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9 条记录 (耗时 0.036 秒)

    Preparation of 2-amino-7-(1-substituted-2-hydroxyethyl)-3, 5-dihydropyrrolo[3,2-d]pyrimidin-4-ones
    1.
    发明授权
    Preparation of 2-amino-7-(1-substituted-2-hydroxyethyl)-3, 5-dihydropyrrolo[3,2-d]pyrimidin-4-ones 失效
    制备2-氨基-7-（1-取代-2-羟乙基）-3,5-二氢吡咯并[3,2-d]嘧啶-4-酮

    公开(公告)号：US6043365A

    公开(公告)日：2000-03-28

    申请号：US86043

    申请日：1998-05-28

    申请人： Leslie W. McQuire ,  Benjamin B. Mugrage ,  Mahavir Prashad ,  John H. van Duzer

    发明人： Leslie W. McQuire ,  Benjamin B. Mugrage ,  Mahavir Prashad ,  John H. van Duzer

    IPC分类号： A61K31/519 ,  A61P17/06 ,  A61P31/12 ,  A61P35/00 ,  A61P37/02 ,  A61P37/06 ,  A61P43/00 ,  C07D487/04

    CPC分类号： C07D487/04 ,  Y02P20/55

    摘要： The compounds of formula I ##STR1## wherein Ar represents biaryl, carbocyclic or heterocyclic aryl, are prepared, as substantially pure enantiomers, by(a) condensing a compound of the formula ##STR2## as a substantially pure enantiomer, wherein Ar has meaning as defined above and R.sub.6 is on O-protecting group with a lower alkyl ester of formic acid;(b) then condensing the compound so obtained with a compound of the formula ##STR3## wherein R.sub.8 is hydrogen or COOR.sub.3 and R.sub.3 is lower alkyl; (c) then cyclizing the compound so obtained to a compound of the formula ##STR4## as a substantially pure enantiomer; (d) and then condensing the compound so obtained(1) with a carbocyclic aroyl isothiocyanate and treatment of the product so obtained with an alkyl halide followed by anhydrous ammonia; or(2) with cyanamide in acid, optionally followed by treatment with a base.

    摘要翻译： 制备其中Ar表示联芳基，碳环或杂环芳基的式I化合物，作为基本上纯的对映异构体，通过（a）将式的化合物作为基本上纯的对映异构体缩合，其中Ar具有如上定义的含义， O-保护基与甲酸的低级烷基酯; （b）然后将所得化合物与下式化合物缩合：其中R8是氢或COOR3，R3是低级烷基; （c）然后将所得化合物环化为基本上纯的对映体的式的化合物; （d），然后将所得化合物（1）与碳环异硫氰酸酯缩合并用烷基卤，然后用无水氨处理得到的产物; 或（2）在氰酸中，然后用碱处理。

    Certain 5-alkyl-2-arylaminophenylacetic acids and derivatives
    3.
    发明授权
    Certain 5-alkyl-2-arylaminophenylacetic acids and derivatives 失效
    某些5-烷基-2-芳基氨基苯基乙酸及其衍生物

    公开(公告)号：US06727281B2

    公开(公告)日：2004-04-27

    申请号：US10201336

    申请日：2002-07-23

    申请人： Roger A. Fujimoto ,  Leslie W. McQuire ,  Benjamin B. Mugrage ,  John H. van Duzer

    发明人： Roger A. Fujimoto ,  Leslie W. McQuire ,  Benjamin B. Mugrage ,  John H. van Duzer

    IPC分类号： C07C22942

    CPC分类号： C07C229/42

    摘要： Disclosed are the compounds of formula I wherein R is methyl or ethyl; R1 is chloro or fluoro; R2 is hydrogen or fluoro; R3 is hydrogen, fluoro, chloro, methyl, ethyl, methoxy, ethoxy or hydroxy; R4 is hydrogen or fluoro; and R5 is chloro, fluoro, trifluoromethyl or methyl; and pharmaceutically acceptable salts thereof, as selective COX-2 cyclooxygenase inhibitors; and pharmaceutically acceptable prodrug esters thereof.

