Imperial Chemical Industries Limited

David J Brown

Rodney B Hargreaves

Stuart D Mills

Robert I Dowell

Bernard J McLoughlin

Brian G Main

Frederick Rowe

Robert Hugh Bradbury

David Waterson

David R Brittain

David A Roberts

Robin Wood

Gordon J Marrs

Roger P Heath

This invention concerns novel nitrogen derivatives of the formula I ##STR1## (and their pharmaceutically-acceptable salts), together with pharmaceutical compositions containing them. The nitrogen derivatives are inhibitors of the catalytic action of renin. The invention further concerns novel processes for the manufacture of said inhibitors.

5-(heterocyclylalkanoyl)amino-4-hydroxypentanamides

A herbicidal composition comprising a herbicidal cyclohexane dione of partial structure (I): ##STR1## and a surfactant having terminal hydroxy groups in which the hydroxy groups have been replaced by organic blocking groups.

Herbeicidal composition

Heterocyclic compounds of the formula ##STR1## wherein either X is --CR.sup.1 R.sup.2 and Y is --O--, --S-- 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;

5-phenyl-3H,6H-1,3,4-oxadiazine-2-ones in treatment of heart failure and

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

Heterocyclic compounds of the formula ##STR1## wherein either X is --CR.sup.1 R.sup.2 and Y is --O--, --S-- 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 --O--, --S-- or --NH-- and Y is --CR.sup.1 R.sup.2 -- wherein R.sup.1 and R.sup.2 have the meanings stated above; wherein either R.sup.4 is hydrogen, fluoro or chloro, or alkyl, alkenyl, halogenoalkyl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or alkoxy each of up to 6 carbon atoms, and R.sup.5, R.sup.6 and R.sup.7, which may be the same or different, each is hydrogen, fluoro, chloro, bromo or iodo, or alkyl, alkenyl, halogenoalkyl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or alkoxy each of up to 6 carbon atoms, provided that R.sup.4, R.sup.5, R.sup.6 and R.sup.7 are not all hydrogen; or R.sup.4 is bromo and R.sup.5, R.sup.6 and R.sup.7 have the meanings stated above, provided that R.sup.5, R.sup.6 and R.sup.7 are not all hydrogen; or R.sup.4 and R.sup.5 together, or R.sup.5 and R.sup.6 together, or R.sup.4 and R.sup.7 together, form the --CH.dbd.CH--CH.dbd.CH-- group and the other two of R.sup.4, R.sup.5, R.sup.6 and R.sup.7 have the meanings stated above; processes for their manufacture and pharmaceutical compositions containing them. The compounds possess cardiotonic and/or antihypertensive activity.

Triazinones

The invention concerns novel trifluoromethyl derivatives of 1'-halogenobenzyl-spiro[imidazolidine-4,3'-indoline]-2,2',5-trione (I), their pharmaceutically acceptable salts, and non-toxic, biodegradable precursors thereof. The derivatives are potent inhibitors of the enzyme aldose reductase and are useful in treating or preventing certain complications of diabetes. The invention also provides pharmaceutical compositions and processes for the manufacture of the derivatives.

7'-Trifluoromethyl-spiro[imidazolidine-4,3'-indoline]-2,2',5-triones as

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

1,2,4-Triazin-3(2H) ones

1,3,4-Thiadiazin-2-ones

Process and apparatus for pyrolysis of a heavy hydrocarbon feedstock in which the feedstock is countercurrently contacted with a hot hydrogenating gas stream flowing spirally from the periphery of a substantially circular reactor (1). The hydrocarbon feedstock is injected through an inlet (4) located toward the center of reactor (1). The hot hydrogenating gas is preferably formed by combustion, using a steam-oxygen mixture injected through inlet (2), of carbonaceous by-products from the pyrolysis. Product is removed centrally through outlet (3).

Pyrolysis of hydrocarbons

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

Process and apparatus for pyrolysis of a heavy hydrocarbon feedstock in which the feedstock is counter-currently contacted with a hot hydrogenating gas stream flowing spirally from the periphery of a substantially circular reactor (1). The hydrocarbon feedstock is injected through an inlet (4) located toward the center of reactor (1). The hot hydrogenating gas is preferably formed by combustion, using a steam-oxygen mixture injected through inlet (2), of carbonaceous by-products from the pyrolysis. Product is removed centrally through outlet (3).

Growing community of inventors

Camberley, United Kingdom

David J Brown