Abstract: The invention relates to N-acyl-N-heterocyclylalkylamino acids of the formula ##STR1## R.sub.1 is C.sub.1 -C.sub.7 alkyl that is unsubstituted or substituted by halogen or by hydroxy, or is C.sub.2 -C.sub.7 -alkenyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.3 -C.sub.7 cycloalkoxy, C.sub.1 -C.sub.7 alkoxy or C.sub.3 -C.sub.7 cycloalkyl-C.sub.1 -C.sub.7 alkoxy;R.sub.2 is 1H-tetrazol-5-yl, carboxy, C.sub.1 -C.sub.7 alkoxycarbonyl, SO.sub.3 H, PO.sub.2 H.sub.2, PO.sub.3 H.sub.2 or halo-C.sub.1 -C.sub.7 alkanesulfonylamino;R.sub.3 is 1H-tetrazol-5-yl, hydroxymethyl, C.sub.1 -C.sub.7 alkoxymethyl, formyl, carboxy, C.sub.1 -C.sub.7 alkoxycarbonyl, C.sub.1 -C.sub.7 alkoxy-C.sub.1 -C.sub.7 alkoxycarbonyl, phenyl-C.sub.1 -C.sub.4 alkoxycarbonyl or carbamoyl, the amino group of which is unsubstituted or mono-substituted by C.sub.1 -C.sub.7 alkyl, C.sub.3 -C.sub.7 alkenyl or by phenyl-C.sub.1 -C.sub.7 alkyl or di-substituted by C.sub.1 -C.sub.7 alkyl, C.sub.3 -C.sub.7 alkenyl or by phenyl-C.sub.1 -C.sub.

Abstract: Disclosed are compounds of formula ##STR1## wherein R is OR' and R' is aryl-lower alkyl, biaryl-lower alkyl, lower alkyl or cycloalkyl-lower alkyl; or R is arylsulfonylamido;n is 1, 2 or 3;m is 1, 2 or 3;Y is vinylene, ethylene or methyleneoxy; a stereoisomer or optical isomer thereof; and their pharmaceutically acceptable esters or salts; which are useful as thromboxane synthetase inhibitors and thromboxane receptor antagonists.

Abstract: The invention relates to pharmaceutical compositions for peroral administration comprising (a) pharmaceutically useful methanediphosphonic acid derivatives, e.g. those of formula I ##STR1## wherein R.sub.1 and R.sub.2 are as defined in the specification, or pharmaceutically acceptable salts thereof, (b) specific macrocyclic polyethers and optionally (c) pharmaceutically acceptable adjuvants. The pharmaceutical compositions are prepared in a manner known per se. A method of treating hypercalcemia and osteolytic bone metastases with these compositions is also disclosed herein.

Abstract: Substituted 2-aminoalk-3-enoic acid derivative of formula I ##STR1## wherein R.sub.1 is an aliphatic hydrocarbon radical that is substituted by optionally acylated or aliphatically or araliphatically etherified hydroxy, by halogen, by optionally acylated and/or aliphatically substituted amino or by an aza-, diaza-, azoxa- or oxa-cycloaliphatic radical, or is an oxacycloaliphatic hydrocarbon radical bonded via a carbon atom, or is an optionally aliphatically N-substituted or N-acylated azacycloaliphatic hydrocarbon radical, and R.sub.2 is free or esterified carboxy, and their salts exhibit NMDA-antagonistic properties and are useful as active ingredients of anticonvulsive medicaments.

Abstract: Amino-substituted piperazine derivatives of formula I ##STR1## wherein R.sub.1 -R.sub.6, X and Y are as defined in the description, and salts thereof, have properties inhibiting the biosynthesis of interleukin-1 (IL-1) as well as analgesic properties and can therefore be used as active ingredients in medicaments. They are prepared in a manner known per se.

Abstract: An oral sustained release composition for slightly soluble pharmaceutically active agents comprising a core, a wall around said core, and a bore through said wall connecting said core and the environment outside of said wall; wherein said core comprises a slightly soluble active agent, optionally a crystal habit modifier, at least two osmotic driving agents, at least two different (or two different grades of) hydroxyalkyl celluloses, and optionally lubricants, wetting agents, and carriers; said wall being substantially impermeable to said core components and permeable to water and gastro-intestinal fluids. The composition is most especially adapted for administering carbamazepine.

Abstract: The invention relates to a dry formulation, in particular a dry formulation obtainable by lyophilisation, which is suitable for the preparation of a stable, aqueous suspension for the parenteral administration of a diclofenac salt. The dry formulation contains a pharmaceutically acceptable and micronised salt of diclofenac and optional pharmaceutically acceptable adjuvants.

Abstract: N-substituted aminomethanediphosphonic acids of the formula I, ##STR1## wherein R.sub.1, X, alk.sub.1, R.sub.2 and n are as defined in the description, and salts thereof, have valuable pharmaceutical properties and are effective e.g. in the treatment of conditions which can be associated with disorders of the calcium metabolism. They are manufactured in a manner known per se.

