amides and related compounds having analgesic and/or immuno stimulant activity

The compounds shown by their structural formulas in the specification have analgesic and or immunostimulant activity in mammals.

Compounds having analgesic and/or immunostimulant activity

The invention relates to compounds of the formula wherein R', R, through Rand Ar are as defined herein. These compounds are useful as inhibitors of phosphodiesterase 10 (PDE10A) which are useful in treating central nervous system diseases such as psychosis and also in treating, for example, obesity, type II diabetes, metabolic syndrome, glucose intolerance, pain and ophthalmic diseases.

Substituted 6,7-dialkoxy-3-isoquinolinol derivatives as inhibitors of phosphodiesterase 10 (PDE10A)

Compounds of Formulas 1 and 2 where the variables have the meaning disclosed in the specification, have analgesic and in some cases immunostimulant activity.

3-aryl-3-hydroxy-2-amino-propionic acid amides, 3-heteroaryl-3-hydroxy-2-amino-propionic acid amides and related compounds having analgesic and/or immuno stimulant activity

Compounds according to the formula below are disclosed herein: Therapeutic methods, compositions, and medicaments related thereto are also disclosed.

3-(4-fluorophenyl)-3-hydroxy-2-amino-propionic acid amides and related compounds having analgesic activity

Compounds of the formula where the variables have the meaning defined in the specification have analgesic and/or immunostimulant effect in mammals.

3-heteroaryl-3-hydroxy-2-amino-propyl amines and related compounds having analgesic and/or immuno stimlant activity

The present invention relates to compounds and methods for inhibiting histone deacetylase enzymatic activity. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit histone deacetylases (IIDACs), and in the treatment of conditions mediated by HDAC, cancer, proliferative conditions, psoriasis, and also central nervous system diseases. It further deals with processes for preparing said compounds.

Tricyclic hydroxamate and benzamide derivatives, compositions and methods

Different-sequence peptoids, including lipid- and sterol-conjugated peptoids, are found to be effective in transfection of cells with oligonucleotides. Combinatorial libraries of such peptoids can be screened efficiently in a high-throughput format, and selected peptoids are identified post-screening.

Oligonucleotide transfection screening method

Provided are peptidomimetic protein-binding arrays, their manufacture, use, and application. The protein-binding array elements of the invention include a peptidomimetic segment linked to a solid support via a stable anchor. The invention contemplates peptidomimetic array element library synthesis, distribution, and spotting of array elements onto solid planar substrates, labeling of complex protein mixtures, and the analysis of differential protein binding to the array. The invention also enables the enrichment or purification, and subsequent sequencing or structural analysis of proteins that are identified as differential by the array screen. Kits including proteomic microarrays in accordance with the present invention are also provided.

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Paris, France

Eric Beausoleil