Abstract: The invention relates to a process for the preparation of the compound of the formula I, ##STR1## which comprises (a.sub.1) splitting off the ethylene ketal protecting group from the azetidinone derivative of the formula IVa, ##STR2## reducing the compound of the formula III thus obtained, ##STR3## treating the resulting compound of the formula II ##STR4## with concentrated aqueous hydrogen chloride solution; or (a.sub.2) reducing the compound of the formula III, treating the compound of the formula II thus obtained with concentrated aqueous hydrogen chloride solution; or (a.sub.3) treating the compound of the formula II with concentrated aqueous hydrogen chloride solution; and isolating the compound of the formula I thus obtained from the reaction mixture. The compound of the formula I is useful as an intermediate in the production of thienamycin, a highly potent antibiotic.

Abstract: The invention relates to racemic or optically active eburnane derivatives of the formula (I), ##STR1## wherein R represents an alkyl group having 1 to 6 carbon atoms,A stands for hydroxyl andY is hydrogen, orA and Y together form an oxo group,and the configuration of the hydrogen in the 3-position and of R is .alpha.,.alpha. and/or .beta.,.beta. or .alpha.,.beta. and/or .beta.,.alpha.,and acid addition salts thereof.The new compounds possess valuable pharmaceutical properties, thus their certain representatives show antiallergic activity, while others are potent antidepressive, gastric secretion inhibiting and anticonvulsive agents. The compounds of the formula (I) and pharmaceutically acceptable acid addition salts thereof can therefore be employed as active ingredients of pharmaceutical compositions, which are also within the scope of the invention.

Abstract: The invention relates to new piperidine derivatives of the formula (I) ##STR1## wherein R.sub.1 is halogen, trihalomethyl, alkyl having from one to 4 carbon atoms or alkoxy having from one to 4 carbon atoms; andR.sub.2 is hydrogen or alkyl having from one to 4 carbon atoms, 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 compounds of the formula (I) are pharmacologically active. In particular, they inhibit the microsomal monooxigenase enzyme system of the liver. Pharmaceutical compositions containing them as active ingredient are also within the scope of the invention.

Abstract: The invention relates to optically active or racemic eburnane-oxime ethers of the formulae (Ia) and/or ##STR1## wherein R represents an alkyl group having 1 or 2 carbon atoms,R.sup.2 represents an alkyl group having 1 to 6 carbon atoms,and the configuration of the hydrogen in the 3-position and the R.sup.2 group is .alpha.,.alpha. and/or .beta.,.beta. or .alpha.,.beta. and/or .beta.,.alpha. and acid addition salts thereof.The new compounds show valuable pharmaceutical activities, thus are potent CNS-tranquillants, smooth muscle relaxants, sedatives and hypnotic agents, and can therefore be employed as active ingredients of pharmaceutical compositions, which are also within the scope of the present invention.

Abstract: The invention relates to new heterocyclic compounds containing a protected C-acetyl group. More particularly, the invention concerns new compounds of the Formula (V) ##STR1## wherein R is a group suitable for the protection of amides;Z is alkyl; andY.sup.1 and Y.sup.2 together form a group suitable for temporary protection of a keto group. The new compounds are valuable intermediates in the synthesis of thienamycin.

Abstract: Process for the extraction of solids from liquids containing solids granulated by heat effect and/or solids the moisture content of which is reducible by heat effect, especially from colloidal solutions with protein content, suspensions and slurries for reducing the fat content of the solid material, in the course of this process grains are formed in the liquid with heat effect, or the moisture content of the grains is reduced, then they are removed from the liquids and dried. The equipment for implementation of the process is also subject of the invention. The process is characterized by heating the liquid to 50.degree.-125.degree. C. temperature with heat transfer ("instant heating ") for a short period, maximum for 2 minutes, then the heated material is kept at 50.degree.-125.degree. C. temperature for at least 2, preferably for 5-15 minutes. This is followed by separation of the grains from the liquid phase with filtration in a space containing vapor of 50.degree.-125.degree. C.

Abstract: The invention relates to a new crystal modification of N-methyl-N'-{2-[(5-methylimidazol-4-yl)-methylthio]-ethyl}-N"-cyanoguanidi ne (cimetidine), a histamine H-2 receptor antagonist having the Formula (I) ##STR1## as well as to a process for preparing same. In the description, this new modification is named N-methyl-N'-{2-[(5-methylimidazol-4-yl)-methylthio]-ethyl}-N"-cyanoguanidi ne Z (cimetidine Z).

Abstract: The invention relates to new, pharmaceutically active copolymers with heparin-like activity, pharmaceutically acceptable salts thereof and a process for their preparation.

Abstract: Microbiological conversions of cyclodextrins are intensified by adding to the reaction mixture 0.2 to 3 moles of .alpha.-, .beta.- or .gamma.-cyclodextrin or an optical mixture thereof pro mole of the steroid substrate, before, at the beginning or during the conversion. The cyclodextrin if desired, can be removed after the reaction. In this way the reaction velocity can be increased, the reaction time is reduced, the substrate concentration in the solution, i.e. its solubility is increased or the so called product inhibition may be avoided. In certain cases of more alternatives the desired reaction can be catalyzed and in this manner the selectivity is increased.

