John Wyeth Brother, Limited

John Lambert Jackson

John Leheup Archibald

Brian John Bushell

The invention provides compounds of general formula I ##STR1## and pharmaceutically acceptable acid addition and quaternary ammonium salts thereof, wherein R represents hydrogen or lower alkyl, R.sup.1 represents hydrogen or lower alkyl, R.sup.2 represents hydrogen or lower alkyl, R.sup.3 represents hydrogen, halogen, lower alkoxy, hydroxy, or lower alkyl, R.sup.4 represents hydrogen, lower alkyl, cycloalkyl of 5 to 7 carbon atoms, thienyl, furyl, phenyl; phenyl mono- or disubstituted by halogen, lower alkyl, lower alkoxy, hydroxy or trifluoromethyl; or benzoyl, halobenzoyl, lower alkanoyl, cycloalkanoyl of 6 to 8 carbon atoms, or thienoyl, A represents an alkylene, mono- or diketo- or hydroxy-alkylene radical having from 1 to 5 carbon atoms and X is oxygen or sulphur. The compounds exhibit action on the cardiovascular system particularly hypotensive and/or anti-hypertensive activity.

1-[(3-Indolyl)-alkyl]-piperidyl ureas and hypotensive compositions

This invention relates to compounds having the general formula: ##STR1## WHEREIN W represents a phenyl or indolyl radical, either of which radicals may be unsubstituted or substituted by halogen, lower alkyl, lower alkoxy or hydroxy. A represents a lower alkylene radical, an oxo lower alkylene radical or a hydroxy lower alkylene radical; R represents a phenyl radical optionally substituted by halogen, lower alkyl, lower alkoxy or hydroxy, a cycloalkyl radical of 5 to 7 carbon atoms or a lower alkyl radical; R.sup.1 represents hydrogen or a lower alkyl radical or a pharmaceutically acceptable acid addition or quaternary ammonium salt thereof; which possess hypotensive activity.

Hypotensive sulphonamidopiperidyl indoles

The invention relates to novel benzoquinolizines of the general formula (I) ##STR1## and the pharmaceutically acceptable acid addition salts thereof, wherein R.sup.1 and R.sup.2 which may be the same or different, each represent hydrogen, lower alkyl, lower alkoxy or halogen, R.sup.3 represents hydrogen, lower alkyl or aryl and R.sup.4 represents --SO.sub.2 R.sup.5 (where R.sup.5 is lower alkyl or aryl, --CONH.sub.2 or --CXNHR.sup.6 (where X is oxygen or sulphur and R.sup.6 is aryl or aryl.CO.--). The compounds have hypotensive activity.

Benzoquinolizines and hypotensive compositions containing them

This invention relates to compounds having the formula: ##STR1## and acid addition and quaternary ammonium salts thereof, wherein R represents hydrogen or lower alkyl, R.sup.1 represents hydrogen, lower alkyl, cycloalkyl of 5 to 7 carbon atoms, substituted or unsubstituted aralkyl of 7 to 12 carbon atoms, substituted or unsubstituted aryl (including heterocyclic aryl), or substituted or unsubstituted aroyl, Ar represents a substituted or unsubstituted phenyl radical and X represents oxygen or sulphur, which exhibit action on the cardiovascular system.

Piperidino ureas and thioureas

Ureidopiperidino-ketoalkyl indoles

This invention relates to compounds having the general formula: ##STR1## wherein W represents a phenyl or indolyl radical, either of which radicals may be unsubstituted or substituted by halogen, lower alkyl, lower alkoxy or hydroxy; A represents a lower alkylene radical an oxo lower alkylene radical or a hydroxy lower alkylene radical; R represents a phenyl radical optionally substituted by halogen, lower alkyl, lower alkoxy or hydroxy, or a cycloalkyl radical of 5 to 7 carbon atoms; R.sup.1 represents hydrogen or a lower alkyl radical or a pharmaceutically acceptable acid addition or quaternary ammonium salt thereof; which possess hypotensive activity.

Piperidyl-glycylamide derivatives

The invention provides 4-benzamido-1-[4-(indol-3-yl)-4-oxobutyl] piperidine and the pharmaceutically acceptable acid addition salts thereof. The compound and its salts exhibit hypotensive and anti-hypertensive activity.

Novel indole derivative

Sulphonamidopiperidyl derivatives

Thioureas of the formula ##SPC1## Wherein R represents hydrogen, halogen, lower alkyl or lower alkoxy, R.sup.1 represents hydrogen or lower alkyl and R.sup.2 represents aroyl can be hydrolysed to compounds in which R.sup.2 is hydrogen. The compounds in which R.sup.2 is hydrogen exhibit anorectic activity.

Thiourea derivatives

The invention provides indolo[2,3-a]quinolizine derivatives which are active as hypotensive and anti-histamine agents. The invention also provides a pharmaceutical composition comprising an indolo[2,3-a]quinolizine derivative together with a pharmaceutical carrier.

1,2,3,4,6,7,12,12B-Octahydro-2-benzamidoindolo[2,3-a]quinolizine

The invention relates to thioureas of formula: ##EQU1## wherein R is phenyl, substituted phenyl or furyl and R.sup.1 is hydrogen or methyl. The compounds are useful as anorexiants.

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Royston, United Kingdom

John Lambert Jackson