    摘要翻译： 公开了式I的化合物，其中R是甲基或乙基; R1是氯或氟; R2是氢或氟; R3是氢，氟，氯，甲基，乙基，甲氧基，乙氧基或羟基; R4是氢或氟; R5是氯，氟，三氟甲基或甲基; 作为选择性COX-2环加氧酶抑制剂; 及其药学上可接受的前药酯。

    Certain 5-alkyl-2-arylaminophenylacetic acids and derivatives
    5.
    发明授权
    Certain 5-alkyl-2-arylaminophenylacetic acids and derivatives 有权
    某些5-烷基-2-芳基氨基苯基乙酸及其衍生物

    公开(公告)号：US06451858B2

    公开(公告)日：2002-09-17

    申请号：US09950957

    申请日：2001-09-13

    申请人： Roger A. Fujimoto ,  Leslie W. McQuire ,  Benjamin B. Mugrage ,  John H. van Duzer

    发明人： Roger A. Fujimoto ,  Leslie W. McQuire ,  Benjamin B. Mugrage ,  John H. van Duzer

    IPC分类号： C07C22942

    CPC分类号： C07C229/42

    摘要： Disclosed are the compounds of formula I wherein R is methyl or ethyl; R1 is chloro or fluoro; R2 is hydrogen or fluoro; R3 is hydrogen, fluoro, chloro, methyl, ethyl, methoxy, ethoxy or hydroxy; R4 is hydrogen or fluoro; and R5 is chloro, fluoro, trifluoromethyl or methyl; and pharmaceutically acceptable salts thereof, as selective COX-2 cyclooxygenase inhibitors; and pharmaceutically acceptable prodrug esters thereof.

    摘要翻译： 公开了式I的化合物，其中R是甲基或乙基; R1是氯或氟; R2是氢或氟; R3是氢，氟，氯，甲基，乙基，甲氧基，乙氧基或羟基; R4是氢或氟; R5是氯，氟，三氟甲基或甲基; 作为选择性COX-2环加氧酶抑制剂; 及其药学上可接受的前药酯。

    2-amino-7-(1-substituted-2-hydroxyethyl)-3,5-dihydropyrrolo[3,2-D]pyrimidin-4-ones
    6.
    发明授权
    2-amino-7-(1-substituted-2-hydroxyethyl)-3,5-dihydropyrrolo[3,2-D]pyrimidin-4-ones 失效
    2-氨基-7-（1-取代-2-羟乙基）-3,5-二氢吡咯并[3,2-D]嘧啶-4-酮

    公开(公告)号：US06174888B1

    公开(公告)日：2001-01-16

    申请号：US09085791

    申请日：1998-05-28

    申请人： Leslie W. McQuire ,  Benjamin B. Mugrage ,  John H. van Duzer

    发明人： Leslie W. McQuire ,  Benjamin B. Mugrage ,  John H. van Duzer

    IPC分类号： C07D48704

    CPC分类号： C07D487/04 ,  A61K31/519

    摘要： The invention relates to the 2-amino-7-(1-substituted-2-hydroxyethyl)-3, 5-dihydro-pyrrolo[3,2-d] pyrimidin-4-ones of formula I and tautomers thereof, wherein Ar represents biaryl, carbocyclic or heterocyclic aryl; pharmaceutically acceptable prodrug ester derivatives; and pharmaceutically acceptable salts thereof, which are particularly useful as potent purine nucleoside phosphorylase (PNP) inhibitors.

    摘要翻译： 本发明涉及式I的2-氨基-7-（1-取代-2-羟乙基）-3,5-二氢 - 吡咯并[3,2-d]嘧啶-4-酮及其互变异构体，其中Ar表示联芳基 ，碳环或杂环芳基; 药学上可接受的前药酯衍生物; 其药学上可接受的盐，其特别用作有效的嘌呤核苷磷酸化酶（PNP）抑制剂。