Abstract: The invention relates to NEP inhibitors for treating cardiovascular disorders wherein R1 is C1-C6alkyl, C1-C6alkoxyC1-C3alkyl or C1-C6alkoxyC1-C6alkoxyC1-C3alkyl; R2 is hydrogen or C1-C6alkyl; L is an aromatic heterocyclic ring, optionally substituted with C1-C6alkyl or halo; R3 is C1-C6alkyl optionally substituted by halo, alkoxy, haloalkoxy, alkylthio, haloalkylthio or nitrile group, or R3 is phenyl or aromatic heterocyclyl each of which may be independently substituted by one or more alkyl, halo, haloalkyl, alkoxy, haloalkoxy, alkylthio, haloalkylthio or nitrile group; R4 and R5 are either both hydrogen, or one of R4 and R5 is hydrogen and the other is a biolabile ester-forming group that in the body of a patient is replaced by hydrogen; p is 0, 1 or 2; and q is 1 or 2.

Abstract: A pharmaceutical for use in damaged tissue, such as wound, treatment (e.g. healing) is described. The pharmaceutical comprising a composition which comprises: (a) a growth factor; and (b) an inhibitor agent; and optionally (c) a pharmaceutically acceptable carrier, diluent or excipient; wherein the inhibitor agent can inhibit the action of at least one specific adverse protein (e.g. a specific protease) that is upregulated in a damaged tissue, such as a wound, environment.

Abstract: Compounds of formula (I) and pharmaceutically-acceptable derivatives thereof, are matrix metalloprotease inhibitors, useful in treatment of conditions mediated by matrix metalloproteases, such as chronic dermal ulcers.

Abstract: Compounds of formula (I): or pharmaceutically or veterinarily acceptable salts thereof, or pharmaceutically or veterinarily acceptable solvates of either entity, wherein the broken line represents an optional bond; A is C or CH; B is CH2, O or absent; R1 and R2 are each independently selected from hydrogen, C1 to C6 alkyl optionally substituted with C1 to C4 alkoxy or phenyl, and C1 to C6 alkenyl; or, together with the carbon atom to which they are attached, form a C3 to C6 cycloalkyl group which optionally incorporates a heteroatom linkage selected from O, SO, SO2 and NR6 or which is optionally benzo-fused; R3 is hydrogen, halo, R7 or OR7; R4 is hydrogen, C1 to C4 alkyl, C1 to C4 alkoxy, trifluoromethyl or halo; R6 is hydrogen or C1 to C4 alkyl; R7 is an optionally substituted monocyclic or bicyclic ring system; m is 1 or 2; and n is 0, 1 or 2; with the proviso that B is not O when A is C; are MMP inhibitors useful in the treatment of, inter alia, tissue ulceration, wound repair and skin di

Abstract: Compounds of general formula (I): 1

Abstract: Compounds of formula (I): or pharmaceutically or veterinarily acceptable salts thereof, or pharmaceutically or veterinarily acceptable solvates of either entity, wherein the broken line represents an optional bond; A is C or CH; B is CH2, O or absent; R1 and R2 are each independently selected from hydrogen, C1 to C6 alkyl optionally substituted with C1 to C4 alkoxy or phenyl, and C1 to C6 alkenyl; or, together with the carbon atom to which they are attached, form a C3 to C6 cycloalkyl group which optionally incorporates a heteroatom linkage selected from O, SO, SO2 and NR6 or which is optionally benzo-fused; R3 is hydrogen, halo, R7 or OR7; R4 is hydrogen, C1 to C4 alkyl, C1 to C4 alkoxy, trifluoromethyl or halo; R6 is hydrogen or C1 to C4 alkyl; R7 is an optionally substituted monocyclic or bicyclic ring system; m is 1 or 2; and n is 0, 1 or 2; with the proviso that B is not O when A is C; are MMP inhibitors useful in the treatment of, inter alia, tissue ulceration, wound repair and skin di

