Trans apovincaminic acid ester derivatives as drugs

• Main Authors: JANOS KREIDL, ANDRAS VEDRES, EGON KARPATI, MARGIT PELLIONISZNE PAR¤CZAI, ISTVAN MOLDVAI, ANIKO GERE, MARIA INCZE, CSABA SZANTAY, FERENC AUTH, IDA DEUTSCHNE JUHASZ, ADAM SARKADI, SANDOR FARKAS, JENOOE"NE (KIRJAK MARIA) FARKAS, LASZLO CZIBULA, BELA KISS, ERZSEBET LAPIS, ANDRAS SZEKERES, MARIA ZAJERNE BALAZS
• Format: Patent
• Language: English
• Published: 17.07.1997
• 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

PCT No. PCT/HU96/00075 Sec. 371 Date Jun. 9, 1998 Sec. 102(e) Date Jun. 9, 1998 PCT Filed Dec. 13, 1996 PCT Pub. No. WO97/23481 PCT Pub. Date Jul. 3, 1997The invention relates to novel racemic and optically active trans apovincaminic acid ester derivatives of formula (I), wherein R means hydrogen or a group (a), wherein Z stands for C1-4 alkyl, optionally substituted aryl, aralkyl, heteroaryl or 14-eburnameninyl group; and n is an integer of 2, 3 or 4, as well as therapeutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing these compounds as well as a process for the preparation of the above compounds and compositions, and in addition, to a method of treatment. The novel compounds of Formula (I) exhibit particularly antioxidant, antiischemic as well as antiamnesic effects and are useful for inhibiting lipid peroxidation and for protection from or treatment of ischemia and amnesia as well as for treating various degenerative neurological diseases, e.g. Alzheimer's disease.