Asta Pharma Aktiengesellschaft

Degussa Aktiengesellschaft

Asta-werke Aktiengesellschaft, Chemische Fabrik

Asta-werke Aktiengesellschaft

Asta Medica, Aktiengesellschaft

Aasta Pharma Ag

Asta Pharma Aktiengesellshaft

Gerhard Scheffler

Jurgen Engel

Peter Emig

Ilona Fleischhauer

Norbert Brock

Jorg Pohl

Helmut Hettche

Reinhard Muckenschnabel

Wolfgang Morick

Ulf Niemeyer

Hans Pohle

Bernd Nickel

Klaus Thiemer

Hans-Dieter Lenke

Bernhard Kutscher

Winfried Orth

Ulrich Werner

Dieter Sauerbier

Stefan Szelenyi

Juergen Engel

Carl-Heinrich Weischer

Vladimir Jakovlev

Carl H Weischer

Rolf Rebling

Klaus D Schenk

Klaus Pressler

Salts of azelastine with acetic acid, gluconic acid, lactic acid or malic acid.

Salts of azelastine having improved solubility effective at treating

The present invention relates to salts of azelastine having improved solubility in water. The salts of the present invention are prepared by reacting azelastine with acetic acid, gluconic acid, lactic acid, or malic acid. The azelastine salts are effective in providing a cytoprotective effect.

Salts of azelastine having improved solubility useful at providing a

The present invention relates to salts of azelastine having improved solubility in water. The salts of the present invention are prepared by reacting azelastine with acetic acid, gluconic acid, lactic acid or malic acid. A pharmaceutical composition may be prepared containing an azelastine salt and a pharmaceutically-acceptable carrier or diluent therefor. The pharmaceutical composition is useful in the treatment of allergies, asthma, inflammatory and psoriasis disorders and provides a cytoprotective effect.

Salts of azelastine having improved solubility

Pharmacologically active compounds of the General Formula ##STR1## where X is oxygen or sulphur and the radical R represents a quinuclidyl radical, an C.sub.1 -C.sub.6 -alkyl radical, a phenyl radical, a pyridyl radical, a phenyl or pyridyl radical substituted by the radicals R.sub.1, R.sub.2, and/or R.sub.3, a C.sub.1 -C.sub.6 -alkyl radical substituted by pyridyl or alkylpyridyl or a C.sub.1 -C.sub.6 -alkyl radical substituted by phenyl, where each phenyl radical may also be substituted by the radicals R.sub.1, R.sub.2 and/or R.sub.3 and the radicals R.sub.1, R.sub.2 and R.sub.3 are the same or different and represent hydrogen, halogen, trihalogenmethyl, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -alkoxy, carboxy, Carb-C.sub.1 -C.sub.6 -alkoxy, amino, C.sub.1 -C.sub.6 -alkylamino, C.sub.1 -C.sub.6 -dialkylamino, C.sub.1 -C.sub.6 -trialkylamino, C.sub.2 -C.sub.6 -alkanoylamino, or C.sub.2 -C.sub.6 -alkanoylamino which contains one more amino group in the alkyl portion, and their physiologically acceptable acid addition salts. The compounds provide analgesic, anti-inflammatory, anti-convulsive and anti-pyretic effects.

Phthalazines containing an aromatic ether or thioether group in the

An embonic acid salt of azelastine is disclosed which does not possess the bitter taste of azelastine, and which therefore is suitable for orally administered formulations.

Azelastine embonate and compositions which contain it

Method of treating inflammatory disorders and psoriasis with salts of

This invention relates to new oxzaphosphorin-4-thio-alkanesulphonic acids and to the neutral salts thereof corresponding to the general formula I ##STR1## and to methods to use such compounds to treat cancer diseases and to produce immunosuppression in humans and animals.

oxazaphosphorin-4-thio alkanesulphonic acids, neutral salts thereof and

2,6-diamino-3-halobenzylpyridines of the formula I: ##STR1## wherein R.sub.1 is fluorine and R.sub.2 is hydrogen or chlorine as well as their physiologically acceptable acid addition salts, processes for their manufacture and their use in pharmaceuticals.

