Abstract: Phenylalanine derivatives of formula (1) are described: 1

Abstract: Phenylalanine derivatives of formula (1) are described: in which: Ar1 is an aromatic or heteroaromatic group; L1 is a linker atom or group; R is a carboxylic acid or a derivative thereof; Ar2 is an optionally substituted aromatic or heteroaromatic group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of &agr;4 integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders.

Abstract: Compounds of formula (1) are described: wherein L1 is a covalent bond or a linker atom or group; R is a carboxylic acid (—CO2H) or a derivative threof; R6 and R7 which may be the same or different is each an atom or group —L2(Alk2)tL3R12 in which L2, L3, Alk2 and t are as previously defined and R12 is a hydrogen or halogen atom or an —OR9, —NR9R10, —NO2, —CN, —CO2R9, —CONR9R10, —COR9, —N(R9)COR10, —N(R9)CSR10, —SO2N(R9)(R10), —N(R9)SO2R9, —N(R9)CON(R10)(R11), —N(R9)CSN(R10)(R11), —N(R9)SO2N(R10)(R11), or an optionally substituted aliphatic, heteroaliphatic, cycloaliphatic, heterocycloaliphatic, aromatic or heteroaromatic group provided that R6 and R7 are not both hydrogen atoms and when R7 is a hydrogen atom then R4 and R5 is each a hydrogen or halogen atom or an alkyl, alkoxy or nitro group; and the salts, solvates, hydrates and N-oxides thereof, for use in modulating cell adhesion.

Abstract: Phenylalanine derivatives of formula (1) are described: wherein R is a carboxylic acid or a derivative thereof; L1 is a linker atom or group; Het is an optionally substituted heteroaromatic group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of alpha4 integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders.

Abstract: Propanoic acid derivatives of formula (1) are described: Ar—X1—Ar1—Z—R  (1) in which Ar is a nitrogen base containing group; X1 is linker atom or group; Ar1 is an optionally substituted 5- or 6-membered nitrogen-containing aromatic or non-aromatic monocycle; Z is a group —CH(R13)CH2— [in which R13 is an optionally substituted aliphatic, cycloaliphatic, heteroaliphatic, heterocycloaliphatic, aromatic or heteroaromatic group], —C(R12a)(R13)—CH(R12b)— [in which R12a and R12b together with the carbon atoms to which they are attached form a C3-7cycloalkyl group] or C(R13)═CH—; R is a carboxylic acid (—CO2H) or a derivative or biostere thereof; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of &agr;V integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders.

Abstract: Compounds of general formula (1): 1

Abstract: Compounds of the general formula (1) are described wherein W is a ═N—, and Z and L are described in the specifications. These compounds are phosphodiesterase type IV inhibitors and are useful in the prophylaxis and treatment of diseases such as asthma where an unwanted inflammatory response or muscular spasm is present.

Abstract: Squaric acid derivatives of formula (1) are described: 1

Abstract: Benzodiazapine derivatives of formula (1) are described: wherein Ar1 is an aromatic or heteroaromatic group; L1 is a linker atom or group; Ar2 is an optionally substituted aromatic or heteroaromatic group; R5 is a carboxylic acid (—CO2H) or a derivative thereof; The compounds are able to inhibit the binding of alpha 4 integrins to their ligands and are of use in the prophylaxis and treatment of immune in inflammatory disorders.

Abstract: Compounds of general formula (1) are described: wherein ═W— is (1) ═C(Y)— where Y is a halogen atom, or an alkyl or —XRa group where X is —O—, —S(O)m— [where m is zero or an integer of value 1 or 2], or —N(Rb)— [where Rb is a hydrogen atom or an optionally substituted alkyl group] and Ra is a hydrogen atom or an optionally substituted alkyl group or, (2) ═N—; L is (1) a —C(R)═C(R1)(R2) or [—CH(R)]nCH(R1)(R2) group; is (2) a —(Xa)nAlk′Ar′, or Alk′XaAr′ group; or is (3) XaR1; Z is a group (A), (B), (C) or (D):  wherein Ar is a monocyclic or bicyclic aryl group optionally containing one or more heteroatoms selected from oxygen, sulphur or nitrogen atoms; Z1is a group —NR12C(O)— [where R12 is a hydrogen atom or an optionally substituted alkyl or (Alk)tAr group], —C(O)NR12—, —NR12

