Hoffmann-la Roche Inc.

F. Hoffmann-la Roche Ag

Lothar Lindemann

Georg Jaeschke

Eric Vieira

Heinz Stadler

Antonio Ricci

Daniel Rueher

Synese Jolidon

Wolfgang Guba

Luke Green

Fionn O'Hara

Barbara Biemans

Rainer Eugen Martin

Juergen Wichmann

Henner Knust

Luca Claudio Gobbi

Jean-Marc Plancher

Fionn O`hara

The present invention relates to ethynyl derivatives of formula I with variables as defined herein, or to a pharmaceutically acceptable acid addition salt thereof Compounds of formula I are metabotropic glutamate receptor antagonists (negative allosteric modulators) for use in the treatment of, e.g., anxiety and pain, depression, Fragile-X syndrome, autism spectrum disorders, Parkinson's disease, and gastroesophageal reflux disease (GERD).

Ethynyl derivatives

The present invention provides new arylsulfonamide compounds having the general formula (I) wherein L, R, R, Rand Rare as described herein, compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds.

Arylsulfonamide derivatives

The present invention relates to positive allosteric modulators (PAMs) of metabotropic glutamate receptor 4 (mGluR4) that may be used for the treatment of conditions such as Parkinson's disease, anxiety, emesis, obsessive compulsive disorder, autism, neuroprotection, cancer, depression and diabetes type 2.

The present invention relates to ethynyl derivatives of formula I with variables as defined herein, or to a pharmaceutically acceptable acid addition salt thereof. Compounds of formula I are metabotropic glutamate receptor antagonists (negative allosteric modulators) for use in the treatment of, e.g., anxiety and pain, depression, Fragile-X syndrome, autism spectrum disorders, Parkinson's disease, and gastroesophageal reflux disease (GERD).

The present invention relates to ethynyl derivatives as metabotropic glutamate receptor antagonists (negative allosteric modulators) for use in the treatment of, e.g., anxiety and pain, depression, Fragile-X syndrome, autism spectrum disorders, Parkinson's disease, and gastroesophageal reflux disease (GERD).

The present invention relates to ethynyl derivatives of formula I wherein It has now surprisingly been found that the compounds of general formula I are metabotropic glutamate receptor antagonists (negative allosteric modulators) for use in the treatment of anxiety and pain, depression, Fragile-X syndrom, autism spectrum disorders, Parkinson's disease, and gastroesophageal reflux disease (GERD).

The present invention relates to ethynyl derivatives of formula I wherein It has been found that the compounds of general formula I are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5).

Arylethynyl derivatives

The present invention relates to ethynyl derivatives of formula I wherein

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  It has now surprisingly been found that the compounds of general formula I are metabotropic glutamate receptor antagonists (negative allosteric modulators) for use in the treatment of anxiety and pain, depression, Fragile-X syndrome, autism spectrum disorders, Parkinson's disease, and gastroesophageal reflux disease (GERD).

The present invention relates to ethynyl derivatives of formula I wherein It has now surprisingly been found that the compounds of general formula I are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5) which show advantageous biochemical-, physicochemical- and pharmacodynamic-properties compared to compounds of prior art.

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.

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Basel, Switzerland

Lothar Lindemann