Abstract: The oxazolidines of the formula ##STR1## wherein n signifies the number 1 or 2,T signifies lower carbalkoxy,X signifies phenoxymethyl optionally mono-fluorinated or mono-chlorinated in the ortho-position or phenyl optionally monosubstituted by fluorine, chlorine, trifluoromethyl or lower-alkoxy,Y signifies hydrogen or methyl, andZ signifies a phenyl or thienyl residue substituted in a defined manner,and the physiologically compatible salts thereof have catabolic activity and can be used for the treatment of obesity and diabetes mellitus or for the treatment of conditions which are associated with an increased protein breakdown, or as feed additives for fattening animals. They are manufactured starting from corresponding primary amines.

Abstract: Dihydropyridine derivatives of the formula ##STR1## wherein the symbols A, R and R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 are as described herein.Compounds of formula I have a pronounced calcium-antagonistic activity and can accordingly be used as medicaments, especially for the control or prevention of angina pectoris, ischemia, high blood pressure and/or migraine.

Abstract: Suppositories containing as the active substance a therapeutically effective amount of ceftriaxone, a pharmaceutically compatible salt thereof or a hydrate of one of these compounds, a stabilizer consisting of a mono-, di- or triglyceride of a C.sub.12 -C.sub.18 -fatty acid or of a mixture of such glycerides, a potentiator consisting of an aliphatic C.sub.2 -C.sub.18 -fatty acid, a mono-, di- or triglyceride of a C.sub.2 -C.sub.12 -fatty acid, a partial ester or complete ester of propylene glycol, polyethylene glycol or a carbohydrate with a C.sub.2 -C.sub.12 -fatty acid, a pharmaceutically compatible ester or ether thereof or of a mixutre of the said potentiators and, if desired, customary therapeutically inert adjuvants for suppositories, and their manufacture are described. These have valuable antimicrobial properties.

Abstract: The present disclosure relates to the use of thromboxane synthase inhibitors as antiobesity agents and insulin lowering agents. Such compounds fall into a variety of classes among which are 1-substituted imidazoles, 4-substituted imidazoles, 3-substituted pyridines, 3-substituted indoles, 4-substituted pyrimidines, 5-substituted tetrazoles, pyrazolidines, quinazolines, and substituted xanthene carboxylic acids.

Abstract: The invention relates to a process for depositing I-125 on a substrate which comprises contacting a predetermined surface area of substrate with Xe-125 gas, whereby the Xe-125 decays to I-125 and the I-125 in turn deposits as a solid on the surface of the substrate, the contact being for a time sufficient to deposit at least about 1 microcurie of I-125. I-125 is thereby deposited in a relatively uniform amount over the surface area of the substrate. The substrate is then assayed to determine how much I-125 has been deposited. The substrate is then divided into pieces of measured surface area, each piece therefore containing a measured amount of deposited I-125, and each piece can then be used in the manufacture of an I-125 source.

Abstract: The invention relates to acridanone derivatives of the formula ##STR1## wherein the dotted line is an optional bond, R.sup.1 is hydrogen, halogen or nitro,R.sup.2 is hydrogen or lower alkyl,one of R.sup.3 and R.sup.4 is hydrogen or lower alkyl and the other together with R is an additional bond,A is lower alkylene,R.sup.5 is a 5-membered nitrogen-containing, optionally lower alkyl-substituted aromatic heterocycle, amino or the group ##STR2## the symbol is a 5- or 6-membered, optionally lower alkyl-substituted saturated heterocycle which can contain as a ring member oxygen or sulfur or the group >NH or >N(B).sub.n --A.sup.1 --R.sup.6, B is the group --CO--, --COO-- or --SO.sub.2 --, n is the number 0 or 1, A.sup.1 is lower alkylene, R.sup.6 is hydrogen, amino, lower alkylamino or di(lower alkyl)amino and R.sup.7 is hydrogen or lower alkyl, and pharmaceutically acceptable acid addition salts thereof, their preparation and pharmaceutical compositions based thereon.

Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, lower alkyl or acyl; R.sub.2 and R.sub.3 independently are lower alkyl, aralkyl or alkenyl or R.sub.2 and R.sub.3 together form a ring of 5 to 8 carbon atoms; R.sub.4 is phenyl, substituted phenyl, cyclohexyl, substituted cyclohexyl, cyclopentyl, substituted cyclopentyl, cycloheptyl, or substituted cycloheptyl; R.sub.5 is hydrogen or lower alkyl; R.sub.6 is hydrogen, lower alkyl or acyl; and pharmaceutically acceptable acid addition salts thereof are described. The compounds of formula I and pharmaceutically acceptable acid addition salts thereof are anti-emetic agents which lack central nervous system side effects.

