Abstract: Novel acrylic amide derivatives of the Formula (I) ##STR1## wherein R.sup.1 represents a hydrogen or a halogen atom or a C.sub.1-4 alkyl, a C.sub.1-4 alkoxy or a nitro group.n is an integer of 0 to 2,A represents an amino acid residue derived from a naturally occurring amino acid or an antipode thereof which is bonded to the acrylic acyl residue through its amino group; or a residue derived from thiazolidinecarboxylic acid, bonded to the acrylic acyl group through its nitrogen, or a derivative of the above residues wherein any free carboxy group is esterified with a C.sub.1-4 alkyl group or is amidated; or A represents a group of the formula ##STR2## wherein R.sub.2 is a hydrogen atom or a phenyl, C.sub.1-4 alkyl or C.sub.1-4 alkoxycarbonyl group,and their salts which have cytoprotective and antiulcer to activities. A process is also described for the preparation of said compounds.

Abstract: The present invention relates to novel compounds of the general formula (I) ##STR1## wherein R means hydrogen or C.sub.1-4 alkyl group; andY stands for cyano, trifluoromethyl, aryloxy or aryl(C.sub.1-4 alkyl)oxy group.The compounds according to the invention show a gastric acid secretion-inhibiting effect and therefore, they are useful for the treatment of gastric and duodenal ulcers. In addition, they exert a cytoprotective action against gastric laesions induced, e.g. by indomethacin or acid-containing alcohol.

Abstract: The invention relates to novel pyridine derivatives of formula (I), ##STR1## wherein Q stand for a nitro or cyano group; andX.sup.1 and X.sup.2, independently from each other, represent hydrogen or halogen or a trifluoromethyl, a lower alkyl or alkoxy or nitro group bound to any of the carbon atoms of the phenyl ring.The invention further relates to pharmaceutical compositions containing these compounds and a process for their preparation.The compounds of formula (I) possess gastric acid secretion inhibiting, tissue-protecting, analgetic and mild antiinflammatory effects and are useful for therapeutical purposes.

Abstract: The present invention relates to compounds of the general formula (I), ##STR1## wherein R.sub.1 stands for hydrogen, halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy or nitro group;R.sub.2 means a C.sub.1-7 alkyl group optionally substituted by: a hydroxyl or oxo group; or an ester group containing 1 to 4 carbon atoms in the alkoxy moiety; or a C.sub.1-4 alkoxy, cyano, amino, C.sub.1-4 alkylamino, or dialkylamino group; or an acyl group containing 1 to 7 carbon atoms in the alkyl moiety; orR.sub.2 means an aryl-C.sub.1-7 alkyl group optionally bearing the substituents defined above for R.sub.2 in the alkyl chain and optionally substituted by halogen, nitro, C.sub.1-4 alkyl or alkoxy group in the benzene ring; orR.sub.2 represents an allyl, phenylallyl or phenylsulfonyl group, both latter groups optionally being substituted by halogen or a C.sub.1-4 alkyl group in the benzene ring; orR.sub.2 stands for a carbamoyl group substituted by one or two C.sub.1-4 alkyl group(s) or phenyl group on the nitrogen atom.

Abstract: The present invention relates to novel compounds of the formula (I), ##STR1## wherein R.sub.1 and R.sub.2 stand independently from each other, for hydrogen, C.sub.1-4 alkyl, phenyl, phenyl-C.sub.1-4 alkyl, piridyl or piridyl-C.sub.1-4 alkyl group;E means a straight or branched, saturated hydrocarbon chain containing 1 to 6 carbon atoms;R.sub.3 represents: a phenyl group ortho-substituted by a C.sub.2-5 alkanoylamino, N-C.sub.2-5 alkanoyl-N-C.sub.1-4 alkylamino or di(C.sub.1-4 alkyl)amino group and optionally further substituted by halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy or C.sub.2-5 alkanoyloxy group; or a pyridyl group optionally mono- or polysubstituted by halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.2-5 alkanoyloxy or phenyl-C.sub.1-4 alkoxy groupas well as their acid addition salts and tautomeric forms of these compounds.

Abstract: Novel acrylic acid salts of formula ##STR1## wherein R represents a hydrogen or a halogen atom, a C.sub.1-4 alkyl, a C.sub.1-4 alkoxy or a nitro group,M represents a cation derived from bismuth, zinc or a pharmaceutically acceptable organic base,X represents an inorganic anion,n is an integer of from 0 to 2,m is an integer of from 1 to 3,p is 0 or 1, andr is an integer of from 0 to 6having cytoprotective and antiulcer activities are provided. A process is also described for the preparation of said compounds.

Abstract: The present invention relates to a method of treating a gastric ulcer by administering a 2-thia-zolone of the formula (I), ##STR1## wherein X stands for --CN, --CONH.sub.2, --CO.sub.2 H or --CO.sub.2 R group, wherein R is a C.sub.1-5 alkyl group; andn is 0, 1 or 2, with the proviso, that when X stands for CO.sub.2 H, CO.sub.2 R, n is other than 0.

