Patent ID: 6265397
Filing Date: 2001-07-24
Classification: A61P,C07D

Abstract:
A compound of formula I, ##STR28##whereinR.sup.1 represents OR.sup.1d ;R.sup.1d represents H, C(O)R.sup.11, SiR.sup.12 R.sup.13 R.sup.14 or C.sub.1-6 alkyl, which latter group is optionally substituted or terminated by one or more substituents selected from OR.sup.15 or (CH.sub.2).sub.q R.sup.16 ;R.sup.12, R.sup.13 and R.sup.14 independently represent H, phenyl or C.sub.1-6 alkyl;R.sup.16 represents C.sub.1-4 alkyl, phenyl, OH, C(O)OR.sup.17 or C(O)N(H)R.sup.18 ;R.sup.18 represents H, C.sub.1-4 alkyl or CH.sub.2 C(O)OR.sup.19 ;R.sup.15 and R.sup.17 independently represent H, C.sub.1-6 alkyl or C.sub.1-3 alkylphenyl;R.sup.11 and R.sup.19 independently represent H or C.sub.1-4 alkyl; andq represents 0, 1 or 2;R.sub.x represents a structural fragment of formula IIa, IIb or IIc, ##STR29##whereinthe dotted lines independently represent optional double bonds;A and B independently represent O or S, CH or CH.sub.2 (as appropriate), or N or N(R.sup.21) (as appropriate);D represents --CH.sub.2 --, O, S, N(R.sup.22), --(CH.sub.2).sub.2 --, --CH.dbd.CH--, --CH.sub.2 N(R.sup.22)--, --N(R.sup.22)CH.sub.2 --, --CH.dbd.N--, --N.dbd.CH--, --CH.sub.2 O--, --OCH.sub.2 --, --CH.sub.2 S-- or --SCH.sub.2 --;X.sub.1 represents C.sub.2-4 alkylene; C.sub.2-3 alkylene interrupted by Z; --C(O)--Z--A.sup.1 ; --Z--C(O)--A.sup.1 --; --CH.sub.2 --C(O)--A.sup.1 ; --Z--C(O)--Z--A.sup.2 --; --CH.sub.2 --Z--C(O)--A.sup.2 --; --Z--CH.sub.2 --C(O)--A.sup.2 --; --Z--CH.sub.2 --S(O).sub.m --A.sup.2 --; --CH.sub.2 --Z--S(O).sub.m --A.sup.2 --; --C(O)--A.sup.3, --Z--A.sup.3 --; or --A.sup.3 --Z--;X.sub.2 represents C.sub.2-3 alkylene, --C(O)--A.sup.4 -- or --A.sup.4 --C(O)--X.sub.3 represents CH or N;X.sub.4 represents a single bond, O, S, C(O), N(R.sup.23), --CH(R.sup.23)--, --CH(R.sup.23)--CH(R.sup.24)-- or --C(R.sup.23).dbd.C(R.sup.24)--;A.sup.1 represents a single bond or C.sub.1-2 alkylene;A.sup.2 represents a single bond or --CH.sub.2 --;A.sup.3 represents C.sub.1-3 alkylene;A.sup.4 represents C(O) or C.sub.1-2 alkylene;Z represents, at each occurrence, O, S(O).sub.m or N(R.sup.25);m represents, at each occurrence, 0, 1 or 2;R.sup.2 and R.sup.4 independently represent one or more optional substituents selected from C.sub.1-4 alkyl (which latter group is optionally substituted by one or more halo substituent), C.sub.1-4 alkoxy, methylenedioxy, halo, hydroxy, cyano, nitro, SO.sub.2 NH.sub.2, C(O)OR.sup.26 or N(R.sup.27)R.sup.28 ;R.sup.3 represents an optional substituent selected from OH or C.sub.1-4 alkoxy; R.sup.21, R.sup.22, R.sup.23, R.sup.24, R.sup.25, R.sup.26, R.sup.27 and R.sup.28 independently represent H or C.sub.1-4 alkyl;Y represents CH.sub.2 ;R.sup.y represents H or C.sub.1-4 alkyl;n represents 0, 1, 2, 3 or 4; andB represents a structural fragment of formula IIIa or IIIc ##STR30##whereinX.sup.5, X.sup.6, X.sup.7 and X.sup.8 independently represent CH, N or N--O; and R.sup.31 represents an optional substituent selected from halo and C.sub.1-4 alkyl; or a pharmaceutically acceptable salt thereof;provided that:(a) in formula IIa, A and B do not both represent O or S;(b) in formula IIa, B and D do not both represent O or S;(c) when X.sub.1 represents --C(O)--Z--A.sup.1,--Z--CH.sub.2 S(O).sub.m --A.sup.2 --, --CH.sub.2 --Z--S(O).sub.m --A.sup.2 or --Z--C(O)--Z--A.sup.2, then A.sup.1 or A.sup.2 (as appropriate) do not represent a single bond; and(d) when X.sub.4 represents --CH(R.sup.23)--, R.sup.1 does not represent OH.