2H-AZETO(2,1-A -ISOQUINOLINE DERIVATIVES, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM

• Main Authors: DR ALAJOS KALMAN, DR JENO KOBOR, DR LASZLO DENES, ELEMER EZER, DR GYORGY HAJOS, DR GABOR BERNATH, DR FERENC FULOP, DR EVA PALOSI, DR LASZLO SZPORNY, DR PAL SOHAR
• Format: Patent
• Language: English
• Published: 04.09.1985
• Edition: 4
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

The invention relates to new 2H-azeto[2,1-a]isoquinoline derivatives of formula (I) (I) wherein R1 and R2 represent hydroxyl or alkoxy having from 1 to 6 carbon atoms, R3 is hydroxyl, halogen or an group, wherein X is oxygen or sulfur, R4 is optionally substituted phenyl, and acid addition, metal and quaternary salts thereof. According to the invention the new compounds are prepared by cyclization of the corresponding compounds of formula (II), (II) wherein R1, R2 and R3 are as defined above, and Hal is halogen. Compounds of formula (I) are pharmaceutically active, in particular are potent analgesic and antipyretic agents.