NOVEL ADENINE COMPOUND
    53.
    发明申请
    NOVEL ADENINE COMPOUND 审中-公开
    新颖的化合物

    公开(公告)号:US20110028715A1

    公开(公告)日:2011-02-03

    申请号:US12905012

    申请日:2010-10-14

    摘要: A novel adenine compound represented by the formula (1): wherein A represents an (un)substituted aromatic carbocycle or (un)substituted aromatic heterocycle; L1 and L2 each independently represents straightened or branched alkylene, etc.; R1 represents halogen, (un)substituted alkyl, (un)substituted alkenyl, (un)substituted alkynyl, (un)substituted cycloalkyl, (un)substituted aryl, or (un)substituted heteroaryl; R2 and R3 each independently represents hydrogen, or (un)substituted alkyl, (un)substituted alkenyl, (un)substituted alkynyl, (un)substituted cycloalkyl, (un)substituted saturated heterocycle, (un)substituted aryl, or (un)substituted heteroaryl, or R2 combines together with L2 or R3 to form (un)substituted 4- to 8-membered nitrogen-containing saturated heterocycle; X is oxygen, sulfur, SO, SO2, NR7, NR7CO wherein R7 is hydrogen or alkyl, or a single bond; provided that X is a single bond when R1 is halogen, or a pharmaceutically acceptable salt thereof. The compound and salt are useful as a medicine.

    摘要翻译: 由式(1)表示的新型腺嘌呤化合物:其中A表示(un)取代的芳族碳环或(un)取代的芳族杂环; L1和L2各自独立地表示直链或支链亚烷基等; R 1表示卤素,(未)取代的烷基,(未)取代的烯基,(未)取代的炔基,(未)取代的环烷基,(未)取代的芳基或(未)取代的杂芳基; R2和R3各自独立地表示氢,或(未)取代的烷基,(未)取代的烯基,(未)取代的炔基,(未)取代的环烷基,(未)取代的饱和杂环,(未)取代的芳基或(未) 或R 2与L 2或R 3一起形成(未)取代的4-至8-元含氮饱和杂环; X是氧,硫,SO,SO 2,NR 7,NR 7 CO,其中R 7是氢或烷基,或单键; 条件是当R 1为卤素时X为单键,或其药学上可接受的盐。 化合物和盐可用作药物。

    Theophylline-based nitophenylpiperazine derivatives for enhancing aortic smooth muscle relaxation
    56.
    发明申请
    Theophylline-based nitophenylpiperazine derivatives for enhancing aortic smooth muscle relaxation 审中-公开
    基于茶碱的硝基苯基哌嗪衍生物,用于增强主动脉平滑肌松弛

    公开(公告)号:US20080064705A1

    公开(公告)日:2008-03-13

    申请号:US11520174

    申请日:2006-09-12

    申请人: Ing-Jun Chen

    发明人: Ing-Jun Chen

    IPC分类号: A61K31/522 C07D473/02

    CPC分类号: A61K31/522 C07D473/08

    摘要: A substance for enhancing an aortic smooth muscle relaxation is provided. The substance is one selected from the group consisting of a compound of formula (I), a pharmaceutical acceptable therefrom and a solvate therefrom, wherein either of R1 and R2 is one of a hydrogen and a nitro group.

    摘要翻译: 提供了用于增强主动脉平滑肌松弛的物质。 该物质是选自式(I)化合物,其可接受药物和其溶剂化物的化合物,其中R1和R2中的任一个是氢和硝基之一。

    METHOD FOR PRODUCING NUCLEOSIDE DERIVATIVES
    57.
    发明申请
    METHOD FOR PRODUCING NUCLEOSIDE DERIVATIVES 失效
    生产核苷衍生物的方法

    公开(公告)号:US20070282104A1

    公开(公告)日:2007-12-06

    申请号:US11782695

    申请日:2007-07-25

    IPC分类号: C07D473/02 C07D473/10

    摘要: The present invention relates to a method for producing a nucleoside derivative represented by formula (2), comprising the step of reducing a nucleoside of formula (1) in the presence of a noble metal catalyst comprising a carrier and a noble metal supported thereby, selected from the group consisting of (A) a homogeneously supported catalyst where the specific surface area of the noble metal is 95.0 m2/g or more and the particle size of the noble metal is 4.3 nm or less, and (B) a surface-loaded catalyst where the specific surface area of the noble metal is 56.0 m2/g or more and the particle size of the noble metal is 8.0 nm or less, wherein R1 is hydrogen or a protective group, R2 is NH2 or OH, R3 is an acyl group, and X is a chlorine or bromine atom. According to the present invention, the yield can be made equal even when the amount of catalyst is smaller than that used for the conventional products.

    摘要翻译: 本发明涉及一种制备由式(2)表示的核苷衍生物的方法,包括在贵金属催化剂存在下还原式(1)的核苷的步骤,所述贵金属催化剂包含载体和由其所支持的贵金属,所选择的贵金属被选择 来自由(A)贵金属的比表面积为95.0m 2 / g以上的均匀负载的催化剂组成的组,贵金属的粒径为4.3nm以下, 和(B)贵金属的比表面积为56.0m 2 / g以上,贵金属的粒径为8.0nm以下的表面负载型催化剂,其中,R' R 1是氢或保护基,R 2是NH 2或OH,R 3是酰基, X是氯或溴原子。 根据本发明,即使当催化剂的用量小于常规产品所用量时,产率也可以相等。

    Nonpolar thymidine analogs
    60.
    发明申请
    Nonpolar thymidine analogs 失效
    非极性胸苷类似物

    公开(公告)号:US20070065360A1

    公开(公告)日:2007-03-22

    申请号:US11519385

    申请日:2006-09-11

    申请人: Eric Kool

    发明人: Eric Kool

    摘要: Nonpolar thymidine analogs are provided comprising a dihalogenated or trihalogenated base of the structure: where R1 is a sugar moiety; R2 is H or CH3; an imaging moiety or a cytotoxic moiety and X1 and X2 are independently selected from I, Cl, Br, and F, with the proviso that not more than one F will be present at these positions.

    摘要翻译: 提供非极性胸苷类似物,其包含以下结构的二卤代或三卤代碱:其中R 1是糖部分; R 2是H或CH 3 N; 成像部分或细胞毒素部分,X 1和X 2独立地选自I,Cl,Br和F,条件是不超过一个F将 在这些位置出席。