Burroughs Wellcome Co.

The Wellcome Foundation Limited

Samuel Wilkinson

Lawrence Alfred Lowe

Christopher Raymond Beddell

George W Hardy

Roderick John Flower

Sergio H Ferreira

Roger Wrigglesworth

Compounds of the general formula ##STR1## wherein Ph is a phenyl group which is optionally substituted by one or more substituents selected from halo (i.e. fluoro, chloro, bromo or iodo), C.sub.1-4 alkyl, amino, C.sub.1-4 alkylamino, di-C.sub.1-4 alkylamino, nitro, sulphonyl, aminosulphonyl, trihalomethyl, carboxy, C.sub.1-4 alkoxycarbonyl, amido, C.sub.1-4 alkylamido, C.sub.1-4 alkoxy, C.sub.2-4 alkenyl, cyano, aminomethyl, or methylsulphonyl; Y is a group of formula ##STR2## where R.sup.1 is hydrogen or methyl; R.sup.2 is alkyl of 1 to 3 carbon atoms or is methylthiomethyl; and Z is --OR.sup.3 or --NR.sup.4 R.sup.5 where R.sup.3, R.sup.4 and R.sup.5 are each hydrogen or alkyl of 1 to 4 carbon atoms and R.sup.3 can further be phenylalkyl having 1 to 3 carbon atoms in the alkylene moiety thereof, or phenyl; and basic salts thereof. These compounds have an advantageous enkephalinase inhibitory activity which renders the compounds useful in medical therapy, e.g. to prolong and/or potentiate in a mammal, the effects of endogenous or exogenous enkephalins. The latter includes synthetic enkephalin analogues.

Pharmaceutical amides, and preparation, formulations and use thereof

Compounds of the general formula ##STR1## wherein Ph is a phenyl group which is optionally substituted by one or more substituents selected from halo (i.e. fluoro, chloro, bromo or iodo), C.sub.1-4 alkyl, amino, C.sub.1-4 alkylamino, di-C.sub.1-4 alkylamino, nitro, sulphonyl, aminosulphonyl, trihalomethyl, carboxy, C.sub.1-4 alkoxycarbonyl, amido, C.sub.1-4 alkylamido C.sub.1-4 alkoxy, C.sub.2-4 alkenyl, cyano, aminomethyl or methylsulphonyl; R.sup.a and R.sup.b, which may be the same or different, each represents a hydrogen or alkali metal (e.g. sodium or lithium) atom or a C.sub.1-4 (e.g. ethyl) group; m is 0 or 1; Y is a group of formula:

Pharmaceutical amides, and preparation, formulations and use of thereof

Peptides, acid addition salts, salts, and pharmaceutical compositions thereof, and their use as morphine agonists, and especially Tyr.D.Met.Gly.Phe (4NO.sub.2).ProNH.sub.2 and Tyr.D-Met(O). Gly. Phe(4NO.sub.2). ProNH.sub.2 as anti-diarrhoeals and anti-tussives.

Biologically active amides

Peptides, acid addition salts, salts, and pharmaceutical compositions thereof, and their use as morphine agonists, and especially Tyr.D.Met. Gly.Phe(4NO.sub.2).ProNH.sub.2 and Tyr.D-Met(O).Gly.Phe(4NO.sub.2).ProNH.sub.2 as anti-diarrhoeals and anti-tussives.

Peptides, acid addition salts, salts, and pharmaceutical compositions thereof, and their use as morphine agonists, and especially Tyr.D.Met.Gly.Phe(4NO.sub.2).ProNH.sub.2 and Tyr.D-Met(O).Gly.Phe(4NO.sub.2).ProNH.sub.2 as anti-diarrhoeals and anti-tussives.

Peptides, acid addition salts, salts, and pharmaceutical compositions thereof, and their use as morphine agonists, and especially Tyr.D.Met. Gly.Phe (4NO.sub.2). ProNH.sub.2 and Tyr. D-Met(O). Gly. Phe(4NO.sub.2). ProNH.sub.2 as anti-diarrhoeals and anti-tussives.

The present invention provides novel peptides of formula (I):

A method for the induction and/or maintenance of anaesthesia or of neuroleptanalgesia in a mammal comprising the administration to the mammal of an anaesthetic-effective or of a neuroleptanalgesic-effective, non-toxic amount of a peptide of formula

Biologically active substance

Treatment of diarrhoea and dysentery

Reagent of value in the radioimmunoassay of digoxin. Also provided by the invention are a radioimmunoassay method utilizing such reagent and a test kit suitable for use in performing the assay.

Digoxin oxidized product

Method for anaesthesia by use of a pentapeptide

Immunogenic conjugates of prostaglandins of the A, B, D and E series and their structural analogues of value in the proplylaxis or therapy in mammals of pathological conditions in which prostaglandins are involved. Also provided are pharmaceutical formulations comprising the conjugates together with a carrier therefor and methods for the treatment of mammals comprising the administration thereto of a conjugate or formulation thereof.

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Beckenham, United Kingdom

Samuel Wilkinson