Abstract: A heparin-enriched material capable of long-term storage and particularly adapted for use as a raw material in processes for the extraction of heparin is produced by storing the animal organ material for a period of 0.5 to 15 hours (preferably 4 to 6 hours) at a temperature of 10.degree. to 50.degree. C. (preferably 30.degree. to 50.degree. C.), then injecting steam to effect a heat treatment at a temperature between 75.degree. and 100.degree. C. The heat treatment precipitates heparin-containing aggregate which is filtered from the aqueous phase and dried to a dry substance content of 90 to 95%.

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 benzhydrylpiperazine derivatives of the formula (I) ##STR1## wherein n is 2 or 3, and acid addition salts thereof. 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. More particularly, they inhibit the microsomal monooxigenase enzyme system of liver. Pharmaceutical compositions containing them as active ingredient 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: The invention relates to a novel process for the preparations of pregnane derivatives of formula I, ##STR1## wherein R.sup.1 stands for a methyl or an ethyl group,R.sup.2 represents a hydrogen atom or a methyl group, andX is a hydrogen atom or a formyl or acetyl group, and the bond indicated by a dotted and a continuous line stands for a single or a double bond beween the two neighboring carbon atoms.According to the invention a trifluoroacetate ester of formula II, ##STR2## wherein R.sup.1 and R.sup.2 are as defined above, is reacted with formic acid or acetic acid in the presence of a catalytic amount of a mercury salt in a dipolar proton-free or basic solvent. The formyl or acetyl group being in the place of X can be split off in a way known per se.The process provides a novel advantageous method for building up the pregnane side chain characteristic of corticoids.

Abstract: The invention relates to racemic or optically active E-homo-eburnane derivatives of the formula /I/, ##STR1## wherein R.sup.1 and R.sup.2 independently represent an alkyl group having 1 to 6 carbon atoms,and acid addition salts thereof.The new compounds are pharmaceutically active, for example their certain representatives, in particular from the cis-series, show antidepressive activity, while others, especially the compounds of the trans-series, are potent anthypoxial agents. The compounds of the formula /I/ and pharmaceutically acceptable acid addition salts thereof can therefore be employed as active ingredients of pharmaceutical compositions.

Abstract: The invention relates to t-butyloxy-carbonyl-D-phenylalanyl-L-prolyl-L-arginine aldehyde hemisulfate and D-phenylalanyl-L-prolyl-L-arginine aldehyde sulfate, which is highly stable in aqueous solution, and to a process for preparing D-phenylalanyl-L-prolyl-L-arginine aldehyde sulfate from D-phenylalanyl-L-prolyl-L-arginine aldehyde hemisulfate or N.sup.G -carboxy derivative containing an acid-sensitive protecting group at its amino terminal, wherein the acid sensitive amino terminal protecting group or optionally the N.sup.G -carboxy group is removed with 1 to 12 N sulfuric acid, applied in 1 to 12 equivalent amounts and the resulting free tripeptide aldehyde sulfate isolated. The D-phenylalanyl-L-prolyl-L-arginine aldehyde sulfate of the invention possesses valuable anti-coagulant activity.

Abstract: A process is disclosed for the preparation of racemic cis or trans apovincaminic acid esters of the formula (I) ##STR1## and the corresponding optically active derivatives of the formulae (Ia) ##STR2## wherein R.sup.1 and R.sup.2 are identical or different alkyl groups having 1 to 6 carbon atoms. Apovincaminic acid alkyl esters are well-known vasodilating compounds.

Abstract: Analgesic compounds having the formula (I):Tyr-A-Gly-Phe-B-X-YwhereinA is a D-aminoacid group having a lower alkyl group or a lower thioalkyl group as a side chain,B is an aminoacid or a cyclic iminoacid group, either of which has a lower alkyl group as a side chain,X is an oxygen atom or an NH group, andY is a hydrogen atom or a lower alkyl group,or a pharmaceutically effective amide, ester or salt thereof.

Abstract: The invention relates to a new process for the preparation of apovincaminic acid esters. More particularly, the invention concerns a process for preparing racemic and optionally active vincaminic acid esters of the formula (I) ##STR1## in which R.sup.1 and R.sup.2 independently stand for alkyl having from one to 6 carbon atoms, and 14-epimers thereof.According to the invention an octahydroindolo[2,3-a]quinolizine-oxime ester of the formula (II) ##STR2## in which R.sup.1 and R.sup.2 have the same meaning as defined above, is reacted with an aqueous solution of sulfurous acid or a salt thereof at a temperature of 80.degree. to 110.degree. C. and the 14-epimeric mixture obtained is epimerized or separated in a known manner and if desired, the racemic vincaminic acid esters are resolved.