Hoffmann-la Roche Inc.

Serge Burner

Emmanuel Pinard

Georg Jaeschke

Alexander Alanine

Marie-Paule Heitz Neidhart

Ulrich Widmer

Ren&eacute; Wyler

Bernd Buettelmann

Bernd B&uuml;ttelmann

Phenyl substituted quinolin 4-yl derivatives and pharmaceutical compositions with activity as NMDA-receptor subtype selective blockers. The compounds of the invention modulate neuronal activity and plasticity.

Quinolin-4-yl derivatives

Isoquinoline derivatives

The invention relates to compounds of the general formula

Ethanesulfonyl-piperidine derivatives

The pyridone derivatives of the formula ##STR1## wherein Ra is hydrogen or halogen, Rb is --OR.sup.1 or --NR.sup.2 R.sup.3 ; R.sup.1 is an unsubstituted lower alkyl or a lower alkyl substituted by hydroxy, lower alkoxy, amino, lower alkylamino, di(lower alkyl)amino, di(lower alkyl)carbamoyl or lower alkoxycarbonylamino; R.sup.2 is hydrogen or a lower alkyl group which is unsubstituted or substituted by hydroxy, lower alkoxy, amino, lower alkylamino, di(lower alkyl)-amino, di(lower alkyl)carbamoyl or lower alkoxycarbonyl-amino; and R.sup.3 is hydrogen or lower alkyl optionally unsubstituted or mono- or disubstituted by lower alkyl, hydroxy, lower alkoxy, lower hydroxyalkyl, lower alkoxyalkyl or phenyl; B and the carbon atom denoted by .alpha. taken together is a group of the formula &gt;C.sub..alpha. --CR.sup.4 .dbd.CH--CH.dbd.CH-- and R.sup.4 is hydrogen, fluorine or chlorine, that can be used for the control or treatment of muscle tension, stress, insomnia, anxiety and/or convulsions.

Tricyclic pyridone derivatives

The novel pyridone derivatives of the formula ##STR1## wherein Ra is hydrogen or halogen, Rb is --OR.sup.1 or --NR.sup.2 R.sup.3 ; R.sup.1 is an unsubstituted lower alkyl or a lower alkyl substituted by hydroxy, lower alkoxy, amino, lower alkylamino, di(lower alkyl)amino, di(lower alkyl)carbamoyl or lower alkoxycarbonylamino; R.sup.2 is hydrogen or a lower alkyl group which is unsubstituted or substituted by hydroxy, lower alkoxy, amino, lower alkylamino, di(lower alkyl)-amino, di(lower alkyl)carbamoyl or lower alkoxycarbonyl-amino; and R.sup.3 is hydrogen or lower alkyl or R.sup.2 and R.sup.3 taken together with the nitrogen atom to which they are attached is a 1-azetidinyl, 1-pyrrolidinyl, 1-piperidinyl, 4-morpholinyl, 4-thiomorpholinyl or 1-piperazinyl which is unsubstituted or mono- or disubstituted by lower alkyl, hydroxy, lower alkoxy, lower hydroxyalkyl, lower alkoxyalkyl or phenyl; B and the carbon atom denoted by a taken together is a group of the formula &gt;C.sub..alpha. --S--CH.dbd.CH-- or &gt;C.sub..alpha. --CR.sup.4 .dbd.CH--CH.dbd.CH-- and R.sup.4 is hydrogen, fluorine or chlorine, can be used for the control or prevention of illnesses. In particular, they have muscle relaxant, sedative-hypnotic, anxiolytic and/or anticonvulsive activity and can accordingly be used in the control or prevention of muscle tensions, stress conditions, insomnia, anxiety states and/or convulsions.

The novel pyridone derivatives of the formula ##STR1## wherein Ra is hydrogen or halogen, Rb is --NR.sup.2 R.sup.3 wherein R.sup.2 and R.sup.3 taken together with the nitrogen atom to which they are attached is a 1-azetidinyl, 1-pyrrolidinyl, 1-piperidinyl which is unsubstituted or mono- or disubstituted by lower alkyl, hydroxy, lower alkoxy, lower hydroxyalkyl, lower alkoxyalkyl or phenyl; B and the carbon atom denoted by .alpha. taken together is a group of the formula &gt;C.sub..alpha. --CR.sup.4 .dbd.CH--CH.dbd.CH-- and R.sup.4 is hydrogen, fluorine or chlorine, can be used for the control or prevention of illnesses. In particular, they have muscle relaxant, sedative-hypnotic, anxiolytic and/or anticonvulsive activity and can accordingly be used in the control or prevention of muscle tensions, stress conditions, insomnia, anxiety states and/or convulsions.

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Durmenach-Ferrette, France

Serge Burner