Imperial Chemical Industries Limited

Zeneca Limited

Robert J Pearce

Alan Wellington Faull

Andrew G Brewster

Peter W Caulkett

Richard E Shute

Michael J Smithers

David A Roberts

John Wall Rayner

Michael Garth Wayne

Robert Hugh Bradbury

Stuart D Mills

Robin Wood

Keith H Gibson

Arnold H Ratcliffe

David James Le Count

Ronald Hilson Galt

Craig W Thornber

Brian B Masek

Andrew Peter Thomas

Allen John Guildford

Richard William Luke

Simon T Russell

Sturat D Mills

Barry Cox

Thomas P Blackburn

The invention concerns acid derivatives of formula I

Acid derivatives

Certain�(piperidin-4-yl-alkanoyl)carbazoyl!-carboxy-phenoxy derivatives

Compounds of formula I ##STR1## and metabolically labile esters and amides thereof, and pharmaceutically acceptable salts thereof, in which R.sup.13, M.sup.2, X.sup.1, Z.sup.1, Z.sup.1a, X.sup.2 and A.sup.1 have the meanings given in the specification. The compounds are useful as inhibitors of the binding of fibrinogen to glycoprotein IIb/IIIa. Novel intermediates are also disclosed.

Heterocyclic derivatives

Certain diacyl hydrazine derivatives

Heterocyclic compounds

Compounds of formula I ##STR1## and metabolically labile esters and amides thereof, and pharmaceutically acceptable salts thereof, in which R.sup.13, M.sup.2, X.sup.1, Z.sup.1, Z.sup.1a, X.sup.2 and A.sup.1 have the meanings given in the specification. The compounds are useful as inhibitors of the binding of fibrinogen to glycoprotein IIb/IIIa. Intermediates are also disclosed.

The invention concerns pharmaceutically useful novel compounds of the formula I, in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, Ra, A, X and Z have the various meanings defined herein, and their non-toxic salts, and pharmaceutical compositions containing them. The novel compounds are of value in treating conditions such as hypertension and congestive heart failure. The invention further concerns processes for the manufacture of the novel compounds and the use of the compounds in medical treatment. ##STR1##

Quinoline derivatives and use thereof as angiotensin II antagonists

There are disclosed quinolines of the formula ##STR1## wherein R.sup.1 is hydrogen, or hydrocarbyl. R.sub.3 and R.sub.4 are independently, H, alkyl, various functional groups or alkylenedioxy, X is phenylene optionally bearing a substituent, R.sub.a is (1-4)C alkyl optionally bearing one or more F's, Z is various carboxyl derivatives, useful as angiotensin II antagonists.

Biphenylene branched alkyleneoxy quinolines

The invention concerns pharmaceutically useful compounds of the formula I, in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, Ra, Rb, A, X and Z have the various meanings defined herein, and their non-toxic salts, and pharmaceutical compositions containing them. The novel compounds are of value in treating conditions such as hypertension and congestive heart failure. The invention further concerns processes for the manufacture of the novel compounds and the use of the compounds in medical treatment.

1,6-naphthyridinone derivatives having angiotension II antagonist

The invention concerns pharmaceutically useful novel compounds of the formula I, in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, X, X.sup.1 and Z have the various meanings defined herein, and their non-toxic salts, and pharmaceutical compositions containing them. The novel compounds are of value in treating conditions such as hypertension and congestive heart failure. The invention further concerns processes for the manufacture of the novel compounds and the use of the compounds in medical treatment.

Angiotensin II antagonizing compounds containing a 1,5-naphthyridine or

1,6-naphthyridone derivatives having angiotensin II antagonist activity

The invention concerns pharmaceutically useful novel compounds of the formula I, in which ring B, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, X and Z have the various meanings defined herein, and their non-toxic salts, and pharmaceutical compositions containing them. The novel compounds are of value in treating conditions such as hypertension and congestive heart failure. The invention further concerns processes for the manufacture of the novel compounds and the use of the compounds in medical treatment.

Diazine derivatives and pharmaceutical use

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 A stands for --(CH.sub.2).sub.2 --, which may optionally bear one or two methyl substituents, or for --(CH.sub.2).sub.3 --, R.sup.1 stands for a defined (3-4C)alkyl radical, a cyclopropyl radical, or a phenyl radical which may optionally bear a defined substituent, and R.sup.2 and R.sup.3, which may be the same or different, stand for a methyl or ethyl 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 5-hydroxytryptamine antagonists.

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Wilmslow, United Kingdom

Robert J Pearce