Abstract: Compounds of the formula: ##STR1## wherein R.sub.1 is --alkylene'-13 NH.sub.2 or --alkylene'--A'; R.sub.2, R.sub.3 and R.sub.4 are independently hydrogen or methyl; A and A' are, independently, unsubstituted or lower alkyl or aryl substituted pyridinyl, imidazolyl, or pyrimidinyl; and when, an asymmetric carbon is present, enantiomers thereof, or racemic mixtures thereof; or pharmaceutically acceptable salts thereof, are described. These compounds are useful as antiarrhythmic agents.

Abstract: Mixtures of active substances and pharmaceutical compositions useful in malaria therapy comprising a quinolinemethanol derivative of the formula ##STR1## wherein R.sup.1 is hydrogen, fluorine, chlorine, bromine, methyl or trifluoromethyl, R.sup.2 is hydrogen, fluorine, chlorine, bromine, methyl or methoxy (at least one of R.sup.1 and R.sup.2 is other than hydrogen), and R.sup.3 is C.sub.1-6 -alkylamino-C.sub.1-3 -alkyl, di-C.sub.1-6 -alkylamino-C.sub.1-3 -alkyl, 2-piperidyl or 3-piperidyl, or a pharmaceutically acceptable acid addition salt thereof; a compound which acts as a p-aminobenzoic acid antagonist; and a compound which acts as a dihydrofolic acid reductase inhibitor, are described.

Abstract: Compounds of the general formula ##STR1## wherein two of the residues R.sup.1, R.sup.2 and R.sup.3 represent C.sub.10-30 -alkyl residues with at least 8 C-atoms in a straight chain, at least one of these residues being substituted by at least 2 C.sub.1-3 -alkyl residues and the sum of the C-atoms in the two residues being greater than 20; and the third residue is a residue --P(O)(O.sup.-)OR.sup.4 in which R.sup.4 represents a lower-alkyl or C.sub.5-7 -cycloalkyl residue which is substituted by a quaternary ammonium group or a C.sub.5-7 -cycloalkyl residue which contains a di-(lower-alkyl)-substituted nitrogen atom,are useful for the manufacture of colloidal solution systems. The compounds of formula I can be prepared starting from glycerol derivatives as described in more detail in the specification.

Abstract: 1-[2-(4,5,10,11-Tetrahydro-1H-dibenzo[a,d]cyclohepten-5-yl)ethyl]pyrrolidin e of the formula ##STR1## and its pharmaceutically acceptable acid addition salts, prepared through various intermediates, are described. The compounds have valuable histamine-H.sub.1 antagonistic properties and are suitable for the control or prevention of allergic reactions,such as, urticaria, hay fever, anaphylaxis and over-sensitivity to medicaments.

Abstract: The invention is concerned with a process for the preparation of 1 hydrogen or hydroxy cholesterol derivatives and intermediates therefor. The compounds of the present invention are useful as intermediates in the preparation of 24,25-dihydroxy and 1.alpha.,24,25-trihydroxycholecalciferol.

Abstract: Phenyl-quinolizidines of the general formula ##STR1## wherein X is hydrogen, fluorine, chlorine, lower-alkoxy, lower-alkyl or trifluoromethyl; Y is hydrogen, fluorine, chlorine, lower-alkoxy or lower-alkyl; and R.sup.1 acyl, acylamino or a group A of the formula ##STR2## wherein R.sup.2 is oxygen or sulfur; R.sup.3 is hydrogen or lower-alkyl; and one of R.sup.4 and R.sup.5 is hydrogen and the other is bromine, iodine, cyano, lower-alkoxycarbonyl or sulfamoyl,as racemates or enatiomers, as well as acid addition salts thereof, utilizing various intermediates, are described. The foregoing compounds are useful as neuroleptic, antiemetic and analgesic agents.

