NEUROGEN CORPORATION;NOVARTIS INTERNATIONAL PHARMACEUTICAL LTD.
发明人:
LEE, KYUNGAE,YUAN, JUN,MAYNARD, GEORGE D.,HUTCHISON, ALAN,MITCHELL, SCOTT
申请号：
ES05747952
公开号：
ES2384619T3
申请日:
2005.05.06
申请国别(地区):
ES
年份:
2012
代理人:
摘要：
A compound according to formula I ** Formula ** or a pharmaceutically acceptable salt thereof, wherein: R1 is selected from hydrogen, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, alkoxy of C1-C6, C1-C6 haloalkyl, C1-C6 haloalkoxy, (C3-C7 cycloalkyl) -C0-C4 alkyl； R2 is - (CRARB) OR4； R3 represents between 0 and 4 substituents, each of which is independently selects halogen, hydroxy, amino, cyano, optionally substituted alkyl, optionally substituted haloalkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted cycloalkyl, optionally substituted alkoxythio, optionally substituted haloalkoxy, optionally substituted alkoxyalkyl, mono- and di-substituted optionally substituted alkylamino, optionally substituted aminoalkyl, -E- (CRCRD) mZ, and -E- (CRCRD) m-XRA； R4 is: (i) C2-C8 alkyl, C2-C8 alkenyl, C2-C8 alkynyl, (C3-C7 cycloalkyl) -C0-C alkyl 4, mono- or di- (C1-C4-amino) -C2-C4 alkyl, (3-7 membered heterocycloalkyl) -C0-C4 alkyl, C0-C4 aryl-alkyl, or (heteroaryl) -alkyl C0-4, each of which is substituted with 0 to 4 substituents independently selected from Rx, C2-C4 alkanoyl, mono- and di- (C1-C4 alkyl) amino (C1-C4 alkyl), mono- and dialkyl C1-C4-amino (C1-C4 alkoxy), (3-7 membered heterocycloalkyl) C0-C4 alkyl and XRy； or (ii) joins R5 to form, with the nitrogen to which R4 and R5 are attached, a heterocycle having 1 to 3 rings, 5 to 7 ring members in each ring, in which the heterocycle is substituted with 0 to 4 substituents independently selected from Rx, oxo and WZ； R5 is: (i) hydrogen； (ii) C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, (C3-C7 carbocycle) -C0 alkyl -C4, each of which is substituted with 0 to 3 substituents independently selected from halogen, hydroxy, amino, cyano, C1-C4 alkyl, C1-C4 alkoxy, methylamino, dimethylamino, trifluoromethyl and trifluoromethoxy； or (iii) is attached to R4 to form, with the nitrogen to which R5 and R4 are attached, a heterocycle having 1 to 3 rings, 5 to 7 ring members in each ring, in whi