2,6-diamino-3-halobenzylpyridines and processes for their manufacture as

There are provided 4-benzyl-1-(2H)-phthalazinone derivatives having antiallergic activity of the formula ##STR1## wherein R.sub.1 represents fluorine, chlorine, bromine, trifluoromethyl, C.sub.1 -C.sub.6 -alkyl, hydroxy, C.sub.1 -C.sub.6 -alkoxy, C.sub.2 -C.sub.6 -alkanoyloxy, amino, C.sub.1 -C.sub.6 -alkylamino, di-C.sub.1 -C.sub.6 -alkylamino, C.sub.2 -C.sub.6 -alkanoylamino, C.sub.2 -C.sub.6 -alkanoyl-C.sub.1 -C.sub.6 -alkylamino or a nitro group, R.sub.2 represents hydrogen or has one of the meanings given for R.sub.1, whereby R.sub.1 and R.sub.2 may be the same or different, the radicals R.sub.3 and R.sub.4 are the same or different and represent hydrogen, halogen, C.sub.1 -C.sub.6 -alkyl, hydroxy, C.sub.1 -C.sub.6 -alkoxy, benzyloxy or C.sub.2 -C.sub.6 -alkanoyloxy and A represents an azacycloalkanyl radical, the aza nitrogen of which contains a C.sub.1 -C.sub.6 -alkyl group which is substituted by various radicals, and processes for their manufacture.

4-benzyl-1-(2H)-phthalazinone-derivates

There is described a process for the production of 2-amino-3-nitro-6-(4-fluorobenzylamino)-pyridine which consists essentially of reacting 2-amino-3-nitro-6-methoxypyridine with 4-fluorobenzylamine in water at elevated temperature; in a given case the nitro group can be subsequently reduced and a carbethoxy group introduced.

Process for the production of

This invention relates to new compounds corresponding to the general formula: ##STR1## R.sub.1 represents a C.sub.3 -C.sub.10 cycloalkyl group substituted by C.sub.1 -C.sub.6 alkyl radicals, a C.sub.3 -C.sub.19 -cycloalkyl-C.sub.1 -C.sub.4 alkyl group which may be substituted by C.sub.1 -C.sub.6 alkyl radicals, a C.sub.6 -C.sub.8 bicycloalkyl group, a C.sub.6 -C.sub.8 bicycloalkyl-C.sub.1 -C.sub.4 alkyl group, a C.sub.6 -C.sub.10 tricycloalkyl group, a C.sub.6 -C.sub.10 tricycloalkyl-C.sub.1 -C.sub.4 alkyl group, a C.sub.6 -C.sub.9 tetracycloalkyl group or a C.sub.6 -C.sub.9 -tetracycloalkyl-C.sub.1 -C.sub.4 alkyl group,

Ethylenediamine and guanidine-derivatives

Compounds of the formula ##STR1## wherein R is a benzyl group, a phenylethyl group, a methoxyethyl group or an allyl group having an antiallergic activity.

N-benzyl, phenethyl, methoxyethyl or allyl substituted

There are disclosed pyridine-2-ethers and pyridine-2-thioethers having a nitrogen-containing cycloaliphatic ring corresponding to the formula ##STR1## the pyridine-N-oxides and/or amine oxides thereof and the pharmaceutically acceptable salts thereof. The compounds show analgesic activity.

Analgesic pyridine-2-ethers or pyridine-2-thioethers having a

This invention relates to new oxazaphosphorin-4-thio-alkanesulphonic acids and to the neutral salts thereof corresponding to the general formula I ##STR1## and to methods to use such compounds to control cancer diseases and to produce immunosuppression in humans and animals.

Oxazaphosphorin-4-thio-alkanesulphonic acids, and neutral salts thereof

The present invention relates to new 4-carbamoyloxy-oxazaphosphorins of the general Formula I ##STR1## as well as to a method for the treatment of malign tumor diseases in humans using such compounds as active agent.

Growing community of inventors

Bruchkobel, Germany

Gerhard Scheffler