Abstract: The invention relates to antiinflammatory compounds of the formula (I), ##STR1## wherein A stands for hydrogen, hydroxyl or trifluoroacetoxy group;X stands for hydrogen or halogen with the proviso that if A is hydrogen, then X also means hydrogen;R stands for hydrogen, benzoyl or C.sub.1-8 alkanoyl group; andrepresents a single or double bond between two adjacent carbon atoms,as well as pharmaceutical compositions containing these compounds and a process for their preparation.

Abstract: The invention relates to antiinflammatory compounds of the formula (I), ##STR1## wherein A stands for hydrogen or hydroxyl group;X stands for hydrogen or halogen with the proviso that if A is hydrogen, then X also means hydrogen;R stands for hydrogen, benzoyl or C.sub.1-8 alkanoyl group;R.sup.1 and R.sup.2, which are the same or different, stand for hydrogen or a C.sub.1-4 alkyl group; or one of R.sup.1 and R.sup.2 is hydrogen and the other is phenyl group; or R.sup.1 and R.sup.2 together form a C.sub.4-5 alkylene group;means a single or double bond between two adjacent carbon atoms,as well as pharmaceutical compositions containing these compounds and a process for their preparation.

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 the preparation of 17,18-dehydro-apovincaminol-trimethoxy-benzoate of the formula (I) ##STR1## and acid addition salts thereof. According to the invention compound of the formula (I) is prepared starting from 17,18-dehydrovincamine of the formula (IIa) ##STR2## and/or 17,18-dehydro-epivincamine of formula (IIb) ##STR3## by reducing with a complex metal hydride, acylating the new hydroxy-vincaminol derivative obtained selectively with 3,4,5-trimethoxy-benzoic acid or a derivative thereof capable of acylation, optionally in the presence of a catalyst and/or an acid binding agent, and treating the corresponding acylated hydroxylderivative obtained with formic acid, in the presence of an acid chloride, and, if desired, converting the compound of formula (I) obtained into an acid addition salt thereof.

Abstract: The invention relates to new apovincaminol derivatives of the formula /I/ ##STR1## wherein R.sub.1 is hydrogen, nitro or halogen,R.sub.2 is a substituted or unsubstituted alkyl or phenyl group,R.sub.3 and R.sub.4 together form a valency bond or each independently represents hydrogen, hydroxyl or an --OR.sub.5 group, in whichR.sub.5 is substituted or unsubstituted alkanoyl or benzoyl group,with the proviso that if R.sub.2 stands for a 3,4,5-trimethoxyphenyl group and R.sub.1 is hydrogen, R.sub.3 and R.sub.4 together do not form a valency bond, or if R.sub.2 is a 3,4,5-trimethoxyphenyl group and R.sub.3 and R.sub.4 both are hydrogen, R.sub.1 is other than hydrogen, nitro or bromine, and acid addition salts thereof.The compounds may be used in the therapy of various skin diseases accompanied by a pathological cell proliferation, preferably psoriasis.

Abstract: The invention relates to new dialkylaminoalkoxybenzylalcohol derivatives of the formula (I) ##STR1## wherein R.sub.1 is hydrogen, halogen, trihalomethyl, alkyl having from one to 4 carbon atoms or alkoxy having from one to 4 carbon atoms;R.sub.2 is halogen, trihalomethyl, alkyl having from one to 4 carbon atoms or alkoxy having from one to 4 carbon atoms;R.sub.3 and R.sub.4 independently stand for an alkyl group having from 3 to 5 carbon atoms; andn is 2, 3, 4 or 5,and acid addition and quanernary ammonium salts thereof.According to another aspect of the invention there are provided processes for the preparation of these compounds.The new compounds provided by the invention are pharmaceutically active, in particular, they are suitable for the treatment of acute ethanolic intoxication. Pharmaceutical compositions containing them as active ingredient are another aspect of the invention.

Abstract: The invention relates to new aminopropanol derivatives of the formula (I) ##STR1## wherein R.sub.1 is halogen, trihalomethyl, alkoxy having from one to 3 carbon atoms or alkyl having from one to 3 carbon atoms,R.sub.2 is alkyl having from one to 3 carbon atoms, andR.sub.3 is cycloalkyl having from 3 to 6 carbon atoms, orR.sub.2 and R.sub.3 together with the nitrogen they are attached to form an up to 8 membered ring optionally containing oxygen or a further nitrogen as an additional hetero atom, and optionally substituted with alkyl having from one to 4 carbon atoms or benzyl,and acid addition and quaternary ammonium salts thereof.According to another aspect of the invention there are provided processes for the preparation of these compounds.The new compounds are suitable for the treatment of acute ethanolic intoxication. Pharmaceutical compositions containing them are also within the scope of the invention.

