Akzo Nobel N.v.

N.v. Organon

Neurosearch A/s

Niall Morton Hamilton

Koc-Kan Ho

Lene Teuber

David Jonathan Bennett

Simon James Anthony Grove

Naheed Mirza

Steven G Kultgen

John Richard Morphy

Andrew Cooke

Susan Elizabeth Napier

Frank Wätjen

Celia Kingsbury

Brad Sherborne

Michael John Kiczun

Morag Ann MacCall Easson

Peter Thomas Albert Littlewood

Angus Richard Brown

Michael Ohhlmeyer

The invention provides for compounds having the structure according to the formula I wherein: X is a carbon or nitrogen atom; Ar is phenyl or heteroaromatic ring; Ris hydrogen, halogen, CN or (1C-4C)alkyl; Ris hydrogen, halogen or optionally fluorinated (1C-3C)alkoxy; Rand Rare independently hydrogen, optionally halogenated (1C-4C)alkyl, optionally halogenated (1C-4C)alkoxy, optionally halogenated aryl(1C-4C)alkoxy, optionally halogenated (1C-4C)alkenyl or hydroxylmethyl; Ris hydrogen, halogen, optionally halogenated (1C-4C)alkoxy or optionally halogenated aryl(1C-4C)alkoxy; Ris hydrogen, benzyl, optionally substituted with one or more halogens or (1C-4C)alkyl, or Ris optionally halogenated (1C-4C)alkyl; each Rindependently is hydrogen, halogen, optionally halogenated (1C-4C)alkyl or optionally halogenated (1C-4C)alkoxy and pharmaceutically suitable acid addition salts thereof for use as glucocorticoid receptor modulators, in particular for treatment of central nervous system disorders.

Compounds with medicinal effects due to interaction with the glucocorticoid receptor

This invention relates to novel 1,5,7-trisubstituted benzimidazole derivatives, pharmaceutical compositions containing these compounds, and methods of treatment therewith. The compounds of the invention are useful in the treatment of central nervous system diseases and disorders, which are responsive to modulation of the GABAreceptor complex.

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The present invention relates to alanine 2,6-dialkoxyphenyl ester derivatives having the general formula I  The invention also relates to pharmaceutical compositions comprising said derivatives, and to the use of these alanine 2,6-dialkoxyphenyl ester derivatives as hypnotics for the induction and maintenance of general anaesthesia.

Alanine 2,6-dialkoxyphenyl ester derivatives as hypnotics

The present invention relates to &agr;-amino acid phenyl ester derivatives having general formula (I) wherein R is (C )alkyloxy; R is (C )alkyl, (C )alkyloxy or (C )alkenyl; R is hydrogen, (C )alkyl, (C )alkyloxy or (C )alkenyl; R is (C )alkyl; R and R are independently (C )alkyl, (C )alkenyl, (C )alkynyl or aralkyl, each of which may be optionally substituted with (C )alkyloxy, (C )alkyloxycarbonyl, cyano or NR R ; R and R are independently (C )alkyl; or a pharmaceutically acceptable salt thereof. The invention also relates to pharmaceutical compositions comprising said derivatives, and to the use of these &agr;-amino acid phenyl ester derivatives as hypnotics for the induction and maintenance of general anaesthesia.

&agr;-amino acid phenyl ester derivatives

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Newhouse, United Kingdom

Niall Morton Hamilton