Beecham Group Plc

Charles S Fake

John M Evans

Graham A Showell

Gordon Burrell

Compounds of formula (I), or a pharmaceutically acceptable salt, quaternized derivative, N-oxide or solvate thereof:

Benzisothiazoles, their pharmaceutical compositions, and method of use

Compounds of the formula (I) ##STR1## and salts and pro-drugs thereof, wherein: R.sub.1 is a hydrogen atom or a lower alkyl group;

Anti-hypertensive chromanol derivatives

Compounds of the formula (I): ##STR1## and salts and pro-drugs thereof, wherein: R.sub.1 is a hydrogen atom or a lower alkyl group;

Compounds of the formula (II): ##STR1## and pharmaceutically acceptable acid-addition salts thereof wherein Ar is a pyridyl or optionally substituted phenyl group of the sub-formula --C.sub.6 H.sub.3 R.sub.1 R.sub.2 wherein R.sub.1 is a hydrogen, fluorine, chlorine or bromine atom or a lower alkyl, lower alkoxyl, lower acyl, lower acyloxyl or lower alkoxycarbonyl group; and R.sub.2 is a hydrogen, fluorine or chlorine atom or a lower alkyl or lower alkoxy group having useful anti-hypertension activity, their preparation, and pharmaceutical compositions containing them.

Chromanone derivatives and compositions containing them

Orally administrable pharmaceutical compositions for reducing the rate of gastric acid secretion and acid addition salts thereof containing an effective amount of halo-substituted 2-pyridyl thioureas and a pharmaceutical carrier and a method of treating gastric ulcers and reducing gastric acid secretion with such compositions.

Derivatives of 2-pyridylthiourea and pharmaceutical compositions

Compounds of the formula: ##STR1## and their pharmaceutically acceptable non-toxic salts, wherein R.sub.1 is alkyl of 5 to 8 carbon atoms which is straight chained or .alpha.-substituted by a methyl group or .alpha.,.alpha.-disubstituted by methyl groups and R.sub.5 is hydrogen, R.sub.6 or CO.R.sub.6 wherein R.sub.6 is alkyl of 1 to 4 carbon atoms or alkyl of 1 to 4 carbon atoms substituted by NR.sub.7 R.sub.8 wherein R.sub.7 and R.sub.8 are each hydrogen or alkyl of 1 to 4 carbon atoms or NR.sub.7 R.sub.8 is pyrrolidino, piperidino or morpholino, have been found to possess good antihypertensive activity while being of low-toxicity and substantially free of sedative side effects.

Tetrahydropyrid-4-yl-chroman-5-ol derivatives in the treatment of

Chromanols of the formula (II) ##SPC1## wherein R.sub.1 is a non-aromatic hydrocarbon group of 1-20 carbon atoms, R.sub.2 is a hydrocarbon group of 1-20 carbon atoms optionally substituted by a halogen atom and X is an optionally salted, etherified or acylated hydroxyl group, and N-oxides, acid-addition and quaternary salts thereof are shown to have anti-hypertensive activity. Their preparation and compositions containing them are described.

Anti-hypertensive polycyclic compounds for treating hypertension

Compounds of the formula (I) ##SPC1## wherein R.sub.1 is an alkyl group of 4 - 8 carbon atoms, R.sub.2 is a naphthylmethyl group and their salts, ethers and esters have been found to possess good antihypertensive activity coupled with low toxicity. Such compounds may be prepared by the reduction of a quaternary salt of the correpsonding pyridyl compound.

Non-toxic ADL antihypertensives

Compounds of the formula: ##SPC1## And their pharmaceutically acceptable non-toxic salts, wherein R.sub.1 is alkyl of 5 to 8 carbon atoms which is straight chained or .alpha.-substituted by a methyl group or .alpha.,.alpha.-disubstituted by methyl groups and R.sub.5 is hydrogen, R.sub.6 or CO.R.sub.6 wherein R.sub.6 is alkyl of 1 to 4 carbon atoms or alkyl of 1 to 4 carbon atoms substituted by NR.sub.7 R.sub.8 wherein R.sub.7 and R.sub.8 are each hydrogen or alkyl of 1 to 4 carbon atoms or NR.sub.7 R.sub.8 is pyrrolidino, piperidino or morpholino, have been found to possess good antihypertensive activity while being of low-toxicity and substantially free of sedative side effects.

Growing community of inventors

Harlow, United Kingdom

Charles S Fake