NEW PYRAZOLE-3-CARBOXAMIDE DERIVATIVE POSSESSING ANTAGONIST ACTIVITY ON 5-НТ RECEPTOR Russian patent published in 2014 - IPC C07D401/14 C07D403/14 C07D413/12 C07D413/14 C07D417/14 C07D471/04 C07D487/04 C07D401/04 C07D403/04 C07D403/12 A61K31/4155 A61K31/4439 A61K31/4709 A61K31/5377 A61K31/5386 A61K31/553 A61P1/00 A61P3/04 A61P9/00 A61P11/00 A61P17/02 A61P19/02 A61P25/00 A61P25/28 A61P29/00 A61P31/12 

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to compounds of formula (I), wherein A means morpholinyl, 1,4-oxazepamyl, piperidinyl, pyrrolidinyl or azetidinyl which is bound to N; R¹ means C₁-C₆-alkyl group; R² means bicyclic aryl group specified in 1H-indolyl, 1H-pyrrolo[3,2-b]pyridyl, quinolyl, naphthyl, 1H-pyrrolo[2,3-b]pyridyl, 5H-pyrrolo[3,2-d]pyrimidinyl, 7H-pyrrolo[2,3-d]pyrimidinyl, benzo[b]thiophenyl, imidazo[1,2-a]pyridyl, benzo[b]thiazolyl, 5H-pyrrolol[2,3-b]pyrazinyl and quinoxalinyl which can be substituted by R⁴; R³ means hydrogen or halogen atom; R⁴ means C₁-C₆-alkyl group, C₁-C₆-halogenalkyl group, OR^1A, halogen, -(CH₂)aOH, CN, NHCOR^1A, SO₂R^1A or NHSO₂R^1A; R⁵ means C₁-C₆-alkyl group, -(CH₂)aOH, -(CH₂)aOR^1B, halogen or CONH₂; provided p is a plural number, R⁵ can be identical or different, or R⁵ can be combined with another R⁵; each of R^1A and R^1B independently means C₁-C₆-alkyl group; a is equal to 0, 1 or 2; n is equal to 1 or 2; p is equal to 0, 1, 2, 3, 4 or 5. Besides, the invention refers to intermediate compounds of formulas (IA) and (IB) for preparing the compounds of formula (I), to a preventive or therapeutic agent containing the compounds of formula (I), pharmaceutical compositions, using the compounds of formula (I) and to a method for preventing or treating diseases.

EFFECT: compounds of formula (I) as selective 5-HT_2B receptor antagonists.

11 cl, 1 dwg, 18 tbl, 88 ex