Novartis Ag

Ciba-geigy Corporation

Ciba-geigy Ag

Robert Portmann

Walter Scherrer

Martin Szelagiewicz

Andreas Burkhard

Urs Christoph Hofmeier

Dean Franklin Rigel

Kaspar Zimmermann

The invention relates to dosage forms and formulations comprising the novel crystal modification A of the compound I-(2,6-difluorobenzyl)-I H-I,2,3-triazole-4-carboxamide, wherein crystal modification A is characterized by characteristic lines with interplanar spacings (d values) of 10.5 &#x212b;, 5.14 &#x212b;, 4.84 &#x212b;, 4.55 &#x212b;, 4.34 &#x212b;, 4.07 &#x212b;, 3.51 &#x212b;, 3.48 &#x212b;, 3.25 &#x212b;, 3.19 &#x212b;, 3.15 &#x212b;, 3.07 &#x212b;, and 2.81 &#x212b;, determined by means of an X-ray powder pattern. Dosage forms of crystal modification A of the compound I-(2,6-difluorobenzyl)-I H-I,2,3-triazole-4-carboxamide may be for oral or parenteral administration, in the form of a solid or liquid, and in a dosage range of 20 mg to less than 500 mg. Solid dosage forms comprise a tablet or capsule, and further comprise a pharmaceutically-acceptable carrier and film-coat.

Crystal modification A of 1-(2,6-difluorobenzyI)-1 H-1,2,3-triazole-4-carboxamide and dosage forms and formulations thereof

The invention relates to the novel modifications B and C of the compound 1-(2,6-difluorobenzyl)-1H-1,2,3-triazole-4-carboxamide of the formula its use and pharmaceutical preparations comprising this crystal modifications.

Crystal modifications of 1-(2,6-difluorobenzyl)-1H-1, 2,3-triazole-4-carboxamide

The invention provides compounds of formula (I) wherein R is as defined in the description, and the preparation thereof. The compounds of formula (I) are useful as pharmaceuticals, for use in the treatment of any state associated with high levels of activeted PARP.

Indoloquinazolinones

Crystal modification of 1-(2,6-difluorobenzyl)-1H-1,2,3-triazole-4-carboxamide and its use as antiepileptic

Crystal modifications of 1-(2,6-difluorobenzyl)-1H-1,2,3-triazole-4-carboxamide

The invention relates on the one hand to a novel preparation of compounds of the formula (I)

Process for preparing 1-substituted 4-cyano-1,2,3-triazoles

The invention relates to a novel process for producing 2-methoxybenzanthrones, starting with 1-aminoanthraquinones, which process is characterized in that, by application of a special reaction medium, namely a dimethylalkanephosphonate, which at the same time acts as a methylation agent in one of the reaction steps, the reaction is performed from beginning to end according to the principle of the single-vessel reaction, that is to say, without isolation of intermediates. The 2-methoxybenzanthrones obtained by this process are important intermediate products for vat dyes.

Process for producing 2-methoxybenzanthrones

The invention relates to a process for the preparation of azo dyes of the formula ##STR1## or mixtures thereof, in which Ar is a substituted or unsubstituted phenyl, naphthyl or aromatic heterocyclic radical and Y is a group of the formula --O--R, --S--R or ##STR2## in which R is a substituted or unsubstituted alkyl, aryl or heterocyclic radical and R.sub.1 and R.sub.2 independently of one another are hydrogen or a substituted or unsubstituted alkyl, aryl or heterocyclic radical, and the groups R.sub.1 and R.sub.2, together with the nitrogen atom to which they are bonded, can form a ring. The process comprises first coupling dimeric malonodinitrile with a diazo component and cyclizing the resulting intermediate with an alcohol, thioalcohol or amine.

Certain 3-phenylhydrazono-2-amino-1,1,3-propene tricarbonitrile

The invention relates to a process for the preparation of azo dyes of the formula ##STR1## or mixtures thereof, in which Ar is a substituted or unsubstituted phenyl, naphthyl or aromatic heterocyclic radical and Y is a group of the formula --O-R, --S-R or ##STR2## in which R is a substituted or unsubstituted alkyl, aryl or heterocyclic radical and R.sub.1 and R.sub.2 independently of one another are hydrogen or a substituted or unsubstituted alkyl, aryl or heterocyclic radical, and the groups R.sub.1 and R.sub.2, together with the nitrogen atom to which they are bonded, can form a ring. The process comprises first coupling dimeric malonodinitrile with a diazo component and cyclizing the resulting intermediate with an alcohol, thioalcohol or amine.

Process for the preparation of azo dyes

A process for the production of 2-bromo-3-cyano-4,6-diaminopyridine by cyclization of malodinitrile with hydrogen bromide, which comprises reacting malodinitrile in lower aliphatic hydrogenated hydrocarbons with hydrogen bromide used in an excess of 1 to 10% above the stoichiometric amount at temperatures of -10.degree. C. to +30.degree. C.

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Pratteln, Switzerland

Robert Portmann