Abstract: Compounds of the general formula (1) wherein: ═W— is ═N—; Y is halogen or an alkyl or —XRa group; X is —O—, —S(O)m— or —N(Ra)—, where m is zero or an integer 1 or 2; Ra is hydrogen or an optionally substituted alkyl group; R2 is an optionally substituted cycloalkyl or cycloalkenyl group; R3 is R13 or —L1R13, where R13 is a halogen atom, an optionally substituted straight or branched chain C2-6alkenyl group or an optionally substituted C6-12 monocyclic or bicyclic aryl group and L1 is an optionally substituted straight or branched chain C1-6alkylene, C2-6alkenylene or C2-6alkynylene group; R4 is a hydrogen atom or a group —(CH2)nAr where Ar is an optionally substituted monocyclic aryl group and n is zero or an integer 1, 2 or 3; R5 is hydrogen; R6 is an optionally substituted 2-, 3- or 4-pyridyl group; and each of R7 and R8 is independently hydrogen or an optionally substituted straight or branched alkyl group.

Abstract: Phenylalanine derivatives of formula (1) are described: in which L1 is a linker atom or group; A is a chain —[C(R7)(R8)]pY[C(R9)(R10)]q— in which Y is a sulphur atom or a —S(O)— or —S(O)2— group, R7, R8, R9 and R10, which may be the same or different, is each a hydrogen atom or a straight or branched alkyl or optionally substituted aromatic group, or R7 and R8 together with the carbon atom to which they are attached, or R9 and R10 together with the carbon atom to which they are attached, each forms a C3-7cycloalkyl group, and p and q, which may be the same or different, is each zero or an integer 1 or 2, provided that when one of p or q is zero the other is an integer 1 or 2; L2 is a linker group selected from —C(O)—, —C(O)O—, —C(S)—, —S(O)2—, —CON(R11)—, [where R11 is a hydrogen atom or a straight or branched alkyl group], —CSN(R11)—, —SON(R11)&m

Abstract: Aromatic amines of formula (1) are described: ##STR1## wherein Az is an optionally substituted monocyclic six-membered nitrogen-containing aromatic group;L.sup.1 is a linker atom or group;R is a carboxylic acid or a derivative thereof;and R.sup.5 is a group --L.sup.2 (CH.sub.2).sub.t R.sup.6 in which L.sup.2 is a --N(R.sup.7)CO-- or --N(R.sup.7)CS-- group.The compounds are able to inhibit the binding of .alpha..sub.4 integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders.

Abstract: Tyrosine derivatives of formula (1) are described: ##STR1## in which R is (1) a group R.sup.1 X.sup.1 -- where R.sup.1 is an optionally substituted alkyl or aromatic group, and X.sup.1 is a covalent bond or a --(CH.sub.2).sub.n -- [where n is an integer 1 or 2], --C(O)--, --CH.sub.2 C(O)--, --NHC(O)--, --CH.sub.2 NHC(O)--, or --SO.sub.2 -- group, or (2) a group (Hal.sup.1).sub.3 CSO.sub.2 --, where Hal.sup.1 is a fluorine or chlorine atom;R.sup.2 and R.sup.3, which may be the same or different, is each a hydrogen or halogen atom or an alkyl, alkoxy, hydroxyl or nitro group;Alk is an alkylene chain;m is zero or an integer 1;R.sup.4 is a hydrogen atom or a methyl group;R.sup.5 is a group --(CH.sub.2).sub.p CO.sub.2 R.sup.8 where p is zero or an integer 1 and R.sup.8 is a hydrogen atom or an alkyl group;R.sup.6 is a hydrogen atom or an alkyl group;Y is a sulphur atom or a --S(O).sub.q -- group where q is an integer 1 or 2;X.sup.2 is a --C(O)--, --C(O)O--, --CONH-- or --S(O).sub.2 -- group;R.sup.

Abstract: 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.

Abstract: Tri-substituted phenyl derivatives and processes for their preparation. In a preferred embodiment, the compounds have the general formula (1) ##STR1## wherein L may be --OR; Z may be --C(R.sup.3)(R.sup.4)--C(R.sup.5)(R.sup.6)(R.sup.7); R may be an optionally substituted cycloalkyl group; R.sup.3, R.sup.6 and R.sup.7 may be hydrogen; R.sup.4 may be --(CH.sub.2).sub.t --Ar--(L.sup.1).sub.n --Ar'; R.sup.5 may be --(CH.sub.2).sub.t Ar; Ar may be a monocyclic or bicyclic aryl or heteroaryl group; L.sup.1 may be a divalent linking group; and Ar' is Ar or an Ar containing group. Compounds of the invention may be potent and selective phosphodiesterase type IV inhibitors and are useful in the prophylaxis and treatment of various diseases, such as asthma, which are associated with an unwanted inflammatory response or muscular spasm.

