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NMDA receptor spiro-lactam modulators and uses thereof
专利权人:
Aptinyx Inc.
发明人:
LOWE, John,KHAN, M.
申请号:
ES14703750
公开号:
ES2618421T3
申请日:
2014.01.29
申请国别(地区):
ES
年份:
2017
代理人:
摘要:
A compound represented by formula I: ** Formula ** or a pharmaceutically acceptable salt, stereoisomer or N-oxide thereof, wherein Rb is selected from the group consisting of H, halogen, hydroxyl, cyano and C1- alkyl C6; R is H, C1-C6 alkyl or -C (O) -C1-C6 alkyl; R1 is H or C1-C6 alkyl; R2 is H or C1-C6 alkyl; R3 is C1-C6 alkyl; C1-C6 alkoxy; -O-C1-C6 alkylene-phenyl; C2-C6 alkenyl; C2-C6 alkynyl; C3-C6 cycloalkyl; phenyl; or heteroaryl which includes 5 to 6 ring atoms, wherein 1, 2 or 3 of the ring atoms are independently selected from the group consisting of N, NH, N (C1-C3 alkyl), O and S; wherein R3 is optionally substituted with one, two or three substituents independently selected from the group consisting of amino, protected amino, halogen, C1-C6 alkyl, C1-C6 alkoxy, hydroxyl, phenyl (optionally substituted with one, two or three substituents each independently selected from Ra), benzyl (optionally substituted with one, two or three substituents each independently selected from Ra), and -C1-C6-alkyl C3-C6 cycloalkyl (optionally substituted with one, two or three substituents independently selected from halogen and C1-C6 alkyl); Ra is selected from the group consisting of halogen, C1-C6 alkyl (optionally substituted with one, two or three halogens), C3-C6 cycloalkyl (optionally substituted with one, two or three halogens), and C1-C6 alkoxy (optionally substituted with one, two or three halogens); R4 is H or C1-C6 alkyl; R5 is H or C1-C6 alkyl; X is selected from the group consisting of: H; C1-C6 alkyl; -OH; C1-C6 alkoxy; -CO2H; -C (O) NRcRd; and heteroaryl that includes 5 to 6 ring atoms, wherein 1, 2 or 3 of the ring atoms are independently selected from the group consisting of N, NH, N (C1-C3 alkyl), O and S, wherein the heteroaryl ring may be optionally substituted with one, two or three substituents independently selected from the group consisting of halogen, C1-C6 alkyl, C1-C6 alkoxy, hydroxyl and phenyl; and Rc and Rd are each independently selected fro
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