Burroughs Wellcome Co.

William R Mallory

Virgil L Styles

Robert W Morrison, Jr

The present invention provides pyrimido (4,5-c) pyridazines, to methods for preparing them, formulations containing them and the preparation of such formulation and the use of such compounds in human therapy. These pyrimido (4,5-c)pyridazines of this invention are useful due to their activity as inhibitors of dihydropteroic and biosynthesis.

2-Amino-4-(substituted hydrazino)-6-oxo pyrimidines

The present invention provides pyrimido(4,5-c)pyridazines, to methods for preparing them, formulations containing them and the preparation of such formulation and the use of such compounds in human therapy. These pyrimido(4,5-c)pyridazines of this invention are useful due to their activity as inhibitors of dihydropteroic and biosynthesis.

Pyrimido(4,5-c)pyridazines

Compounds of the general formula (I) ##STR1## wherein R.sup.1 and R.sup.2 are selected from a lower alkyl group, a phenyl group (optionally substituted by one or more hydroxy or lower alkoxy groups), a pyridyl group or a group --CO.sub.2 R where R is a lower alkyl group, (provided that when R.sup.1 is a group --CO.sub.2 R, R.sup.2 is a lower alkyl group) are disclosed. The compounds of formula (I) are useful as intermediates to compounds of other ring systems which are of pharmacological interest. Certain of the compounds of formula (I) are also useful as antimicrobial agents.

Method of using 1H-pyrimido-4,5-c -1,2-diazepines as antibacterial and

2-Amino-4-(substituted hydrazino)-6-imino pyrimidines

2-Amino-4-imino-6-hydrazinopyrimidine

6-(1-Methylhydrazino)isocytosine

Pyrido derivatives

Novel compounds of the general formula (XIX) ##STR1## where R.sup.9 is selected from lower alkyl, phenyl, phenyl substituted by one or more hydroxy or lower alkoxy, or pyridyl, are disclosed. A method of making the compounds of Formula (XIX) is disclosed, which comprises heating in aqueous acid a compound of formula (XX) ##STR2## wherein R.sup.10 is selected from lower alkyl, phenyl, phenyl substituted by one or more hyroxy or lower alkoxy or pyridyl and R.sup.11 is selected from lower alkyl, phenyl, substituted by one or more hydroxy or lower alkoxy, pyridyl or --CO.sub.2 R where R is lower alkyl.

Pyrazolo (3,4-d) pyrimidines and methods of making

This invention provides pyrimido (4,5-c)pyridazines, process for their preparation, veterinary compositions containing them and the preparation of such compositions. These pyrimido (4,5-c)pyridazines are useful in the treatment of coccidiosis.

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Raleigh, NC, United States of America

William R Mallory