Pyridopyrazine and quinoxaline derivatives, processes for their preparation, and pharmaceutical compositions containing them.

摘要

There are described compounds of formula I,
<Chemistry id="chema01" num="0001"><Image id="ia01" he="20" wi="50" file="IMGA0001.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /></Chemistry>

in which R<Sub>1</Sub> is phenyl substituted by halogen, alkoxy, alkyl, carboxy-alkyl, -NR<Sub>4</Sub>R<Sub>5</Sub>, carboxy or alkoxy carbonyl,

R<Sub>3</Sub> is hydrogen, alkyl, mono- or di-carboxy alkyl, halo, alkoxy, phenyl, halo-phenyl, hydroxy, phenoxy, thiol, thioalkoxy, thiophenoxy, -NR<Sub>4</Sub>R<Sub>s</Sub>, cyano, -COOH, carboxyureido, -CF<Sub>3</Sub>, -CORe, hydroxyalkyl, aminoalkyl, or alkoxy substituted by NR<Sub>4</Sub>R<Sub>5</Sub>,

ring A is a benzene or a pyridine ring which optionally carries up to 4 substituents R<Sub>3</Sub>, which may be the same or different,

R<Sub>4</Sub> and R<Sub>s</Sub>, which may be the same or different, each represent hydrogen, phenyl, halophenyl or alkyl, the alkyl optionally being substituted by alkoxy or by a mono- or di- alkyl or unsubstituted amino group; or R<Sub>4</Sub> and R<Sub>s</Sub>, together with the nitrogen atom to which they are attached, form a piperidine, morpholine or an optionally alkyl substitued piperazine ring, and

R<Sub>6</Sub> is hydrogen or alkyl,

provided that (i) when R, is phenyl substituted by chlorine or bromine, ring A is not a benzene ring substituted by chlorine or bromine, or (ii) when R, is phenyl substituted by methoxy R<Sub>3</Sub> is not phenyl,

and pharmaceutically acceptable salts, esters and amides thereof.

There are also described methods for making the compounds and pharmaceutical, e.g. anti-inflammatory, compositions containing the compounds.