Hoffmann-La Roche Inc.

F. Hoffmann-La Roche Ag

Walter Hunkeler

Emilio Kyburz

Heinz Stadler

Max Gerecke

Thierry Godel

Willy Haefely

Hanns Mohler

Petar Polc

Lorenzo Pieri

Patrick Schnider

Guido Galley

Torsten Hoffmann

Michael B&ouml;s

Claus Riemer

Quirico Branca

Marc Meier

Matthias Heinrich Nettekoven

Roland Jakob-Roetne

Ulrich Widmer

Fabienne Hoffmann-Emery

Andrew Sleight

Michael Bos

Gerda Huber Trottmann

Gavin John Kilpatrick

James Richard Martin

Fran&ccedil;ois Jenck

Heinz Carmann

Michael Boes

5-phenyl-pyrimidine derivatives

The present invention is a series of compounds formed from phenyl substituted pyridine or benzene derivatives and their pharmaceutically acceptable salts. These compounds have shown high affinity as antagonists to the NK-1 receptor.

Phenyl substituted pyridine and benzene derivatives

Biphenyl substituted amides with activity as antagonists of the neurokinin 1 (NK-1, substance P) receptor.

Biphenyl derivatives

Compounds of the present invention are 4-phenyl-pyridine derivatives with activity as NK-1 receptor antagonists.

4-phenyl-pyridine derivatives

Imidazodiazepine derivative

Amino-triazolopyridine derivatives

The compounds of the related invention are related to 4-phenyl-pyridine derivatives connected by a bridge containing oxygen or nitrogen to a phenyl derivative.

The invention relates to compounds of the formula

The invention provides compounds of the formula

4-phenyl-pyrimidine derivatives

3-phenyl-pyridine-derivatives

The present invention relates to novel compounds of the general formula ##STR1## wherein R.sup.1 is hydrogen;

Benzosulfone derivatives

The invention relates to compounds of the formula ##STR1## wherein A together with the two carbon atoms denoted by .alpha. and .beta. is one of the residues ##STR2## Q is one of the residues ##STR3## R.sup.1 and R.sup.2 each independently are hydrogen, lower alkyl, lower alkenyl, lower alkynyl, lower hydroxyalkyl, lower alkoxy-lower alkyl, (C.sub.3 -C.sub.6)-cycloalkyl, (C.sub.3 -C.sub.6)-cycloalkyl-lower alkyl, amino-lower alkyl, lower alkylamino-lower alkyl, di-lower alkylamino-lower alkyl or aryl-lower alkyl or together with the nitrogen atom are a 5- to 8-membered membered heterocycle optionally containing a further hetero atom or a fused benzene ring,

Imidazodiazepines

Radioiodine 5,6-dihydro-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine derivatives and their use as brain imaging agents.

Radioiodine benzodiazepines as brain imaging agents

Imidazodiazepine derivatives of the formula ##STR1## wherein A together with the two carbon atoms denoted by .alpha. and .beta. represent one of the following groups ##STR2## R.sup.1 is a partially unsaturated lower hydrocarbon group which is optionally substituted with hydroxy, oxo, aryl or the group --OR, --SR or --OCOR or a lower alkyl group which is substituted with aryl or the group --OR', --SR' or --OCOR'. R and R' each represents aryl or a saturated or partially unsaturated C.sub.1-18 -hydrocarbon group which is optionally substituted with aryl or lower alkoxy, R.sup.2 is hydrogen and R.sup.3 is lower alkyl or R.sup.2 and R.sup.3 together represent dimethylene or trimethylene and R.sup.4 and R.sup.5 each is hydrogen, halogen, trifluoromethyl, cyano, nitro or lower alkyl, the group --OR' being different from lower alkoxy and the compounds of formula I having the (S)- or (R,S)-configuration with reference to the carbon atom denoted by .gamma. when R.sup.2 and R.sup.3 together represent dimethylene or trimethylene, can be used in the control or prevention of convulsions, anxiety states, stress conditions, excitation states and sleep disorders, or in the partial or complete selective antagonism of some or all activities which 1,4-benzodiazepines having tranquillizing activity or other substances exhibit via the central benzodiazepine receptors.

Imidazodiazepine derivatives

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Magden, Switzerland

Walter Hunkeler