Smith Kline & French Laboratories Limited

Other

Smithkline Beecham Corporation

Andrew D Gribble

Robert John Ife

Graham J Durant

Roland Ellwood Dolle

Daniel F Veber

David G Cooper

Robert A Slater

Jason Witherington

Robert W Marquis

Antony N Shaw

Pieter H Groot

Ashley Edward Fenwick

The invention relates to 3-hydroxy-and 3-keto-cyclohetero-substituted leucine compounds that are inhibitors of cysteine proteases, particularly cathepsin K, and are useful in the treatment of diseases in which inhibition of bone loss is a factor. The 3-hydroxy-or 3-keto-moiety is bonded to a tetrahydrothiophene, tetrahydrothiopyran, tetrahydrofuran or tetrahydropyran ring.

Protease inhibitors

Phenylderivate as inhibitors of ATP citrate lyase

Phenylalkanoic acids containing a sulphonamido group, and their use in a method of treatment of thromboxane-A.sub.2 mediated diseases are disclosed. A compound of the invention is 4-[4-(phenyl-sulphonamido)phenyl]butyric acid.

Sulphonamido containing phenylalkanoic acids as thromboxane A.sub.2

The invention provides a class of sulphonamide-containing tetrahydroisoquinolinyl compounds having thromboxane antagonist activity.

Biologically active compounds

The invention relates to a class of tetrahydroisoquinolinylalkanoic acids containing an aryl sulphonamide group which have activity as thromboxane A.sub.2 antagonists.

Pharmaceutically active compounds

New 3,4-diamino-1,2,5-thiadiazole oxide derivatives which are histamine H.sub.1 -antagonists. A specific compound of this invention is 3-[3-[N-(4-fluorobenzyl)-N-pyrid-2-yl-amino]propylamino]-4-[pyrimidin-4-yl -methylamino]-1,2,5-thiadiazole-1-oxide.

Histamine antagonist triadiazole derivatives, compositions, and method

This invention describes tricyclic derivatives which are useful as histamine H.sub.1 -antagonists. A particular compound of this invention is 3-[3-(pyrido[3,2-b][1,4]-benzothiazin-10-yl)propylamino]-4-(pyrid-4-ylmeth ylamino)-1,2,5-thiadiazole-1-oxide.

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Knebworth, United Kingdom

Andrew D Gribble