Abstract: The invention relates to fused heterocyclic compounds with ring junction nitrogen atom of the formula: ##STR1## wherein Q stands for 2-indolizinyl, 2-imidazo[1,2-a]pyridinyl, 2-imidazo[1,2-a]pyrimidinyl, 6-(2,3-dihydroimidazo[2,1-b]thiazol)-yl or 6-imidazo[2,1-b]thiazolyl group; and n is an integer from 2 to 4, as well as therapeutically useful 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. The compounds of formula (I) exhibit mainly antipsychotic effects so the invention relates also to a method of treatment of schizophrenia, organic mental disorders, affective disorders, anxiety and personality disorders.

Abstract: The invention relates to novel racemic and optically active trans apovincaminic acid ester derivatives of formula (I), ##STR1## wherein R means hydrogen or a group (a), wherein Z stands for C.sub.1-4 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.

Abstract: The invention relates to novel N-hydroxy-substituted 1,2,3,6-tetrahydropyridine and piperidine derivatives of the formula ##STR1## wherein A, B, D, E, G, I and R are as defined in the specification, m is 0, 1 or 2, with the proviso that:m is 0 or 2, or both G and I are hydrogen, when A is benzyl or halogen-monosubstituted benzyl group; andm is 1, when A is 2-picolyl, as well as their pharmaceutically acceptable acid addition salts. The compounds of formula (I) are useful for enhancing the tolerance of mammals (including man) against hypoxic and/or ischaemic states as well as for treating the degenerative and functional disturbances arising from hypoxic and/or ischaemic results.

Abstract: New compounds with the ability to inhibit calcium uptake in the brains of mammals are disclosed of the Formula (I) ##STR1## wherein R.sup.1 is hydrogen, C.sub.1 to C.sub.4 alkyl, phenyl, or phenyl-C.sub.1 to C.sub.4 alkyl;one of R.sup.2 and R.sup.3 is C.sub.1 to C.sub.4 alkoxy and the other one is phenyl-C.sub.1 to C.sub.4 alkoxy optionally substituted by C.sub.1 to C.sub.4 alkyl in the aromatic nucleus; andR.sup.4 is phenyl optionally substituted by C.sub.1 to C.sub.4 alkyl in the aromatic nucleus, or their solvates, individual optically active and geometric isomers, mixtures of such isomers, as well as pharmaceutically acceptable acid addition salts thereof. The compounds of the Formula (I) are capable of inhibiting calcium uptake to brain cells and have a protective effect on hypobaric hypoxia.

Abstract: The present invention relates to novel 1,2,3,6-tetrahydropyridine derivatives of the general formula (I) ##STR1## wherein R stands for hydrogen or an alkyl group,X stands for an unsubstituted phenyl or benzyl group or for a phenyl or benzyl group substituted with a halogen atom,Y stands for hydrogen or halogen or a trifluoro-methyl groupas well as enantiomers acid addition salts thereof.The invention further extends to pharmaceutical compositions containing said compounds as active ingredient mainly for improving cerebral blood circulation and antihypoxic activity.

Abstract: The invention relates to novel 15-nitro-2.beta.,3.beta.-dihydro- and 15-nitro-2.beta.,3.beta.,6,7-tetrahydrotabersonine derivatives of the formula (I), ##STR1## wherein R.sup.1 stands for hydrogen;R.sup.2 stands for hydrogen or a C.sub.1-6 alkyl group; and the symbolrepresents a single or double bond as well as their salts.The invention further relates to pharmaceutical compositions containing the above compounds as well as a process for the preparation of the above compounds of formula (I) and of the pharmaceutical compositions.The compounds of formula (I) exert a reducing or inhibitory effect on cerebral edema and show antihypoxic properties. Thus, they are useful for the prevention or treatment of brain injuries of various origin induced by hypoxia of the brain.

