Patent ID: 6197794
Filing Date: 2001-03-06
Classification: A61K,A61P,C07K

Abstract:
A compound of formula (1): ##STR7##whereinR.sup.1 is a hydrogen atom or an optionally substituted cycloaliphatic, polycycloaliphatic, heterocycloaliphatic, polyheterocycloaliphatic, aromatic or heteroaromatic group;Alk.sup.1 and Alk.sup.2, which may be the same or different, is each an optionally substituted aliphatic or heteroaliphatic chain;L.sup.1 is a linker atom or group;r, s, t and u is each zero or an integer 1;Alk.sup.3 is a straight or branched 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 hydrogen atom or a straight or branched alkyl group;A is a chain {C(R.sup.7)(R.sup.8)}.sub.p Y{C(R.sup.9 (R.sup.10)}.sub.q -- in which Y is a sulphur atom or a --SO-- or --S(O).sub.2 -- group, R.sup.7, R.sup.8, R.sup.9 an R.sup.10, which may be the same or different is each a hydrogen atom or a straight or branched alkyl or optionally substituted aromatic group, or R.sup.7 and R.sup.8, together with the carbon atom to which they are attached, or R.sup.9 and R.sup.10, together with the carbon atom to which they are attached, each forms a C.sub.1-7 cycloalkyl 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;L.sup.1 is a linker group selected from --C(O)--, --C(O)O--, --C(S)--, --S(O).sub.2 --, --CON(R.sup.11)--, (where R.sup.11 is a hydrogen atom or a straight or branched alkyl group), --CSN(R.sup.11)--, --SON(R.sup.11)-- or --SO.sub.2 N(R.sup.11)--;R.sup.2 and R.sup.3, which may be the same or different is each an atom or group, --L.sup.3 (CH.sub.2).sub.p L.sup.4 (R.sup.2a), in which L.sup.3 and L.sup.4 is each a covalent bond or a linker atom or group, p is zero or the integer 1, q is an integer 1, 2, or 3 and R.sup.2a is a hydrogen or halogen atomn or a group selected from straight or branched alkyl, --OR.sup.12 (where R.sup.12 is a hydrogen atom or an optionally substituted straight or branched alkyl group), --SR.sup.12, NR.sup.12 R.sup.13 (where R.sup.13 is as just defined for R.sup.12 and may be the same or different), --NO.sub.2, --CN, CO.sub.2 R.sup.12, SO.sub.3 H, --SO.sub.2 R.sup.12, --OCO.sub.2 R.sup.12, --CON.sup.12 R.sup.13, --OCONR.sup.12 R.sup.13, --CSNR.sup.12 R.sup.13, --COR.sup.12, --N(R.sup.12)COR.sup.13, --N(R.sup.12)CSR.sup.13, --SO.sub.2 N(R.sup.12)(R.sup.13), --N(R.sup.12)SO.sub.2 R.sup.13, --N(R.sup.12)CON(R.sup.13)(R.sup.14), (where R.sup.14 is a hydrogen atom or an optionally substituted straight or branched alkyl group), --N(R.sup.12)CSN(R.sup.13)(R.sup.14) or --N(R.sup.12)SO.sub.2 N(R.sup.13)(R.sup.14);R is a carboxylic acid or a derivative thereof;R.sup.6 is a hydrogen atom or an optionally substituted cycloaliphatic, polycycloaliphatic, heterocycloaliphatic, polyheterocycloaliphatic, aromatic or heteroaromatic group, provided that:(1) when --R.sup.1 (Alk.sup.1).sub.r (L.sup.1).sub.s is --R.sup.1 (Alk.sup.1).sub.r O--, --R.sup.1 (Alk.sup.1).sub.r C(O)O--, --R.sup.1 (Alk.sup.1).sub.r NHC(O)O-- or --R.sup.1 (Alk.sup.1).sub.r S(O).sub.2 O--, (in which R.sup.1 is a hydrogen atom or an optionally substituted aromatic group and Alk.sup.1 is an optionally substituted alkyl group) and R.sup.6 (Alk.sup.2).sub.u (L.sup.2).sub.t -- is R.sup.6 (Alk.sup.2).sub.u CO--, R.sup.6 (Alk.sup.2).sub.u C(O)O--, R.sup.6 (Alk.sup.2).sub.u NHCO-- or R.sup.6 (Alk.sup.2).sub.u S(O).sub.2 -- (in which Alk.sup.2 is an optionally substituted alkyl chain), then R.sup.6 is an optionally substituted cycloaliphatic, polycycloaliphatic, heterocycloaliphatic or heteroaromatic group, and(2) Alk.sup.2, when present, is not a --(CH.sub.2).sub.n S--, --(CH.sub.2).sub.n SS-- or --(CH.sub.2).sub.n SC(O)-- chain, where n is an integer 1, 2 or 3;when A is a sulphur atom, m, p, q, r and s are 1 R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are H, and Alk.sup.3 is CH, R.sup.1 is not H:and the salts, solvates and hydrates thereof.