Imperial Chemical Industries Limited

Avecia Limited

Brian G Main

Rodney B Hargreaves

Robert I Dowell

David J Brown

Jeffrey J Barlow

A polymer support is provided which comprises hydroxypolyC alkyleneoxy chains attached to a cross-linked polymer. The hydroxypolyC alkyleneoxy chain contains from 2 to 8 C alkyleneoxy groups and the polymer support has from about 0.1 to about 5 meq free hydroxy groups per gram of polymer. Preferably, the cross linked polymer is a copolymer comprising phenylethylene and 4-hydroxyphenylethylene units or phenylethylene and 4-chloromethylphenylethylene units.

Polymer supports containing polyoxyalkylenes

Compounds of the general formula I ##STR1## wherein R.sup.1 represents a halophenyl, dihalophenyl, nitrophenyl, cyanophenyl or trifluoromethylphenyl group;

Diamine compounds

This invention concerns novel 1,3-dioxan-4-yl-alkenoic and alkanoic acids of formula I wherein Ra is (1-6C)alkyl, halogeno-(1-6C)alkyl, Rb is hydrogen or as Ra, or Ra and Rb together form (2-5C)polymethylene or (2-4C)oxypolymethylene, n is 2, 3 or 4, A is vinylene or ethylene, benzene ring B optionally bears a single substituent and the substituents at positions 4 and 5 of the dioxane ring have trans-relative stereochemistry; together with pharmaceutically acceptable salts, (1-6C)-alkyl esters and (1-6C)alkanesulphonamides thereof. The compounds of formula I are antagonists of thromboxane A.sub.2 and are of value in treating a variety of disease conditions. The invention also provides processes for the manufacture of, and pharmaceutical compostions of, the compounds of formula I.

1,3-dioxan-4-ylalkenoic acids

Novel heterocyclic compounds of the formula: ##STR1## wherein either X is --CR.sup.1 R.sup.2 -- and Y is oxygen, sulphur or --NR.sup.3 --, wherein R.sup.1, R.sup.2 and R.sup.3, which may be the same or different, each is hydrogen or alkyl of up to 4 carbon atoms; or X is oxygen, sulphur or --NH-- and Y is --CH.sub.2 --; wherein R.sup.4 and R.sup.5, which may be the same or different, each is hydrogen, cyano, nitro, amino or hydroxy, or alkylthio of up to 4 carbon atoms, or has various other meanings defined in claim 1, provided that R.sup.4 and R.sup.5 are not both hydrogen; or wherein R.sup.4 and R.sup.5 are joined together such that with the benzene ring A they form a benzheterocyclic ring as defined in claim 1; and therein the benzene ring A may optionally bear one or more further substituents; or a salt thereof where appropriate. These compounds possess cardiotonic properties, and some of them possess peripheral vasodilator properties, and they are useful for the treatment of acute or chronic heart failure. Representative of the compounds is N,N-dimethyl-p-(5,6-dihydro-5-oxo-4H-1,3,4-thiadiazin-2-yl)benzamide. Also disclosed are processes for the manufacture of the compounds and pharmaceutical compositions containing them.

Heterocyclic compounds having cardiotonic use

1,3,4-thiadiazin-2-ones

6-Aryl-1,2,4-triazin-6-ones which possess cardiotonic properties

Novel heterocyclic compounds of the formula: ##STR1## wherein either X is --CR.sup.1 R.sup.2 -- and Y is oxygen, sulphur or --NR.sup.3, wherein R.sup.1, R.sup.2 and R.sup.3, which may be the same or different, each is hydrogen or alkyl of up to 4 carbon atoms; or X is oxygen, sulphur or --NH-- and Y is --CH.sub.2 --; wherein R.sup.4 and R.sup.5, which may be the same or different, each is hydrogen, cyano, nitro, amino or hydroxy, or alkylthio of up to 4 carbon atoms, or has various other meanings defined in claim 1, provided that R.sup.4 and R.sup.5 are not both hydrogen; or wherein R.sup.4 and R.sup.5 are joined together such that with the benzene ring A they form a benzheterocyclic ring as defined in claim 1; and therein the benzene ring A may optionally bear one or more further substituents; or a salt thereof where appropriate. These compounds possess cardiotonic properties, and some of them possess peripheral vasodilator properties, and they are useful for the treatment of acute or chronic heart failure. Representative of the compounds is N,N-dimethyl-p-(5,6-dihydro-5-oxo-4H-1,3,4-thiadiazin-2-yl)benzamide. Also disclosed are processes for the manufacture of the compounds and pharmaceutical compositions containing them.

Thiadizines

1-Hydroxyphenoxy-3-ureidoethylamino-2-propanol derivatives, processes for their manufacture, pharmaceutical compositions containing them and methods of using them in the treatment of heart failure. The compounds possess cardioselective .beta.-adrenergic stimulant activity. Representative of the compounds disclosed is 1-p-hydroxyphenoxy-3-.beta.-(morpholinocarbonamido)ethylamino-2-propanol.

Cardiac stimulants

1-Hydroxyphenoxy-3-ureidoethylamino-2-propanol derivatives, processes for their manufacture, pharmaceutical compositions containing them and methods of using them in the treatment of heart failure. The compounds possess cardio-selective .beta.-adrenergic stimulant activity. Representative of the compounds disclosed is 1-p-hydroxyphenoxy-3-.beta.-(morpholinocarbonamido)ethylamino-2-propanol.

Morpholine carboxamides and use thereof

Novel 1-hydroxyaryl-2-amidoalkylaminoethanol derivatives, processes for their manufacture, pharmaceutical compositions containing them and methods of using them in the treatment of heart failure and other diseases. The compounds possess .beta.-adrenergic stimulant activity. Representative of the compounds disclosed is 1-p-hydroxyphenyl-2-(.beta.-isobutyramidoethyl)aminoethanol.

Growing community of inventors

Sandbach, United Kingdom

Brian G Main