Abstract: Compounds of formula (I), and their pharmaceutically acceptable derivatives, wherein R1 and R2 are optional substituents and independently represent C1-6 alkyl, C2-6 alkenyl, optionally substituted by CO2H or CO2(C1-6 alkyl), C2-6 alkynyl, halogen, C1-3 perfluoroalkyl, (CH2)mAr1, (CH2)mHet1, (CH2)mCONR7R8, (CH2)mCO2R8, O(CH2)qCO2R8, (CH2)mCOR8, (CH2)mOR8, O(CH2)pOR8, (CH2)mNR7R8, CO2(CH2)qNR7R8, (CH2)mCN, S(O)nR8, SO2NR7R8, CONH(CH2)mAr1 or CONH(CH2)mHet1; R3 represents H, C1-6 alkyl, (CH2)pNR9R10, SO2R10, SO2NR9R10, (CH2)mCO2R10, C2-6 alkenyl, C2-6 alkynyl, (CH2)mCONR9R10, (CH2)mCO2R10, (CH2)pCN, (CH2)pR10 or (CH2)pOR10; R4 represents H or C1-6 alkyl; R5 represents H or OH; R6 represents phenyl optionally fused to a heterocyclic ring, the group as a whole being optionally substituted; R7-10 are fully defined herein and may independently represent Ar2 or Het2; Z represents CO2H, CONH(tetrazol-5-yl), CONHSO2O(C1-4 alkyl), CO2Ar3, CO2(C1-6 alkyl), tetrazol-5-yl, CONHSO2Ar3, CONHSO2(CH2)qAr3 or

Abstract: Compounds of formula (I): or pharmaceutically acceptable salts thereof, or solvates of either entity, wherein the substituents have the values described herein, are useful as matrix metalloprotease (MMP) inhibitors

Abstract: Compounds of formula (I), and their pharmaceutically acceptable derivatives, wherein R1 and R2 are optional substituents and independently represent C1-6 alkyl, C2-6 alkenyl, optionally substituted by CO2H or CO2(C1-6 alkyl), C2-6 alkynyl, halogen, C1-3 perfluoroalkyl, (CH2)mAr1, (CH2)mHet1, (CH2)mCONR7R8, (CH2)mCO2R8, O(CH2)qCO2R8, (CH2)mCOR8, (CH2)mOR8, O(CH2)pOR8, (CH2)mNR7R8, CO2(CH2)qNR7R8, (CH2)mCN, S(O)nR8, SO2NR7R8, CONH(CH2)mAr1 or CONH(CH2)mHet1; R3 represents H, C1-6 alkyl, (CH2)pNR9R10, SO2R10, SO2NR9R10, (CH2)mCO2R10, C2-6 alkenyl, C2-6 alkynyl, (CH2)mCONR9R10, (CH2)mCO2R10, (CH2)pCN, (CH2)pR10 or (CH2)pOR10; R4 represents H or C1-6 alkyl; R5 represents H or OH; R6 represents phenyl optionally fused to a herterocyclic ring, the group as a whole being optionally substituted; R7-10 are fully defined herein and may independently represent Ar2 or Het2; Z represents CO2H, CONH(tetrazol-5-yl), CONHSO2O(C1-4 alkyl), CO2Ar3, CO2(C1-6 alkyl), tetrazol-5-yl, CONHSO2Ar3, CONHSO2(CH2)qAr3 o

Abstract: 1

Abstract: The invention provides S-(+)-3-{1-(1,3-benzodioxol-5-yl)-2-[(2-methoxy-4-methylphenyl)sulfonylamino]-2-oxoethyl}-1-methyl-1H-indole-6-carboxylic acid, which is substantially free from its (R)-(−)-enantiomer, and pharmaceutically acceptable derivatives thereof. The compounds are useful in the treatment of inter alia acute renal failure, restenosis and pulmonary hypertension.

Abstract: Compounds of formula (I): ##STR1## where the substituents are as defined herein, and salts thereof, are matrix metalloprotease inhibitors.

Abstract: Compounds of formula I, ##STR1## wherein X represents O or S(O).sub.m ;R.sup.1 and R.sup.2 independently represent phenyl, naphthyl or heteroaryl; each of which is optionally fused and optionally substituted;Y represents a bond, O, (CH.sub.2).sub.n, O(CH.sub.2).sub.n, (CH.sub.2).sub.n O, or CH(C.sub.1-6 alkyl)O;R.sup.3 represents H or C.sub.1-6 alkyl;m represents 0, 1, or 2; andn represents 1, or 2;and pharmaceutically acceptable salts thereof, are useful in therapy, in particular in the treatment of restenosis, renal failure and pulmonary hypertension.

