ACETYLENYL-PYRAZOLE-PYRIMIDINE DERIVATIVES AS mGluR2 ANTAGONISTS Russian patent published in 2011 - IPC C07D487/04 C07D471/04 A61K31/519 A61K31/4745 A61K31/5025 A61P25/28 A61P25/18 

FIELD: chemistry.

SUBSTANCE: invention relates to novel acetylenyl-pyrazole-pyrimidine derivatives of general formula (I), having mGluR2 (metabotropic glutamate receptor) antogonist properties). In compounds of general formula (I): either E and J denote N, G denotes C and L denotes N, M denotes CH, or M denotes N, L denotes CH; or L and G denote N, E denotes C, and J and M denote CH; or J, G and L denote N, E denotes C, and M denotes CH; or E and L denote N, J and M denote CH, and G denotes C; R¹ denotes H, halogen, CF₃, CHF₂ or C₁-₆alkyl; R² denotes H, halogen, C₁-₆-alkyl, C₁-₆-alkoxy, CF₃ or CHF₂, wherein R¹=R²≠H; R³ denotes H; -C(CH₃)₂OH; linear C₁-₄-alkyl or C₃-₄-cycloalkyl, which are possibly substituted with one or more substitutes selected from a group comprising 1-3 F and 1-2 OH; A is selected from a group comprising phenyl or a 5- or 6-member heteroaryl having in the ring 1-2 heteroatoms selected from nitrogen, sulphur or nitrogen and sulphur in the 5-member ring, and 1-2 nitrogen atoms i the 6-member ring, and possibly substituted with 1-3 R^a; R^a denotes halogen; hydroxy; cyano; CF₃; NR^eR^f; C₁-C₆-alkyl, possibly substituted amino or hydroxy; ; C₁-₆-alkoxy; C_3-4-cycloalkyl; CO-NR^bR^c, SO₂-NR^bR^c; or SO₂-R^d-; R^b and R^C can be identical or different and are selected from a group comprising H; normal or branched C_1-6-alkyl, possibly substituted with one or more substitutes selected from a group comprising F, cyano, hydroxy, C₁-₆-alkoxy, -NH-C(O)-O-C₁-₆-alkyl, amino, (C₁-₆-alkyl)amino, di(C₁-₆-alkyl)amino, heterocycloalkyl having 6 ring atoms, from which 1-2 heteroatoms are selected from nitrogen or nitrogen and oxygen, or a 6-member heteroaryl with one nitrogen heteroatom in the ring; or a 6-membeer heteroaryl with one nitrogen heteroatom in the ring; or R^b and R^c, together with the nitrogen atom with which they are bonded, can form a heterocyclic ring having 6 members in the ring, from which 1-2 atoms are selected from nitrogen and/or oxygen, and which can be substituted with C₁-₆-alkyl; R^d denotes OH or C₁-₆-alkyl; R^e and R^f denote H, C₁-₆-alkyl, possibly substituted hydroxy, -C(O)- C₁-₆-alkyl; S(O)₂-C₁-₆-alkyl.

EFFECT: compounds can be used in preparing medicinal agents for treating central nervous system (CNS) disorders, such as Huntington's chorea, amyotrophic lateral sclerosis, dementia caused by AIDS, parkinsonism etc.

55 cl, 6 dwg, 321 ex