Hoffmann-La Roche Inc.

F. Hoffmann-La Roche Ag

Rosa Maria Rodriguez Sarmiento

Andrew William Thomas

Rene Wyler

Luca Claudio Gobbi

Georg Jaeschke

Lucinda Steward

Juergen Wichmann

Synese Jolidon

Olivier Roche

Andrea Cesura

Hasane Ratni

Werner Neidhart

Roland Jakob-Roetne

Anja Limberg

Guido Galley

Wolfgang Wostl

Bjoern Bartels

Matthias Heinrich Nettekoven

Bernd Kuhn

Mark Rogers-Evans

Eric Vieira

Hans G Richter

Jens-Uwe Peters

Michelangelo Scalone

Alexander Flohr

Jean-Marc Plancher

Katrin Groebke Zbinden

Konrad H Bleicher

Sven Taylor

Thomas Luebbers

Markus Rudolph

Matthias Koerner

Hans Iding

Beat Wirz

Annick Goergler

Michael Reutlinger

Karlheinz Baumann

Christian Schnider

Daniela Krummenacher

Daniela Alberati

Michael Pech

Tobias Gabriel

Felix Gruber

Björn Bartels

Stefan Berchtold

Roland Jakob-roetne

René Wyler

The present invention relates to a compound of formula I, HetAr is a five or six membered heteroaryl group, selected from wherein Ris hydrogen, halogen, lower alkyl, lower alkoxy or lower alkyl substituted by halogen, and may be the same or different, if two Roccur; Ris lower alkyl or a mono- or polydeutered derivative thereof, lower alkyl substituted by halogen or lower alkoxy, lower alkenyl unsubstituted or substituted by halogen, cycloalkyl or CH-cycloalkyl unsubstituted or substituted by halogen, heterocycloalkyl or CH-heterocycloalkyl unsubstituted or substituted by lower alkyl; Ris halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy substituted by halogen or S(O)-lower alkyl; n is 1, 2 or 3; if n is &#x3e;1, then Rmay be the same or different; or to a pharmaceutically active acid addition salt thereof, to a racemic mixture or to its corresponding enantiomer and/or an optical isomer and/or stereoisomer thereof. The compounds may be used for the treatment of Alzheimer's disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica or Down syndrome. 

Phenoxytriazoles

The present invention relates to compounds of formula  

Triazolopyridines

The present invention relates to compounds of formula  The compounds may be used for the treatment of Alzheimer's disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica or Down syndrome.

Bridged piperidine derivatives

The present invention is concerned with novel pyridazinone derivatives of formula (I) wherein R, R, Rand Rare as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit PDE10A and can be used as pharmaceuticals.

Substituted pyridazines as PDE10A inhibitors

The present invention is concerned with novel selective dual modulators of the 5-HTand Dreceptors of formula (I) wherein R, R, R, n, and Y are as described herein, as well as pharmaceutically acceptable salts and esters thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as pharmaceuticals.

Benzofurane-piperidine compounds

The present invention is concerned with novel dual modulators of the 5-HTand Dreceptors of formula (I) wherein n, x, Y, R, R, R, and Rare as described herein, as well as pharmaceutically acceptable salts and esters thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as pharmaceuticals.

Benzofurane compounds

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.

[object Object]

The present invention is concerned with novel dual modulators of the 5-HTand Dreceptors of formula (I) wherein n, Y, R, R, R, and Rare as described herein, as well as pharmaceutically acceptable salts and esters thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions containing them and their use as pharmaceutical agents.

Benzodioxole piperazine compounds

The present invention is concerned with novel dual modulators of the 5-HTand Dreceptors of formula (I) wherein n, Y, R, R, R, and Rare as described herein, as well as pharmaceutically acceptable salts and esters thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions containing them and their use as pharmaceuticals.

Benzodioxole piperidine compounds

The present invention is concerned with novel dual modulators of the 5-HTand Dreceptors of formula (I) wherein X, Y, A, R, R, and Rare as described herein, as well as pharmaceutically acceptable salts and esters thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as therapeutics.

Anellated pyridine compounds

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 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 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 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

Rosa Maria Rodriguez Sarmiento