Abstract: Metal complexes of the general formula I[R.sup.1 (CH.sub.2).sub.m C(O)CR.sup.3 C(O)R.sup.2 ].sub.2 M(OR.sup.4).sub.2-n X.sub.n (I)wherein M denotes titanium, zirconium or hafnium, R.sup.1 denotes hydrogen, C.sub.1 -C.sub.8 -alkyl or phenyl, which can be monosubstituted or polysubstituted by fluorine, chlorine, bromine, nitro, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy or trifluoromethyl, R.sup.2 denotes C.sub.1 -C.sub.8 -alkyl, or phenyl, which can be monosubstituted or polysubstituted by fluorine, chlorine, bromine, nitro, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy or trifluoromethyl, R.sup.3 denotes hydrogen or phenyl, R.sup.4 denotes C.sub.1 -C.sub.18 -alkyl, which can be substituted by hydroxyl, C.sub.1 -C.sub.3 -alkylamino or alkali metal sulfonato groups, or denotes C.sub.5 -C.sub.8 -cycloalkyl, which can be substituted by C.sub.1 -C.sub.
Abstract: Tricyclic ethers of the general formula I ##STR1## wherein R represents a bond and R1 represents a 1-2C-alkylene radical which is completely or partly substituted by fluorine, or a chlorotrifluoroethylene radical, or R and R1 each represent a difluoromethylene radical, R2 represents hydrogen or a 1-3C-alkyl radical, R3 represents hydrogen or a 1-3C-alkyl or 1-3C-alkoxy radical, R4 represents hydrogen or a 1-3C-alkyl radical and n represents the number 0 or 1, and their salts are new compounds with a marked protective effect on the stomach.
Abstract: Fluoroalkoxy compounds of the general formula I ##STR1## wherein R1 represents a 1-3C-alkyl radical which is completely or predominantly substituted by fluorine, or a chlorodifluoromethyl radical, R1' represents hydrogen, halogen, trifluoromethyl, a 1-3C-alkyl radical, or a 1-3C-alkoxy radical which is optionally completely or predominantly substituted by fluorine, R2 represents hydrogen or a 1-3C-alkyl radical, R3 represents hydrogen or a 1-3C-alkyl or 1-3C-alkoxy radical, R4 represents hydrogen or a 1-3C-alkyl radical and n represents the number 0 or 1, and their salts are new compounds with a marked protective effect on the stomach.
Abstract: The potential of dyphylline as a bronchodilator is severely limited by its short half-life. By administering an anionic blocker prior to or concurrently with dyphylline, this shortcoming is overcome, and effective plasma levels can be maintained for as long as eight hours.
Abstract: Substituted thienobenzodiazepinones of the general formula I ##STR1## [wherein R.sup.1 denotes a hydrogen atom (--H) or an alkyl radical with 1 to 4 carbon atoms; R.sup.2 represents a halogen atom (halo) or has one of the meanings of R.sup.1 ; R.sup.3 denotes a halogen atom (halo) or the group --N(R.sup.4)R.sup.5 ; R.sup.4 denotes an alkyl radical with 1 to 4 carbon atoms or an alkenyl radical with 3 to 5 carbon atoms; R.sup.5 has one of the meanings of R.sup.4 or represents the group --(CH.sub.2).sub.m --N(R.sup.6)R.sup.7 ; or R.sup.4 and R.sup.5, together with the nitrogen atom to which both are bonded, denote a morpholino group, a pyrrolidino group, a piperidino group, a hexahydroazepin-1-yl group, a piperazin-1-yl group (which is optionally substituted in the 4-position by a methyl, ethyl or benzyl group), a 2,4-dimethylpiperazin-1-yl group, or a hexahydro-1H-1,4-diazepin-1-yl group (which is substituted in the 4-position by a methyl or ethyl group); R.sup.
