Abstract: Compounds of general formula (II) wherein X is a hydroxamic or carboxylic acid group, Y is carbonyl or sulphonyl and R.sub.1 and R.sub.2 are as defined in the claims, are matrix metalloproteinase inhibitors.

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: 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 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: 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: Compound of formula (I) ##STR1## wherein Ar represents an optionally substituted phenyl or heteroaryl group, m is 1 or 2, n is 0, 1, 2, 3 or 4, X represents --COOH or --CONHOH and R.sub.1, R.sub.3 and Y are as defined in the specification,are inhibitors of metalloproteinases involved in tissue degradation.

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: 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: A tie down strap includes two end portions and a main body portion extending therebetween having a plurality of openings integrally formed therein. The openings extend in a sequential manner linearly aligned along the main body portion intermediate the end portions and are dimensioned to receive therethrough a main body portion of another strap when the main body portion defining the opening is elongated. Specifically, the main body portion comprises two side members that extend between the two end portions in spaced parallel relation and a plurality of bridge portions that extend between and secure the two side members in their parallel relation. Moreover, the end portions have securement members such as hooks and each bridge portion is configured to be received within each securement member in substantially continuous contact therewith.

Abstract: Compounds of general formula (I), wherein W represents a 5- or 6-membered aromatic heterocyclic ring containing one or more non-quaternised sp2 nitrogen atoms in its ring, which heterocyclic ring may be optionally fused to a benzene ring or to a further 5- or 6-membered aromatic heterocyclic ring containing one or more nitrogen atoms, wherein at least one of the said heterocyclic rings may also contain an oxygen or sulphur atom, and wherein any of the rings may be optionally substituted with one or more substituents selected from --C.sub.1 -C.sub.6 alkyl, --OC.sub.1 -C.sub.6 alkyl, halo, --CF.sub.3 and --CN; Z represents a) a divalent alkanediyl group from 1 to 8 carbon atoms which may be a straight or branched-chain, wherein the said group is either unsubstituted or substituted by one or more substituents selected from hydroxy, --OC.sub.1 -C.sub.6 alkyl, --SC.sub.1 -C.sub.

Abstract: Compounds of general formula I: ##STR1## wherein W represents imidazo [4,5-c]pyridin-1-yl, imidazo [4,5-c]pyridin-3-yl and imidazo [4,5-c]pyridin-5-yl optionally substituted with one or more --C.sub.1 -C.sub.6 alkyl substituents; Z represents a) a divalent alkanediyl, alkenediyl or alkynediyl group; b) a --(CH.sub.2).sub.q U(CH.sub.2).sub.r -- group, optionally substituted, wherein q is an integer from 0-3, r is an integer from 0-3 and U is --O-- or --S--; Q represents a carbonyl, thiocarbonyl or sulphonyl group; B represents a) a --VR.sup.8 group wherein V is --C(.dbd.O)O-- or --CH.sub.2 O--; are antagonists of platelet activating factor (PAF).

Abstract: The present invention is directed to compounds of general formula I as well their pharmaceutically and veterinarily acceptable acid addition salts or hydrates thereof. The present invention is further directed to pharmaceutical and veterinary compositions containing the compounds of general formula I. The present compounds of general formula I are antagonist of platelet activating factor (PAF). Accordingly, the present invention is also directed to methods for preventing, treating or ameliorating in human or mammalian animals, various diseases or physiological conditions mediated by PAF.

Abstract: Compounds of the general formula I; ##STR1## wherein: A.sup.1 is .dbd.N--, .dbd.CH-- or .dbd.CR.sup.1 --;A.sup.2 is --N.dbd., --CH.dbd. or --CR.sup.2 .dbd.;provided that, when one of A.sup.1 and A.sup.2 is a nitrogen atom, the other of A.sup.1 and A.sup.2 is other than a nitrogen atom;wherein the remainder of the variables are defined in the specification;and their pharmaceutically and veterinarily acceptable acid addition salts and hydrates are antagonists of platelet activating factor (PAF) and as such are useful in the treatment or amelioration of various diseases or disorders mediated by PAF.

Abstract: Compounds of formula I: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9, and B are variables. These compounds are antagonists of platelet activating factor (PAF) and as such are useful in the treatment or amelioration of various diseases or disorders mediated by PAF.