Imperial Chemical Industries Limited

Zeneca Limited

Ralph Howe

Balbir S Rao

Brian R Holloway

Donald Stribling

Stuart D Mills

David S Thomson

Andrew J Bilski

Compounds of the formula (I): ##STR1## and bioprecursors and pharmaceutically acceptable salts thereof are described as .beta..sub.3 -adrenoceptor agonists having anti-obesity, hypoglycaemic and related therapeutic utilities. Processes for their preparation are described as are compositions containing them.

Chemical compounds

Compounds of the formula (I): ##STR1## and bioprecursors and pharmaceutically acceptable salts thereof are described as .beta..sub.3 -adrenoceptor agonsists having anti-obesity, hypoglycaemic and related therapeutic utilities. Processes for their preparation are described as are compositions containing them.

The invention concerns novel phenoxyacetic acid amide derivatives of the formula I (and pharmaceutically acceptable salts thereof) in which R.sup.1 is hydrogen or fluoro, R.sup.2 is phenyl, cycloalkyl, alkyl or alkenyl as defined herein, and R.sup.3 is hydrogen, methyl or ethyl, or R.sup.2 and R.sup.3 together form polymethylene as defined herein. The invention also includes pharmaceutical compositions containing the amide derivatives, means for the manufacture of the said derivatives and for their use in the treatment of obesity and related conditions and/or in the manufacture of novel medicaments.

Amide derivatives

A method of treatment of obesity or diabetes mellitus in a warm-blooded animal requiring such treatment which comprises administering to said animal an effective amount of the compound N-(2-[2-hydroxy-3-phenoxypropyl]aminoethyl)-isobutyramide in racemic (R,S) or levorotatory optically active (S) form, or of a pharmaceutically acceptable acid-addition salt thereof.

Method of treatment of obesity

The invention concerns a series of novel phenoxyacetic acid ethers (and pharmaceutically acceptable salts thereof) of the formula I in which R.sup.1 is H or F, R.sup.2 and R.sup.3 are H or (1-3C)alkyl, Z is CH.sub.2 OH or a group --CO.R.sup.4 in which R.sup.4 is OH, NH.sub.2 or (1-6C)alkoxy. The invention also includes pharmaceutical compositions for use in treating obesity and related conditions and provides processes for the manufacture of the novel ethers.

Phenyl ethers

The invention includes novel pharmaceutical compositions for topical use in the therapy or prophylaxis of inflammatory skin diseases, a method of treating one or more such diseases, a novel, optically active N-substituted-isobutyramide as an active ingredient and a process for the manufacture of said novel active ingredient.

Pharmaceutical compositions

The invention concerns novel 1-benzyl-1,2,5,6-tetrahydropyridine-3-carboxylic acid derivatives of the formula: ##STR1## wherein R.sup.1 is hydroxy, amino, (1-4C)alkylamino, di-[(1-4C)alkyl]amino, benzyloxy optionally substituted by halogeno, or (1-6C)alkoxy optionally substituted by (1-4C)alkoxy, morpholino or di-[(1-4C)alkyl]amino; and benzene ring A bears one or two substituents selected from halogeno, (1-4C)alkyl, cyano, carboxamido, trifluoromethyl and hydroxy; and their pharmaceutically acceptable salts; together with pharmaceutical compositions thereof; and analogy processes for their manufacture. The compounds of formula I are inhibitors of the aggregation of blood platelets and may be of application in the treatment or prophylaxis of thrombosis or occlusive vascular disease. A representative compound of the invention is 1-(2-chlorobenzyl)-1,2,5,6-tetrahydropyridine-3-carboxylic acid.

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MacClesfield, United Kingdom

Ralph Howe