The invention relates to a process for producing a contrast agent-containing pharmaceutical preparation, which contains as the contrast agent a complex of a lanthanide, in particular gadolinium, and a macrocyclic chelate, in particular DOTA.
The invention relates to an aqueous pharmaceutical preparation containing a complex of gadolinium and a macrocyclic chelate, in particular DOTA, as a contrast agent for magnetic resonance imaging. In addition, the invention relates to advantageous methods for producing the preparation containing the contrast agent.
A61K 49/18 - Nuclear magnetic resonance [NMR] contrast preparationsMagnetic resonance imaging [MRI] contrast preparations characterised by a special physical form, e.g. emulsions, microcapsules, liposomes
A formulation which can be used as a photosensitizer in the therapy of cancer, for example bladder cancer, contains polyvinylpyrrolidone-bound or polyvinylpyrrolidone-complexed hypericin sodium salt.
A formulation which can be used as a photosensitizer in the early detection of cancer, for example bladder cancer, contains polyvinylpyrrolidone-bound or polyvinylpyrrolidone-complexed hypericin sodium salt.
A method for producing a liquid pharmaceutical preparation which contains a complex consisting of DOTA and gadolinium and a base such as L-lysine or meglumine, comprises the following steps: a) An aqueous solution containing free DOTA, free gadolinium and a base such as L-lysine or meglumine is produced. b) The yield of free DOTA and free gadolinium is determined in the solution obtained according to step a). c) Free gadolinium and/or free DOTA is added in order to adjust a stoichiometric excess of free DOTA in the solution. d) The complexation is executed at an increased temperature. e) Additional base such as L-lysine or meglumine is added in order to adjust the pH value. f) The final volume of the preparation is adjusted.
The invention relates to the use of galanthaminium bromide having the nomenclature name 6H-benzofuro[3a,3,2-ef] [2]benzazepinium, 4a,5,9,10-tetrahydro-6-hydroxy-3-methoxy-11-methyl bromide (4aS,6R,8aS) for producing ophthalmic formulations for treating glaucoma.
A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
The present disclosure is directed to methods for providing tolperisone having extremely low levels of 4-MMPPO (2-methyl-1-(4-methylphenyl)-propenone), as well as related compositions. The invention further relates to methods of treating a subject with tolperisone under conditions that limit exposure of the subject to tolerable levels of 4-MMPPO, among other features.
C07D 295/108 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by doubly bound oxygen or sulfur atoms with the ring nitrogen atoms and the doubly bound oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
A61K 31/4453 - Non-condensed piperidines, e.g. piperocaine only substituted in position 1, e.g. propipocaine, diperodon
9.
METHOD FOR THE PRODUCTION OF HIGHLY PURE 2,4'-DIMETHYL-3-PIPERIDINO-PROPIOPHENONE (TOLPERISONE), PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME, AND AGENT FORMULATIONS CONTAINING TOLPERISONE
The invention relates to a method for producing highly pure 2,4'-dimethyl-3-piperidino-propiophenone (tolperisone) (formula I) and the pharmaceutically acceptable salts, hydrochlorides, and hydrates thereof. Said method allows the content of the undesired byproduct 2-methyl-1-(4-methyphenyl) propenone (4-MMPPO) to be kept significantly lower than in previously known methods. The invention further relates to active substance formulations which contain tolperisone and are suitable, among other things, for producing combination preparations used for treating patients suffering from Alzheimer's disease. The invention also relates to topical formulations, controlled release (CR) formulations, and transdermal therapeutic systems, such as active substance patches, which contain less than 50 ppm, preferably less than 10 ppm, more preferably less than 7 ppm, and most preferably less than 3 ppm or 0 ppm (i.e. less than the detectable amount) of the undesired byproduct 2-methyl-1-(4-methylphenyl) propenone (4-MMPPO) in relation to 100 percent by weight of active substance.
C07D 295/108 - Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by doubly bound oxygen or sulfur atoms with the ring nitrogen atoms and the doubly bound oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
A61K 31/4453 - Non-condensed piperidines, e.g. piperocaine only substituted in position 1, e.g. propipocaine, diperodon
10.
METHOD FOR THE PRODUCTION OF HIGH-PURITY 4A, 5, 9, 10, 11, 12,-HEXAHYDRO-6H-BENZOFURO [3A, 3, 2-EF] [2] BENZAZEPINE, AND THE DERIVATIVES THEREOF
The invention relates to a method for the production of high-purity galanthamine, or high-purity galanthamine derivatives, wherein racemic bromine narwedine is utilized as a base, which is debrominated under palladium catalysis. The processing of the reaction mixture is substantial to the invention and is carried out in the presence of oxygen or peroxides such that the palladium catalyst is transferred into an insoluble, easy to cleave form. The subsequent reaction is carried out by means of the reduction of enantiomer-pure narwedine into enantiomer-pure galanthamine, wherein alylating or dealkylating takes place subsequently such that a corresponding substitution is achieved at the ring nitrogen atom. Residual amounts of palladium of below 5 ppm are obtained by further purification, such as recrystallization, such that the direct use as a pharmaceutical raw material is enabled.
A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
A61P 25/28 - Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
11.
NOVEL 6-AMINO-MORPHINAN DERIVATIVES, METHOD OF MANUFACTURING THEM AND THEIR APPLICATION AS ANALGESICS
This invention relates to a class of 6-amino-morphinan compounds of formula (I) which can be used as highly active analgesics. This invention also relates to their pharmaceutically acceptable salts and easily accessible derivatives (e.g. esters or amides of the amino acid derivatives) , to a process for their manufacture and their application in the manufacture of pharmaceutical specialities.
The invention relates to a method for isolating 5-substituted tetrazoles of general formula (I) in which R represents a substituted biphenyl radical during which the ring closure, starting from a corresponding nitrile, is carried out in organic solvents while using alkali, alkaline-earth or organotin azides. The organic phases containing the nitrile and the tetrazol are firstly mixed with water while firstly forming three liquid phases, after which the aqueous phase containing the azide and the phase containing the nitrile are separated out, and the middle organic phase containing the tetrazol is subsequently processed. In the case of ester groups to be saponified, this phase is mixed with alkali lye, after which the organic phase is separated out and the aqueous phase is acidified or otherwise, this phase is immediately acidified and purified.
C07D 403/10 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing aromatic rings
C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
