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HETEROARYL PYRROLIDINYL AND PIPERIDINYL KETONE DERIVATIVES
专利权人:
F. KHOFFMANN-LJA ROSH AG
发明人:
AJER Pravin (US),АЙЕР Правин (US),LIN Klara Jeu Jen (US),ЛИН Клара Йеу Йен (US),LUKAS Meht'ju K. (US),ЛУКАС Мэтью К. (US),LINCh Stiven M. (US),ЛИНЧ Стивен М. (US),MADERA Ehnn Mari (US),МАДЕРА Энн Мари,AJER PRAVIN,АЙЕР Правин,LIN KLARA JEU JEN,ЛИН Клара Йеу Йен,LUKAS MEHTJU K.,ЛУКАС Мэтью К.,LINCH STIVEN M.,ЛИНЧ Стивен М.,MADERA EHNN MARI,OZBOJA KEREM EHROL,ОЗБОЯ Керем Эрол,SHOENFELD
申请号:
RU2009122666/04
公开号:
RU0002479575C2
申请日:
2007.12.11
申请国别(地区):
RU
年份:
2013
代理人:
摘要:
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: C1-6alkyl; hetero-C1-6alkyl; halo-C1-6alkyl; halo-C2-6alkenyl; C3-7cycloalkyl; C3-7cycloalkyl-C1-6alkyl; C1-6alkyl-C3-6cycloalkyl-C1-6alkyl; C1-6alkoxy; C1-6alkylsulphonyl; phenyl; tetrahydropyranyl-C1-6alkyl; phenyl-C1-3alkyl, where the phenyl part is optionally substituted; heteroaryl-C1-3alkyl; R2 is: hydrogen or C1-6alkyl; and each Ra and Rb is independently: hydrogen; C1-6alkyl; C1-6alkoxy; halo; hydroxy or oxo; or Ra and Rb together form C1-2alkylene; 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)rRf; -(CH2)q-C(=O)-NRgRh; -(CH2)q-N(Rf)-C(=O)-Ri or -(CH2)q-C(=O)-Ri; where q is 0, r is 0 or 2, each Rf, Rg and Rh 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 consis
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