Hoffmann-la Roche Inc.

Rejuveron Telomere Therapeutics Ag

F. Hoffmann-la Roche Ag

Patrick Schnider

Christophe Grundschober

Hasane Ratni

Mark Rogers-Evans

Caterina Bissantz

Torsten Hoffmann

Raffaello Masciadri

Heinz Stadler

Cosimo Dolente

Thierry Godel

Guido Galley

Walter Hunkeler

Michael B&ouml;s

Andrew Sleight

Bernhard Fasching

Valerie Runtz-Schmitt

Sonia Maria Poli

Sabine Kolczewski

Georg Jaeschke

Eric Vieira

Jens-Uwe Peters

Erwin Goetschi

Quirico Branca

Andreas Koblet

Emmanuel Pinard

Roland Jakob-Roetne

Stephan Roever

Michelangelo Scalone

Stephan Bachmann

Richard Hugh Philip Porter

Theresa Maria Ballard

Lukas Kreis

Chien-Chi Hsiao

Fedor Romanov Michailidis

Christian Kramer

Richard H P Porter

Holger Kuehne

John G Cumming

Richard HP Porter

Michael Boes

The present invention provides spiro-oxazolones, which act as V1a receptor modulators, and in particular as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The present compounds are useful as therapeutics acting peripherally and centrally in the conditions of inappropriate secretion of vasopressin, anxiety, depressive disorders, obsessive compulsive disorder, autistic spectrum disorders, schizophrenia, aggressive behavior and phase shift sleep disorders, in particular jetlag.

Spiro-oxazolones

The present invention relates to 9-oxo-9,10-dihydro-6H-pyrano[3,2-b:4,5-b′]dipyridine-8-carboxylic acid derivatives, their manufacture, pharmaceutical compositions containing them and their use as a medicament.

9-oxo-9,10-dihydro-6H-pyrano[3,2-b:4,5-b′]dipyridine-8-carboxylic acid derivatives

This invention relates to a new medical use for certain chemical compounds and pharmaceutical compositions containing them. The invention relates to compounds which are selective V1a antagonists for use in the treatment of phase shift sleep disorders, in particular jetlag. In another aspect, the invention relates to a pharmaceutical composition for use in the treatment of phase shift sleep disorders comprising a compound according to the invention and a pharmaceutically acceptable carrier.

V1A antagonists to treat phase shift sleep disorders

Spiro-thiazolones

The present invention provides 4H,6H-5-oxa-2,3,10b-triaza-benzo[e]azulenes, which act as V1a receptor modulators, and in particular as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful as therapeutics acting peripherally and centrally in the conditions of dysmenorrhea, male or female sexual dysfunction, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, anxiety, depressive disorders, obsessive compulsive disorder, autistic spectrum disorders, schizophrenia, and aggressive behavior. 

Cyclohexyl-4H,6H-5-oxa-2,3,10b-triaza-benzo[e]azulenes as V1a antagonists

The present invention provides 4H,6H-5-oxa-2,3,10b-triaza-benzo[e]azulenes of the formula 

Oxy-cyclohexyl-4H,6H-5-oxa-2,3,10b-triaza-benzo[E]azulenes as V1A antagonists

The present invention is concerned with spiro-dihydrotetraazabenzoazulenes, i.e. spiro-5,6-dihydro-4H-2,3,5,10b-tetraaza-benzo[e]azulenes of formula I wherein R, R, R, X, Y, Z, m and n are as described herein. The compounds according to the invention act as V1a receptor modulators and are useful as therapeutics acting peripherally and centrally in the conditions of dysmenorrhea, male or female sexual dysfunction, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, anxiety, depressive disorders, obsessive compulsive disorder, autistic spectrum disorders, schizophrenia, and aggressive behavior.

Spiro-5,6-dihydro-4H-2,3,5,10b-tetraaza-benzo[e]azulenes

The present invention is concerned with alkylcyclohexylethers of dihydro-tetraazabenzoazulenes, i.e. alkylcyclohexylethers of 5,6-dihydro-4H-2,3,5,10b-tetraaza-benzo[e]azulene s of formula I wherein R, Rand Rare as described herein, their manufacture, and pharmaceutical compositions containing them. The compounds according to the invention act as V1a receptor modulators, and in particular as V1a receptor antagonists. The compounds are useful as therapeutics acting peripherally and centrally in the conditions of dysmenorrhea, male or female sexual dysfunction, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, anxiety, depressive disorders, obsessive compulsive disorder, autistic spectrum disorders, schizophrenia, and aggressive behavior.

Alkylcyclohexylethers of dihydrotetraazabenzoazulenes

The present invention relates to trans-derivatives of formula wherein R, R, R, and the dotted line are as defined herein and to pharmaceutically acceptable acid addition salts thereof. The compounds of formula I are good inhibitors of the serotonin transporter (SERT inhibitors) and simultaneously, they have good activity on the NK-1 receptor (dual effect). By virtue of their efficacy as SERT inhibitors, the compounds in the present invention are particularly useful for the treatment of CNS disorders and psychotic disorders, in particular in the treatment or prevention of depressive states and/or in the treatment of anxiety.

Serotonin transporter (SERT) inhibitors for the treatment of depression and anxiety

The present invention provides heteroaryl-cyclohexyl-tetraazabenzo[e]azulenes of formula I  The compounds according to the invention act as V1a receptor modulators, and in particular as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful as therapeutics acting peripherally and centrally in the conditions of dysmenorrhea, male or female sexual dysfunction, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, anxiety, depressive disorders, obsessive compulsive disorder, autistic spectrum disorders, schizophrenia, and aggressive behavior.

Heteroaryl-cyclohexyl-tetraazabenzo[E]azulenes

The present invention is concerned with heteroaryl-cyclohexyl-tetraazabenzo[e]azulenes of formula I  The compounds according to the invention act as V1a receptor modulators, and in particular as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful as therapeutics acting peripherally and centrally in the conditions of dysmenorrhea, male or female sexual dysfunction, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, anxiety, depressive disorders, obsessive compulsive disorder, autistic spectrum disorders, schizophrenia, and aggressive behavior.

Heteroaryl-cyclohexyl-tetraazabenzo[e]azulenes

The present invention relates to heterobiaryl-cyclohexyl-tetraazabenzo[e]azulenes of formula I wherein R, Rand Rare as described herein. The compounds according to the invention act as V1a receptor modulators, and in particular as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful as therapeutics acting peripherally and centrally in the conditions of dysmenorrhea, male or female sexual dysfunction, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, anxiety, depressive disorders, obsessive compulsive disorder, autistic spectrum disorders, schizophrenia, and aggressive behavior.

Heterobiaryl-cyclohexyl-tetraazabenzo[e]azulenes

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Bottmingen, Switzerland

Patrick Schnider