Hoffmann-la Roche Inc.

F. Hoffmann-la Roche Ag

Raffaello Masciadri

Hasane Ratni

Mark Rogers-Evans

Patrick Schnider

Caterina Bissantz

Christophe Grundschober

Bernd Kuhn

Roger David Norcross

Andrew William Thomas

Henrietta Dehmlow

Matthew Wright

Narendra Panday

Parichehr Malherbe

Eric Prinssen

Helmut Link

Erwin Gotschi

Hisao Shimada

Mikio Arisawa

Tsutomu Kamiyama

Junko Watanabe

Juergen Wichmann

Paul Hebeisen

Erwin Goetschi

Emmanuel Pinard

Roland Jakob-Roetne

Synese Jolidon

Henri Stalder

Werner Hofheinz

Philippe Guerry

Will Spooren

Rudolf L Then

Paulfaello Hebeisen

Pari Malherbe

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 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.

The present invention relates to compounds of the formula (I) wherein R, R, R, R, R, X, X, X, X, n, and k are defined in the description and claims, and pharmaceutically acceptable salts and/or pharmaceutically acceptable esters thereof. The compounds are useful for in the treatment and prophylaxis of diseases which are modulated by LXR&#x3b1; and/or LXR&#x3b2; agonists, including increased lipid and cholesterol levels, particularly low HDL-cholesterol, high LDL-cholesterol, atherosclerotic diseases, diabetes, particularly non-insulin dependent diabetes mellitus, metabolic syndrome, dyslipidemia, Alzheimer's disease, sepsis, inflammatory diseases such as colitis, pancreatitis, cholestasis/fibrosis of the liver, and diseases that have an inflammatory component such as Alzheimer's disease or impaired/improvable cognitive function.

Tetrahydrocarbazoles and derivatives

The invention is concerned with novel hexafluoroisopropanol derivatives of formula (I) wherein Rto R, m and n are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds bind to LXR alpha and LXR beta and can be used as medicaments.

Hexafluoroisopropanol derivatives

The present invention relates to compounds of formula I wherein R, Rand Rare as defined in the specification, which are active at the GABAreceptor and which can be used for the treatment of CNS disorders.

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Basel, Switzerland

Raffaello Masciadri