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P2X7 ANTAGONISTS REPLACED WITH QUINOLINE OR ISOQUINOLINE.
专利权人:
JANSSEN PHARMACEUTICA; N.V.
发明人:
LOVE, CHRISTOPHER,LEENAERTS, JOSEPH,COOYMANS, LUDWIG,LEBSACK, ALEC,BRANSTETTER, BRYAN,RECH, JASON,GLEASON, ELIZABETH,VENABLE, JENNIFER,WIENER, DANIELLE,SMITH, DEBORAH,BREITENBUCHER, JAMES
申请号:
ES09735472
公开号:
ES2376092T3
申请日:
2009.04.21
申请国别(地区):
ES
年份:
2012
代理人:
摘要:
Compound of formula (I) including any stereochemically isomeric form thereof, wherein n is an integer 1, 2 or 3; m is an integer 1, 2 or 3; p is an integer 1 or 2; R3 is hydrogen, halo, C1-4 alkyl or C1-4 alkyloxy; X represents O, S, SO2, CR4R5 or NR6; wherein R4 and R5 are each independently selected from each other from hydrogen, halo, hydroxyl, C1-4 alkyl, C1-4 alkyloxy or aryl; wherein R6 is hydrogen, phenyl, -CO-R7 or -CO-O-R7, wherein R7 is C1-6 alkyl or amino; R1 is a heterocycle selected from pyridinyl or pyrimidinyl, wherein said heterocycle is substituted with one or two substituents each independently selected from hydrogen, halo, hydroxyl, C1-6 alkyl, C1-6 alkyloxy, C1-4 polyhaloalkyl, phenyl, C3-6 cycloalkyl, C3-6 cycloalkyloxy, C3-6 cycloalkyl-C1-4 alkyloxy or NR8R9; wherein R8 and R9 are independently selected from each other from hydrogen, C1-6 alkyl, C1-6 hydroxyalkyl, C3-6 cycloalkyl, and wherein R8 and R9 can be taken together with the nitrogen atom to which they are attached to forming an azetidinyl, pyrrolidinyl, piperidinyl, piperazinyl or morpholinyl ring which may be optionally substituted with one or two substituents each independently selected from each other from C 1-4 alkyl, C 1-4 alkyloxy, halo, hydroxyl or C 1-4 alkylcarbonyl; R2 is a heterocycle selected from quinolinyl or isoquinolinyl, wherein said heterocycle is substituted with one or two substituents each independently selected from hydrogen, halo, hydroxyl, C1-6 alkyl, C1-6 alkyloxy, C3-6 cycloalkyl, C1-6 cycloalkyloxy, C1-4 polyhaloalkyl, NR10R11 and OR12; wherein R10 and R11 are independently selected from each other from hydrogen, C1-6 alkyl, C3-6 cycloalkyl, C1-4 polyhaloalkyl, tetrahydrofuranyl, tetrahydropyranyl, piperidinyl, N- (1,5-dioxa-9-azaspiro [5.5 ] undec-9-yl), N- (1, 7-diaza-spiro [4.4] non-7-yl), N- (2, 6-diaza-spiro [4.5] dec-2-yl) and C1-alkyl -6 substituted with one or two substituents selected from hydroxyl, halo, aryl1, C1-4 alkyloxy, C3-6 cycloalkyl, hydrox
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