Abstract: The invention relates to a novel process for the manufacture of (3R,1'R)-4-acyloxy-3-(1'-hydroxyethyl)-2-azetidinones of formula ##STR1## in which R.sup.1 represents lower alkyl or aryl, by enantioselective reduction of the carbonyl group in a suitable .alpha.-acylaminomethyl-acetoacetic acid ester, cyclisation of the resulting .alpha.-acylaminomethyl-.beta.-hydroxybutyric acid ester to a 5,6-dihydro-1,3,4H-oxazine with inversion of the carbon atom carrying the hydroxy group, equilibration to form the preferred trans-substituted dihydrooxazine, recleaving to form the configuratively uniform .alpha.-aminomethyl-.beta.-hydroxybutyric acid, ring-closure to form the .beta.-lactam and oxidative acylation at C(4) of the .beta.-lactam. Compounds of formula I can be used as starting materials for the manufacture of .beta.-lactam antibiotics. The invention relates also to novel intermediates.

Abstract: The invention relates to pharmaceutical compositions in the form of parenterally, especially intravenously, administrable liposome dispersions or dry preparations, especially lyophilisates, that can be used therefor, comprising the zinc-phthalocyanine complex and synthetic, substantially pure phospholipids.

Abstract: Staurosporin derivatives of the formula I are described, ##STR1## in which R.sub.1 is hydrogen, hydroxyl, lower alkoxy or oxo and R.sub.2 is a radical of the formula II ##STR2## in which the configuration of the sugar moiety is derived from D-glucose, D-galactose or D-mannose, and R.sub.3 -R.sub.7 are as defined below.These compounds have a pronounced and selective inhibitory action on the enzyme proteinkinase C and have, inter alia, an antitumor action.

Abstract: An inhaler for introducing a metered amount of solids, for example pharmaceutically active powders, into a stream of air drawn in by a user comprises a storage chamber into which a metering rod extends. The metering rod is provided with a metering recess which fixes the amount of solids to be mixed with the air stream. The storage chamber and the metering rod are movable relative to each other in such a manner that in a first relative position of the metering rod and the storage chamber the metering recess of the metering rod is located in the storage chamber, where it is filled with solids, and in a second relative position it is located in the air channel, where the solids are mixed with the air stream. The axial relative movement can be brought about by the rotation of two housing parts over sloping surfaces.

Abstract: The invention concerns the use of IgE-binding factor (IgE-bf) for the stimulation of the maturation, i.e. of the differentiation and proliferation, of myeloid precursor cells in context with interleukin-1 (IL-1). The invention further concerns a a pharmaceutical preparation comprising IgE-bf either alone or in combination with IL-1 for the treatment or prevention of diseases by stimulating the maturation of myeloid precursor cells.

Abstract: Compounds of formula I ##STR1## wherein Z is thiazolyl or isothiazolyl, and X, R, R.sub.0, R.sub.1, R.sub.2 and R.sub.3 are as defined in the description, have valuable pharmaceutical properties and are effective especially against tumors.

Abstract: The invention concerns a pharmaceutical preparation comprising the 25K IgE-binding factor (25K IgE-bf) and interleukin-1 (IL-1), and the use of said pharmaceutical preparation for the stimulation of the maturation of prothymocytes, e.g. for the treatment of T cell immunodeficiencies and prothymocyte leukemias.

Abstract: Compounds having GABA.sub.B -antagonistic properties, for example those of formula I ##STR1## wherein one of the radicals R.sub.1, R.sub.2 and R.sub.3 is hydrogen or an aliphatic, cycloaliphatic, araliphatic or aromatic radical, another is hydrogen or, in the case of R.sub.1 or R.sub.2, hydroxy or, in the case of R.sub.1, halogen or, in the case of R.sub.2 together with R.sub.2 ', oxo, and the remaining radical is hydrogen, R.sub.1 ' is hydrogen or halogen, R.sub.2 ' is hydrogen, hydroxy or, together with R.sub.2, is oxo, R.sub.4 and R.sub.5 are hydrogen or R.sub.4 is an araliphatic or heteroarylaliphatic radical and R.sub.5 is hydrogen or an aliphatic radical, and R is an aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, araliphatic, heteroarylaliphatic or aromatic radical having at least 2 carbon atoms or, when R.sub.1 is hydrogen or hydroxy, R.sub.2 is an aromatic radical and R.sub.1 ', R.sub.2 ' and R.sub.

Abstract: The invention relates to azo compounds, especially to compounds of formula ##STR1## wherein R.sub.1 is lower alkyl, R.sub.2 is lower alkyl, R.sub.3 is hydrogen, carboxy or sulfo, R.sub.4 is carboxy or sulfo, G is an unsubstituted or substituted 1,4-phenylene group or an unsubstituted or substituted 1,4-naphthylene group, and wherein either R.sub.5 and R.sub.6 together are an additional bond and L is an oxygen or sulfur atom or wherein R.sub.5 is hydrogen, R.sub.6 is halomethyl and L is an oxygen atom, and salts thereof, to the use of compounds I and their salts, to a process for the preparation of compounds I and their salts, to starting materials used in that preparation process, and salts thereof, to a process for the preparation of those starting materials and their salts, to a device in which the compounds I and their salts are used, and to a process in which that device is used.

Abstract: A light diffuser for simultaneous photodynamic therapy and hyperthermic treatment in the oesophagus has an arrangement (14 to 18) which disperses radially the light (10) fed in by way of an optical fiber (6) and has a tube (12) filled with silicone to which are added concentrations, modulated in the axial direction, of quartz grains having a diameter of approximately 40 .mu.m which bring about a refraction having little dependence on the wavelength.