WISSNER, ALLAN,JOHNSON, BERNARD DEAN,REICH, MARVIN FRED,FLOYD, MIDDLETON BRAWNER JR.,KITCHEN, DOUGLAS B.,TSOU, HWEI-RU
申请号：
CA2285241
公开号：
CA2285241C
申请日:
1998.04.02
申请国别(地区):
CA
年份:
2013
代理人:
摘要：
This invention provides compounds having formula (1), wherein: X is cycloalkylwhich may be optionally substituted； or is a pyridinyl, pyrimidinyl, or phenylring； wherein the pyridinyl, pyrimidinyl, or phenyl ring may be optionallysubstituted； n is 0-1； Y is -NH-, -O-, -S-, or -NR-； R is alkyl of 1-6 carbonatoms； R1, R2, R3 and R4 are each, independently, hydrogen, halogen, alkyl,alkenyl, alkynyl, alkenyloxy, alkynyloxy, hydroxymethyl, halomethyl,alkanoyloxy, alkenoyloxy, alkynoyloxy, alkanoyloxymethyl, alkenoyloxymethyl,alkynoyloxymethyl, alkoxymethyl, alkoxy, alkylthio, alkylsulphinyl,alkylsulphonyl, alkylsulfonamido, alkenylsulfonamido, alkynylsulfonamido,hydroxy, trifluoromethyl, cyano, nitro, carboxy, carboalkoxy, carboalkyl,phenoxy, phenyl, thiophenoxy, benzyl, amino, hydroxyamino, alkoxyamino,alkylamino, dialkylamino, aminoalkyl, N-alkylaminoalkyl, N,N-dialkylaminoalkyl, phenylamino, benzylamino, formulae (a, b, c, d, e, f, g, h,i, j, k, l, m, n, o, p, q or r)； R5 is alkyl which may be optionallysubstituted, or phenyl which may be optionally substituted； R6 is hydrogen,alkyl, or alkenyl； R7 is chloro or bromo； R8 is hydrogen, alkyl, aminoalkyl, N-alkylaminoalkyl, N,N-dialkylaminoalkyl, N-cycloalkylaminoalkyl, N-cycloalkyl-N-alkylaminoalkyl, N,N-dicycloalkylaminoalkyl, morpholino-N-alkyl, piperidino-N-alkyl, N-alkyl-piperidino-N-alkyl, azacycloalkyl-N-alkyl, hydroxyalkyl,alkoxyalkyl, carboxy, carboalkoxy, phenyl, carboalkyl +, chloro, fluoro, orbromo； Z is amino, hydroxy, alkoxy, alkylamino, dialkylamino, morpholino,piperazino, N-alkylpiperazino, or pyrrolidino； m = 1-4, q = 1-3, and p = 0-3；any of the substituents R1, R2, R3 or R4 that are located on contiguous carbonatoms can together be the divalent radical -O-C(R8)2-O-； or a pharmaceuticallyacceptable salt thereof with the proviso that when Y is -NH-, R1, R2, R3 andR4 are hydrogen, and n is O, X is not 2-methylphenyl, which are inhibitors ofprotein t
