PYRAZOLEPYRIDINE DERIVATIVES Russian patent published in 2015 - IPC C07D471/04 A61K31/437 A61P25/18 

FIELD: medicine, pharmaceutics.

SUBSTANCE: claimed invention relates to compound of formula

,

where R¹ represents hydrogen atom, lower alkyl, lower alkyl, substituted with halogen atom, benzyl, -C(O)-lower alkyl, -C(O)-CH₂-lower alkoxy, -C(O)-C_3-6-cycloalkyl, -(CH₂)_o-C(O)-NR,R', -(CH₂)_oS(O)₂-lower alkyl or -S(O)₂-NR,R'; o is equal 0 or 1; R, R' represent independently on each other hydrogen atom or lower alkyl or can form together with atom N, which they are bound to, 5- or 6-membered hetercycloalkyl ring; R² represents hydrogen atom or lower alkyl; R³ represents halogen atom, lower alkoxy, lower alkyl, substituted with halogen atom, or lower alkoxy, substituted with halogen atom; and they can be similar or different in case, when n is equal 2; n is equal 1 or 2; Ar represents phenyl, optionally substituted with one or two substituents, selected from lower alkyl, halogen atom, lower alkoxy, lower alkyl substituted with hydroxyl or cyano, or represents five- or six-membered heteroaryl group, selected from thiophenyl or pyridinyl, which is optionally substituted with lower alkyl or halogen atom; or to its pharmaceutically acceptable acid addition salt. Invention also relates to pharmaceutical composition, application of compound and method of treating positive and negative symptoms in case of schizophrenia.

EFFECT: formula I compounds demonstrate high affinity simultaneously with both receptors NK1 and NK3 (double antagonists of receptors NK1/NK3), useful in treatment of schizophrenia.

13 cl, 1 tbl, 38 ex