Hoffmann-la Roche Inc.

F. Hoffmann-la Roche Ag

Christophe Grundschober

Patrick Schnider

Caterina Bissantz

Hasane Ratni

Mark Rogers-Evans

Raffaello Masciadri

Konrad H Bleicher

Matthias Heinrich Nettekoven

Jean-Marc Plancher

Erwin Goetschi

Walter Vifian

Kanchan Chakraborty

Goutam Saha

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

The present compounds compounds are oxytocin receptor agonists for the treatment of autism, stress, including post traumatic stress disorder, anxiety, including anxiety disorders and depression, schizophrenia, psychiatric disorders and memory loss, alcohol withdrawal, drug addiction and for the treatment of Prader-Willi Syndrome.

Peptides as oxytocin agonists

The invention relates to compounds of formula wherein variables are defined herein. It has been found that the present compounds are oxytocin receptor agonists for the treatment of autism, stress, including post traumatic stress disorder, anxiety, including anxiety disorders and depression, schizophrenia, psychiatric disorders and memory loss, alcohol withdrawal, drug addiction and for the treatment of Prader-Willi Syndrom.

The invention relates to the use of a compound of formula I wherein

Oxytocin receptor agonists for the treatment of CNS diseases

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 is concerned with novel indol-2-yl-carbonyl-spiro-piperidine derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use for the treatment of anxiety, depressive disorders and other diseases. The compounds of present invention are represented by the general formula (I) wherein Rto R, X and Y are as defined in the specification.

Spiro-piperidine derivatives

The present invention is concerned with novel indol-3-yl-carbonyl-piperidine-benzopyrrolone, -benzoxazolone and -benzotriazole derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use for the treatment of anxiety and depressive disorders and other diseases. In particular, the present invention is concerned with compounds of formula (I) wherein X, Y and Rto Rare as described in the specification.

Indoles

The present invention is concerned with novel spiro-piperidine derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use for the treatment of anxiety and depressive disorders and other diseases. The compounds of present invention are described with formula (I) wherein Rto R, R', Rto R, R&#x2032;, R&#x2032;, X and Y are as defined in the specification.

Spiropiperidine derivatives

The present invention is concerned with novel indol-2-yl-carbonyl-piperidine derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful in the prevention and/or treatment of anxiety and depressive disorders and other diseases. Present invention is concerned with compounds of the general formula (I) wherein Rto R, Rto R, R, R, X and Y are as defined in the specification.

The present invention is concerned with novel indol-2-yl-carbonyl-piperidin-benzoimidazolon and indol-2-yl-carbonyl-piperidin-benzoxazolon derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use for the treatment of anxiety and depressive disorders and other diseases. In particular, the present invention concerns compounds of formula (I) wherein Rto R, X and Y are as defined in the specification.

The present invention is concerned with novel indol-3-yl-carbonyl-azaspiropiperidine derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use for the treatment of anxiety and depressive disorders and other diseases. In particular, the present invention is concerned with compounds of the general formula (I) wherein Rto R, U, V, W, X, Y and Z are as defined in the specification.

Azaspiro derivatives

Present invention is concerned with novel indol-2-yl-carbonyl-spiro-piperidine derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them. The active compounds of the present invention are useful in the treatment of anxiety and depressive disorders and other diseases. The compounds of present invention have the general formula (I) wherein Rto Rand X are as defined in the description.

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Rodersdorf, Switzerland

Christophe Grundschober