Abstract: Steroids of the formula ##STR1## wherein n represents the number 2, 3 or 4; R.sup.1 represents hydrogen, lower-alkyl or lower-alkylidene; R.sup.2, R.sup.3 and R.sup.4 represent hydrogen or lower-alkyl and the dotted C--C bonds in the 5(6)-, 7(8)-, 22(23)-, 24(28)- and 25(26)-position are optional, whereby the B-ring can contain only one double bond and the side-chain is either saturated or is mono-unsaturated or is di-unsaturated in the 22(23), 25(26)-position; and whereby R.sup.1 is lower-alkyl or lower-alkylidene when a 5(6)-double bond is present, n is 2 and R.sup.2, R.sup.3 and R.sup.4 are methyl,and pharmaceutically acceptable salts of these steroids have activity inhibiting the intestinal resorption of cholesterol. They can be manufactured from steroids which are otherwise substituted in the 3.beta.-position.

Abstract: Tetrahydronaphthalene derivatives of the formula ##STR1## wherein Y, m, n, R and R.sup.1 to R.sup.9 are as set forth herein, are described.These compounds have a pronounced calcium-antagonistic and anti-arrhythmic activity and can accordingly be used as medicaments, especially for the control or prevention of angina pectoris, ischaemia, arrhythmias and high blood pressure. The compounds of formula I can be prepared by the amination of a compound of the formula ##STR2## with a corresponding N-methyl-phenylalkylamine and optional subsequent O-acylation. Compounds of formula II and IV are also described and are within the scope of the invention.

Abstract: Compounds of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, and A are as described herein, are set forth.These compounds are useful as anti-allergic agents and agents for the treatment of cardiovascular diseases.

Abstract: 2,4-Diamino-5-benzylpyrimidines of the formula ##STR1## wherein R.sup.1, R.sup.2, A, Z and n are as hereinafter set forth, are described. The 2,4-diamino-5-benzylpyrimidines of the invention have useful antibacterial activity. More particularly, they inhibit bacterial dihydrofolate reductase and potentiate the antibacterial activity of sulfonamides.

Abstract: Novel compounds of the formula ##STR1## wherein B represents a methylene, ethylene or vinylene group, R.sup.1 represents a hydrogen atom or an alkyl, aralkyl, amino-alkyl, mono-alkylamino-alkyl, dialkylamino-alkyl, acylamino-alkyl, phthalimido-alkyl, alkoxycarbonylamino-alkyl, aryloxycarbonylamino-alkyl, aralkoxycarbonylamino-alkyl, alkylaminocarbonylamino-alkyl, arylaminocarbonylamino-alkyl, aralkylaminocarbonylamino-alkyl, alkylsulphonylamino-alkyl or arylsulphonylamino-alkyl group, R.sup.2 represents a carboxyl, alkoxycarbonyl or aralkoxycarbonyl group or a group of the formula ##STR2## R.sup.3 represents a carboxyl, alkoxycarbonyl or aralkoxycarbonyl group, R.sup.4 and R.sup.5 each represent a hydrogen atom or R.sup.4 and R.sup.5 together represent an oxo group, R.sup.6 and R.sup.7 each represent a hydrogen atom or an alkyl or aralkyl group or R.sup.6 and R.sup.

Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is phenyl substituted with 1 to 3 lower alkoxy groups or 1 to 3 halogens; R.sub.2 is hydroxy, lower alkoxy, lower alkanoyloxy, lower cycloalkylcarbonyloxy; ##STR2## R.sub.3 and R.sub.4 are independently lower alkyl, phenyl lower alkyl or together form a piperidine or pyrrolidine ring; n is 2 to 4; m is 1 to 2; or pharmaceutically acceptable acid addition salts thereof are described. The compounds of formula I have activity as calcium channel blockers and accordingly, are useful as agents for lowering blood pressure, and as agents for treating ischemia.

Abstract: Aziridine and phenethanolamine derivatives of formulae I and II-1 ##STR1## wherein R.sup.1 and R.sup.2 are hydrogen or lower-alkyl; Z.sup.1 is phenyl or a phenyl group substituted in a defined manner; Z.sup.2 and Z.sup.21 are phenyl or thienyl substituted in a defined manner; and, n is an integer from 1-4. The disclosed compounds have catabolic activity and can be used for the treatment of obesity and/or of sugar illnesses. The compounds of formula I are obtained by dehydrating .beta.-aminoalcohols (e.g. those of formula II-1) which, in turn, can be prepared by adding amines to epoxides or by reducing corresponding iminoketones, iminoalcohols a-keto-.beta.-hydroxyamines or .beta.-ketoamines.