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Thiazolopyrimidinones as modulators of NMDA receptor activity
专利权人:
F. Hoffmann-La Roche AG
发明人:
YU, Jiang,WU, Guosheng,YUEN, Po-Wai,VILLEMURE, Elisia,SCHWARZ, Jacob,LY, Cuong,SELLERS, Benjamin,VOLGRAF, Matthew
申请号:
ES14781878
公开号:
ES2690355T3
申请日:
2014.10.08
申请国别(地区):
ES
年份:
2018
代理人:
摘要:
A compound of formula (II): ** Formula ** wherein Ra is C1-6 alkyl or C2-6 alkenyl, each optionally substituted with one or more Rb substituents; C2-6 alkynyl; halo; -C (O) Rc; -NRdRe; -C (O) NRdRe; -C (S) NRdRe; -C (>; = N-OH) -C 1-4 alkyl; -C 1-4 alkyl; -Chaloalkyl C1-4; -C1-4 alkyl; -SO2 C1-4alkyl; cyano; C3-6 cycloalkyl optionally substituted with one or more Rf substituents; or a phenyl, monocyclic heteroaryl or heterocycloalkyl ring, each ring optionally substituted with one or more Rg substituents; wherein each Rb substituent is independently selected from the group consisting of -OH, -C 1-4 alkoxy, -NRdRe, -C (O) NRdRe, -C1-4 alkyl, -SO2C 1-4 alkyl, cyano, halo, cycloalkyl C3-6 and monocyclic heteroaryl; Rc is C1-4 alkyl, C1-4 haloalkyl, C3-6 cycloalkyl or a carbon monocyclic heterocycloalkyl; Rd is H or C1-4 alkyl; Re is H; C1-4 alkyl optionally substituted with -CN, -CF3, -OH or a monocyclic heterocycloalkyl; C3-6 cycloalkyl; -OH; or C1-4alkoxy; or Rd and Re, taken together with the nitrogen to which they are linked, form a heterocycloalkyl, optionally substituted with C1-4 alkyl or -OH; each Rf substituent is independently selected from the group consisting of: C1-4 alkyl optionally substituted with -OH, cyano or C1-4 alkoxy; -OH; halo; C1-4 haloalkyl; -CONH2; and cyano; and each Rg substituent is independently selected from the group consisting of C1-4 alkyl, -CF3, halo, -NH2, -OCH3, cyano and -OH; R 1 is selected from the group consisting of H, C 1-6 alkyl, C 1-4 haloalkyl, C 3-6 cycloalkyl, halo, -C 1-4 alkyl, -C 1-4 haloalkyl, cyano and -C (O) C 1-4 alkyl ; or Ra and R1, taken together with the carbons to which they are attached, form a 5 to 7 member ring, optionally containing an O or NH, and optionally substituted with one or more Rh substituents; wherein each Rh substituent is independently -C (O) NRiRj, cyano, or is C1-4 alkyl optionally substituted with -OH, -OCH3, cyano, or -C (O) NRiRj; or two Rh groups, bonded to the same carbon and taken to
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