N-(INDOLCARBONYL)PIPERAZINE DERIVATIVES, METHODS FOR PRODUCTION THE SAME, PHARMACEUTICAL COMPOSITION, AND COMPOUNDS Russian patent published in 2005 - IPC

FIELD: organic chemistry, pharmaceutical compositions.

SUBSTANCE: invention relates to N-(indolcarbonyl)piperazine derivatives of general formula I

, wherein R¹ is optionally substituted phenyl or naphthyl; R² and R³ are independently Hal or Het¹, A, OA, CN; R⁴ is H, CN, acyl, Hal, CONH₂, CONHA or CONA; R¹ is H; or R⁴ and R⁵ together form C₃-C₅-group; Het¹ is aromatic heterocyclic ring, optionally substituted with one or two halogen atoms and containing 1-3 similar or different heteroatoms such as nitrogen, sulfur and oxygen, A-(C₁-C₆)-alkyl; Hal is F, Cl,Br, and J; and indole ring may be substituted with isatin, except for (1H-indole-5-yl)-(4-phenethylpiperazine-1-yl)-methanone and 1-((5-methoxy-1H-indole-7-yl)-carbonyl)-4-(2-phenethyl)-piperazine. Claimed compounds are potent 5-HT_2A antagonists and are useful in treatment of psychosis, schizophrenia, depression, neurological diseases, dismepodia, Parlinson's disease, Alzheimer's disease, Hungtington's disease, amyotrophic lateral sclerosis, bulimia or anorexia, premenstrual syndrome, and/or in alleviation of hypomania.

EFFECT: new pharmaceutical agents.

9 cl, 10 ex, 1 tbl