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Stephen Clements-Jewery

Robert Westwood

Peter D Kennewell

David A Rowlands

Wilfred R Tully

Peter Wilfred Hairsine

Colin R Gardner

Roger J Gillespie

Ian R Ager

A compound selected from the group consisting of 8-phenylthio-tetrahydroquinolines of the formula ##STR1## wherein R.sub.1 and R.sub.2 are individually selected from the group consisting of hydrogen, halogen, alkyl of 1 to 6 carbon atoms optionally substituted with hydroxy, alkoxy of 1 to 6 carbon atoms, alkanoyloxy of 1 to 6 carbon atoms, alkoxycarbonyl of 2 to 6 carbon atoms, --OH, --NO.sub.2, --NH.sub.2, --COOH, --CN and aminosulfonyl or when R.sub.1 and R.sub.2 are on adjacent carbon atoms form with the said carbon atoms phenyl and their non-toxic, pharmaceutically acceptable acid addition salts having anti-allergic activity.

8-phenylthio-tetrahydroquinolines and anti-allergic use thereof

A compound selected from the group consisting of a compound of the formula ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are individually selected from the group consisting of hydrogen, halogen and alkyl and alkoxy of 1 to 6 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts having anti-allergic and anti-inflammatory properties.

Novel benzimidazolyl-thiomethyl-benzothiazoles

Novel 8-thiotetrahydroquinolines of the formula ##STR1## wherein X is selected from the group consisting of ##STR2## Alk is alkyl of 1 to 6 carbon atoms, R.sub.1 and R.sub.2 are Alk individually selected from the group consisting of hydrogen and aryl or taken together with the carbon atoms to which they are attached form a phenyl optionally substituted with at least one member of the group consisting of alkyl, alkoxy and alkylthio of 1 to 6 carbon atoms, halogen, ##STR3## and Alk' is alkyl of 1 to 6 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts having antiallergic activity and their preparation.

8[2-(imidazolyl)thio] and

Novel benzothiopyranopyridinones of the formula ##STR1## wherein A,B,C and D are individually selected from the group consisting of hydrogen, alkyl and alkoxy of 1 to 6 carbon atoms, nitro, halogen, amino and acylamino of 2 to 7 carbon atoms or A and B or C and D taken with the carbon atoms to which they are attached form a benzene ring, R is selected from the group consisting of hydrogen and R', R' is selected from the group consisting of alkyl of 1 to 9 carbon atoms, alkenyl of 2 to 9 carbon atoms optionally substituted with an --OH, cycloalkyl of 3 to 9 carbon atoms, phenyl, aralkyl of 7 to 9 carbon atoms and --(CH.sub.2).sub.n --Z, n is an integer from 1 to 4, Z is selected from the group consisting of cycloalkyl and cycloalkenyl of 3 to 9 carbon atoms, dioxanyl, 2-oxobenzimidazolyl, benzoyl, halo substituted benzoyl, cyano, alkoxy carbonyl of 2 to 7 carbon atoms and carbamoyl and their non-toxic, pharmaceutically acceptable acid addition salts having antipsychotic and antidepressant and antidopaminergic activity.

Benzothiopyranopyridinones

Novel triazoloquinazolones of the formula ##STR1## wherein R and R' are individually selected from the group consisting of hydrogen, halogen, nitro and alkyl and alkoxy of 1 to 3 carbon atoms, Y is selected from the group consisting of alkyl of 1 to 6 carbon atoms, alkenyl of 2 to 4 carbon atoms, cycloalkyl of 3 to 8 carbon atoms, aryl of 6 to 8 carbon atoms and aralkyl of 7 to 8 carbon atoms, B is an alkylene of 1 to 3 carbon atoms, X is selected from the group consisting of ##STR2## R.sub.1 and R.sub.2 are individually selected from the group consisting of hydrogen, alkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 8 carbon atoms, aryl of 6 to 8 carbon atoms, aralkyl of 7 to 8 carbon atoms, aminoalkyl of 2 to 4 carbon atoms, mono- and dialkylaminoalkyl with each alkyl having 2 to 4 carbon atoms, piperidinoalkyl of 1 to 4 alkyl carbon atoms, morpholinoalkyl of 1 to 4 alkyl carbon atoms and piperazinylalkyl of 1 to 4 alkyl carbon atoms or R.sub.1 and R.sub.2 taken together with the nitrogen to which they are attached form a saturated mono- or bicyclic heterocyclic ring with 4 to 8 carbon atoms optionally substituted with 1 to 2 methyls and optionally containing in the ring a heteroatom selected from --O--, --S-- and ##STR3## and R.sub.3 is selected from the group consisting of hydrogen, alkyl of 1 to 3 carbon atoms, hydroxyalkyl of 1 to 3 carbon atoms, alkoxycarbonyl of 2 to 5 carbon atoms, aryl of 6 to 8 carbon atoms and aralkyl of 7 to 8 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts having antihistaminic and bronchospasmolytic activity and their preparation and intermediates.

Triazoloquinazolones having antihistaminic and bronchospasmolytic

Novel compounds selected from the group consisting of compounds of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of hydrogen and alkyl of 1 or 5 carbon atoms, R.sub.2 is selected from the group consisting of hydrogen, halogen and methyl, R.sub.3, R.sub.4 and R.sub.5 are individually selected from the group consisting of hydrogen, halogen, alkyl of 1 to 5 carbon atoms, alkoxy of 1 to 3 carbon atoms, --NH.sub.2 and mono- and dialkylamino of 1 to 3 alkyl carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts having antidepressant and neuroleptic activity and their preparation.

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Near Swindon, United Kingdom

Stephen Clements-Jewery