Abstract: The invention relates to new N-hydroxy-4-(3-phenyl-5-methyl-isoxazole-4-yl)-benzenesulfonamide solvates of formula (I). wherein n represents 0 or 1 mol, [solvate] represents water, C1-C4 alcohol, C1-C4 alkylester of C1-C3 carboxylic acid or dioxane, and the mixture of solvated (wherein n=1) and solvat-free forms (wherein n=0). Furthermore, the invention relates their process for production and use for the treatment of osteoarthritis and rheumatoid arthritis and surgical and primary dysmenorrheal pains, based on anti-inflammatory and analgesic pharmacological model experiments.

Abstract: The invention relates to R-2-[3-([1,4]benzodioxan-2-ylmethylamino)-1-propyl]-3(2H)-pyridazinone of formula (1), and to S-2-[3-([1,4]benzodioxan-2-ylmethylamino)-1-propyl]-3(2H)-pyridazinone of formula (2), and to acid-addition salts thereof as well as pharmaceutical compositions containing these compounds. Furthermore, the invention relates to a process for the preparation of the above compounds. The new starting compounds of formulae (4) and (5) are also involved in the scope of the invention. The compounds according to the invention possess &agr;1- and &agr;2-adrenoceptor antagonistic effects and urogenital selectivity. Thus, they are useful for the treatment of the benign prostate hyperplasia.

Abstract: The invention relates to R-2-[3-([1,4]benzodioxan-2-ylmethylamino)-1-propyl]-3(2H)-pyridazionone of formula (1) and to S-2-[3-([1,4]benzodioxan-2-ylmethylamino)-1-propyl]-3(2H)-pyridazionone of formula (2) and to acid-addition salts thereof as well as pharmaceutical compositions containing these compounds. Furthermore, the invention relates to a process for the preparation of the above compounds. The new starting compounds of formula (4) and (5) are also involved in the scope of the invention. The compounds according to the invention possess &agr;1- and &agr;2-adrenoceptor antagonistic effects and urogenital selectivity. Thus, they are useful for the treatment of the benign prostate hyperplasia.

Abstract: The invention relates to novel spiro[2H-1-benzopyran-2,4'-piperidine]-4(3H)-one derivatives of formula (I), ##STR1## wherein R stands for halogen, nitro group or a straight or branched chain C.sub.1-6 alkyl group, and their acid addition salts, as well as their quaternary salts of formula (Ia) ##STR2## wherein R and R' are the same or different and are identical to the meaning of said (above) R or can mean also hydrogen; and Z represents one equivalent of an anion. The compounds of formulas (I) and (Ia) exert an improving effect on dementias of various pathological origin and accompanying symptoms thereof. Furthermore, the invention relates to a process for the preparation of compounds of formulas (I) and (Ia); to pharmaceutical compositions containing as active gents the above compounds of formulas (I) and (Ia); and to a method of treatment.

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: New monoquaternary and diquaternary 5-alpha-hydroxy-3,16-diaminoandrostane salts are disclosed with curare-like muscle relaxant activity. The new salts are characterized by a surprisingly rapid onset time.

Abstract: A method of treating a mammalian subject for Parkinson's disease or to provide a central muscle relaxant effect, which comprises the step of administering to the mammalian subject in need of the treatment, a therapeutically effective amount of a compound of the Formula (I) ##STR1## wherein m is 1,2 or 3;R.sub.1 and R.sub.2 each independently stand for hydrogen, C.sub.1 to C.sub.4 straight or branched chain alkyl, C.sub.1 to C.sub.4 alkoxy, C.sub.5 to C.sub.7 cycloalkyl, or halogen; andB is a 5- or 6-membered saturated or unsaturated heterocyclic group containing a nitrogen heteroatom, the heterocyclic group being bound through its heterocyclic nitrogen atom to the remainder of the compound, and which can contain one or two additional heteroatoms selected from the group consisting of an oxygen heteroatom, a sulfur heteroatom, and one or two additional nitrogen heteroatoms, which may be as an .dbd.N--, --NH-- or --NR-- group, where R is a C.sub.1 to C.sub.5 alkyl or C.sub.1 to C.sub.

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: A method of treating a mammalian subject for Parkinson's disease or to provide a central muscle relaxant effect, which comprises the step of administering to the mammalian subject in need of the treatment, a therapeutically effective amount of a compound of the Formula (I) ##STR1## wherein m is 1,2 or 3;R.sub.1 and R.sub.2 each independently stand for hydrogen, C.sub.1 to C.sub.4 straight or branched chain alkyl, C.sub.1 to C.sub.4 alkoxy, C.sub.5 to C.sub.7 cycloalkyl, or halogen; andB is a 5- or 6-membered saturated or unsaturated heterocyclic group containing a nitrogen heteroatom, the heterocyclic group being bound through its heterocyclic nitrogen atom to the remainder of the compound, and which can contain one or two additional heteroatoms selected form the group consisting of an oxygen heteroatom, a sulfur heteroatom, and one or two additional nitrogen heteroatoms, which may be as an .dbd.N--, --NH-- or --NR-- group, where R is a C.sub.1 to C.sub.5 alkyl or C.sub.1 to C.sub.

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 novel, sulfur-containing 5-substituted benzimidazole derivatives of formula I ##STR1## and acid-addition salts thereof antihyperlipoproteinemic action, a process for preparing the same, pharmaceutical formulations comprising the novel compound as active ingredient and a method for inhibiting atherosclerosis, trombus formation and treating hyperlipoproteinemic diseases.

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.