Hoffmann-la Roche Inc.

F. Hoffmann-la Roche Ag

Olivier Roche

Matthias Heinrich Nettekoven

Jean-Marc Plancher

Mark Rogers-Evans

Hans G Richter

Emmanuel Pinard

Henner Knust

Sven Taylor

Lucinda Steward

Rosa Maria Rodriguez-Sarmiento

Patrizio Mattei

Thomas Johannes Woltering

Juergen Wichmann

Johannes Aebi

Sabine Kolczewski

Luca Claudio Gobbi

Luke Green

Fabienne Ricklin

Alfred Binggeli

Hans Peter Maerki

Guido Hartmann

Claus Riemer

Georg Jaeschke

Thomas Luebbers

Rosa Maria Rodriguez Sarmiento

Cornelia Hertel

Susanne Raab

Silvia Gatti Mcarthur

Franz Schuler

Parichehr Malherbe

Wolfgang Haap

Wolfgang Guba

Konrad H Bleicher

Alexander Alanine

Jean-Michel Adam

Tadakatsu Takahashi

Dagmar Kube

Gisbert Schneider

Jochen Zuegge

Li Chen

Peter Mohr

Silvia Gatti McArthur

Valerie Runtz-Schmitt

Delphine Gaufreteau

Sebastien Schmitt

Sébastien Schmitt

Wayne Wen Lai

Deye Zheng

Peter Zahm

The present invention relates to compounds of the formula (I) wherein R, R, X and n are as defined in the specification as dual modulators of the serotonin 5-HTand dopamine Dreceptors, their manufacture, pharmaceutical compositions containing them and their use for the treatment of psychotic disorders, as well as other diseases such as depression and anxiety, drug dependence, dementias and memory impairment.

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The present invention is concerned with novel sulfonamides of formula I wherein R, R, Ar, Hetaryl, m and n are as described in the description and claims. The compounds are orexin receptor antagonists, useful in the treatment of disorders, in which orexin pathways are involved.

Pyrrolidin-3yl-methylamine quinoxaline derivatives

The present invention relates to piperidine sulphonamide derivatives of formula wherein Ar, Ar, R, R, m and n are as defined in the description and claims, or pharmaceutically suitable acid addition salts thereof. The compounds of formula I are orexin receptor antagonists and the related compounds can be useful in the treatment of sleep apnea, narcolepsy, insomnia, parasomnia, jet lag syndrome, circadian rhythms disorder or sleep disorders associated with neurological diseases.

Piperidine sulphonamide derivatives

The present invention relates to compounds of the general formula as dual modulators of the 5-HTand Dreceptors useful against CNS disorders, wherein A, R, R, n, p, q and r are as defined in the specification.

The present invention is concerned with 2-aminoquinoline derivatives of formula I wherein Rand Rare as described herein and pharmaceutically acceptable salts thereof, pharmaceutical compositions containing them, and methods for their manufacture. These compounds are 5-HTreceptor antagonists, useful for the prevention and/or treatment of depression, anxiety disorders, schizophrenia, panic disorders, agoraphobia, social phobia, obsessive compulsive disorders, post-traumatic stress disorders, pain, memory disorders, dementia, disorders of eating behaviors, sexual dysfunction, sleep disorders, abuse of drugs, motor disorders such as Parkinson's disease, psychiatric disorders or gastrointestinal disorders.

2-aminoquinolines

The invention is concerned with novel heteroaryl carboxamide derivatives of formula (I), wherein m, X, Y, R, R, Rand Rare as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds are antagonists of CCR-2 receptor, CCR-5 receptor and/or CCR-3 receptor and can be used as medicaments.

Heteroaryl carboxamide derivatives

Substituted benzothiazoles as orexin antagonists

The present invention relates to compounds of formula (I) wherein A, R, R, R, R, and Rare as described herein, pharmaceutical compositions containing them, and methods for their manufacture. These compounds are 5-HTreceptor antagonists and are useful in the prevention and/or treatment of depression, anxiety disorders, schizophrenia, panic disorders, agoraphobia, social phobia, obsessive compulsive disorders, post-traumatic stress disorders, pain, memory disorders, dementia, disorders of eating behaviors, sexual dysfunction, sleep disorders, abuse of drugs, motor disorders such as Parkinson's disease, psychiatric disorders or gastrointestinal disorders.

The present invention is concerned with 2-aminoquinoline derivatives of formula I where R, R, R, R, R, R, A, and n are as defined in the specification and claims, their use 5-HTreceptor antagonists, their manufacture, and pharmaceutical compositions containing them.

The present invention is concerned with 6-substituted benzoxazine derivatives of formula (I) wherein X, Y, Rand Rare as described herein, their manufacture, and pharmaceutical compositions containing them. The active compounds of the present invention are 5-HTreceptor antagonists, useful in the prevention and/or treatment of depression, anxiety disorders, schizophrenia, panic disorders, agoraphobia, social phobia, obsessive compulsive disorders, post-traumatic stress disorders, pain, memory disorders, dementia, disorders of eating behaviors, sexual dysfunction, sleep disorders, abuse of drugs, motor disorders, Parkinson's disease, psychiatric disorders or gastrointestinal disorders.

6-substituted benzoxazines

The invention is concerned with novel biaryl derivatives of formula (I), wherein m, R, R, R, X, Xand Xare as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds are antagonists of CCR-2 receptor, CCR-5 receptor and/or CCR-3 receptor and can be used as medicaments.

Biaryl derivatives

The invention is concerned with novel heterocyclyl compounds of formula (I): wherein A, X, R, R, R, R, R, R, R, R, m, n and p are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds are antagonists of CCR2 receptor, CCR5 receptor and/or CCR3 receptor and may be used as medicaments.

Heterocyclyl compounds

The present invention is concerned with novel sulfonamides of formula wherein R, R, R, R, R, Ar, Ar, Ar, n, o and p are as described in the description and claims. The compounds are orexin receptor antagonists that may be useful in the treatment of disorders, in which orexin pathways are involved.

Heteroaromatic monoamides as orexinin receptor antagonists

The invention is concerned with novel heterocyclyl compounds of formula (I) wherein A, X, Y, Y, Y, R, R, R, R, R, R, R, R, m, n and p are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds are antagonists of CCR2 receptor, CCR5 receptor and/or CCR3 receptor and can be used as medicaments.

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Folgensbourg, France

Olivier Roche