Abstract: The present invention relates to novel 2-thiazolidinone derivatives of the general formula (I), ##STR1## wherein A stands for hydrogen, halogen or a C.sub.1-4 alkyl, C.sub.1-4 alkoxy or nitro group; andn is 0 or 1.The compounds according to the invention show a cytoprotective and gastric acid secretion-inhibiting effect and thus, may be used in the therapy of gastric and duodenal ulcers.

Abstract: The present invention relates to novel compounds of the general formula (I), ##STR1## wherein R stands for hydrogen, halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy or a C.sub.1-4 acylamino group; andR.sup.1 is hydrogen or a carboxyl-protective group or E and/or Z configuration as well as their salts.The compounds according to the invention show a cytoprotecive effect and in addition, a valuable anti-inflammatory action. Their toxicity is low.

Abstract: The invention relates to new 1,2,3,4,6,7,12,12b-octahydroindolo[2,3,-a]quinolizin-1-yl-alkanecarboxylic acid amides of the formula (I), ##STR1## wherein R.sub.1 and R.sub.2 stand independently for a hydrogen or halogen atom, or a hydroxyl, nitro or C.sub.1-4 alkoxy group;R.sub.3 and R.sub.4 stand independently for a hydrogen atom or a C.sub.1-4 alkyl group;R.sub.5 and R.sub.6 stand independently for a hydrogen atom, C.sub.1-8 alkyl group, C.sub.3-8 alkenyl or cycloalkyl group, aryl or aralkyl group, heteroaryl or heteroaralkyl group containing oxygen, nitrogen or sulphur atom, all these groups being optionally substituted; orR.sub.5 and R.sub.6 together form an optionally substituted C.sub.2-8 .alpha.,.omega.-alkylene group, wherein one carbon atom may optionally be replaced by an oxygen or nitrogen atom; andG means a C.sub.1-4 straight chained alkylene group, as well as to their therapeutically suitable acid addition salts and pharmaceutical compositions containing these compounds.

Abstract: The invention relates to novel butenoic acid derivatives of the general formula (Ia) having E-configuration ##STR1## as well as to their Z-izomers of the general formula ##STR2## wherein R stands for a (-)-menthyl or a (+)-menthyl group. as well as pharmaceutical compositions containing these compounds.The novel butenoic acid derivatives of the general formulae (Ia) and (Ib) possess valuable pharmacological properties, mainly gastric cytoprotective effect.

Abstract: The invention relates to new 2-pyridine-thiol derivatives of the formula (I), ##STR1## wherein R is hydrogen or alkyl having from 1 to 4 carbon atoms,Z is phenyl optionally substituted by one or more halogen atoms and/or alkyl groups having from 1 to 4 carbon atoms,R.sup.1 and R.sup.2 each independently represents hydrogen, alkyl having from 1 to 4 carbon atoms, alkylphenyl having from 1 to 4 carbon atoms in the alkyl moiety or an ##STR2## group, in which R has the same meaning as defined above, and the substituent ##STR3## is attached to the pyridine ring in the position 3 or 4, with the proviso that if R.sup.1 and R.sup.2 are both methyl and Z is 4-chlorophenyl, R is other than hydrogen, and acid addition salts thereof.The invention further relates to processes for the preparation of the above compounds and to pharmaceutical compositions containing them as active ingredient.The compounds are pharmaceutically active, in particular show cytoprotective activity.

Abstract: New intermediate compounds of the formula (I) are disclosed ##STR1## wherein R is hydrogen or C.sub.1 to C.sub.4 alkyl;Z is phenyl optionally substituted by one or more halogen atoms and/or alkyl groups having 1 to 4 carbon atoms; andD is hydroxy, mesyloxy, p-tosyloxy, or halogen; or pharmaceutically acceptable acid addition salt thereof. The compounds of the Formula (I) are intermediates in the preparation of new compounds having anti-ulcer activity.

Abstract: The invention relates to new 1-[6-(2'-substituted-5', 6', 7', 8'-tetrahydro-4'-oxo-quinazolino)]-3,4-dihydro-6,7-disubstituted-isoquinol ine derivatives of the formula (I) ##STR1## wherein R.sup.1 and R.sup.2 each independently represents hdyroxyl or alkoxy having from 1 to 6 carbon atoms,R.sup.3 is alky having from 1 to 6 carbon atoms, optionally substituted phenyl, optionally substituted alkylphenyl having from 1 to 4 carbon atoms in the alkyl moiety or an optionally substiutted heterocyclic group,and acid addition and quaternary salts thereof.Compounds of the formula (I) are pharmaceutically active, in particular show spasmolytic, analgesic, antipyretic activity and have a protecting effect in acute alcoholic intoxication.

