Merck Patent Gesellschaft MIT Beschrankter Haftung

Merck Patent Gesellschaft MIT Beschraenkter Haftung

Michael Klockow

Rochus Jonas

Michael Wolf

Ingeborg Lues

Hans-Jochen Schliep

Jaime Piulats

Klaus-Otto Minck

Helmut Prucher

Christoph Seyfried

Norbert Beier

Joachim Gante

Joachim Leibrock

Dieter Orth

Maria Christadler

Hans-Eckart Radunz

Albrecht Wild

Klaus Otto Minck

Norbert Hennrich

Wolfgang Brummer

Hans Dieter Orth

Gunter Schneider

Michael Arlt

Arylalkyl-thiadiazinone derivatives of the formula I ##STR1## and physiologically unobjectionable salts thereof in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and Q have the meanings given in claim 1, exhibit phosphodiesterase IV inhibition and can be used for the therapy of asthmatic disorders.

Arylalkyl-thiadiazinones

5-Pyrazolinone derivatives of the general formula I: ##STR1## in which the R.sup.1 -R.sup.3 variables are as defined herein and the physiologically acceptable salts thereof; processes for the preparation of these compounds, and in particular their use as selective inhibitors of cGMP-specific phosphodiesterase (cGMP PDE), thus as pharmaceutically active compounds.

4-(arylaminomethylene)-2,4-dihydro-3-pyrazolones

The present invention relates to thiadiazinones of the formula I ##STR1## having a phosphodiesterase-inhibiting action and which are suitable for combating cardiovascular and asthmatic disorders.

Thiadiazinones

Thiadiazinones of the formula I ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and n have the meaning given in claim 1, show antiarrhythmic action and are suitable for the control of cardiovascular disorders.

Thiadizinones

Compounds of formula I ##STR1## in which R.sup.1 and R.sup.2 are each independently of one another H or A,

Thiadiazinones of the formula I ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 have the meaning given in claim 1, show positively inotropic and vasodilating action and are suitable for combating cardiovascular diseases.

New benzimidazolylpyridazinones of the formula I ##STR1## in which R.sup.1 is a styryl or mononculear of binuclear heteroaryl radical which contains 1-4 heteroatoms, each of which is unsubstituted or singly or multiply substituted by alkyl, alkoxy, alkylthio, halogen, OH, SH, amino, alkylamino, dialkylamino, acylamino having 1-8 C atoms, nitro, COOH, COOalkyl and/or CN,

Benzimidazolylpyridazinones

New benzimidazolylpyridazinones of the formula I ##STR1## in which R.sup.1 is a styryl or mononuclear of binuclear heteroaryl radial which contains 1-4 heteroatoms, each of which is unsubstituted or singly or multiply substituted by alkyl, alkoxy, alkylthio, halogen, OH, SH, amino, alkylamino, dialkylamino, acylamino having 1-8 C atoms, nitro, COOH, COOalkyl and/or CN,

Thiadiazinones of the formula I ##STR1## wherein A is --CHR.sup.4 --CHR.sup.5 --, --CH.sub.2 --CR.sup.4 R.sup.5 --, --CR.sup.4 R.sup.5 --CH.sub.2 --, --CHR.sup.4 --CHR.sup.5 --CH.sub.2 --, --CHR.sup.4 --CH.sub.2 --CHR.sup.5 --, --CH.sub.2 --CHR.sup.4 --CHR.sup.5 --, --CR.sup.4 R.sup.5 --CH.sub.2 CH.sub.2 --, --CH.sub.2 --CR.sup.4 R.sup.5 --CH.sub.2 -- or --CH.sub.2 CH.sub.2 --CR.sup.4 R.sup.5 --,

Pyrazole derivatives of the formula ##STR1## wherein R.sup.1 is H or Cl; R.sup.2 is 1-methyl-4-piperidyloxy-carbonyl, 2-(4-phenylpiperazino)-ethoxycarbonyl, benzoxazol-2-yl, benzthiazol-2-yl, tetrazol-5-yl or 3-R.sup.3 -4-R.sup.4 -thiazolidin-2-yl; R.sup.3 is H, alkanoyl of 1-7 carbon atoms or benzoyl; and R.sup.4 is H or COOH,

Pyrazole derivatives, pharmaceutical formulations thereof

Biochemically active compounds e.g., proteins and particulate biological materials such as bacteria and viruses, are immobilized on a water-swellable or water-insoluble matrix by covalent bonding to a partially crosslinked polymer containing reactive groups capable of binding the biochemically active compound thereto.

Growing community of inventors

Rossdorf, Germany

Michael Klockow