Celltech Therapeutics Limited

Celltech Limited

Other

Ucb Pharma, S.a.

Michael Anthony Eaton

Graham John Warrellow

Ewan C Boyd

Rikki Peter Alexander

John Robert Porter

Timothy John Norman

David Parker

Thomas A Millican

David G Parker

Richard C Titmas

The present invention provides an albumin-binding compound essentially of the following elements: a spacer group, a water-soluble bridging group, a fatty acid chain and an acidic group characterised in that the acidic group is attached to the distal end of the fatty acid chain. The invention also provides an albumin-binding compound to which one or more biologically active moieties are attached.

Albumin-binding conjugates comprising a fatty acid and PEG

Compounds of formula (1) ##STR1## are described wherein Y represents a halogen atom or a group --OR.sup.1, where R.sup.1 is an optionally substituted alkyl group; R.sup.2 represents an optionally substituted cycloalkyl or cycloalkenyl group; R.sup.3 is a monocyclic or bicyclic aryl group optionally containing one or more heteroatoms selected from oxygen or sulphur atoms or a group --N(R.sup.4)-- where R.sup.4 is a hydrogen atom or an alkyl group; X is --O--, --S--, or --N(R.sup.5)--, where R.sup.5 is a hydrogen or an alkyl group; with the proviso that when X is --O-- then R.sup.3 is not a 3-cyanamino-6-pyridazinyl or a 3-chloro-6-pyridazinyl group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are selective and potent inhibitors of phosphodiesterase IV and are useful for the prophylaxis and treatment of inflammatory diseases and the alleviation of conditions associated with central nervous malfunction.

Tri-substituted phenyl derivatives and processes for their preparations

Compounds of general formula (1): ##STR1## wherein Y is a halogen atom or a group --OR.sup.1 where R.sup.1 is an optionally substituted alkyl group;

Trisubstituted phenyl derivatives and processes for their preparation

Compounds of formula (1) ##STR1## are described wherein Y represents a halogen atom or a group --OR.sup.1, where R.sup.1 is an optionally substituted alkyl group; R.sup.2 represents an optionally substituted cycloalkyl or cycloalkenyl group; R.sup.3 is a monocyclic or bicyclic aryl group optionally containing one or more heteroatoms selected from oxygen or sulphur atoms or a group --N(R.sup.4)-- where R.sup.4 is a hydrogen atom or an alkyl group; X is --O--, --S--, or --N(R.sup.4)--, where R.sup.5 is a hydrogen or an alkyl group; with the proviso that when X is --O-- then R.sup.3 is not a 3-cyanamino-6-pyridazinyl or a 3-chloro-6-pyridazinyl group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are selective and potent inhibitors of phosphodiesterase IV and are useful for the prophylaxis and treatment of inflammatory diseases and the alleviation of conditions associated with central nervous malfunction.

Tri-substituted phenyl derivatives and processes for their preparation

Tri-substituted phenyl derivatives and their use in pharmaceutical

##STR1## Tetra-aza macrocycles of formula (I), wherein m and n, which may be the same or different, is each zero or an integer 1,2, or 3; d is zero or an integer 1, 2 or 3; q is zero or an integer from 1 to 6 inclusive; R, R.sup.1, R.sup.2 and R.sup.3, which may be the same or different, is each a hydrogen atom or a group --P(O)(XH)R.sup.4 (where X is an oxygen or sulphur atom and R.sup.4 is a hydrogen atom or an alkyl or alkoxy group), with the proviso that at least one of R, R.sup.1, R.sup.2 and R.sup.3 is a --P(O)(XH)R.sup.4 group; L is a covalent bond or a linker group; Z is a hydrogen atom or a reactive functional group; and metal complexes and/or salts thereof; are described together with processes for their preparation and compositions containing them. The compounds are useful for imaging and in the treatment of abnormal cell disorders, such as in the treatment of tumours, and may be coupled to other molecules, such as proteins for use in diagnosis and therapy.

Tetra-aza macrocycles and processes for their preparation

##STR1## Tri-aza macrocycles of formula (I), wherein m and n, which may be the same or different, is each zero or an integer 1, 2, or 3; p is zero or an integer 1 or 2; q is zero or an integer from 1 to 6 inclusive; R.sup.1, R.sup.2 and R.sup.3, which may be the same or different, is each a hydrogen atom or a group --CO.sub.2 H or --P(O)(XH)R.sup.4 (where X is an oxygen or sulpher atom and R.sup.4 is a hydrogen atom or an alkyl or alkoxy group), with the proviso that at least one of R.sup.1, R.sup.2 and R.sup.3 is a --P(O)(XH)R.sup.4 group; L is a covalent bond or a linker group; Z is a hydrogen atom or a reactive functional group; and metal complexes and/or salts thereof; are described together with processes for their preparation and compositions containing them. The compounds are useful as imaging agents, and in the treatment of abnormal cell disorders, such as in the treatment of tumours, and may be coupled to other molecules, such as proteins, for use in diagnosis and therapy.

Growing community of inventors

Watlington, United Kingdom

Michael Anthony Eaton