Hoffmann-la Roche Inc.

Lonza Inc.

F. Hoffmann-la Roche Ag

Synese Jolidon

Emmanuel Pinard

Robert Narquizian

Roger David Norcross

Andrew William Thomas

Eric Vieira

Georg Jaeschke

Heinz Stadler

Lothar Lindemann

Rene Wyler

Luke Green

Wolfgang Guba

Antonio Ricci

Daniel Rueher

Wolfgang Wostl

Philippe Guerry

Thomas Luebbers

Rosa Maria Rodriguez-Sarmiento

Matthias Heinrich Nettekoven

Rosa Maria Rodriguez Sarmiento

Erwin Goetschi

Henri Stalder

Karlheinz Baumann

Johannes Aebi

Alexander Flohr

Olivier Morand

Pierre-Charles Wyss

Hans Iding

Beat Wirz

Ivan Kompis

Ekkehard Weiss

Rene Zurfluh

Daniela Krummenacher

Rita Locher

Helmut Jacobsen

Daniela Alberati-Giani

Philipe Guerry

Anja Limberg

Leander Tenud

Juergen Wichmann

Henner Knust

Christian N Hubschwerlen

Michael J Klaus

Henrietta Dehmlow

Simona Maria Ceccarelli

Raffaello Masciadri

Vincent Mutel

Jean-Marc Lapierre

Thomas Meul

Jean-Luc Specklin

Gerard Schmid

Jacques Himber

Hans Lengsfeld

Paula Nanette Belloni

Rudolf L Then

Henri Stadler

Ku-Hua Ji

The present invention relates to ethynyl compounds of formula I-C1 whereinR, R, R, R, R, R, U, V and W are as defined herein and to a pharmaceutically acceptable acid addition salts, to a racemic mixtures, or to its corresponding enantiomers and/or optical isomers and/or stereoisomers thereof, which are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5).

Arlethynyl derivatives

The present invention relates to ethynyl derivatives of formula I X, G, R, R, R, R, R, R, R, R, R, m, and n are as defined herein or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. Compounds of formula I are positive allosteric modulators (PAM) of the metabotropic glutamate receptor subtype 5 (mGluR5). They can be used for the treatment of schizophrenia or cognitive disorders.

Ethynyl compounds

The invention relates to compounds of formula wherein the substituents are as described in claim. Compounds of formula I are modulators for amyloid beta and thus, they may be useful for the treatment or prevention of a disease associated with the deposition of &#x3b2;-amyloid in the brain, in particular Alzheimer's disease, and other diseases such as cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome.

Modulators of amyloid beta

The present invention relates to ethynyl compounds of formula wherein X, Y, Z, and Rare as defined hereinor to a pharmaceutically acceptable salt or acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. Compounds of formula I are positive allosteric modulators (PAM) of the metabotropic glutamate receptor subtype 5 (mGluR5) and they are therefore useful for the treatment of diseases related to this receptor.

Ethynyl compounds useful for treatment of CNS disorder

The present invention relates to ethynyl derivatives of formula I wherein

Phenyl or pyridinyl-ethynyl derivatives

The present invention relates to phenylethynyl compounds of formula I wherein

Positive allosteric modulators (PAM)

The present invention relates to ethynyl derivatives of formula I wherein G, X, R, R, R, R, R, and Rare as defined hereinor to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. Compounds of formula I are positive allosteric modulators (PAM) of the metabotropic glutamate receptor subtype 5 (mGluR5).

Ethynyl nitrogen containing heteroaryl pyrazolidin-3-one derivatives

The present invention relates to ethynyl compounds of formula I whereinR1, R2, R2', R3, R3&#x2032;, R4, R4&#x2032;, U, V, W, Y, m, and n are as defined herein and to a pharmaceutically acceptable acid addition salts, to a racemic mixtures, or to its corresponding enantiomers and/or optical isomers and/or stereoisomers thereof. Compounds of formula I are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5).

Arylethynyl derivatives

Ethynyl compounds useful for treatment of CNS disorders

The invention relates to compounds of formula where hetaryl I, hetaryl II,

Heteroaryl substituted piperidines

The present invention relates to ethynyl compounds of formula I wherein

The invention relates to compounds of formula wherein R, R, R3, R4, and Ar are as defined in the specification and claims, or to pharmaceutically active acid addition salts of such compounds. Compounds of formula I are modulators for amyloid beta and may be useful for the treatment or prevention of a disease associated with the deposition of &#x3b2;-amyloid in the brain, in particular Alzheimer's disease, and other diseases such as cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome.

Modulators for amyloid beta

The present invention relates to phenylethynyl compounds of formula I whereinR, R, X, L, R, R, R, cyc, and n are as defined in the specification and claims and to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. Compounds of formula I are positive allosteric modulators (PAM) of the metabotropic glutamate receptor subtype 5 (mGluR5). They are useful for the treatment of schizophrenia or cognitive diseases.

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Blauen, Switzerland

Synese Jolidon