Abstract: Compounds of formula (I), and their pharmaceutically acceptable derivatives, wherein R.sup.1 and R.sup.2 are optional substituents and independently represent C.sub.1-6 alkyl, C.sub.2-6 alkenyl [optionally substituted by CO.sub.2 H or CO.sub.2 (C.sub.1-6 alkyl)], C.sub.2-6 alkynyl, halogen, C.sub.1-3 perfluoroalkyl, (CH.sub.2).sub.m Ar.sup.1, (CH.sub.2).sub.m Het.sup.1, (CH.sub.2).sub.m CONR.sup.7 R.sup.8, (CH.sub.2).sub.m CO.sub.2 R.sup.8, O(CH.sub.2).sub.q CO.sub.2 R.sup.8, (CH.sub.2).sub.m COR.sup.8, (CH.sub.2).sub.m OR.sup.8, O(CH.sub.2).sub.p OR.sup.8, (CH.sub.2).sub.m NR.sup.7 R.sup.8, CO.sub.2 (CH.sub.2).sub.q NR.sup.7 R.sup.8, (CH.sub.2).sub.m CN, S(O).sub.n R.sup.8, SO.sub.2 NR.sup.7 R.sup.8, CONH(CH.sub.2).sub.m Ar.sup.1 or CONH(CH.sub.2).sub.m Het.sup.1 ; R.sup.3 represents H, C.sub.1-6, alkyl, (CH.sub.2).sub.p NR.sup.9 R.sup.10, SO.sub.2 R.sup.10, SO.sub.2 NR.sup.9 R.sup.10, (CH.sub.2).sub.m COR.sup.10, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, (CH.sub.2).sub.m CONR.sup.9 R.sup.10, (CH.sub.2).sub.

Abstract: Compounds of formula (I): ##STR1## and pharmaceutically acceptable salt and biolabile esters thereof, wherein R.sup.1 is H, C.sub.1 -C.sub.4 alkyl, phenyl optionally substituted by up to three substituents independently selected from C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, halogen and CF.sub.3, or is 1-imidazolyl, 3-pyridyl or 4-pyridyl; R.sup.2 is H or C.sub.1 -C.sub.4 alkyl, R.sup.3 is SO.sub.2 R.sup.4 or COR.sup.4 where R.sup.4 is C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.3 perfluoroalkyl(CH.sub.2).sub.p, C.sub.3 -C.sub.6 cycloalkyl(CH.sub.2).sub.p, aryl(CH.sub.2).sub.p, or heteroaryl(CH.sub.2).sub.p, p being 0, 1 or 2, or R.sup.4 may be NR.sup.5 R.sup.6 where R.sup.5 is H or C.sub.1 -C.sub.4 alkyl and R.sup.6 is C.sub.1 -C.sub.6, alkyl, C.sub.3 -C.sub.6 cycloalkyl or aryl, or R.sup.5 and R.sup.

Abstract: Compounds of formula: ##STR1## or a biolabile ester thereof, or a pharmaceutically acceptable salt of either,whereinR.sup.1, R.sup.2, R.sup.3 and R.sup.4 are each independently selected from H or C.sub.1 -C.sub.4 alkyl;R.sup.5 is (CH.sub.2).sub.m SO.sub.2 R.sup.6, (CH.sub.2).sub.m NHSO.sub.2 R.sup.6 or (CH.sub.2).sub.m NHCOR.sup.7 ;R.sup.6 and R.sup.7 are C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.3 perfluoroalkyl-(CH.sub.2).sub.n, C.sub.3 -C.sub.6 cycloalkyl(CH.sub.2).sub.n, aryl(CH.sub.2).sub.n or heteroaryl(CH.sub.2).sub.n ; orR.sup.6 is NR.sup.8 R.sup.9 ;R.sup.8 is H or C.sub.1 -C.sub.4 alkyl;R.sup.9 is C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl(CH.sub.2).sub.n, aryl(CH.sub.2).sub.n or heteroaryl(CH.sub.2).sub.n ; orR.sup.8 and R.sup.9 together with the nitrogen atom to which they are attached from a 5- to 7-membered heterocyclic ring;X is CH.sub.2, CHCH.sub.3, C(OH)CH.sub.3, C.dbd.CH.sub.2 or O;m is 0 or 1;n is 0, 1, 2 or 3; andHet is 3- or 4-pyridyl or 1-imidazolyl;are combined thromboxane A.sub.