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    AZETIDINE ANALOGUES NUCLEOSIDASE AND PHOSPHORYLASE INHIBITORS
    39.
    发明申请
    AZETIDINE ANALOGUES NUCLEOSIDASE AND PHOSPHORYLASE INHIBITORS 有权

    公开(公告)号：US20100168141A1

    公开(公告)日：2010-07-01

    申请号：US12448397

    申请日：2007-12-21

    申请人： Gary Brian Evans ,  Richard Hubert Furneaux ,  Ben William Greatrex ,  Vern L. Schramm ,  Peters Charles Tyler

    发明人： Gary Brian Evans ,  Richard Hubert Furneaux ,  Ben William Greatrex ,  Vern L. Schramm ,  Peters Charles Tyler

    IPC分类号： A61K31/519 ,  C07D487/04 ,  A61P35/00

    CPC分类号： C07D471/04

    摘要： Azetidine analogues of nucleosidase and nucleoside phosphorylase inhibitors having the general formula (I), the use of these compounds as pharmaceuticals, pharmaceutical compositions containing the compounds, methods of treating certain diseases using the compounds, processes for preparing the compounds, and intermediates useful in the preparation of the compounds wherein W and X are each independently selected from hydrogen, CH2OH, CH2OQ and CH2SQ; Y and Z are each independently selected from hydrogen, halogen, CH2OH, CH2OQ, CH2SQ, SQ, OQ and Q; Q is an alkyl, aralkyl or aryl group each of which may be optionally substituted with one or more substituents selected from hydroxy, halogen, methoxy, amino, or carboxy; R1 is a radical of the formula (II) or R1 is a radical of the formula (III) A is selected from N, CH and CR2, where R2 is selected from halogen, alkyl, aralkyl, aryl, OH, NH2, NHR3, NR3R4 and SR5, where R3, R4 and R5 are each alkyl, aralkyl or aryl groups optionally substituted with hydroxy or halogen, and where R2 is optionally substituted with hydroxy or halogen when R2 is alkyl, aralkyl or aryl; B is selected from hydroxy, NH2, NHR6, SH, hydrogen and halogen, where R6 is an alkyl, aralkyl or aryl group optionally substituted with hydroxy or halogen; D is selected from hydroxy, NH2, NHR7, hydrogen, halogen and SCH3, where R7 is an alkyl, aralkyl or aryl group optionally substituted with hydroxy or halogen; E is selected from N and CH; G is a C1-4 saturated or unsaturated alkyl group optionally substituted with hydroxy or halogen, or G is absent; or a tautomer thereof, or a pharmaceutically acceptable salt thereof, or an ester thereof, or a prodrug thereof.

    摘要翻译： 具有通式（I）的核苷酸的氮杂环丁烷类似物和具有通式（I）的核苷磷酸化酶抑制剂，这些化合物作为药物的用途，含有该化合物的药物组合物，使用该化合物治疗某些疾病的方法，制备该化合物的方法和用于 其中W和X各自独立地选自氢，CH 2 OH，CH 2 OQ和CH 2 SQ的化合物的制备; Y和Z各自独立地选自氢，卤素，CH 2 OH，CH 2 OQ，CH 2 SQ，SQ，OQ和Q; Q是烷基，芳烷基或芳基，其各自可以任选被一个或多个选自羟基，卤素，甲氧基，氨基或羧基的取代基取代; R 1是式（II）的基团或R 1是式（III）的基团。A选自N，CH和CR 2，其中R 2选自卤素，烷基，芳烷基，芳基，OH，NH 2，NHR 3， NR 3 R 4和SR 5，其中R 3，R 4和R 5各自为任选被羟基或卤素取代的烷基，芳烷基或芳基，并且当R 2为烷基，芳烷基或芳基时，其中R 2任选被羟基或卤素取代; B选自羟基，NH 2，NHR 6，SH，氢和卤素，其中R 6是任选被羟基或卤素取代的烷基，芳烷基或芳基; D选自羟基，NH 2，NHR 7，氢，卤素和SCH 3，其中R 7是任选被羟基或卤素取代的烷基，芳烷基或芳基; E选自N和CH; G是任选被羟基或卤素取代的C1-4饱和或不饱和烷基，或G不存在; 或其互变异构体，或其药学上可接受的盐或其酯，或其前药。