Smith Kline & French Laboratories Limited

Sk&f Lab Co.

Graham J Durant

Charon R Ganellin

John C Emmett

Rodney C Young

Thomas H Brown

Hunter Douglas Prain

George S Sach

Geoffrey R Owen

Robert John Ife

Margaret R Vickers

George R White

Zev Tashma

Peter D Miles

James Whyte Black

Michael Edward Parsons

Tsutomu Toyonaka Teraji

Robert A Slater

Yoshiharu Nakai

Andrew D Gribble

Charon R Genellin

Torben Hesselbo

Charo R Ganellin

Zeav Tashma

Charon F Ganellin

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

This invention relates to 5-oxypyrimidinone compounds having H.sub.2 -antagonist activity. A particular compound of the invention is 2-[3-(3-piperidinomethyl)phenoxy)propyl]-5-benzyloxypyrimidin-4-one.

Chemical compounds

S-(Aminoalkyl)isothioureas which have immunosuppressant activity. Two specific compounds are 2-(3-dimethylaminopropylthio)-2-imidazoline and N,N'-dimethyl-S-(3-dimethylaminopropyl)isothiourea.

Pharmaceutical compositions

Heterocyclic compounds which are inhibitors of histamine activity, in particular, inhibitors of H-2 histamine receptors. A specific compound of this invention is 2-[2-(4-methyl-5-imidazolymethylthio)ethylamino]-4-pyrimidone.

Pharmacologically active compounds

Heterocyclic compounds which are inhibitors of histamine activity, in particular, inhibitors of H-2 histamine receptors. A specific compound of this invention is 2-[2-(4-methyl-5-imidazolylmethylthio)ethylamino]-4-pyrimidone.

Heterocyclic alkylaminoheterocycles

The compounds are C.sub.2 -C.sub.8 straight chain alkanes terminally substituted, symmetrically or unsymmetrically, by N-(N'-substituted guanidino), N-(N',N'-disubstituted guanidino). N-(N'-substituted thioureido), N-(nitromethylene amidino) or S-(N-substituted isothioureido) groups. Two compounds of the invention are 1,3-bis-[N'-(2-(5-methyl-4-imidazolylmethylthio)ethyl)guanidino]propane and 1,3-bis-[S-(N-2-(5-methyl-4-imidazolylmethylthio)ethyl)isothioureido]p ropane. The compounds of this invention are inhibitors of H-2 histamine receptors.

Unsymmetrical guanidino, thioureido, isothioureido and

The compounds are guanidinothiazolyl derivatives which are histamine H.sub.2 -antagonists. A specific compound of the present invention is 2-[2-(2-guanidino-4-thiazolylmethylthio)ethylamino]-5-(6-methyl-3-pyridylm ethyl)-4-pyrimidone.

Guanidinothiazolyl derivatives

The compounds are N,N'-substituted thioureas, ureas and guanidines which are H-2 histamine receptor inhibitors. Two compounds of this invention are N,N'-bis[2-((4-methyl-5-imidazolyl)methylthio)ethyl]thiourea and N,N'-bis[2-((4-methyl-5-imidazolyl)methylthio)ethyl]-N'-cyanoguanidine.

Pharmacologically active isoxazole and triazole compounds

S-(Aminoalkyl)isothiourens which have immunosuppressant activity. Two specific compounds are 2-(3-dimethylaminopropylthio)-2-imidazoline and N,N'-dimethyl-S-(3-dimethylaminopropyl)isothiourea.

Heterocyclic alkyl(or methylthioalkyl)amino-1,2,4-triazine compounds which are inhibitors of histamine activity, in particular, inhibitors of H-2 histamine receptors.

1,2,4-Triazines

The compounds are novel N-substituted-N'-heterocyclic alkylthioureas, guanidines and 1-nitro-2,2-diaminoethylene compounds which are histamine H.sub.2 -antagonists.

Azolyl alkylthioureas and guanidines alkylaminonitroethylene compounds

Amidinoformic acids and amidinosulphinic acids which are histamine H.sub.2 -antagonists. Two specific compounds of the present invention are N-[2-(5-methyl-4-imidazolylmethylthio)-ethyl]amidinoformic acid and N-methyl-N'-[2-(5-methyl-4-imidazolylmethylthio)ethyl]amidiniosulphinic acid.

The compounds are alkoxypyridine compounds which are histamine H.sub.2 -antagonists. Two specific compounds of the present invention are N-cyano-N'-methyl-N'-[2-((3-methoxy-2-pyridyl)methylthio)ethyl]guanidine and 1-methylamino-1-[2-((3-methoxy-2-pyridyl)methylthio)ethylamino]-2-nitroeth ylene.

Growing community of inventors

Welwyn Garden City, United Kingdom

Graham J Durant