Abstract: Phenalkoxyalky- and phenoxyalkyl-substituted oxiranecarboxylic acids of the formula ##STR1## wherein R.sup.1 denotes a hydrogen atom (--H), a halogen atom, a lower alkyl group, a lower alkoxy group, a nitro group or a trifluoromethyl group,R.sup.2 has one of the meanings of R.sup.1,R.sup.3 denotes a hydrogen atom (--H) or a lower alkyl group,Y denotes --O--(CH.sub.2).sub.m --,m denotes O or an integer from 1 to 4, andn denotes an integer from 2 to 8, with the proviso that the sum of m and n is an integer from 2 to 8,and the salts of the acids are new compounds. They display a hypoglycaemic action in warm-blooded animals. Processes for the preparation of the new compounds and of the intermediate products required for their preparation are described.
Abstract: 4-Phenoxypiperidines of the general formula I ##STR1## wherein R.sup.1 denotes a hydrogen atom, an alkyl group with 1 to 5 carbon atoms, an alkenyl group with 3 to 5 carbon atoms, a cycloalkylmethyl group with 3 to 7 carbon atoms in the cycloalkyl part or a phenylalkyl group with 1 to 3 carbon atoms in the alkyl part,R.sup.2 denotes a hydrogen atom, a nitro group, an amino group or an acylamino group andR.sup.3 denotes a phenyl group or a benzyl group,and their N-oxides and their acid-addition salts are new compounds. They have an antiptotic and analgesic action and are suitable for the treatment of depressions and painful conditions. Processes for the preparation of the new compounds are provided.
Abstract: Pyrazol-4-acetic acid compounds, such as substituted pyrazol-4-acetic acid, its esters, amides, nitriles and their pharmaceutically acceptable salts and method for the preparation of these compounds are disclosed. The novel compounds are useful analgesics, anti-inflammatory, and antipyretics.
Abstract: The invention relates to .omega.-[2-(N-lower alkyl-benzamido)-phenyl]-alkanoic acids, their use and preparation, and medicaments containing them.
Abstract: 1-(Lower)alkyl-4-(substituted)aminoalkylcarbonyl-1,4,9,10-tetrahydropyrazol o[4,3-b][1,5]benzodiazepin-10-ones are useful, e.g., to protect warm blooded animals against the formation of gastric ulcers. They are active ingredients in otherwise conventional medicament compositions administered enterally or parenterally in standard dosage forms. Their synthesis, their novel intermediates and their acid-addition salts are described.
Abstract: 11-Acyl-2-phenyl- and 11-acyl-5,6-dihydropyrimido[4,5-b][1,5]benzodiazepin-5-ones, their acid-addition salts and their N-oxides provide protective action for the stomach and intestines of warm-blooded animals and inhibit the formation of gastric and intestinal ulcers.
Abstract: By injecting a host animal with a member of a particular group of antigens [a theophylline-(7)-alkanecarboxylic acid covalently bonded to an immunogenic carrier (IGC) via the carboxyl group], antibodies, advantageously employed in determining small amounts of theophylline in biological liquids by immunoassay methods, are obtained.
Abstract: Substituted pyridazines of formula I ##STR1## wherein A denotes a lower alkylene group,R.sup.1 denotes an optionally-substituted or derivatized amino group,R.sup.2 denotes an alkyl group, an alkoxy group, an alkylmercapto group, an optionally-substituted aryl group, a phenalkoxy group or an optionally-substituted amino group andX denotes an oxygen atom or a sulfur atom, and their acid-addition salts with inorganic and organic acids are new compounds. They have an anti-hypertensive effect and are suitable for the treatment of hypertension. Processes for the preparation of the new, pharmacologically-effective compounds, new intermediate products required for their preparation, therapeutic use of the compounds, compositions for such use and unit dosage forms of the compositions are disclosed.
Abstract: Phenylaminothiophenacetic acids of formula I ##STR1## wherein R.sup.1 denotes a hydrogen atom, a chlorine atom, a bromine atom or a methyl group,R.sup.2 denotes a --CH.sub.2 --COOH group or a --CH.sub.2 --COOR.sup.6 group,R.sup.3 denotes a hydrogen atom, a halogen atom, an alkyl group, an alkoxy group or a trifluoromethyl group,R.sup.4 has one of the meanings of R.sup.3,R.sup.5 denotes a hydrogen atom, a halogen atom or an alkyl group,R.sup.6 denotes an alkyl group (with from 1 to 5 carbon atoms), which is optionally substituted by hydroxyl, hydroxyalkoxy or alkanoyloxy groups, or a benzyl group andn denotes 1 or 2,and salts of the acids have outstanding antiphlogistic, analgesic and antipyretic activities.
