Hoffmann-la Roche Inc.

F. Hoffmann-la Roche Ag

Lucinda Steward

Sabine Kolczewski

Luca Claudio Gobbi

Olivier Roche

Juergen Wichmann

Thomas Johannes Woltering

Claus Riemer

Georg Jaeschke

Thomas Luebbers

Rosa Maria Rodriguez Sarmiento

Jens-Uwe Peters

Alexander Alanine

Alexander Flohr

Rosa Maria Rodriguez-Sarmiento

Sonia Maria Poli

Jean-Luc Moreau

Sonia Poli

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 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 relates to 2-aminoquinolines of formula I wherein R, Rand Rare as defined in the specification, as 5-HTreceptor antagonists, their manufacture, pharmaceutical compositions containing them and their use for the treatment of CNS disorders.

Quinolines

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 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 present invention relates to compounds of formula (I) wherein Rand A 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 as medicaments. Compounds of general formula (I) have high affinity for the dopamine Dand serotonin (5-Hydroxytryptamine; 5-HT) 5-HTreceptors and are effective in the treatment of psychotic disorders, as well as other diseases such as depression and anxiety, drug dependence, dementias and memory impairment.

Benzoyl-piperidine derivatives as dual modulators of the 5-HT2A and D3 receptors

The present invention is concerned with 5-substituted benzoxazine derivatives of formula (I) wherein X, Rand Rare as described herein, as well as their manufacture, pharmaceutical compositions containing them. Compounds of the present invention 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.

5-substituted benzoxazines

The present invention is concerned with 2-aminoquinoline derivatives, in particular compounds of formula (I) wherein Rand Rare as described herein, pharmaceutical compositions containing such compounds, and methods for their manufacture. The compounds of the 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 such as Parkinson's disease, psychiatric disorders or gastrointestinal disorders.

2-aminoquinoline derivatives

The present invention is concerned with 2-aminoquinoline derivatives of formula I wherein Z, R1, and Ar1 are as defined herein, pharmaceutical compositions containing them, methods for their manufacture. The 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 provides compounds of the general formula (I), having affinity and selectivity for the dopamine D3 receptors, their manufacture, pharmaceutical compositions containing them and their use for the therapeutic and/or prophylactic treatment of cognitive disorders. 

Benzo[D]isoxazol-3-yl-piperazin derivatives useful as modulators of dopamine D3 receptors

The present invention relates to 2-Aminoquinoline derivatives of general formula I and pharmaceutically-acceptable acid-addition salts thereof, wherein R, Rand X are as defined in the specification. The compounds may be used as 5-HTreceptor antagonists. The present invention relates also to processes for making such a compound and a pharmaceutical composition comprising such a compound. Compounds of the present invention are useful in the prevention and/or treatment of anxiety 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, withdrawal from abuse of drugs, motor disorders such as Parkinson's disease, psychiatric disorders and gastrointestinal disorders.

The present invention provides compounds of the general formula (I) wherein X, n and Rare as described herein, as well as pharmaceutically acceptable salts and esters thereof, methods for their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are dual modulators of the serotonin 5-HTand dopamine Dreceptors, useful in the treatment and/or the prevention of cognitive disorders, drug addiction, depression, anxiety, drug dependence, dementias, memory impairment, psychotic disorders comprising schizophrenia, schizoaffective disorders, bipolar disease, mania, psychotic depression, and psychoses comprising paranoia and delusions.

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Basel, Switzerland

Lucinda Steward