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11 条记录 (耗时 0.028 秒)

    Process for preparing antiviral nucleoside derivatives
    6.
    发明申请
    Process for preparing antiviral nucleoside derivatives 审中-公开
    制备抗病毒核苷衍生物的方法

    公开(公告)号：US20050080252A1

    公开(公告)日：2005-04-14

    申请号：US10939819

    申请日：2004-09-13

    申请人： Andrew Briggs ,  Charles Dvorak ,  Anthony Prince ,  Keith McCarthy

    发明人： Andrew Briggs ,  Charles Dvorak ,  Anthony Prince ,  Keith McCarthy

    IPC分类号： C07H19/056

    CPC分类号： C07H19/056

    摘要： Process and novel intermediates for preparing 2-aminocarboxylic acid esters of the 5-hydroxymethyl group of levovirin (1-(3S,4R-dihydroxy-5S-hydroxymethyl-tetrahydro-furan-2S-yl)-1H-[1,2,4]triazole-3-carboxylic acid amide; Id: R1═R2═R3═H) and acid addition salts thereof. The present process provides the monoesters selectively in high purity with increased efficiency with reduced number of production steps. The process involves condensation of a cyclopentylidene levovirin compound with a N-urethane-N-carboxylic anhydride and subsequent deprotection to directly provide the hydrochloride salt of the product. The mono esters are useful for treatment of viral diseases and are absorbed more efficiently than the parent compound.

    摘要翻译： 用于制备左旋病毒5-羟甲基的2-氨基羧酸酯的方法和新型中间体（1-（3S，4R-二羟基-5S-羟甲基 - 四氢 - 呋喃-2S-基）-1H- [1,2,4 ]三唑-3-羧酸酰胺; Id：R 1 = R 2 = R 3 = H）及其酸加成盐。 本方法提供了选择性高纯度的单酯，其生产步骤减少，效率提高。 该方法包括将亚环戊基纤溶蛋白化合物与N-氨基甲酸酯-N-羧酸酐缩合并随后脱保护直接提供产物的盐酸盐。 单酯可用于治疗病毒性疾病，并且比母体化合物更有效地吸收。

    Process for preparing 1,3-dioxolane derivatives
    7.
    发明授权
    Process for preparing 1,3-dioxolane derivatives 失效

    公开(公告)号：US5274108A

    公开(公告)日：1993-12-28

    申请号：US993789

    申请日：1992-12-21

    申请人： Norman H. Dyson ,  John O. Gardner ,  Anthony Prince ,  Denis J. Kertesz

    发明人： Norman H. Dyson ,  John O. Gardner ,  Anthony Prince ,  Denis J. Kertesz

    IPC分类号： C07D521/00 ,  C07D405/00 ,  C07D405/14

    CPC分类号： C07D249/08 ,  C07D231/12 ,  C07D233/56

    摘要： This invention provides an improved process for the preparation of compounds of formula (I): ##STR1## wherein: n is 0, 1 or 2;each R.sup.1 is independently halo or lower alkyl;R.sup.2 is nitro or --N(R.sup.3)R.sup.4 whereR.sup.3 is hydrogen or lower alkyl;R.sup.4 is hydrogen, lower alkyl, lower alkylsulfonyl or --C(Y)R.sup.5 where Y is oxygen or sulfur and R.sup.5 is hydrogen, lower alkyl, lower alkoxy or --N(R.sup.6)R.sup.7 where R.sup.6 is hydrogen or lower alkyl and R.sup.7 is hydrogen, lower alkyl or lower alkoxycarbonyl; orR.sup.3 and R.sup.4 together with N is pyrrolidino, piperidino, morpholino, thiomorpholino or piperazino, wherein the piperazino is optionally substituted at the 4-position by --C(O)R.sup.8 where R.sup.8 is hydrogen, lower alkyl, lower alkoxy or amino;or pharmaceutically acceptable salts thereof. These compounds are useful in treating disease-states characterized by hypercholesterolemia.

    Process for preparing 1,3-dioxolane derivatives
    10.
    发明授权
    Process for preparing 1,3-dioxolane derivatives 失效
    1,3-二氧戊环衍生物的制备方法

    公开(公告)号：US5208331A

    公开(公告)日：1993-05-04

    申请号：US900568

    申请日：1992-06-18

    申请人： Norman H. Dyson ,  John O. Gardner ,  Anthony Prince ,  Denis J. Kertesz

    发明人： Norman H. Dyson ,  John O. Gardner ,  Anthony Prince ,  Denis J. Kertesz

    IPC分类号： C07D233/60 ,  C07D405/06 ,  C07D521/00

    CPC分类号： C07D249/08 ,  C07D231/12 ,  C07D233/56

    摘要： This invention provides an improved process for the preparation of compounds of formula (I): ##STR1## wherein: n is 0, 1 or 2;each R.sup.1 is independently halo or lower alkyl;R.sup.2 is nitro or --N(R.sup.3)R.sup.4 whereR.sup.3 is hydrogen or lower alkyl;R.sup.4 is hydrogen, lower alkyl, lower alkylsulfonyl or --C(Y)R.sup.5 where Y is oxygen or sulfur and R.sup.5 is hydrogen, lower alkyl, lower alkoxy or --N(R.sup.6)R.sup.7 where R.sup.6 is hydrogen or lower alkyl and R.sup.7 is hydrogen, lower alkyl or lower alkoxycarbonyl; orR.sup.3 and R.sup.4 together with N is pyrrolidino, piperidino, morpholino, thiomorpholino or piperazino, wherein the piperazino is optionally substituted at the 4-position by --C(O)R.sup.8 where R.sup.8 is hydrogen, lower alkyl, lower alkoxy or amino;or pharmaceutically acceptable salts thereof. These compounds are useful in treating disease-states characterized by hypercholesterolemia.

    摘要翻译： 本发明提供了制备式（I）化合物的改进方法：其中：n为0,1或2; 每个R 1独立地为卤素或低级烷基; R2是硝基或-N（R3）R4，其中R3是氢或低级烷基; R4是氢，低级烷基，低级烷基磺酰基或-C（Y）R5，其中Y是氧或硫，R5是氢，低级烷基，低级烷氧基或-N（R6）R7，其中R6是氢或低级烷基，R7是氢 ，低级烷基或低级烷氧基羰基; 或R 3和R 4与N一起为吡咯烷子基，哌啶子基，吗啉代，硫代吗啉代或哌嗪子基，其中哌嗪基在4-位被-C（O）R 8任选取代，其中R 8是氢，低级烷基，低级烷氧基或氨基; 或其药学上可接受的盐。 这些化合物可用于治疗以高胆固醇血症为特征的疾病状态。