Abstract: A process for the preparation of a compound of formula (I) wherein R.sub.2 is a (C.sub.1 -C.sub.6)alkyl, (C.sub.2 -C.sub.6)alkenyl, (C.sub.2 -C.sub.6)alkynyl, phenyl(C.sub.1 -C.sub.6)alkyl, heteroaryl(C.sub.1 -C.sub.6)alkyl, cycloalkyl(C.sub.1 -C.sub.6)alkyl or cycloalkenyl(C.sub.1 -C.sub.6)alkyl group, any one of which may be optionally substituted by one or more substituents selected from (C.sub.1 -C.sub.6)alkyl, (C.sub.1 -C.sub.6)alkyl, --S(C.sub.1 -C.sub.6)alkyl, halo and cyano (--CN); and R.sub.7 is a carboxylic acid protecting group, which process comprises the internal molecular rearrangement of an allyl carboxylate compound of formula (II) wherein R.sub.2 and R.sub.7 are as defined in relation to formula (I) to form the desired compound of formula (I). Compounds (I) are intermediates for the preparation of Matrix metaloproteinase inhibitors.

Abstract: Stem cell inhibitors such as murine and human macrophage inflammatory protein-1alpha (muMIP-1alpha and huMIP-1alpha/LD78) and their analogues and variants enhance the release and mobilization of haematopoietic cells. This property makes them useful in enhancing responses against infection and in cell harvesting.

Abstract: The present invention relates to therapeutically active hydroxamic acid and carboxylic acid derivatives, to processes for their preparation, to pharmaceutical compositions containing them, and to the use of such compounds in medicine. In particular, the compounds are inhibitors of metalloproteinases involved in tissue degradation, and in addition are inhibitors of the release of tumor necrosis factor from cells.

Abstract: The present invention relates to intermediates, useful for the preparation of therapeutically active hydroxamic acid derivatives which are inhibitors of metalloproteinases involved in tissue degradation, and are inhibitors of the release of tumour necrosis factor from cells.

Abstract: Compounds of general Formula I: ##STR1## are presented which have collagenase inhibition activity and are useful in the management of disease involving tissue degradation and the promotion of wound healing. Representative diseases involving include arthropathy (particularly rheumatoid arthritis), inflammation, dermatological diseases, bone resorption disease and tumor invasion.

Abstract: Compounds of formula (I), ##STR1## wherein X is a --CO.sub.2 H or --CONHOH group; R.sub.4 is a group --CHR.sup.x R.sup.y wherein R.sup.x and R.sup.y independently represent optionally substituted phenyl or monocyclic heteroaryl rings, which optionally may be linked covalently to each other by a bond or by a C.sub.1 -C.sub.4 alkylene or C.sub.2 -C.sub.4 alkenylene bridge; and R.sub.1, R.sub.2, R.sub.3 and R.sub.5 are as defined in the specification are selective inhibitors of stromelysin-1 and matrilysin relative to human fibroblast collagenase and 72 KDa gelatinase.

Abstract: Matrix metalloproteinase inhibiting compounds of formula (I), wherein X is a --CO.sub.2 H or --CONHOH group; and one of the groups proximate to the amide bonds is a steric bulky group, showing enhanced oral absorption.

Abstract: Various known compounds which are matrix metalloprotease inhibitors have been found to be useful in the preparation of agents for promoting tumour regression and/or inhibiting cancer cell proliferation.

Abstract: Compounds of general formula (I), principally characterized in that R4 is a polyether group, are water soluble matrix metalloproteinase inhibitors.

Abstract: The present invention relates to therapeutically active hydroxamic acid derivatives, to pharmaceutical compositions containing them, and to the therapeutic use of these compounds. In particular, the compounds are inhibitors of matrix metalloproteinases that are involved in tissue degradation, and in addition, are inhibitors of the release of tumor necrosis factor from cells.

Abstract: L-tert-leucine-2-pyridylamide or an acid addition salt thereof.

Abstract: Proteinaceous molecules with stem cell inhibition activity are analogues of LD78 or MIP-1.alpha. which have mutations to prevent or reduce multimer formation beyond certain stages (for example a dodecamer). Aggregate formation is therefore inhibited, and the resulting low molecular weight monomers (or oligomers) have improved solution properties leading to enhanced productivity and greater therapeutic utility as stem cell protective agents, which are useful in tumour therapy.

Abstract: Insulin-like Growth Factor II (IGF-II) analogues in which at least one of R37 and R38 is replaced with another amino acid residue, the most preferred being IGF-II R37Q R38Q, can readily be produced in E. coli, unlike natural IGF-II, which is cleaved on secretion. The analogues retain activity on the type I and type II IGF receptors but have lower affinity for the insulin receptor; they are therefore more specific in their action.

