Abstract: Compounds of general formula (I) wherein R4 is an ester or thioester group and R, R1, R2, and R3 are as specified in the description, inhibit monocyte and/or macrophage and/or lymphocyte activation and lymphocyte proliferation.

Abstract: The present invention describes processes for preparing desired synthetic products that comprise a covalently bonded hydroxamic acid group —CONHOH by forming a mixture of a liquid reaction medium and a solid phase reaction product that carries a plurality of moieties of formula (A1) or (B1): where X is a residual, non-hydroxamate partial structure of the desired synthetic product, P1 is hydrogen or an amino-protecting group, P2 is hydrogen or a hydroxyl protecting group, and the bond designated (a) covalently links the moieties (A1) or (B1) to the residue of a solid substrate; by cleaving the bond designated (a) in the resultant mixture; and by separating the resultant liquid reaction phase from the resultant reaction solids to recover the desired synthetic product.

Abstract: Therapeutically active hydroxamic acid derivatives, processes for their preparation, pharmaceutical compositions containing them, and the use of such compounds in medicine. The compounds are inhibitors of metalloproteinases involved in tissue degradation.

Abstract: Compounds of general formula (II) ##STR1## wherein R.sub.1, R.sub.2 and Z are defined in the claims, are matrix metalloproteinase inhibitors.

Abstract: A pharmaceutical or veterinary composition comprising a compound of formula I ##STR1## wherein X is a --CO.sub.2 H group and R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 are as defined in the specification, or a salt, hydrate or solvate thereof, and a pharmaceutically or veterinarily acceptable excipient or carrier. A method of treatment of diseases or conditions mediated by MMPs in mammals, such as rheumatoid arthritis, osteoarthritis, periodontitis, gingivitis, corneal ulceration or tumour invasion by secondary means, by administering to the mammal an effective amount of the composition.

Abstract: Compounds of formula (I) wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, X are as defined in the specification and are prepared by elimination of one of the groups X.sub.1 and X.sub.2 from a compound of formula (II) wherein X.sub.1 and X.sub.2 each independently represent a carboxylic acid group or salt thereof, or a protected carboxylic acid group, the non-eliminated group X.sub.1 or X.sub.2 corresponding to the group X in the desired compound of formula (I).

Abstract: This invention is direct to a solid phase reaction product of a solid substrate carrying a plurality of covalently bound hydroxylamine or protected hydroxylamine groups. The solid solid phase reaction product may be used for the synthesis of hydroxamic acid derivatives or a combinatorial library of such compounds.

Abstract: Plasmin precursors are modified so that they exhibit resistance to inhibitors of plasmin. These modified plasmin precursors have fibrinolytic, thrombolytic or antithrombotic properties, which are useful in the treatment of blood clotting diseases or conditions.

Abstract: The invention is directed to therapeutically active hydroxamic acid derivatives of formula (I): ##STR1## wherein the substituents are as defined in the specification. These therapeutically active hydroxamic acid derivatives have high intrinsic activity against a broad spectrum of matrix metalloproteinases (MMPs), good oral bioavailability, and additionally inhibit tissue necrosis factor (TNF) production.

Abstract: This invention relates to imidazopyridine derivatives with the general formula II: ##STR1## These compounds are useful as dual histamine (H.sub.1) and platelet activating factor (PAF) receptor antagonists.

Abstract: Compounds of formula (I), wherein X is a --CO.sub.2 H or --CONHOH group; ##STR1## 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 as defined in the specification are selective inhibitors of stromelysin-1 and matrilysin relative to human fibroblast collagenase and 72 KDa gelatinase.

Abstract: The invention disclosed relates to thrombolytic combination therapy by the administration of an agent capable of activating native plasminogen, and a non-native plasminogen analogue which is cleavable by native thrombin to generate plasmin activity.

Abstract: Compounds of formula (I), or a salt, solvate or hydrate thereof, wherein Z represents a divalent group selected from those of formulae I(a) to I(g) defined in the specification; Y represents a single bond or a divalent group selected from those of formulae I(h) to I(j) defined in the specification; each Z independently represents hydrogen or a hydroxyl protecting group; R.sup.1 represents hydrogen or a group --CH(OZ)CH.sub.2 (OZ) wherein Z has the meaning defined above; R.sup.2 represents hydrogen, a pharmaceutically acceptable cation, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, or (optionally substituted)phenyl-(C.sub.1-4) alkyl; and R.sup.3 represents hydrogen, C.sub.1-6 alkyl, (C.sub.1-4) alkyl-substituted phenyl or benzoate; and n is 1, 2 or 3. The compounds are ligands of E-, P-, and L-selectins and are useful as anti-inflammatory agents and as agents for the control of tumour metastasis.

Abstract: Compounds of general formula (I) wherein R.sup.1 represents a hydrogen atom or a C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkenyl, phenyl, phenyl(C.sub.1 -C.sub.6)alkyl, C.sub.1 -C.sub.6 alkylthiomethyl, phenylthiomethyl, substituted phenylthiomethyl, phenyl(C.sub.1 -C.sub.6)alkylthiomethyl or heterocyclylthiomethyl group; or R.sup.1 represents --S--R.sup.x wherein R.sup.x represents a group .alpha.; R.sup.2 represents a hydrogen atom or a C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkenyl, phenyl(C.sub.1 -C.sub.6)alkyl, cycloalkyl(C.sub.1 -C.sub.6)alkyl, or cycloalkenyl(C.sub.1 -C.sub.6)alkyl; R.sup.3 represents an amino acid side chain or a C.sub.1 -C.sub.6 alkyl, benzyl, (C.sub.1 -C.sub.6)alkoxybenzyl, benzyloxy(C.sub.1 -C.sub.6)alkyl or benzyloxybenzyl group; R.sup.4 represents a hydrogen atom or a methyl group; R.sup.5 represents a group (CH.sub.2).sub.n A; or R.sup.4 and R.sup.5 together represent a group .beta.; Q represents CH.sub.