DERIVATIVES OF EPI-EPIBATIDIN, PROCESS OF THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEREOF

• Main Authors: BLASKO GABOR DR, LADY BLANKA DR, SZEMEREDI KATALIN DR, SZALLASI TAMAS DR, GYERTYAN ISTVAN DR, BALOGH ZSUZSANNA DR, CSORGO MARGIT DR, SIMIG GYULA DR, LAX GYORGYI DR, FEKETE MARTON DR, MANDI ATTILA DR, SOMOGYI MARIA DR, SZANTAY CSABA DR, SZANTAY JR. CSABA DR, GIGLER GABOR, DRABANT SANDOR DR, MOLDVAI ISTVAN DR, TEMESVARI ESZTER DR
• Format: Patent
• Language: English
• Published: 12.07.1995
• 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

The subject-matter of the invention are epi-epibatidine derivatives of general formula wherein R stands for a C1-4-alkyl, C2-4-alkenyl, C2-4-alkinyl, C3-7-cycloalkyl, aryl, heteroaryl, aryl-C1-4-alkyl or heteroaryl-C1-4-alkyl group, said groups optionally being substituted by 1 or more C1-4-alkyl, C2-4-alkenyl, C2-4-alkinyl, C3-7-cycloalkyl, aryl, heteroaryl, aryl-C1-4-alkyl, heteroaryl-C1-4-alkyl, hydroxy, C1-4-alkoxy, phenoxy, halogen, halogeno-C1-4-alkyl and/or amino, amido and/or sulfonamido substituent(s), optionally mono- or di-C1-4-alkyl-, -C2-4-alkenyl- and/or -C2-4-alkinyl substituted, and R' represents hydrogen or a C1-4-alkyl, C2-4-alkenyl, C2-4-alkinyl, C3-7-cycloalkyl, C3-7-cycloalkenyl, C3-7-cycloalkinyl, aryl-C1-4-alkyl, aryl, hetero-aryl, halogeno-C1-4-alkyl, hydroxy-C1-4-alkyl or, preferably C1-4-aliphatic; aromatic or heterocyclic, acyl group with the proviso that, if R' stands for hydrogen, R is different from 6-(chloro)-pyrid-3-yl as well as optically active forms and acid addition salts thereof. Further aspects of the invention are concerned with a process and intermediates for preparing these compounds as well as medicaments containing them and their use.