Abstract: N-substituted .omega.-aminoalkanoyl-.omega.-aminoalkanoic acids and their pharmacologically-acceptable salts (with a base) are useful, e.g., in pharmaceutical-composition form for the treatment or prophylaxis of diseases which are based on inadequate performance of the pancreas, the bile and/or the liver. The compounds are prepared, e.g., by reacting an N-(mono- or di-substituted) .omega.-amino-alkanoic acid with an N-(unsubstituted or monosubstituted) .omega.-aminoalkanoic acid.
Abstract: Compounds of the formula ##STR1## wherein R is (a) optionally-substituted and optionally-hydrogenated biphenylyl, (b) optionally-substituted and optionally-hydrogenated bicyclic aryl having from 8 to 12 ring carbon atoms or (c) a radical of the formula ##STR2## R.sup.1 is aliphatic hydrocarbyl, alicyclic hydrocarbyl or optionally-substituted phenyl;R.sup.2 is --H or lower aliphatic hydrocarbyl;R.sup.3 is --H, lower alkyl, cycloalkyl, optionally-substituted phenyl or, with R.sup.4, alkylene;R.sup.4 is lower alkyl, cycloalkyl, optionally-substituted phenyl, optionally-(nuclearly)-substituted phenalkyl or, with R.sup.3, alkylene;or R.sup.2,R.sup.3 and R.sup.4, together with the carbon to which each is bound, are adamantyl; andn is 3, 4 or 5;and salts thereof with a base are pharmacologically active. Esters thereof are valuable intermediates for the preparation of the pharmacologically-active compounds. Physiologically-acceptable embodiments are administered, e.g.
Abstract: Pyrazol-1-ylphenylacetic acids of the formula ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are the same or different and denote a hydrogen atom or a halogen atom,R.sup.4 denotes a hydrogen atom or an alkyl group,A B denotes a carbon-carbon single or double bond, and their salts are pharmacologically active and are useful as medicaments. Medicament compositions are produced therefrom. Their functional carboxylic acid derivatives and other new intermediates are used in their preparation.
Abstract: Title compounds and their acid-addition salts are physiologically acceptable or are readily converted to physiologically-acceptable counterparts by established procedures. They are pharmacologically active on the central nervous system (CNS) and are thus useful, when administered to warm-blooded animals, to induce central stimulation, to increase vigilance and to promote normal and pathologically-inhibited drive. They are also useful as analgesics and as blood-pressure-reducing agents for warm-blooded animals. These compounds are prepared, e.g., by reducing an appropriate 2-benzylazacycloheptane and are compounded into normal dosage-form medicament compositions.
Abstract: Pharmaceutically-acceptable compositions containing, as an active ingredient, at least one N-acylanilinobutyric acid have uses unrelated to the choleretic activity suggested in U.S. Pat. No. 3,780,095. Moreover, the further uses generally involve administration of smaller doses than would be required to obtain a choleretic effect.The new uses include: (a) increasing the gastrointestinal enzyme secretion and (b) tonicizing the cardiovascular system. The increase of the gastrointestinal enzyme secretion is applied in the treatment of different diseases, such as treatment of sprue, treatment of indigestion, treatment of acute and chronic pancreatitis, therapy for degenerated intestine mucous membrane, treatment of stomach spasms, treatment of stomach ulcers, treatment of diseases where the application of an antigastrin is indicated. The tonicising of the cardiovascular system is applied in, e.g.
Abstract: Selected substituted 1-phenyl-2-pyrrolidin-2-yl-ethanols and their pharmacologically-acceptable acid-addition salts are useful as analgesics in human and veterinary medicine. Such compounds are prepared by reducing corresponding substituted 1-phenyl-2-pyrrolidin-2-yl ethanones and are formulated into medicinal compositions suitable for administration.