Abstract: The invention relates to novel compounds 1-oxa-2-oxo-8- of the formula (I), ##STR1## wherein X means oxygen or an >NR group, whereinR stands for hydrogen, a C.sub.1-12 alkyl, C.sub.3-6 cycloalkyl, carbocyclic C.sub.6-10 aryl or carbocyclic C.sub.6-10 aryl-C.sub.10-4 alkyl group, the latter two groups are optionally substituted on their aromatic moiety by one or more, same or different halogen(s), one or more C.sub.1-4 alkyl or C.sub.1-4 alkoxy group(s);R.sup.1 and R.sup.2 together represent a methylene group or, when X stands for an >NR group, wherein R is as defined above, one of R.sup.1 and R.sup.2 may represent a hydroxyl group whereas the other is a methyl group;R.sup.3 stands for hydrogen or a phenyl group optionally substituted by one or more halogen(s), one or more C.sub.1-4 alkyl or C.sub.1-4 alkoxy or hydroxyl group(s);R.sup.4 means hydrogen, one or more halogen(s), C.sub.1-4 alkyl, C.sub.

Abstract: The invention relates to novel nitrogen- and sulfur-containing heterocyclic compounds of the formula (I), acid addition salts thereof, pharmaceutical compositions containing them and a process for their preparation. In the formula (I) ##STR1## Ar stands for an optionally mono- or polysubstituted aryl or heteroaryl group;R.sup.1 means a carbonyl or (C.sub.2-6 alkenyl)carbonyl group;R.sup.2 stands for hydrogen C.sub.1-6 alkyl, phenyl or phenyl (C.sub.1-4 alkyl) group;R.sup.3 means hydrogen or (C.sub.1-6 alkoxy)carbonyl group;R.sup.4 and R.sup.5 stand, independently from each other, for hydrogen or C.sub.1-6 alkyl group;R.sub.6 ogen, C.sub.1-6 alkyl group or halophenyl group;m is 0 or 1; andn is 1 or 2,with the proviso that R.sup.2 means hydrogen when m is 0.The compounds of formula (I) show a significant cerebral antihypoxic action and thus, they can be used for the treatment of diseases caused by hypoxic brain damages such as e.g.

Abstract: The invention relates to new peptide derivatives which act on the central nervous system and correspond to the general formula (I),X--Y--W--NH.sub.2 (I)whereinX is L-pyroglutamyl, D-pyroglutamyl, L-2-keto-imidazolidine-4-carbonyl, L-6-keto-pipecolyl, L-thiazolidine-4-carbonyl, L-prolyl or orotyl group,Y is L-leucyl, L-norvalyl or L-histidyl group, andW is L-prolyl, D-prolyl, L-thiazolidine-4-carbonyl, L-pipecolyl, L-homoprolyl, L-leucyl, L-isoleucyl, L-methionyl or D-pipecolyl group, orthe W-NH.sub.2 group stands for pyrrolidyl or piperidyl group, with the proviso that if X is L-pyroglutamyl and Y is L-histidyl group, W is other than L-prolyl group, and pharmaceutically acceptable complexes thereof.These compounds are prepared by methods commonly applied in the peptide chemistry.

Abstract: The invention relates to new tetrahydro-1,2,4-oxadiazin-5-one derivatives having a CNS activity. More particularly, the invention concerns new N.sup.4 -substituted tetrahydro-1,2,4-oxadiazin-5-ones of the formula (1) ##STR1## wherein R.sup.2 is benzyloxycarbonyl or alkylcarbonyl containing 1 to 4 carbon atoms in the alkyl moiety, preferably acetyl;R.sup.3 is phenyl optionally substituted with 1 to 3 lower alkoxy groups; andR.sup.4 is an aliphatic or cyclic alkyl group having 1 to 11 carbon atoms, hydroxymethyl, halomethyl or acyloxymethyl.According to another aspect of the invention there are provided processes for the preparation of compounds of formula (1). Still another aspect of the invention is a pharmaceutical composition which comprises as active ingredient a compound of formula (1).

Abstract: The invention relates to new peptide derivatives which act on the central nervous system and correspond to the general formula (I),Glp--X--Y--NH--A (I)whereinX is L-norleucyl, L-leucyl, L-norvalyl, D-leucyl, L-prolyl, L-2-aminobutyryl, L-valyl, L-threonyl, L-isoleucyl, L-2-aminodecanoyl, L-cyclohexylalanyl or L-tert.-butyl-seryl group andY is L-prolyl group, orX is L-histidyl group andY is L-homoprolyl or D-pipecolyl group, furthermoreA is hydrogen, a C.sub.1-10 alkyl group or a C.sub.1-3 alkyl group having a dimethylamino substituent,with the proviso that if X is L-leucyl group, A is other than hydrogen, and pharmaceutically acceptable complexes thereof.These compounds are prepared by methods commonly applied in the peptide chemistry.