W0 2011/000721 A1 I||||||||||||||||||||||||||||||||||||||||||||||||||||||||| - Questel

heterocyclic ring or heteroaromatic ring refer to cycles, cyclic ring or aromatic
ring, respectively, which comprise one or more heteroatoms. For instance,
heterocycle or heterocyclic ring include tetrahydrofuran, tetrahydrothiophene,
pyrrolidine, imidazolidine, pyrazolidine, while heteroaromatic rings include, for
instance, furan, thiophene, pyrrole, imidazole, pyridine, pyrimidine, oxazole,
isoxazole, pyrazole, triazole etc.
According to an embodiment of the invention, preferred compounds are those
of formula (I) above, wherein R 1 is H, M is -0-CH 2 -CH 2 -NH-, a is 1 and Y is a
succinic acid residue.
According to a more preferred embodiment, in particular, the compounds of the
invention are those wherein R 2 is methoxy (-OCH 3 ) or is -NH-R 3 , wherein R 3 is
an A group selected among cyclopropan, cyclohexil, phenyl, benzyl or benzyl
meta or para substituted with methoxy (-OCH 3 ), nitro (-NO 2 ), carboxy (-COOH),
methylester (-COOCH 3 ), hydroxymethyl (-CH 2 -OH), methyl (-CH 3 ), methoxy (-
OCH 3 ), amino (-NH 2 ), isopropyl (-CH(CH 3 ) 2 ) or R 3 is 1,3-thiazole or methyl
substituted 1,3-thiazole; alternatively, R 3 is a methyl group (-CH 3 ) substituted
with the above mentioned A groups.
Thus, the preferred X moieties are those of the following Table I :
Table I