Beecham Group Plc

David G Smith

Anthony T Ainsworth

Derek R Buckle

Geoffrey Stemp

Frederick Cassidy

Gordon Burrell

Ivan L Pinto

Novel Compounds A compound of formula (I): ##STR1## where the substituents are defined later in the specification. The compounds are useful as muscle relaxants and as such have a number of pharmaceutical uses.

Benzopyranols

A compound of formula (IA) in the form of a pharmaceutically acceptable microfine powder is disclosed. ##STR1##

Compound and treatment

A compound of the general formula (I): ##STR1## or a pharmaceutically acceptable ester thereof; or a pharmaceutically acceptable salt thereof, wherein,

Compounds

Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein a and b together form an --O-- or --CH.sub.2 -- linkage or a bond;

Guanidino-substituted benzopyrans and their use as pharmaceuticals

The compounds of the formula (II): ##STR1## and their pharmaceutically acceptable salts wherein R.sub.1 is a hydrogen, fluorine or chlorine atom or a hydroxyl, hydroxymethyl, methyl, methoxyl, amino, formamido, acetamido, methylsulphonylamido, nitro, benzyloxy, methylsulphonylmethyl, ureido, trifluoromethyl or p-methoxybenzylamino group; R.sub.2 is a hydrogen, fluorine or chlorine atom or a hydroxyl group; R.sub.3 is a hydrogen or chlorine atom or a hydroxyl group; R.sub.4 is a carboxylic acid group or a salt, ester or amide thereof; R.sub.5 is a hydrogen, chlorine or fluorine atom or a methyl, methoxyl or hydroxyl group or a carboxylic acid group or a salt, ester or amide thereof; R.sub.6 is a hydrogen atom or a methyl, or propyl group; X is an oxygen atom or a bond; and Y is an alkylene group of up to 6 carbon atoms or a bond have been found to possess anti-obesity and/or anti-hyperglycaemic activity.

Secondary amines, their preparation and use in pharmaceutical

The compounds of the formula (II): ##STR1## and their pharmaceutically acceptable salts wherein R.sub.1 is a hydrogen, fluorine or chlorine atom or a hydroxyl, hydroxymethyl, methyl, methoxyl, amino, formamido, acetamido, methylsulphonylamido, nitro, benzyloxy, methylsulphonylmethyl, ureido, trifluoromethyl or p-methoxybenzylamino group; R.sub.2 is a hydrogen, fluorine or chlorine atom or a hydroxyl group; R.sub.3 is a hydrogen or chlorine atom or a hydroxyl group; R.sub.4 is a carboxylic acid group or a salt, ester or amide thereof; R.sub.5 is a hydrogen, chlorine or fluorine atom or a methyl, methoxyl or hydroxyl group or a carboxylic acid group or a salt, ester or amide thereof; R.sub.6 is a hydrogen atom or a methyl, or propyl group; X is an oxygen atom or a bond; and Y is an alkylene group of up to 6 carbon atoms or a bond have been found to possess anti-obesity and/or antihyperglycaemic activity.

Compounds having the formula: ##STR1## where R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, Y and X are as defined hereinbelow, are useful for the reduction of abnormally high blood glucose and lipid levels in the treatment of obesity or hyperglycaemia.

Compounds of formula (II): ##STR1## or a pharmaceutically acceptable salt, lower alkyl or aralkyl ester or amide thereof, wherein R.sup.1 and R.sup.2, which may be the same or different, are each of a hydrogen atom or a methyl group, n is 1, 2 or 3, and Z is a C.sub.1-6 alkyl or C.sub.1-6 alkoxy group, or a halogen or hydrogen atom are useful in treating obesity and/or hyperglycaemia and/or inflammation in mammals.

Arylethanolamine derivatives, their preparation and use in

The compounds of formula (II): ##STR1## in which R.sub.1 is a hydrogen, fluorine, chlorine or bromine atom or a hydroxyl, hydroxymethyl, methyl, methoxyl, amino, formamido, acetamido, methylsulphonylamido, nitro, benzyloxy, methylsulphonylmethyl, ureido, trifluoromethyl or p-methoxybenzylamino group; R.sub.2 is a hydrogen, fluorine, chlorine or bromine atom or a hydroxyl group; R.sub.3 is a hydrogen, chlorine or bromine atom or a hydroxyl group, R.sub.4 is a hydrogen atom or a methyl group; R.sub.5 is a hydrogen atom or a methyl group; R.sub.6 is a hydrogen, fluorine or chlorine atom or a methyl, methoxyl or hydroxy group; X is an oxygen atom or a bond; Y is an alkylene group of up to 6 carbon atoms or a bond; and Z is an alkylene, alkenylene or alkynylene group of up to 10 carbon atoms, have been found to possess anti-obesity and/or anti-hyperglycaemic activity.

Ethanamine derivatives their preparation and use in pharmaceutical

Compounds of formula (III): ##STR1## and esters, amides and pharmaceutically acceptable salts thereof, wherein A.sup.1 is hydrogen or methyl;

3-Chlorophenyl anti-obesity agents

A compound of the formula (I): ##STR1## or a pharmaceutically acceptable ester, amide or salt thereof wherein R.sub.1 is a hydrogen, fluorine, chlorine or bromine atom or a hydroxyl, hydroxymethyl, methyl, methoxyl, amino, formamido, acetamido, methylsulphonylamido, nitro, benzyloxy, methylsulphonylmethyl, ureido, trifluoromethyl or p-methoxybenzylamino group; R.sub.2 is a hydrogen, fluorine, chlorine or bromine atom or a hydroxyl group; R.sub.3 is a hydrogen, chlorine or bromine atom or a hydroxyl group; R.sub.4 is a hydrogen, chlorine or fluorine atom or a methyl, methoxyl or hydroxyl group or a carboxylic acid group or a salt, ester or amide thereof; R.sub.5 is a hydrogen atom or a methyl group; R.sub.6 is a hydrogen atom or a methyl group; R.sub.7 is a hydrogen atom or a methyl or ethyl group; R.sub.8 is a hydrogen atom or a methyl or ethyl group; X is an oxygen atom or a bond, and Y is an alkylene group of up to 5 carbon atoms, or a bond has been found to possess anti-obesity and/or anti-hyperglycaemic activity.

Growing community of inventors

Redhill, United Kingdom

David G Smith