Abstract: Compounds of the formula ##STR1## in which R.sub.1 is hydrogen or lower alkyl, R.sub.2 is hydrogen or a hydroxyl protective group R.sub.2 ' and R.sub.3 is substituted or unsubstituted phenyl or lower alkyl can be prepared in a three-stage process from readily accessible .beta.-lactam starting materials.

Abstract: The invention relates to a novel process for the manufacture of 4-acetoxy-3-hydroxyethyl-azetidinone of the formula ##STR1## especially 4(R)-acetoxy-3(R)-(1'(R)-hydroxyethyl)-2-azetidinone, from enantiomerically pure compounds of the formula ##STR2## in which R.sup.1 represents lower alkyl and Z.sup.1 represents amino, arylmethylamino, acylamino or azido, by reduction of the C.dbd.C double bond and optionally of the arylmethylamino or azido group with hydrogen, epimerization, opening of the lactone ring, cyclisation to the .beta.-lactam, optionally after hydrolysis of the acylamino group, and oxidative decarboxylation of the original lactone carboxy group in the presence of an acetate-yielding agent. Compounds of the formula I can be used as starting materials for the manufacture of .beta.-lactam antibiotics. The invention also relates to novel intermediates and starting materials.

Abstract: 1-Acylpiperidine compound of the formula I ##STR1## in which R.sub.1 is an optionally substituted aralkyl, aryloxyalkyl, heteroaralkyl, aroyl, heteroaroyl, cycloalkylcarbonyl, aralkanoyl, heteroarylalkanoyl, aralkoxycarbonyl or arylcarbamoyl radical or the acyl radical of an .alpha.-amino acid which is optionally N-substituted by lower alkanoyl or carbamoyl-lower-alkanoyl, R.sub.2 is cycloalkyl or an optionally substituted aryl or heteroaryl radical, R.sub.3 is hydrogen, alkyl, carbamoyl or an alkanoyl or alkenoyl radical which is optionally substituted by carboxyl or esterified or amidated carboxyl, R.sub.4 is an optionally substituted aryl or optionally partially hydrogenated heteroaryl radical, X.sub.1 is methylene, ethylene, a direct linkage, an optionally ketalised carbonyl group or an optionally etherified hydroxymethylene group, X.sub.2 is alkylene, carbonyl or a direct linkage, and X.sub.

Abstract: Compounds of the formula ##STR1## wherein carbon atoms 1 and 2 are linked by a single bond or a double bond, R.sub.1 is hydrogen, methyl or ethyl, and A is a group of the formula --N(--R.sub.2)--X-- wherein R.sub.2 is hydrogen or C.sub.1 -C.sub.4 alkyl and X is C.sub.1 -C.sub.12 alkylene or C.sub.3 -C.sub.6 cycloalkylidene; a group of the formula --N(--R.sub.2)--Y--Phe-- wherein R.sub.2 is as defined above, Y is a direct bond or C.sub.1 -C.sub.6 -alkylene and Phe is an unsubstituted or substituted phenylene radical; a group of the formula --O--X-- wherein X is as defined above, or a group --O--Y--Phe-- wherein Y and Phe are as defined above, are inhibitors of 5.alpha.-reductase and can be used for the therapeutic treatment of the human and animal body.

Abstract: Compounds of the formula I ##STR1## wherein R denotes an aliphatic, cycloaliphatic, cycloaliphatic-aliphatic or araliphatic radical having 2 or more carbon atoms, and wherein one of the groups R.sup.1, R.sup.2 and R.sup.3 represents hydrogen or an aliphatic, cycloaliphatic, araliphatic or aromatic radical, another one of R.sup.1, R.sup.2 and R.sup.3 is hydrogen or, in the case of R.sup.1 and R.sup.2, is hydroxy, and the remaining one of R.sup.1, R.sup.2 and R.sup.3 is hydrogen, or wherein R denotes methyl, R.sub.1 denotes hydrogen or hydroxy, R.sub.2 denotes an aromatic radical and R.sub.3 represents hydrogen, and their salts have GABA.sub.B -antagonistic properties and can be used as GABA.sub.B -antagonists. They are obtained when in a compound of formula II ##STR2## in which R, R.sup.1, R.sup.2 and R.sup.3 have their previous significances, Z represents --NH.sub.2 and R.sup.4 denotes a hydroxy-protective group R.sup.5 or, when R.sup.1 and R.sup.3 denote hydrogen and R.sup.

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: A process for the manufacture of brofaromine and analogues thereof by reaction of a trisubstitued phosphonium methyl dihydroquinone compound with a 1-(substituted carbonyl)-4-(substituted carbonyl)-piperidine with subsequent cyclization and hydrolysis of the remaining carbonyl substituent. The resulting prmary compound can be further interconverted between free and salt forms or between different salt forms as desired.

Abstract: A new polymer, the feed monomers and molar percents of which, exclusive of a polymerization initiator and crosslinker, are:A.(I) 42 mole % to 58 mole % of a siloxy silane of formula I,(II) 42 mole % to 58 mole % of an unsubstituted alkyl (meth)acrylate of formula II,(III) 0 to 5 mole % of a Group A monomer, and(IV) 0 to 16 mole % of an additional vinylic copolymerizable monomer;B.(I) 42 mole % to 58 mole % of a siloxy silane of formula I,(II) 21 mole % up to less than 42 mole % of an unsubstituted alkyl (meth)acrylate of formula II,(III) 0 to 5 mole % of a Group A monomer, and(IV) 0 to 29 mole % of an additional vinylic copolymerizable monomer, orC.

Abstract: Disclosed is a method of removing residual organic solvents from formed compressed articles such as tablets comprised of subjecting the organic solvent laden compressed article to a supercritical fluid or near critical gas whereby residual solvent is transferred from the solvent laden solid article to the supercritical fluid or near critical gas and separating the residual solvent depleted compressed article from the solvent enriched supercritical fluid or near critical gas.

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: P-substituted aminoalkylphosphinic acids of the formula ##STR1## wherein R denotes an optionally fluorinated methyl group, R.sub.1 denotes hydrogen, lower alkyl, lower alkoxy, hydroxy, halogen or a fluorinated methyl group and R.sub.2 and R.sub.3 denote hydrogen or R.sub.2 denotes hydroxy, lower alkoxy or halogen and R.sub.3 is hydrogen or R.sub.2 and R.sub.3 together represent an oxo group, and their pharmaceutically acceptable salts are active as GABA.sub.B.sup.- agonists and can be used in the treatment of spinal spasticity, multiple sclerosis and cerebral palsy, trigeminus neuralgia, drug withdrawal syndromes and/or conditions of pain. They can be manufactured by methods known per se and suitable such methods are described.

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: A method of sealing transdermal drug delivery system components together which comprises contacting the surfaces of the components to be sealed together with each other and exposing the contacted surfaces to ultrasonic forces while said surfaces are still in contact to produce a seal of said surfaces in a predetermined manner.

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: 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.