Astrazeneca Ab

Udo Bauer

Wayne Brailsford

Linda Gustafsson

Tor Svensson

Jan Mattsson

Thomas Olsson

Karolina Nilsson

Ola Fjellström

Maria Saxin

Vijay Chhajlani

Bryan Egner

The present invention relates to novel imidazole derivatives having a positive allosteric GABAreceptor (GBR) modulator effect, methods for the preparation of said compounds and to their use, optionally in combination with a GABAagonist, for the inhibition of transient lower esophageal sphincter relaxations, for the treatment of gastroesophageal reflux disease, as well as for the treatment of functional gastrointestinal disorders and irritable bowel syndrome (IBS). The compounds are represented by the general formula (I) wherein R, R, Rand Rare as defined in the description. For example, Rmay be phenyl, Rmay be dimethylamino pyrrolidin-1-yl, Rmay be alkoxy and Rmay be alkyl, ai arylalkyl, aryloxyalkyl, aryloxy or heterocyclylalkyl.

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The present invention relates to novel imidazole derivatives having a positive allosteric GABAB receptor (GBR) modulator effect, methods for the preparation of said compounds and to their use, optionally in combination with a GABAB agonist, for the inhibition of transient lower esophageal sphincter relaxations, for the treatment of gastroesophageal reflux disease, as well as for the treatment of functional gastrointestinal disorders and irritable bowel syndrome (IBS). The compounds are represented by the general formula (I) wherein R, R, Rand Y are as defined in the description. For example, Rmay be phenyl, Rmay be dimethylamino, Rmay be alkoxy and Y may be a thioylamino- or methyl eneamino- linked substitutuent containing an aryl group. 

Imidazole derivatives for the treatment of gastrointestinal disorders

The present invention relates to novel compounds having a positive allosteric G&#xc0;BAB receptor (GDR) modulator effect, methods for the preparation of said compounds and to their use, optionally in combination with a GABAB agonist, for the inhibition of transient lower esophageal sphincter relaxations, for the treatment of gastroesophageal reflux disease, as well as for the treatment of functional gastrointestinal disorders and irritable bowel syndrome (IBS). A compound of the general formula I. 

Imidazole variants as modulators of GABA receptor for the treatment of GI disorders

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Mölndal, Sweden

Udo Bauer