Abstract: The invention relates to the preparation of new diethylaminoalkoxybenzhydrol derivatives of the formula (I) ##STR1## wherein R.sub.1 is hydrogen, halogen, trihalomethyl, alkyl having from one to 4 carbon atoms or alkoxy having from one to 4 carbon atoms,R.sub.2 is halogen, trihalomethyl, or alkoxy having from one to 4 carbon atoms, andn is 1, 2, 3 or 4,and acid addition and quaternary ammonium salts thereof.According to another aspect of the invention, there are provided new compounds of the formula (I), and acid addition and quaternary salts thereof. The compounds can be used for the treatment of acute ethanolic intoxication and depression syndromes. Pharmaceutical compositions containing them as active ingredient are also within the scope of the invention.

Abstract: The invention relates to the preparation of 3-trifluoromethyl- and 2,5-dimethyl-4'-hydroxy-.alpha.-ethyl-benzhydrol. Both compounds have so far been described only as metabolites of corresponding benzhydrol derivatives containing no hydroxyl group. Neither their physico-chemical characteristics nor their manufacturing processes have been disclosed in the known publications.3-Trifluoromethyl- and 2,5-dimethyl-4'-hydroxy-.alpha.-ethyl-benzhydrol are suitable for the treatment of acute ethanolic intoxication. Accordingly, another aspect of the invention is a pharmaceutical composition containing one of these compounds as active ingredient.

Abstract: The invention relates to new indolo[2,3-g]cyclopent[a]indolizine derivatives of the formulae (II) ##STR1## and/or (III) ##STR2## wherein W is alkoxycarbonyl having from one to four carbon atoms in the alkoxy moiety or cyano,R.sub.1 is hydrogen or alkyl having from one to four carbon atoms,G is a >CH.sub.2 or >C.dbd.O group, andX and Y each stands for hydrogen or together represent a C--C bond.According to another aspect of the invention there is provided a process for the preparation of the above compounds, which are pharmaceutically active, in particular, possess valuable gastric acid secretion inhibiting activity. Pharmaceutical compositions containing compounds of the formulae (II) and/or (III) are also within the scope of the invention.

Abstract: The invention relates to the new monohydrate of N-methyl-N'-{2-[(5-methylimidazol-4-yl)-methylthio]-ethyl}-N"-cyanoguanidi ne (cimetidine), a histamine-H.sub.2 receptor antagonist which is called N-methyl-N'-{2-[(5-methylimidazol-4-yl)-methylthio]-ethyl}-N"-cyanoguanidi ne H (cimetidine H) as well as to a process for the preparation of same, which comprises pouring a hot, homogeneous aqueous solution of N-methyl-N'-{2-[(5-methylimidazol-4-yl)-methylthio]-ethyl}-N"-cyanoguanidi ne, optionally containing also methylamine, onto ice and separating the N-methyl-N'-{2-[(5-methylimidazol-4-yl)-methylthio]-ethyl}-N"-cyanoguanidi ne monohydrate.

Abstract: The invention relates to new 2-azabicyclo[2.2.2]octane derivatives of the formula (I), ##STR1## wherein A is hydrogen, alkoxycarbonyl having from one to 4 carbon atoms in the alkoxy group, phenylalkoxycarbonyl having from one to 4 carbon atoms in the alkoxy moiety, alkyl having from one to 6 carbon atoms, aralkyl containing from one to 4 carbon atoms in the alkyl moiety or substituted acyl,R.sub.1 is hydrogen or alkyl having from one to 4 carbon atoms,Z is hydrogen or halogen,X is hydrogen or halogen,Y is hydrogen, orX and Y together represent a C--C bond,W is alkoxycarbonyl having from one to 4 carbon atoms in the alkoxy moiety, cyano, carboxamido or haloformyl, orif X stands for halogen, X and Y together represent a ##STR2## group. According to another aspect of the invention there is provided a process for the preparation of the above compounds, which are pharmaceutically active, in particular, possess valuable anticonvulsive, vasodilating or gastric acid secretion inhibiting properties.

Abstract: The invention relates to new resorcin derivatives of the formula (I) ##STR1## wherein R.sub.1 and R.sub.2 independently represent hydrogen, halogen, trihalomethyl, alkyl having from one to 3 carbon atoms or alkoxy having from one to 3 carbon atoms.According to another aspect of the invention there are provided processes for the preparation of these compounds.The compounds of the formula (I) are pharmacologically active. In particular, they are suitable for the treatment of acute ethanolic intoxication. Pharmaceutical compositions containing them as active ingredient are also within the scope of the invention.

Abstract: The invention relates to new 4-hydroxy-benzhydrols of the formula (I) ##STR1## wherein R.sub.1 and R.sub.2 independently represent hydrogen, halogen, trihalomethyl, alkyl having from one to 4 carbon atoms or alkoxy having from one to 4 carbon atoms, with the proviso that if R.sub.1 is hydrogen, R.sub.2 is other than hydrogen or a 3-trifluoromethyl group, or if R.sub.1 is a 2-methyl group, R.sub.2 is other than a 5-methyl group.According to another aspect of the invention there are provided processes for the preparation of these compounds.The compounds of the formula (I) are pharmacologically active. In particular, they are suitable for the treatment of acute ethanolic intoxication. Pharmaceutical compositions containing them as active ingredients are also within the scope of the invention.

