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2-吡啶-2-基-吡唑-3(2H)-酮衍生物,其製備及其作為HIF活化劑之醫療用途
专利权人:
SANOFI-AVENTIS
发明人:
ALTENBURGER, JEAN-MICHEL,亚顿柏格 真 麦可,亞頓柏格 真 麥可,法希 维菈利,法希 維菈利,伊莉艾诺 史戴芬,伊莉艾諾 史戴芬,曼诺特 吉雷迪恩,曼諾特 吉雷迪恩,亚顿柏格 真 麦可,亞頓柏格 真 麥可,法希 维菈利,法希 維菈利,伊莉艾诺 史戴芬,伊莉艾諾 史戴芬,曼诺特 吉雷迪恩,曼諾特 吉雷迪恩
申请号:
TW098145336
公开号:
TWI482763B
申请日:
2009.12.28
申请国别(地区):
TW
年份:
2015
代理人:
摘要:
The invention relates to compounds corresponding to formula (I):Rrepresents a group -SO2-NR3R4, a hydrogen atom, a halogen atom, a group -halo (C1-C5)alkyl, a group -CO2R5 or a group -SO2-R4;Rlrepresents a heterocycloalkyl group not containing a nitrogen atom, a group -W-(C3-C6)cycloalkyl, a group -W-aryl, a group -W-heteroaryl, a group -W-heterocycloalkyl, a group -W-COOR5, a group -W-CONR5R6;R2represents a hydrogen atom, a group -(C1-C5)alkyl, a group -(C1 -C5)alkylene-O-(C1-C5)alkyl, a group -halo(C1-C5)alkyl, a group -W-COOR5, a group -W-C(O)NHR5 or a group -W-C(O)-NR5R6;nrepresents 0, 1 or 2;Wis a group -(C1-C5)alkylene- or a group -(C3-C6)cycloalkylene-;R3andR4, which may be identical or different, represent, independently of each other, a hydrogen atom, a group -(C1-C5)alkyl, a group -(C3-C6)cycloalkyl, a group -(C1-C5)alkylene-O-(C1-C5)alkyl, an aryl, a group -CH2-aryl, a heteroaryl, a heterocycloalkyl, a group -W-OH, a group -W-CHOH-CH2OH, a group -W-CO2R5, a group -W-NR5R6 or a group -W-O-(CH2)n-aryl; or alternativelyR3andR4form, together with the nitrogen atom that bears them, a heterocycloalkyl group;R5andR6,which may be identical or different, represent, independently of each other, a hydrogen atom, a group -(C1-C5)alkyl or a group -(C1-C5)haloalkyl, and also to a process for preparing them and to their therapeutic uses.本發明係關於一種對應於式(I)之化合物,R表示基團-SO2-NR3R4、氫原子、鹵素原子、基團-鹵基(C1-C5)烷基、基團-CO2R5或基團-SO2-R4;R1表示不含氮原子之雜環烷基、基團-W-(C3-C6)環烷基、基團-W-芳基、基團-W-雜芳基、基團-W-雜環烷基、基團-W-COOR5、基團-W-CONR5R6;R2表示氫原子、基團-(C1-C5)烷基、基團-(C1-C5)伸烷基-O-(C1-C5)烷基、基團-鹵基(C1-C5)烷基、基團-W-COOR5、基團-W-C(O)NHR5或基團-W-C(O)-NR5R6;n表示0、1或2;W為基團-(C1-C5)伸烷基-或基團-(C3-C6)伸環烷基-;R3及R4可相同或不同,彼此獨立地表示氫原子、基團-(C1-C5)烷基、基團-(C3-C6)環烷基、基團-(C1-C5)伸烷基-O-(C1-C5)烷基、芳基、基團-CH2-芳基、雜芳基、雜環烷基、基團-W-OH、基團-W-CHOH-CH2OH、基團-W-CO2R5、基團-W-NR5R6或基團-W-O-(CH2)n-芳基;或者R3及R4與承載其之氮原子共同形成雜環烷基;R5及R6可相同或不同,彼此獨立地表示氫原子、基團-(C1-C5)烷基或基團-(C1-C5)鹵烷基,且亦係關於其製備方法及其治療用途。
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