Imperial Chemical Industries Limited

David James Le Count

Christopher John Squire

Robert J Pearce

Allen John Guildford

Craig W Thornber

Arthur Michael Barrett

Barry Cox

Roy Hull

Thomas P Blackburn

John Carter

Compounds of the formula: ##STR1## wherein A stands for the radical --(CH.sub.2).sub.2 -- which may optionally be substituted by one or two (1-2C)alkyl radicals; Q stands for an oxygen or sulphur atom; R.degree. stands for a (1-4C)alkyl, (1-4C)alkoxy or cyclopropyl radical; R.sup.1 stands for a defined (3-4C)alkyl radical, a phenyl radical which may optionally bear a defined substituent, or a defined heteroaryl radical of 5 or 6 ring atoms; and R.sup.2 and R.sup.3 stand for hydrogen or a (1-2C)alkyl radical; and pharmaceutically-acceptable acid-addition salts thereof. Processes for the manufacture of said compounds. Pharmaceutical compositions comprising one of said compounds and a pharmaceutical diluent or carrier. The compounds are 5-hydroxytryptamine antagonists.

Quinoline derivatives which are 5-hydroxytryptamine antagonists

Compounds of the formula: ##STR1## wherein X stands for an oxygen or sulphur atom, n stands for 1 or 2, R.sup.1 stands for a defined (3-4C)alkyl radical, a cyclopropyl radical, or a phenyl radical which may optionally bear a halogeno, (1-4C)alkyl or (1-4C)alkoxy substituent, and R.sup.2 stands for hydrogen or a (1-4C)alkyl radical, and pharmaceutically-acceptable acid-addition salts thereof. Process for the manufacture of said compounds. Pharmaceutical compositions comprising one of said compounds and a pharmaceutical diluent or carrier. The compounds are peripherally selective 5-HT antagonists.

Quinoline derivatives

Compounds of the formula: ##STR1## wherein A stands for the radical --(CH.sub.2).sub.2 -- which may bear one or two defined substituents; R.sup.1 stands for a (3-4C) alkyl or cyclopropyl radical, or a phenyl radical which may optionally bear one or two defined substituents, or a heteroaryl radical of five or six ring atoms which may optionally bear a (1-3C)alkyl substituent; R.sup.2 and R.sup.3 stand for hydrogen or a (1-2C)alkyl radical, or R.sup.2 stands for a (2-4C)alkylene radical which is linked to one of the carbon atoms forming the two-carbon-atom-backbone of A so as to form, together with the adjacent nitrogen atom, a pyrrolidinyl or piperidyl radical; and one of R.sup.4 and R.sup.5 stands for hydrogen, and the other stands for hydrogen, a halogen atom or a (1-3C)alkyl or (1-3C)alkoxy radical; and acid-addition salts thereof. Processes for the manufacture of said compounds. Pharmaceutical compositions comprising one of said compounds and a pharmaceutical diluent or carrier. The compounds are 5-hydroxytryptamine antagonists.

New 1-amino-3-(o-carbamoylalkoxyphenoxy)propan-2-ol derivatives, for example 1-t-butylamino-3-(o-N-methylcarbamoylmethoxyphenoxy)propan-2-ol, processes for their manufacture and pharmaceutical compositions containing them. The compounds possess .beta.-adrenergic blocking activity and are useful in the treatment of heart diseases and other conditions in man.

Alkanolamine derivatives

New 1-amino-3-carbamoylalkoxyphenoxypropan-2-ol derivatives, for example 1-t-butylamino-3-(o-N-methylcarbamoylmethoxyphenoxy)propane-2-ol, processes for their manufacture and pharmaceutical compositions containing them. The compounds possess .beta.-adrenergic blocking activity and are useful in the treatment of heart diseases and other conditions in man.

Method for producing .beta.-adrenergic blockage with alkanolamine

1-(ELECTRONEGATIVELY-SUBSTITUTED-ALKYL- OR ALKENYLPHENOXY)-3-ALKYLAMINO-2-PROPANOL DERIVATIVES, FOR EXAMPLE 1-P-CARBAMOYLMETHYLPHENOXY-3-ISOPROPYLAMINO-2-PROPANOL, AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM POSSESS .beta.-ADRENERGIC BLOCKING ACTIVITY AND ARE USEFUL IN THE TREATMENT OF HEART DISEASES AND OTHER COMPLAINTS IN MAN.

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Macclesfield, United Kingdom

David James Le Count