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DERIVES DE 2,4(4,6)PYRIMIDINE
专利权人:
JANSSEN PHARMACEUTICA N.V.
发明人:
FREYNE, EDDY JEAN EDGARD,WILLEMS, MARC,EMBRECHTS, WERNER CONSTANT JOHAN,VAN EMELEN, KRISTOF,VAN BRANDT, SVEN FRANCISCUS ANNA,ROMBOUTS, FREDERIK JAN RITA
申请号:
CA2588761
公开号:
CA2588761C
申请日:
2005.12.08
申请国别(地区):
CA
年份:
2015
代理人:
摘要:
The present invention concerns the compounds of formula (I), the N-oxideforms, the pharmaceutically acceptable addition salts and the stereochemicallyisomeric forms thereof, wherein Z1 and Z2 represent NH; Y represents -C3-9alkyl-, -C3-9alkenyl-, -C1-5alkyl-NR6-C1-5alkyl-, -C1-5alkyl-NR7-CO-C1 -5alkyl-, -C1-6alkyl-CO-NH-, -C1-6alkyl-NH-CO-, -C1-2alkyl-CO-Het10-CO-, -C1-3alkyl-NH-CO-Het3-, -Het4-C1-3alkyl-CO-NH-C1-3alkyl-, -C1-2alkyl-NH-CO-L1-NH-,-NH-CO-L2-NH-, -C1-2alkyl-CO-NH-L3-CO-, -C1-2alkyl-NH-CO-L1-NH-CO-C1-3alkyl-, -C1-2alkyl-CO-NH-L3-CO-NH-C1-3alkyl-, -C1-2alkyl-NR11-CH2-CO-NH-C1-3alkyl-,Het5-CO-C1-2alkyl-, -C1-5alkyl-CO-NH-C1-3alkyl-CO-NH-, -C1-5alkyl-NR13-CO-C1-3alkyl-NH-, -C1-3alkyl-NH-CO-Het27-CO-, or -C1-3alkyl-CO-Het28-CO-NH-; X1represents a direct bond, O, -O-C1-2alkyl-, -CO-C1-2alkyl-, -NR16-C1-2alkyl-, -CO-NR17-, Het23-C1-2alkyl- or C1-2alkyl; X2 represents a direct bond, O, -O-C1-2alkyl-, -CO-C1-2alkyl-, -NR18-C1-2alkyl-, -CO-NR19-, Het24-C1-2alkyl- or C1-2alkyl; R1 and R5 each independently represent hydrogen, halo, C1-6alkyloxy-or C1-6alkyloxy- substituted with Het1 or C1-4alkyloxy-; R2 and R4 eachindependently represent hydrogen or halo; R3 represents hydrogen or cyano; R6,R7, R13, R17 and R19represent hydrogen; R11 represents hydrogen or C1-4alkyl;R16and R18 represent hydrogen, C1-4alkyl or Het17-C1-4alkyl-; L1, L2 andL3each independently represents C1-8alkyl optionally substituted with one orwhere possible two or more substituents selected from phenyl, methylsulfide,cyano, polyhaloC1-4alkyl-phenyl-, C1-4alkyloxy, pyridinyl, mono- or di(C1-4alkyl)-amino- or C3-6cycloalkyl; Het1 , Het2, Het17 each independentlyrepresent morpholinyl, oxazolyl, isoxazolyl, or piperazinyl; Het3, Het4, Het5each independently represent morpholinyl, piperazinyl, piperidinyl orpyrrolidinyl; Het10 represents piperazinyl, piperidinyl, pyrrolidinyl orazetidinyl; Het22 represents morpholinyl, oxazolyl, isoxazolyl or p
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