Beecham Group Plc

Gordon Wootton

Frederick Cassidy

Gareth J Sanger

Richard W Moore

Eric A Watts

Christine Summers

Stephen A Smith

Peptides comprising, in sequence, units selected from the amino acid residues 17 to 24 of VIP, and consisting at least of the amino acid residues 18 to 23, or an analogue thereof wherein one or more of the amino acid residues is replaced by an equivalent other amino acid; having anti-ulcer activity, a process for their preparation and their use as pharmaceuticals.

Peptides containing the 18 to 23 residues of vasoactive intestinal

A method of treatment of emesis, anxiety and/or IBS in mammals, including humans, which method comprises administering an effective amount of a compound of formula (I) or (II) or a pharmaceutically acceptable salt thereof:

Novel treatment

Treatment of emesis, nausea and vomiting

Peptides comprising, in sequence, units selected from the amino acid residues 11 to 23 of vasoactive intestinal peptide (VIP) and consisting at least of the amino acid residues 15 to 20, or an analogue thereof wherein one or more of the amino acid residues is replaced by an equivalent other amino acid, or a pharmaceutically acceptable salt thereof; having pharmacological activity, a process for their preparation and their use as pharmaceuticals.

VIP type peptides

Method of treating emesis, anxiety and/or IBS

Compounds of formula (I), or salts thereof: ##STR1## wherein: X is oxygen or sulphur, or &gt;C.dbd.X represents ##STR2## Y is --CH.sub.2 --CH.sub.2 -- or --CH.dbd.CH--; n is 1 to 5;

Bronchodilating hydantoin derivatives

Compounds of formula (I): ##STR1## wherein: m is 1 or 2; n is 4 to 8; X is CO, protected CO, or CROH wherein R is hydrogen or C.sub.1-4 alkyl and wherein the OH moiety may be protected; R.sub.1 is hydrogen or CO.sub.2 R.sub.1 represents an ester group in which the R.sub.1 moiety contains from 1 to 12 carbon atoms; R.sub.3 is hydroxy, or protected hydroxy; R.sub.2 and R.sub.4 are separately hydrogen, C.sub.1-9 alkyl, C.sub.5-8 cycloalkyl, C.sub.5-8 cycloalkyl-C.sub.1-6 alkyl, phenyl, phenyl C.sub.1-6 alkyl, naphthyl, naphthyl C.sub.1-6 alkyl, any of which phenyl or naphthyl moieties may be substituted by one or more halogen, trifluoromethyl, C.sub.1-6 alkyl, C.sub.1-6 alkoxy or nitro groups; or R.sub.2 and R.sub.4 taken with the carbon atom to which they are joined represent a C.sub.5-8 cycloalkyl group; and salts thereof; except that when one of R.sub.2 and R.sub.4 is hydrogen or C.sub.1-4 alkyl then the other of R.sub.2 and R.sub.4 cannot be hydrogen or C.sub.1-9 alkyl; have useful pharmacological properties including antigastric secretion, bronchodilator and platelet aggregration inhibition activities.

Cycloaliphatic prostaglandin analogues

Compounds of the formula (I): ##STR1## having pharmacological activities similar to those of natural prostaglandins wherein:

Terminal amino prostaglandin analogues

Compounds of the formula (I): ##STR1## wherein: Y is --CH.sub.2 CH.sub.2 --, --CH.dbd.CH-- or --C.dbd.C--

Thiohydantoins having prostaglandin-like activities

Compounds of formula (I): ##STR1## wherein: X is CO, protected CO, CROH in which R is hydrogen or C.sub.1-4 alkyl and in which the OH moiety may be protected;

Oxy-alkylamino carboxylic esters

Compounds of the formula 1: ##STR1## wherein: X is O or S;

Hydantoin derivatives

Compounds of the formula (I): ##STR1## wherein: Y is --CH.sub.2 CH.sub.2 --, --CH.dbd.CH-- or --C.dbd.C-- n is 1 to 5;

1,5-Disubstituted imidazolid-4-ones

A compound of the formula (I): ##STR1## wherein: X is O or S;

Prostaglandin analogues

Oxy-alkylamino acids and esters

Compounds of formula (I): ##STR1## wherein: m is 1 or 2; n is 4 to 8; X is CO, protected CO, or CROH wherein R is hydrogen or C.sub.1-4 alkyl and wherein the OH moiety may be protected; R.sub.1 is hydrogen or CO.sub.2 R.sub.1 represents an ester group in which the R.sub.1 moiety contains from 1 to 12 carbon atoms; R.sub.3 is hydroxy, or protected hydroxy; R.sub.2 and R.sub.4 are separately hydrogen, C.sub.1-9 alkyl, C.sub.5-8 cycloalkyl, C.sub.5-8 cycloalkyl-C.sub.1-6 alkyl, phenyl, phenyl C.sub.1-6 alkyl, naphthyl, naphthyl C.sub.1-6 alkyl, any of which phenyl or naphthyl moieties may be substituted by one or more halogen, trifluoromethyl, C.sub.1-6 alkyl, C.sub.1-6 alkoxy or nitro groups; or R.sub.2 and R.sub.4 taken with the carbon atom to which they are joined represent a C.sub.5-8 cycloalkyl group; and salts thereof; except that when one of R.sub.2 and R.sub.4 is hydrogen or C.sub.1-4 alkyl then the other of R.sub.2 and R.sub.4 cannot be hydrogen or C.sub.1-9 alkyl; have useful pharmacological properties including anti-gastric secretion, bronchodilator and platelet aggregation inhibition activities.

Growing community of inventors

Sawbridgeworth, United Kingdom

Gordon Wootton