Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1990-06-15
1992-08-18
Bond, Robert T.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
540495, A61K 31495, C07D52100
Patent
active
051400251
DESCRIPTION:
BRIEF SUMMARY
FIELD OF USE OF THE INVENTION
The invention relates to the novel use of a dihydrothienobenzodiazepinone for the preparation of medicaments for the treatment of bronchial diseases, the enantiomers of this dihydrothienobenzodiazepinone, processes for their preparation, and their use.
KNOWN TECHNICAL BACKGROUND
From European Patent 0039519 dihydrothienobenzodiazepinones and their use for the treatment of gastric or intestinal diseases are known. Additionally, it is known that dibenzodiazepinones or pyridobenzodiazepinones can occur in two chiral conformations which are mirror images of one another, and the conformer mixtures can be resolved into the optical antipodes in certain cases--depending on the substitution (German Offenlegungsschrift 3,531,682).
DESCRIPTION OF THE INVENTION
It has now been found that a dihydrothienobenzodiazepinone described in European Patent 0039519, namely the compound 4,9-dihydro-3-methyl-4-[(4-methyl-1-piperazinyl)-acetyl]-10H-thieno[3,4-b] [1,5]benzodiazepin-10-one (INN: telenzepine), has unexpectedly pronounced bronchospasmolytic properties. Furthermore, a process has been found, by means of which suitably substituted dihydrothienobenzodiazepinones, in particular telenzepine, can be resolved smoothly and in high yields to their optical antipodes.
The invention therefore relates to the use of 4,9-dihydro-3-methyl-4-[(4-methyl-1-piperazinyl)-acetyl]-10H-thieno[3,4-b] [1,5]benzodiazepin-10-one and its pharmacologically tolerated salts for the preparation of medicaments for the treatment and prophylaxis of diseases of the bronchi.
The invention furthermore relates to the use of the (+)-enantiomer of telenzepine, that is to say the (+)-4,9-dihydro-3-methyl-4-[(4-methyl-1-piperazinyl)-acetyl]-10H-thieno[3, 4-b][1,5]benzodiazepin-10-one and its pharmacologically tolerated salts for the preparation of medicaments for the treatment and prophylaxis of diseases of the bronchi.
The invention also relates to medicaments which contain the compound (+)-4,9-dihydro-3-methyl-4-[(4-methyl-1-piperazinyl)-acetyl]-10H-thieno[3, 4-b]-[1,5]-benzodiazepin-10-one and/or its pharmacologically tolerated salts.
Preferred salts in this context are pharmacologically tolerated salts with inorganic and organic acids usually used in the pharmaceutical sector. The salts with fumaric acid (fumarates), tartaric acid (tartrates) or maleic acid (maleates) may be mentioned as examples. The dihydrochloride may be mentioned as preferred acid addition salt.
The medicaments are prepared by processes known per se, the compounds being used as such, or if required, in combination with suitable pharmaceutical auxiliaries and excipients, in the form of tablets, coated tablets, capsules, suppositories, plasters (for example as TTS), emulsions, suspensions, aerosols or solutions. If, in addition to the active ingredient, the novel pharmaceutical formulations contain pharmaceutical excipients, the content of active ingredient in these mixtures is 0.5 to 95%, preferably 15 to 75%, by weight of the total mixture.
From his technical knowledge, the expert is familiar with the suitable auxiliaries and excipients for the desired medicament formulations. In addition to solvents, gel formers, suppository bases, tablet auxiliaries and other excipients for the active ingredient, it is possible to use, for example, antioxidants, dispersants, solubilizers, dyes, and, in particular, permeation promoters and complex formers (for example cyclodextrins).
The medicaments are used in any suitable formulation, provided that it is ensured that adequate levels of active ingredient are produced and maintained. This can be achieved, for example, by oral or parenteral administration in suitable doses. Usually, the pharmaceutical formulation of the active ingredient is in the form of unit doses adapted to the desired administration. A unit dose may be, for example, a tablet, a coated tablet, a capsule, a suppository or a measured volume of a powder, of granules, of a solution, of an emulsion or of a suspension.
For the purposes of the present in
REFERENCES:
patent: 4381301 (1983-04-01), Rainer
Grundler Gerhard
Kilian Ulrich
Ulrich Wolf-Rudiger
Bond Robert T.
ByK Gulden Lomberg Chemische Fabrik GmbH
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