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 racemic and optically active 1,12b-disubstituted octahydroindolo[2,3-a]quinolizine derivatives of the formula (I) ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and represent hydrogen, halogen, nitro, alkyl having from 1 to 6 carbon atoms, alkoxy having from 1 to 6 carbon atoms or hydroxyl,R.sup.3 and R.sup.5 are the same or different and represent hydrogen, alkyl having from 1 to 6 carbon atoms or aralkyl having from 1 to 6 carbon atoms in the alkyl moiety,R.sup.4 is alkyl having from 1 to 6 carbon atoms, aryl or aralkyl having from 1 to 6 carbon atoms in the alkyl moiety, andR.sup.6 is an electron attracting substitutent, and cis and trans isomers and acid addition salts thereof.The compounds are pharmaceutically active, in particular show an outstanding cardiovascular, e.g. selective peripheral vasodilating activity. Some of these compounds are valuable intermediates in the preparation of other, pharmaceutically active compounds.

Abstract: The invention relates to the preparation of cis and trans stereoisomers of racemic and optically active eburnamenine derivatives of the general formula (Ia) ##STR1## or (Ib), ##STR2## wherein R.sub.1 stands for a C.sub.1-4 alkyl group; andR stands for hydrogen, a C.sub.1-6 alkyl group, a C.sub.2-6 alkenyl group, an acyl or substituted acyl group,as well as their acid addition salts, of which the trans compounds are novel.The invention also relates to the compounds of the general formula (IIIa) ##STR3## and (IIIb), ##STR4## wherein R.sub.1 and R' represent a C.sub.1-4 alkyl group. The compounds of the general formulae (Ia) and (Ib) possess a vasodilatory effect which is substantially higher than that of pentoxifyllin, a known peripheral vasodilator.

Abstract: The invention relates to a new process for preparing novel racemic and optically active 9- or 11-nitroapovincaminic acid derivatives of the general formula (I) ##STR1## wherein R stands for a --CO--X group, wherein X means a halogen atom; orfor a --CO--OR.sup.1 group, wherein R.sup.1 means an optionally mono- or polysubstituted C.sub.1-10 aliphatic group, a C.sub.3-8 alicyclic group or an aromatic C.sub.6-14 hydrocarbyl group; orfor a --CO--NR.sup.2 R.sup.3 group, wherein R.sup.2 and R.sup.3 are the same or different and stand for a hydrogen atom or a C.sub.1-8 alkyl group optionally forming a saturated heterocycle together with the adjacent nitrogen atom and optionally with one or more further nitrogen atoms or other heteroatoms, and R.sup.3 may also represent an amino group when R.sup.2 stands for a hydrogen atom; orfor a cyano group,as well as their salts and pharmaceutical preparations containing these compounds.

Abstract: The invention relates to the new (-)-1.beta.-ethyl-1.alpha.-hydroxymethyl-1,2, 3,4,6,7,12,12b.alpha.-octa-hydroindolo[2,3-a] quinolizine of the formula (I) ##STR1## and acid addition salts thereof. According to another aspect of the invention there is provided a process for the preparation of the compound of formula (I) and acid addition salts thereof by resolution of the corresponding racemic compound and optionally by subsequent hydrolysis and/or salt formation.The compound of formula (I) shows a remarkable peripheral vasodilating and antihypoxial activity. Pharmaceutical compositions comprising it as active ingredient are also within the scope of the invention.

Abstract: The invention relates to a novel process for the preparation of partially new 2-halonicergoline derivatives of the formula (I), ##STR1## wherein X stands for chlorine, bromine or iodine atom, as well as their acid addition salts.The process of the invention comprises esterifying a novel 2-halo-1-methyllumilysergol of the formula (II), ##STR2## wherein X is the same as defined above, or an acid addition salt thereof and, if desired, converting the thus-obtained 2-halonicergoline derivative of the formula (I) to an acid addition salt.The compounds of the invention improve the cognitive function of the brain and show an antihypoxic as well as a strong .alpha.-adrenerg blocking and calcium-antagonistic action.

Abstract: The present invention relates to a compound of the formula (I) ##STR1## wherein R.sup.1 stands for methyl or a group of the formula R.sup.3 --NH--(CH.sub.2).sub.4 --wherein R.sup.3 is hydrogen or a protective group being compatible with the peptide bond,R.sup.2 represents hydrogen, a protective group being compatible with the peptide bond or a cation derived from an organic or inorganic basethe pharmaceutically acceptable salts and diastereomers thereof.The compounds of the invention are useful for inhibiting the effect of the angiotensin converting ensime and they can be used in the therapy as blood pressure reducing agents and for the treatment of cardiac failure and glaucoma.

Abstract: The invention relates to pharmaceutical compositions with a neuroleptic action as well as to a process for preparing these compositions.The active ingredients of the compositions of the invention are 2-halo-6-methyl-9-ergolene derivatives of the formula (I), ##STR1## wherein X represents a chlorine, bromine or iodine atom as well as their acid addition salts.The compositions of the invention contain an effective dose of compound of the general formula (I) or an acid addition salt thereof.