Acyl substituted aminopyrans with a modulating effect on calcium channels

• Main Authors: JUNGE, BODO, DE VRY, JEAN-MARIE-VIKTOR, URBAHNS, KLAUS, HEINE, HANS-GEORG, WITTKA, REILINDE, MAULER, FRANK
• Format: Patent
• Language: English; French; German
• Published: 19.02.1997
• Edition: 6
• 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

Die Erfindung betrifft die Verwendung von Acyl-substituierten Aminopyranen der Formel (I) zur Herstellung von Arzneimitteln, insbesondere von Arzneimitteln zur Behandlung von Erkrankungen des zentralen Nervensystems. A, R -R haben die in der Beschreibung gegebene Bedeutungen. Treatment of CNS conditions using acyl-substd. amino-pyrans of formula (I) and their salts is new. A = 6-10C aryl or pyridyl, opt. up to three times substd. by NO2, CN, Ph, halo, CF3, 1-6C alkylthio or 1-6C alkoxy; R1 = 1-8C alkyl; R2 = 1-6C alkyl; R3,R4 = H, 1-6C alkyl or 1-6C acyl; R5 = 1-8C alkyl or 1-8C alkoxy. Four cpds. falling within the above definitions are new i.e.: 5-acetyl-2-amino-6-methyl-4-(2,3-dichlorophenyl)-4H-pyran-3- carboxylic acid methyl ester (Ia), 5-acetyl-2-amino-6-methyl-4-(3,4-dichlorophenyl)-4H-pyran-3- carboxylic acid methyl ester, 5-acetyl-2-acetylamino-6-methyl-4-(2,3-dichlorophenyl)-4H-pyran- 3-carboxylic acid methyl ester, 5-acetyl-2-amino-6-methyl-4-(3-nitrophenyl)-4H-pyran-3-carboxylic acid methyl ester.