BENZOYLPIPERIDINE DERIVATIVES AS 5HT AND D RECEPTOR MODULATORS Russian patent published in 2010 - IPC C07D401/06 C07D413/06 C07D417/06 A61K31/505 A61P25/18 A61P25/24 A61P25/30 

FIELD: chemistry.

SUBSTANCE: invention relates to novel compounds of the formula (I) where: A is an aryl or a 5-member heteroaryl containing a S heteroatom, possibly substituted with one or two substitutes selected from a group consisting of halogen, C_1-6-alkyl or C_1-6-alkoxy; n equals 1 or 2; p equals 1, 2, 3 or 4; q equals 1; r equals 0 or 1; R¹ is C_2-6-alkynyl substituted with aryl, or C_1-6-alkyl possibly substituted with one-five substitutes selected from a group consisting of halogen, hydroxy, C_1-6-alkyl, C_1-6-halogenoalkyl, -OC(O)-C_1-6-alkyl, C_3-10-cycloalkyl, C_1-6-alkoxy, possibly substituted with one, two or three halogens or aryl, aryl which is possibly substituted with a halogen or C_1-6-alkoxy, 5-9-member heteroaryl, one, two or three ring atoms of which are heteroatoms selected from N or O, and the rest of the ring atoms are C atoms, possibly substituted with C_1-6-alkyl, and phenoxyl, or is C_1-6-alkoxy, or is C_3-10-cycloalkyl which is possibly substituted with one or more R^a, or is a 5- or 6-member heterocycloalkyl containing one, two or three heteroatoms selected from nitrogen, oxygen or sulphur, possibly substituted with one or more R^a, or is an aryl possibly substituted with one or more R^a, or is a 5-10-member heteraryl, one, two or three ring atoms of which are heteroatoms selected from N, O and S, and the rest of the ring atoms are C atoms, possibly substituted with one or more R^a, or is -NR^bR^c, where R^b is H or C_1-6-alkyl and where R^c is H, C_1-6-alkyl or aryl, possibly substituted with one or more R^a, where R^a is selected from: halogen, cyano, oxo, hydroxy, halogenobenzenesulfonyl, C_1-6-alkyl, possibly substituted with one, two or three substitutes selected from a group consisting of 5-10-member heterocycloalkyl and aryl, which is possibly substituted with halogen or C_1-6-alkoxy, C_1-6-halogenoalkyl, C_1-6-halogenoalkoxy, C_1-6-alkoxy, possibly substituted with aryl or 5-10-member heteroaryl, one, two or three ring atoms of which are heteroatoms selected from N, O and S, and the rest of the ring atoms are C atoms, which is possibly substituted with C_1-6-alkyl, aryloxy, -NH(CO)-C_1-6-alkyl, -O(CO)-C_1-6-alkyl, C_1-6-alkylsulfonyl, aryl, 4-6-member heterocycloalkyl containing one, two or three heteroatoms selected from nitrogen, oxygen or sulphur, possibly substituted with hydroxy, C_1-6-alkyl or oxo, 5-10-member heteroaryl,one, two or three ring atoms of which are heteroatoms selected from N and O, and the rest of the ring atoms are C atoms, possibly substituted with C_1-6-alkyl or oxo, and di(C_1-6)alkylamino; R² is H, OH, C_1-6-alkyl or halogen; as well as their pharmaceutically acceptable salts. The invention also relates to medicine and to use of the compounds in any of paragraphs 1-24.

EFFECT: obtaining novel biologically active compounds with affinity to dopamine D₃ receptor and to serotonin 5- HT_2a receptor.

27 cl, 86 ex