Zeneca Limited

Imperial Chemical Industries Limited

Astrazeneca Ab

Syngenta Corporation

Ronald Cotton

Richard William Arthur Luke

Philip N Edwards

Anand Swaroop Dutta

Michael Brian Giles

Keith Oldham

David Timms

Christopher F Hayward

Roger Camble

Philip John Jewsbury

Richard William Luke

Richard Wa Luke

A compound of formula (1), wherein: R is hydrogen, C alkyl, R CH &mdash; or R C(O)&mdash;; R is aryl, heteroaryl, heterocyclyl, aminoC alkyl, N-(C alkyl)aminoC alkyl, NN-(diC alkyl)aminoC alkyl, or R ; wherein the aryl, heteroaryl or heterocyclyl rings may be optionally substituted with up to three substituents independently selected from nitro, C alkyl, C alkoxy, halo, (C alkyl)sulfanyl, C alkoxycarbonyl, N-(C alkyl)carbamoyl, NN-(diC alkyl)carbamoyl, N-(C alkyl)amino or NN-(diC alkyl)amino; wherein R is either a group or formula (2) or formula (3); and wherein L , L , L , L , R , R , R , R , R , R , R , R , R , R , A , n, p, q, r and s are as defined herein. The compounds of formula (1) inhibit the interactions between MDM2 and p53 and may be useful in the treatment of cancers.

Piperizine-4-phenyl derivatives as inhibitors of the interaction between mdm2 and p 53

The invention relates to adsorbing chemical samples onto inert carriers to form highly stable free flowing solid for long term storage in, for example, a proprietary compound collection.

Compound storage

Novel peptide derivatives, pharmaceutically acceptable salts thereof and pharmaceutical compositions containing then are useful in treating MHC class II dependent T-cell method autoimmune or inflammatory diseases, such as rheumatoid arthritis.

Peptide derivatives

The invention concerns pharmaceutically useful peptide derivatives of the formula (I): P&mdash;R &mdash;R &mdash;R &mdash;R , in which P, R , R , R and R have various meanings defined herein, and their pharmaceutically salts, and pharmaceutically compositions containing them. The novel peptide derivatives are of value in treating MHC class II dependent T-cell medicated autoimmune or inflammatory diseases, such as rheumatoid arthritis. The invention further concerns processes for the manufacture of the novel peptide derivatives and the use of the compounds in medical treatment.

The invention concerns pharmaceutically useful peptide derivatives of the formula (I), P&mdash;R,&mdash;R,&mdash;R,&mdash;R,, in which P, R,, R,, R,, and R,have the various meanings defined herein, and their pharmaceutically acceptable salts, and pharmaceutical compositions containing them. The novel peptide derivatives are of value in treating MHC class II dependent T-cell mediated autoimmune or inflammatory diseases, such as rheumatoid arthritis. The invention further concerns processes for the manufacture of the novel peptide derivatives and the use of the compounds in medical treatment.

Peptide analogues containing a 7-membered lactam ring

The invention concerns pharmacologically useful peptide derivatives of the formula (I): P-AA,-AA,-AA,-AA,-AA,-AA,-AA,-AA,-Q, and pharmaceutically acceptable salts thereof, wherein either AA,together with AA,, or AA,together with AA,, or AA,together with AA,form a group of formula (II):

Inhibitors of peptide binding to MHC class II proteins

Peptide derivatives useful in treating autoimmune diseases

A process for the solid phase synthesis of peptides containing a C-terminal aza-amino acid, for example the decapeptide goserelin, which comprises:

Process for making peptides

The invention releates to a polypeptide of formula I

Polypeptide compounds

The invention relates to a polypeptide of formula I:

Bombesin antagonists with deletion of net-residue at the C-terminus

Compounds of the formula: ##STR1## wherein R.sup.1 stands for an alk-2-enyl radical of not more than 5 carbon atoms or a furylmethyl radical, R.sup.2 stands for an alk-2-enyl or alkyl radical of not more than 5 carbon atoms or a furylmethyl radical, &gt;N--A, B, D, E and F stand for defined amino acid or aza-amino-acid residues, and in particular one or both of B and D stand(s) for an amino acid residue of the formula --NH.C(1-3C alkyl)(1-3C alkyl).CO-- or a similar residue, and X stands for --OR.sup.7 or --NR.sup.7 R.sup.8, wherein R.sup.7 and R.sup.8, which may be the same or different, stand for hydrogen or a (1-4C)alkyl radical, and wherein the linkages are all conventional peptide linkages or in the case of D-E the peptide linkage is replaced by the group --CH.sub.2 S--, and pharmaceutically-acceptable salts thereof. Processes for the manufacture of the compounds. Pharmaceutical compositions comprising one of the compounds and a pharmaceutically-acceptable diluent or carrier. The compounds are selective opiate .delta.-receptor antagonists.

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Macclesfield, United Kingdom

Ronald Cotton