HETEROARYL PYRROLIDINYL AND PIPERIDINYL KETONE DERIVATIVES Russian patent published in 2013 - IPC C07D205/04 C07D207/08 C07D211/30 C07D401/06 C07D401/10 C07D403/06 C07D403/14 C07D405/06 C07D409/06 C07D417/14 C07D451/02 C07D487/04 A61K31/4523 A61K31/427 A61K31/416 A61K31/4709 A61K31/40 A61K31/4155 A61K31/4025 A61P25/00 

FIELD: chemistry.

SUBSTANCE: invention relates to a compound of formula I or use thereof to prepare a medicine for treating depression, anxiety or both: or pharmaceutically acceptable salts thereof, where m is 0-3; n is 0-2; Ar is: optionally substituted indolyl; optionally substituted indazolyl; azaindolyl; 2,3-dihydro-indolyl; 1,3-dihydro-indol-2-one-yl; optionally substituted benzothiophenyl; benzothiazolyl; benzisothiazolyl; optionally substituted quinolinyl; 1,2,3,4-tetrahydroquinolinyl; quinolin-2-one-yl; optionally substituted naphthalenyl; optionally substituted pyridinyl; optionally substituted thiophenyl or optionally substituted phenyl; R¹ is: C_1-6alkyl; hetero-C_1-6alkyl; halo-C_1-6alkyl; halo-C_2-6alkenyl; C_3-7cycloalkyl; C_3-7cycloalkyl-C_1-6alkyl; C_1-6alkyl-C_3-6cycloalkyl-C_1-6alkyl; C_1-6alkoxy; C_1-6alkylsulphonyl; phenyl; tetrahydropyranyl-C_1-6alkyl; phenyl-C_1-3alkyl, where the phenyl part is optionally substituted; heteroaryl-C_1-3alkyl; R² is: hydrogen or C_1-6alkyl; and each R^a and R^b is independently: hydrogen; C_1-6alkyl; C_1-6alkoxy; halo; hydroxy or oxo; or R^a and R^b together form C_1-2alkylene; under the condition that, when m is 1, n is 2, and Ar is an optionally substituted phenyl, then R¹ is not methyl or ethyl, and where optionally substituted denotes 1-3 substitutes selected from alkyl, cycloalkyl, alkoxy, halo, haloalkyl, haloalkoxy, cyano, amino, acylamino, monoalkylamino, dialkylamino, hydroxyalkyl, alkoxyalkyl, pyrazolyl, -(CH₂)_q-S(O)_rR^f; -(CH₂)_q-C(=O)-NR^gR^h; -(CH₂)_q-N(R^f)-C(=O)-Rⁱ or -(CH₂)_q-C(=O)-Rⁱ; where q is 0, r is 0 or 2, each R^f, R^g and R^h is independently hydrogen or alkyl, and each Rⁱ is independently alkyl, and where "heteroaryl" denotes a monocyclic radical having 5-6 ring atoms, including 1-2 ring heteroatoms selected from N or S, wherein the rest of the ring atoms are C atoms, "heteroalkyl" denotes an alkyl radical, including a branched C₄-C₇-alkyl, where one hydrogen atom is substituted by substitutes selected from a group consisting of -OR^a, -NR^bH, based on the assumption that the bonding of heteroalkyl radical occurs through a carbon atom, where R^a is hydrogen or C_1-6alkyl, R^b is C_1-6alkyl. Pharmaceutical compositions based on said compound are also disclosed.

EFFECT: obtaining novel compounds which can be used in medicine to treat depression, anxiety or both.

14 cl, 1 tbl, 28 ex