Abstract: A method for the preparation of a compound of formula (I) ##STR1## wherein X is hydrogen; Y is (i) a group --CO.sub.2 R.sub.5 wherein R.sub.5 is a carboxyl protecting group or (ii) a group --CONR.sub.6 OR.sub.7 wherein R.sub.6 is an amino protecting group and R.sub.7 is a hydroxyl protecting group; and S.sub.1, S.sub.2, S.sub.3 and S.sub.4 each represent covalently bound moieties which are substantially non-reactive with the reaction components (II), (III), or (IV) defined below, which method comprises causing the co-condensation in a liquid organic medium of a carboxylic acid reaction component of formula (II); an aldehyde of formula (IIIA); ammonia; and an isonitrile reaction component of formula (IV): ##STR2## wherein Y, S.sub.1, S.sub.2, S.sub.3 and S.sub.4 are as defined with respect to formula (I).

Abstract: A compound of formula (I): ##STR1## wherein: R.sup.1 represents a (C.sub.1 -C.sub.6)alkyl, phenyl, substituted phenyl, or heterocyclyl group; R.sup.2 represents a (C.sub.1 -C.sub.6)alkyl group; R.sup.3 represents:(I) the side chain of arginine, lysine, tryptophan, histidine, serine, threonine, or cysteine, in which any polar amino, hydroxy, mercapto, guanidyl, imidazolyl or indolyl group is rendered substantially non-polar by substitution at the polar N-, O- or S-atom; or(ii) the side chain of aspartic or glutamic acid, in which side chain the carboxylic acid group is amidated;R.sup.4 represents hydrogen or a (C.sub.1 -C.sub.6)alkyl or phenyl (C.sub.1 -C.sub.6)alkyl group; R.sup.5 represents hydrogen or and n is 0, 1 or 2; or substituted phenyl groups; or a salt solvate or hydrate thereof. Compositions containing compound (I) and methods for treatment of diseases or conditions mediated by TNF or MMPs in mammals.

Abstract: A compound of formula (I): ##STR1## wherein R.sub.4 is an optionally substituted C.sub.3 -C.sub.8 cycloalkenyl group. The compounds are inhibitors of matrix metalloproteinases.

Abstract: Described herein are compounds of formula (II) ##STR1## pharmaceutical or veterinary compositions thereof, and methods of treating diseases or conditions mediated by histamine and/or PAF in mammals.

Abstract: The present invention relates to therapeutically active hydroxamic acid and carboxylic acid derivatives, to processes for their preparation, to pharmaceutical compositions containing them, and to the use of such compounds in medicine. In particular, the compounds are inhibitors of metalloproteinases involved in tissue degradation, and in addition are inhibitors of the release of tumor necrosis factor from cells.

Abstract: Compounds of formula (I), wherein: A represents: a) a --VR.sup.6 group wherein v is --C(.dbd.O), --C(.dbd.O)O--, --CH.sub.2 O--, --CH.sub.2 OC(.dbd.O)--, --C(.dbd.S)--, --CH.sub.2 OC(.dbd.O)NH--, --C(.dbd.S)O--, --CH.sub.2 S--, --C(.dbd.O)NHSO.sub.2 --, --SO.sub.2 NHC(.dbd.O)-- or --CH.sub.2 OSiPh.sub.2 --; b) a --CH.sub.2 NR.sup.9 R.sup.10 group or a --CONR.sup.9 R.sup.10 group wherein each of R.sup.9 and R.sup.10 is independently hydrogen, -alkyl-, -alkenyl-, -alkynyl, -cycloalkyl, -cycloalkenyl, pyridyl (any of which may optionally be substituted) or a group --D as defined above or R.sup.9 and R.sup.10 together with the nitrogen atom to which they are attached form a nitrogen-containing heterocyclic ring; c) a group Y where Y is a 5- or 6-membered optionally substituted heterocyclic ring containing one or more heteroatoms selected from nitrogen, oxygen and sulphur; or d) a group --CH.sub.2 Y or --C(.dbd.

Abstract: Compounds of formula (I) have matrix metalloproteinase inhibitory activity, wherein R.sub.2 represents a group R.sub.6 --A-- wherein A represents a divalent straight or branched, saturated or unsaturated hydrocarbon chain of up to 6 C atoms which may be interrupted by an O or S atom, and R.sub.6 represents hydrogen or an optionally substituted phenyl, cycloalkyl or cycloalkenyl group; R.sub.3 represents a group R.sub.7 --(B).sub.n -- wherein n is 0 or 1, B represents a divalent straight or branched, saturated or unsaturated hydrocarbon chain of up to 6 C atoms which may be interrupted by an O or S atom, and R.sub.7 is --CONHOH, carboxyl, esterified or amidated carboxyl, cycloalkyl, cycloalkenyl, heterocyclyl, phenyl, naphtyl, or substituted phenyl or naphtyl in which the substituent(s) are selected from phenyl, hydroxy, C.sub.1 -C.sub.6 alkoxy, benzyloxy, or R.sub.8 --(C.dbd.O)--(C.sub.1 -C.sub.6 alkyl)--O-- wherein R.sub.