Bicyclic pyridines which are angiotensin II inhibitors
AssigneeRoussel Uclaf
InventorsAlain Corbier, Michel Fortin, Jacques Guillaume, Jean-Luc Haesslein, Jean-Paul Vevert
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Abstract
The bicyclic derivatives of pyridines of the formula ##STR1## and their non-toxic, pharmaceutically acceptable salts and a process and intermediates for their preparation which compounds are inhibitors of angiotensin II effects, particularly a vasoconstrictor activity.
Claims7
A compound selected from the group consisting of all possible racemic isomers, enantiomers and disasteroisomers of a compound of the formula ##STR43## wherein one of A and B is nitrogen and the other is carbon, the dotted lines indicate that the pyridinyl ring is optionally unsaturated, Ra is alkyl of 1 to 4 carbon atoms, R.sub.1 a, R.sub.2 a, R.sub.3 a and R.sub.4 a are individually selected from the group consisting of hydrogen, --OH, alkoxy of 1 to 6 carbon atoms, free carboxy, carboxy esterified with alkyl of 1 to 4 carbon atoms and alkyl of 1 to 6 carbon atoms optionally substituted with at least one member of the group consisting of halogen, --OH, amino, carbamoyl and alkoxy of 1 to 4 carbon atoms, R.sub.5 is alkylene of 1 to 4 carbon atoms, or CO Ya is --Y.sub.1 a --Ba--Y.sub.2 a wherein Y.sub.1 a is phenyl, Ba is a single bond or --CONH--, Y.sub.2 a is phenyl optionally substituted with at least one member of the group consisting of halogen, free, salified or esterified carboxy, --CN, tetrazoyl, pyrazolo (1-5a)pyrozole (1-5a) pyridine alkyl, pyridine imidazol (1-2a) pyridine, imidozol (1-2a)pyridine alkyl and --(CH.sub.2).sub.p --SO.sub.2 --Xa --R.sub.14 a, p is 0 or 1, Xa is selected from the group consisting of a single bond, --NH, --NHCO-- and --NHCONH--, R.sub.14 a is selected from the group consisting of methyl, ethyl, propyl, vinyl, allyl, pyridyl, phenyl, benzyl, pyridylmethyl, pyridylethyl, pyrimidyl, tetrazolyl, thiazolyl, diazolyl, piperidinyl and tetrahydrofuranyl, all optionally substituted with at least one member of the group consisting of halogen, --OH, alkyl and alkoxy of 1 to 6 carbon atoms, --CF.sub.3, --CN and --NO.sub.2.
Dependencies are inferred from the claim text.