Abstract: The invention relates to new cytostatic compound, process for their preparation and pharmaceutical compositions containing them. More particularly, there are provided new compounds of the general formula ##STR1## in which R.sup.4 is .beta.-hydroxyl andR.sup.3 is .alpha.-ethyl; orR.sup.4 is hydrogen andR.sup.3 is .beta.-ethyl;R" is a straight chained alkyl having from 1 to 10 carbon atoms, or a branched chained alkyl having from 3 to 10 carbon atoms, in which groups the carbon atom attached to the >N.sub.a --CH.sub.2 --O-- group has a primary or secondary configuration or an alkenyl or alkinyl having from 3 to 6 carbon atoms, or an aralkyl having from 1 to 3 carbon atoms in the alkyl moiety;R.sup.1 is methoxy andR.sup.2 is acetyl, provided that if R.sup.3 is .alpha.-ethyl and R.sup.4 .beta.-hydroxyl,R.sup.4 is other than ethyl.

Abstract: New .DELTA..sup.1,3,5 -3-chloro-pregnane derivatives of the general formula (I), ##STR1## wherein X is hydrogen atom, acetyl group or a chloroacetyl group, andY and Z represent hydrogen atom or a halogen atom, with the proviso that at least one of them is other than hydrogen,are prepared by reacting a .DELTA..sup.1,4 -3-oxo-pregnane derivative of the general formula (II), ##STR2## wherein X' is acetyl group or a chloroacetyl group and Y and Z are as defined above, with a chloromethyleneiminium salt of the general formula (III), ##STR3## wherein A.sup.(-) is a salt-forming anion, in an aprotic solvent in the presence of a tertiary base, and, if desired, subjecting the resulting product to hydrolysis.The compounds of the general formula (I) exert antiphlogistic effects and can be used in the therapy for the treatment of inflammations.

Abstract: The invention relates to the new 17,18-dehydro-apovincaminol-3',4',5'-trimethoxy-benzoate of formula (I) ##STR1## and acid addition salts thereof. According to another aspect of the invention there is provided a process for the preparation of these new compounds. Still another aspect of the invention is a pharmaceutical composition for treating psoriasis.

Abstract: The present invention relates to the compounds of the Formulae 1a and 1b and pharmaceutically acceptable acid addition salts thereof.The new 9-nitro-apovincaminol-3',4',5'-trimethoxybenzoate of the Formula 1a ##STR1## and the 11-nitro-apovincaminol-3',4',5'-trimethoxy-benzoate of the Formula 1b ##STR2## and pharmaceutically acceptable acid addition salts thereof can be prepared by nitrating the apovincaminol-3',4',5'-trimethoxy-benzoate of the Formula 11, ##STR3## if desired separating the mixture of the compounds of the Formulae 1a and 1b thus obtained into its components, if desired converting a compound of the Formula 1a or 1b thus obtained into pharmaceutically acceptable acid addition salts thereof.The new compounds of the present invention can be used in therapy in the treatment of psoriasis.

Abstract: The invention relates to new cytostatic compound, process for their preparation and pharmaceutical compositions containing them. More particularly, there are provided new compounds of the general formula ##STR1## in which R.sup.4 is .beta.-hydroxyl andR.sup.3 is .alpha.-ethyl; orR.sup.4 is hydrogen andR.sup.3 is .beta.-ethyl;R" is a straight chained alkyl having from 1 to 10 carbon atoms, or a branched chained alkyl having from 3 to 10 carbon atoms, in which groups the carbon atom attached to the >N.sub.a -CH.sub.2 -O-- group has a primary or secondary configuration or an alkenyl or alkinyl having from 3 to 6 carbon atoms, or an aralkyl having from 1 to 3 carbon atoms in the alkyl moiety;R.sup.1 is methoxy andR.sup.2 is acetyl,provided that if R.sup.3 is .alpha.-ethyl and R.sup.4 .beta.-hydroxyl, R.sup.4 is other than ethyl.

Abstract: The invention relates to a new method for controlling the level and distribution of alkaloids produced by Claviceps purpurea variant strains capable of producing primarily ergocornine, .alpha.-ergocryptine and .beta.-ergocryptine under saprophytic conditions. According to the invention a compound of the biosynthesis path of isoleucine or a compound which promotes the formation of isoleucine by biochemical control is added to the fermentation broth. In other respects fermentation is performed under conditions known per se.By the method of the invention the ratio of .alpha.- and .beta.-ergocryptine formed in the fermentation broth can be adjusted to the optimum value.