申请人:Kokotos George
公开号:US20110136879A1
公开(公告)日:2011-06-09
The invention provides compounds of formula (I)
wherein X is O or S;
R
1
is H, OH, SH, nitro, NH
2
, NHC
1-6
alkyl, N(C
1-6
alkyl)
2
, halo, haloC
1-6
alkyl, CN, C
1-6
-alkyl, OC
1-6
alkyl, C
1-6
alkylCOOH, C
1-6
alkylCOOC
1-6
alkyl, C
2-6
-alkenyl, C
3-10
cycloalkyl, C
6-10
aryl, C
1-6
alkylC
6-10
aryl, heterocyclyl, heteroaryl, CONH
2
, CONHC
1-6
alkyl, CON(C
1-6
alkyl)
2
, OCOC
1-6
alkyl, or is an acidic group, such as a group comprising a carboxyl, phosphate, phosphinate, sulfate, sulfonate, or tetrazolyl group;
R
2
is as defined for R
1
or R
1
and R
2
taken together can form a 6-membered aromatic ring optionally substituted by up to 4 groups R
5
;
R
3
is H, halo (preferably fluoro), or CHal
3
(preferably CF
3
),
each R
5
is defined as for R
1
;
V
1
is a covalent bond or a C
1-20
alkyl group, or C
2-20
-mono or multiply unsaturated alkenyl group; said alkyl or alkenyl groups being optionally interupted by one or more heteroatoms selected from O, NH, N(C
1-6
alkyl), S, SO, or SO
2
;
M
1
is absent or is a C
5-10
cyclic group or a C
5-15
aromatic group; and
R
4
is H, halo, OH, CN, nitro, NH
2
, NHC
1-6
alkyl, N(C
1-6
alkyl)
2
, haloC
1-6
alkyl, a C
1-20
alkyl group, or C
2-20
-mono or multiply unsaturated alkenyl group, said C
1-20
alkyl or C
2-20
alkenyl groups being optionally interupted by one or more heteroatoms selected from O, NH, N(C
1-6
alkyl), S, SO, or SO
2
;
with the proviso that the group V
1
M
1
R
4
as a whole provides at least 4 backbone atoms from the C(R
3
) group;
or a salt, ester, solvate, N-oxide, or prodrug thereof; for use in the treatment of a chronic inflammatory condition.