SUBSTITUTED BENZAMIDE DERIVATIVES Russian patent published in 2016 - IPC C07D207/09 C07D207/10 C07D207/12 C07D211/26 C07D265/30 C07D267/10 C07D295/12 C07D401/04 C07D401/12 C07D401/14 C07D403/12 C07D413/12 C07D413/14 C07D417/12 C07D417/14 A61K31/40 A61K31/4184 A61K31/4439 A61K31/4462 A61K31/4465 A61K31/4458 A61K31/451 A61K31/4545 A61K31/495 A61K31/496 A61K31/497 A61K31/4709 A61K31/4725 A61K31/5375 A61K31/5377 A61K31/553 A61P25/00 A61P25/06 A61P25/08 A61P25/16 A61P25/18 A61P25/20 A61P25/22 A61P25/24 A61P25/28 A61P25/36 A61P3/00 A61P3/04 A61P3/06 A61P3/10 A61P9/00 A61P9/12 

Abstract RU 2595902 C2

FIELD: chemistry.

SUBSTANCE: invention relates to compound of formula (I), where R is hydrogen or C1-7alkyl;

R1 represents -(CH2)n-(O)o-5-7-member heterocycloalkyl, containing 1-2 heteroatoms selected from N and O, except for piperazine, where said heterocycloalkyl group optionally substituted with C1-7alkyl, hydroxy or halogen; n equals to 0, 1 or 2; o equals to 0 or 1; R2 represents CF3, C3-6-cycloalkyl, possibly substituted C1-7alkoxy or halogen, or represents indane-2-yl, or is 6-member heterocycloalkyl, containing 1-2 heteroatoms selected from N and O, optionally substituted with pyrimidinyl, or is 5-6 mono- or 9-10-member bicyclic heteroaryl containing 1-2 heteroatoms selected from N, O and S, where the heteroaryl is not thiazol and where said aromatic ring, is possibly substituted with one or two substitutes selected from C1-7alkyl, halogen, 5-6-member heteroaryl containing 1-2 heteroatoms selected from N and O, hydroxy, CF3, OCF3, OCH2CF3, OCH2-cycloalkyl, OCH2C(CH2OH)(CH2Cl)(CH3), S-C-1-7alkyl, C1-7alkoxy, CH2-C-1-7alkoxy, C2-7alkynyl or cyano, or substituted with -C(O)-phenyl, -O-phenyl, -O-CH2-phenyl, phenyl, and where said phenyl ring may be substituted with halogen, -C(O)OH or -C(O)O-C-1-7alkyl, or said aromatic ring, is possibly substituted with 5-6-member heterocycloalkyl, containing 1-2 heteroatoms selected from N and O, OCH2-oxetane-3-yl or O-tetrahydropyran-4-yl, possibly substituted C1-7alkyl; X is bond, -CH2NH-, -CHR″-, -(CHR″)q-O-, -O-(CHR″)q- or -(CH2)2-; Y is bond; R″ is hydrogen, C1-7alkyl, CF3, C1-7alkoxy; q is equal to 0, 1, 2 or 3; or pharmaceutically acceptable acid addition salt thereof, except for compounds specified in patent claim. Invention also relates to specific compounds specified in patent claim. Compounds are intended for producing medicinal agents, showing affinity to TAAR1.

EFFECT: technical result: benzamide derivatives having high affinity to receptors associated with TAAR1 trace amines.

9 cl, 1 tbl, 323 ex

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RU 2 595 902 C2

Authors

Grebke Tsbinden Katrin

Norkross Rodzher

Pfliger Filipp

Dates

2016-08-27Published

2010-12-17Filed