ESTER DERIVATIVE OF 2-AMINO-BICYCLO[3,1,0]HEXANE-2,6-DICARBOXYLIC ACID, WITH ANTAGONISTIC PROPERTIES TOWARDS P-GROUP METABOTROPIC GLUTAMATE RECEPTORS Russian patent published in 2009 - IPC C07C229/50 C07D307/88 C07D317/40 A61K31/215 A61K31/341 A61K31/343 A61P25/00 A61P25/18 A61P25/28 A61P25/30 

FIELD: chemistry.

SUBSTANCE: present invention pertains to new ester derivatives of 2-amino-bicyclo[3,1,0]hexane-2,6-dicarboxylic acid, with formula [I] or [II] and their pharmaceutical salts, with antagonistic properties towards II group metabotropic glutamate receptors. In general formulae [I] or [II] R¹ and R² are identical or different, and each stands for a C_1-10alkyl group, or one of R¹ or R² is a hydrogen atom, and the other is a C_1-10alkyl group, C_2-10alkenyl group, C_2-10alkynyl group, C_1-10alkyl group, substituted with a phenyl group, possibly substituted with halogen atoms, C_1-4alkyl group, C_1-4 alkoxyl group; hydroxyC_2-10alkyl group, halogenC_1-10alkyl group, azidoC_1-10alkyl, aminoC_2-10alkyl, C_1-10alkoxycarbonylC_1-10alkyl group, farnesyl group, 4-morpholinyl-C_1-10alkyl group, C_1-10alkyl group, substituted with a group with formula -C(O)NR^aR^b (where R^a and R^b are identical or different and each represents a hydrogen atom or a C_1-10alkyl group), or with a group with formula -CHR^cOC(O)ZR^d (where Z is an oxygen atom or a single bond; R^c represents a hydrogen atom, C_1-10alkyl group or aryl group, chosen from phenyl and naphthyl, which can be substituted with a C_1-4alkyl group or C_1-4alkoxyl group), or substituted with a group with formula [i] [ii], (where R^d denotes the same as described above), or by a group with formula [ii]; X is a fluorine atom; and Y represents -OCHR³R⁴, -SR³, -S(O)_nR⁵, -SCHR³R⁴, -NHCHR³R⁴, -N(CHR³R⁴)(CHR^3'R^4'), -NHCOR³ or -OCOR⁵ (where R³, R^3', R⁴ and R^4' are identical or different, and each represents a hydrogen atom, C_1-10alkyl group, phenyl group, naphthyl group, phenyl group substituted with one-five substitutes, chosen from a group, consisting of a halogen atom, R⁵ represents a phenyl group, or a phenyl group substituted with one-five substitutes, chosen from a group, consisting of a halogen atom, and n is 1 or 2).

EFFECT: invented compounds can be used in treating and preventing mental illnesses, such as schizophrenia, anxiety and anxiety related diseases, depression, bipolar disorders and epilepsy, invention also pertains to a medicinal preparation.

30 cl, 5 tbl, 19 ex