Abstract: A process is disclosed for the preparation of compounds of the formula (I), which compounds are useful as intermediates for the preparation of paroxetine of formula(V).

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 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: The invention relates to carbazolone derivatives of the formula ##STR1## wherein A stands for a group of formula--CH.sub.2 --R (V),wherein R means a hydroxyl or 2-methyl-1H-imidazol-1-yl group;B represents a group of formula ##STR2## wherein R.sub.1 means hydrogen or a methyl or ethyl group; or A and B together form a group of formula ##STR3## wherein R.sub.2 means a methyl or ethyl group; or A and B together form a group of formula ##STR4## The above compounds are useful intermediates in the synthesis of ondansetron of formula ##STR5## chemically 9-methyl-3-[(2-methyl-1H-imidazol-1-yl)methyl]-1,2,3,9-tetrahydro-4H-carba zol-4-one.The invention further relates to a novel process for the preparation of compounds of the formula (I) , wherein A and B are the same as in formula (I) but B may be also hydrogen. Thus, this novel process is suitable for the preparation of ondansetron itself.

Abstract: The invention relates to carbazolone derivatives of the formula ##STR1## wherein A stands for a group of formula--CH.sub.2 --R (V),wherein R means a hydroxyl or 2-methyl-1H-imidazol-1-yl group;B represents a group of formula ##STR2## wherein R.sub.1 means hydrogen or a methyl or ethyl group; or A and B together form a group of formula ##STR3## wherein R.sub.2 means a methyl or ethyl group; or A and B together form a group of formula ##STR4## The above compounds are useful intermediates in the synthesis of ondansetron of formula ##STR5## chemically 9-methyl-3-[(2-methyl)-1H-imidzol-1-yl)methyl]1,2,3,9-tetrahydro-4H-carbaz ol-4-one.The invention further relates to a novel process for the preparation of compounds of the formula (I), wherein A and B are the same as in formula (I) but B may be also hydrogen. Thus, this novel process is suitable for the preparation of ondansetron itself.

Abstract: The invention relates to a novel process for the resolution of an acid mixture (hereinafter: threo acid mixture) containing (+)-threo-3-[(2-aminophenyl)thio]-2-hydroxy-3-(4-methoxyphenyl)-propionic acid [hereinafter: (+)-threo acid]and (-)-threo-3-[(2-aminophenyl)thio]-2-hydroxy-3-(4-methoxyphenyl)-propionic acid [hereinafter: (-)-threo acid].

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 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: Novel antihyperlipoproteinemic compounds are disclosed of the formula I, ##STR1## wherein X is a halogen atom, methyl, ethyl, methoxy or ethoxy group,Y is hydroxy if X is methoxy or ethoxy, otherwise it is a hydrogen atom or a, methoxy or ethoxy group,Z is a methoxy or ethoxy group if X or Y is a methoxy group or an ethoxy group; otherwise it is hydrogen atom,The invention also covers antiartheriosclerotic, antihyperlipoproteinemic pharmaceutical compositions, suitable for inhibiting the formation of thrombuses, comprising the compounds of formula I in an effective dose, a process for preparing the same and methods for the treatment of hyperlipoproteinemia with the aid of the said compounds or compositions.

Abstract: The invention relates to two morphologically homogeneous forms of Famotidine [chemical name: N-sulfamoyl-3-(2-guanidino-thiazole-4-yl-methylthio)-propionamidine]. Said forms are prepared by selective crystallization or precipitation.

Abstract: The invention relates to two morphologically homogeneous forms of Famotidine [chemical name: N-sulfamoyl-3-(2-guanidino-thiazole-4-yl-methylthio)-propionamidine]. Said forms are prepared by selective crystallization or precipitation.

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 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 invention relates to two morphologically homogeneous forms of Famotidine [chemical name: N-sulfamoyl-3-(2-guanidino-thiazole-4-yl-methylthio)-propionamidine]. Said forms are prepared by selective crystallisation or precipitation.

Abstract: The invention relates to a new process for the preparation of N-sulfamyl-3-(2-guanidinothiazol-4-yl-methylthio)-propionitrile (famotidine) of the formula (I) ##STR1## by S-alkylation of 2-guanidino-thiazol-4-yl-methanethiol obtained from S-(2-guanidino-thiazol-4-yl-methyl)-isothiourea dihydrochloride of the formula (III) ##STR2## by in situ treatment with a base, which comprises carrying out S-alkylation with a N-sulfamyl-3-halopropionamidine of the formula (II) ##STR3## wherein X stands for halogen.

Abstract: The invention relates to new propionamidine derivatives of formula (I) ##STR1## wherein X is halogen,and to a process for their preparation. According to the invention compounds of the formula (I) are prepared by reacting a 3-halopropionitrile of the formula (III) ##STR2## wherein X is as defined above,with sulfamide of the formula (II) ##STR3## in the presence of a hydrogen halide. Compounds of the formula (I) are useful intermediates in the preparation of famotidine.

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 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.