Abstract: Compounds of general formula (1) ##STR1## are described wherein Y is a halogen atom or a group --OR.sup.1, where R.sup.1 is an optionally substituted alkyl group; X is --O--, --S-- or --N(R.sup.7)--, where R.sup.7 is a hydrogen atom or an alkyl group; R.sup.2 is an optionally substituted cycloalkyl or cycloalkenyl group; R.sup.3 and R.sup.4, which may be the same or different, is each a hydrogen atom or an alkyl, --CO.sub.2 R.sup.8 (where R.sup.8 is a hydrogen atom or an alkyl, aryl, or aralkyl group), --CONR.sup.9 R.sup.10 (where R.sup.9 and R.sup.10 which may be the same or different is each a hydrogen atom or an alkyl, aryl or aralkyl group), --CSNR.sup.9 R.sup.10, --CN, --CH.sub.2 CN group; Z is --(CH.sub.2).sub.n -- (where n is zero or an integer 1, 2 or 3; R.sup.5 is an optionally substituted monocyclic or bicyclic aryl group optionally containing one or more heteroatoms selected from oxygen, sulphur or nitrogen atoms; R.sup.

Abstract: Compounds of general formula (1) ##STR1## are described wherein Y is a halogen atom or a group --OR.sup.1, wherein R.sup.1 is an optionally substituted alkyl group; X is --O--, --S--, or --N(R.sup.6), wherein R.sup.6 is a hydrogen atom or an optionally substituted alkyl group; R.sup.2 is an optionally substituted cycloalkyl or cycloalkenyl group; R.sup.3 and R.sup.4, which may be the same or different, is each a hydrogen atom or an optionally substituted alkyl, --CO.sub.2 R.sup.7 (wherein R.sup.7 is a hydrogen atom, am optionally substituted alkyl, aralkyl, aryl, aryloxyalkyl, alkanoyloxyalkyl or aroyloxyalkyl group), --CONR.sup.8 R.sup.9 (where R.sup.8 and R.sup.9, which may be the same or different, is as defined for R.sup.7), --CSNR.sup.8 R.sup.9, --CN or --CH.sub.2 CN group; Z is --(CH.sub.2).sub.n -- where n is zero or an integer 1, 2 or 3; R.sup.

Abstract: Tri-substituted phenyl derivatives and pharmaceutical compositions containing them. In a preferred embodiment, the compounds have the general formula (2): ##STR1## wherein L is preferably --OR.sup.1 ; R.sup.a is preferably optionally substituted alkyl; R.sup.1 is preferably optionally substituted indanyl; R.sup.3 is preferably hydrogen, fluorine, hydroxy or an optionally substituted straight or branched chain alkyl group; R.sup.4 and R.sup.5 are preferably independently --(CH.sub.2).sub.t Ar, where t is zero or an integer 1, 2 or 3 wherein Ar is preferably optionally substituted monocyclic or bicyclic aryl or optionally substituted monocyclic or bicyclic heteroaryl; and R.sup.6 and R.sup.7 are preferably independently hydrogen, fluorine or optionally substituted alkyl.

Abstract: Compounds of the general formula (1) ##STR1## are described wherein Y is halogen or --OR.sup.1, where R.sup.1 is optionally substituted alkyl; X is --O--, --S-- or --N(R.sup.8)-, where R.sup.8 is hydrogen or alkyl; R.sup.2 is optionally substituted alkyl, alkenyl, cycloalkyl or cycloalkenyl; R.sup.3 is hydrogen, halogen or --OR.sup.9, where R.sup.9 is hydrogen or optionally substituted alkyl, alkenyl, alkoxyalkyl, or alkanoyl, or formyl, carboxamido or thiocarboxamido; R.sup.4 is --(CH.sub.2).sub.n Ar, where Ar is monocyclic or bicyclic aryl optionally containing one or more heteroatoms selected from oxygen, sulfur and nitrogen atoms, wherein Ar is substituted by an optionally substituted C.sub.3-9 cycloaliphatic group optionally containing one or more heteroatoms selected from oxygen, sulphur or --N(R.sup.8)-, and n is zero or an integer 1, 2 or 3; R.sup.5 is --(CH.sub.2).sub.