Asta Medica, Aktiengesellschaft

Asta Pharma Aktiengesellschaft

Arzneimittelwerk Dresden Gmbh

Ilona Fleischhauer

Gerhard Scheffler

Bernhard Kutscher

Helmut Hettche

Stefan Szelenyi

Reinhard Muckenschnabel

Wolfgang Morick

Jurgen Engel

Ulrich Werner

Istvan Szelenyi

Peter Emig

Rudolf Schindler

Guillaume Lebaut

Peter Metzenauer

Georg Niebch

Ute Achterrath-Tuckermann

Jurgen Schmidt

Fabienne Fouchard

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

N-benzylindole and benzopyrazole derivatives with anti-asthmatic,

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

1,3,5-trisubstituted indazole derivatives of the formula ##STR1## wherein R1 is H, (b) a C.sub.1-6 straight or branched, substituted or unsubstituted alkyl residue, (c) a C.sub.3-7 cycloalkyl residue, (d) an unsustituted or substituted phenyl, naphthyl, anthranyl, or fluorenyl residue, (e) a quinolin-2-ylmethoxy, or pyridin-2-ylmethoxy residue; X is O, or a --NH, --NH--(C.dbd.O)--NH--, --NH--(C.dbd.O)--O--, --NH--(C.dbd.O)--, or --NH--CH.sub.2 --(C.dbd.O)-- residue; Y is O, or S; R.sub.2 is H; Z is a SO, SO.sub.2, --(CH.sub.2).sub.p --, --(CH.sub.2).sub.p --O--, --O--(CH.sub.2).sub.p --, --(CH.sub.2).sub.p --(C.dbd.O)--, --(C.dbd.O)--(CH.sub.2).sub.p --, --(CH.sub.2).sub.p --(C.dbd.O)--NH--, --NH--(C.dbd.O)--(CH.sub.2).sub.p --, --(CH.sub.2).sub.p --CHOH--, --CHOH--(CH.sub.2).sub.p --, --(CH.sub.2).sub.p --CH.dbd.CH--, or --CH.dbd.CH--(CH.sub.2).sub.p -- residue, wherein p is between 1 and 6; A is a phenyl, naphthyl, anthranyl, fluorenyl, thiophenyl, pyridinyl, isoxazolyl, benzimidazolyl, benz�1,3!dioxolyl, pyrimidyl, pyrimidine-2,4-dionyl, quinolinyl, quinoxazolinyl, morpholinyl, or pyrrolidinyl residue; and, R.sub.3, R.sub.4, and R.sub.5, the same or different, are defined in the specification; and pharmaceutically acceptable salts, stereoisomers, racemates, racemic modifications, and enantiomers thereof. The invention also relates to specific compounds, processes for preparing and for treating an allergic, asthmatic, inflamed condition of a host, or for modulating the immune system of a host.

1,3,5-tribsubstituted indazole derivatives, processes for preparing, and

Phthalazinone derivatives and their optical isomers are used as medications to combat heart rhythm disturbances, to combat pain and to break through multi-drug resistance.

Phthalazinone derivatives that modulate multi-drug resistance

6-amino carboxylic acid derivatives having antiasthmatic and antiallergic properties which can be used for the preparation of medicaments. The compounds have the formula: ##STR1## wherein R.sub.1 and R.sub.2 represent hydrogen, a straight-chain or branched alkyl radical with 1-6 carbon atoms, benzyl or phenylethyl, R.sub.3 represents hydrogen, a straight-chain or branched alkyl radical with 1-6 carbon atoms or benzyl, X represents hydrogen, halogen, C.sub.1 -C.sub.6 -alkyl or C.sub.1 -C.sub.6 -alkoxy, Y.sub.1 and Y.sub.2 represent hydrogen, halogen, C.sub.1 -C.sub.6 -alkyl or C.sub.1 -C.sub.6 -alkoxy, where m, n and o can assume the values from 0-4.

Aminocarboxylic acid derivatives having antiallergic/antiasthmatic

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

Method of treating inflammatory disorders and psoriasis with salts of

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Offenbach, Germany

Ilona Fleischhauer