Abstract: The invention relates to new N-substituted bis(hydroxymethyl)-methyl-isoquinoline derivatives of the formula (I), ##STR1## wherein R.sup.1 and R.sup.2 represent hydroxyl or alkoxy having from 1 to 6 carbon atoms,the dotted line is an optional double bond in the 1,2-position,R.sup.3 is alkyl having from 1 to 6 carbon atoms or aralkyl containing from 1 to 4 carbon atoms in the alkyl moiety, or--if there is a single bond in the 1,2-position--represents a group of the formula ##STR2## in which X is oxygen ifR.sup.4 is alkyl having from 1 to 5 carbon atoms, alkoxy having from 1 to 4 carbon atoms, hydroxyl, phenyl or substituted phenyl; orX is oxygen or sulfur ifR.sup.4 is an --NH.sub.2, --NH--C.sub.1-4 -alkyl, --NH--C.sub.3-6 -cycloalkyl, --NH-phenyl or --NH--C.sub.1-4 -alkyl-phenyl group; andR.sup.5 and R.sup.6 independently stand for hydrogen, alkyl having from 1 to 4 carbon atoms or phenyl, with the proviso that at least one of them is other than phenyl,and salts thereof.

Abstract: The invention relates to new 1-[bis(hydroxymethyl)-methyl]-3,4-dihydro- or -1,2,3,4-tetrahydroisoquinoline derivatives of the formula (I) ##STR1## wherein R.sup.1 and R.sup.2 represent hydroxyl or alkoxy having from 1 to 6 carbon atoms,R.sup.3 is hydrogen or a single electron pair,and the dotted line represents an optional double bond,and salts thereof.The new compounds are useful intermediates in the preparation of other, pharmaceutically active isoquinoline derivatives or are pharmaceutically active themselves.

Abstract: The invention relates to new bis(substituted methyl)-methyl-isoquinoline derivatives of the formula (I) ##STR1## wherein R.sup.1 and R.sup.2 represent hydroxyl or alkoxy having from 1 to 6 carbon atoms,R.sup.3 is hydrogen, aralkyl having from 1 to 4 carbon atoms in the alkyl moiety or a ##STR2## group, in which R.sup.4 is alkyl having from 1 to 5 carbon atoms, phenyl, substituted phenyl or --NH--phenyl,X is oxygen or sulfur,R.sup.7 is hydroxyl, halogen or an ##STR3## group, R.sup.8 is halogen, alkoxy from 1 to 4 carbon atoms or an ##STR4## group, in which X has the same meaning as defined above, andR.sup.9 independently from R.sup.4 may have the same meanings as defined for R.sup.4, or is an --NH(C.sub.1-4 -alkyl) or C.sub.3-6 -cycloalkyl group,and salts thereof. According to another aspect of the invention there are provided processes for the preparation of these compounds and pharmaceutical compositions containing them.

Abstract: The compound N-{2-[(3-benzoyl-1-pyridyl)-thio]-ethyl}-N'-cyano-S-methyl-isothiourea and pharmaceutically acceptable acid addition salts thereof are disclosed as well as pharmaceutical compositions containing same and a method of treatment employing same. The compound or its acid addition salts are effective in treating gastric oedema and thus are useful in ulcer therapy.

Abstract: The invention relates to new [1,3]oxazino[4,3-a]-isoquinoline derivatives of the formula (I) ##STR1## wherein R.sup.1 and R.sup.2 represent hydroxyl or alkoxy having from 1 to 6 carbon atoms,R.sup.3 is hydrogen, alkyl having from 1 to 8 carbon atoms, cycloakyl or cycloalkenyl having from 3 to 6 carbon atoms, optionally substituted phenyl, aralkyl having from 1 to 4 carbon atoms in the alkyl moiety or heteroaryl,R.sup.4 is hydrogen or alkyl having from 1 to 4 carbon atoms, orR.sup.3 and R.sup.4 together form a --(CH.sub.2).sub.n -- group, in which n is an integer from 3 to 7,R.sup.5 is hydroxyl, halogen or an ##STR2## group, in which R.sup.6 is optionally substituted phenyl,X is oxygen or sulfur,and salts thereof.According to another aspect of the invention there is provided a process for the preparation of these compounds. Compounds of formula (I) are pharmaceutically active. Pharmaceutical compositions containing them are also within the scope of the invention.

Abstract: The invention relates to new 2H-azeto[2,1-a]isoquinoline derivatives of formula (I) ##STR1## wherein R.sup.1 and R.sup.2 represent hydroxyl or alkoxy having from 1 to 6 carbon atoms,R.sup.3 is hydroxyl, halogen or an ##STR2## group, whereinX is oxygen or sulfur,R.sup.4 is optionally substituted phenyl,and acid addition, metal and quaternary salts thereof.According to the invention the new compounds are prepared by cyclization of the corresponding compounds of formula (II), ##STR3## wherein R.sup.1, R.sup.2 and R.sup.3 are as defined above, and Hal is halogen.Compounds of formula (I) are pharmaceutically active, in particular are potent analgesic and antipyretic agents.