MEHRFACH SUBSTITUIERTE PYRIDIN-1-OXIDE, VERFAHREN ZU IHRER HERSTELLUNG, DIE SIE ENTHALTENDEN ARZNEIMITTEL UND IHRE VERWENDUNG

• Main Authors: RUDOLPHI, KARL, GREVE, WILFRIED, SCHINDLER, URSULA, ELBEN, ULRICH
• Format: Patent
• Language: German
• Published: 15.12.1989
• Edition: 4
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; METALLURGY; ORGANIC CHEMISTRY

PCT No. PCT/EP86/00211 Sec. 371 Date Dec. 16, 1986 Sec. 102(e) Date Dec. 16, 1986 PCT Filed Apr. 10, 1986 PCT Pub. No. WO86/06067 PCT Pub. Date Oct. 23, 1986.Multiply substituted pyridine 1-oxides of the formula I (I) in which R1 and R2 are, in each case, identical or different and represent alkyl having 1 to 6 carbon atoms, R3 denotes hydrogen, and R4 denotes mercaptoalkyl having up to 4 carbon atoms, or R3 and R4 form, together with the nitrogen atom in the 4-position, a five- to seven-membered saturated heterocyclic ring which has up to 2 heteroatoms, the second heteroatom being oxygen, sulfur which can carry up to two oxygen atoms, or nitrogen in the form of the NR6 group, in which R6 is hydrogen, alkyl having up to 2 carbon atoms, phenylalkyl having up to 2 carbon atoms in the alkyl moiety or phenyl, and the phenyl rings in the two latter radicals can carry up to two identical or different substituents from the group comprising halogen and methoxy, and which ring is unsubstituted or carries up to two identical or different substituents from the group comprising hydroxy and alkyl having up to 2 carbon atoms, and X denotes the cyano or nitro group the or the group -CO-R5, in which R5 represents the amino, hydroxyl or an alkoxy group having up to 4 carbon atoms, and the physiologically tolerated salts of these compounds, and medicaments containing or composed of these compounds. The invention further relates to a process for the preparation of the multiply substituted pyridine 1-oxides of the formula I, and to their use for the preparation of medicaments whcih are intended for the prevention and treatment of brain disorders caused by vascular and degenerative factors.