中科微点-全球专利检索

  1. Login
  2. Sign Up

Search Results

34 records (took 0.018 seconds)

    Pyrimidine derivatives and processes for the preparation thereof
    9.
    发明授权
    Pyrimidine derivatives and processes for the preparation thereof 失效
    嘧啶衍生物及其制备方法

    公开(公告)号：US06352993B1

    公开(公告)日：2002-03-05

    申请号：US09381814

    申请日：1999-09-24

    Applicant: Jong Wook Lee ,  Bong Yong Lee ,  Chang Seop Kim ,  Seung Kyu Lee ,  Keun Seog Song ,  Song Jin Lee ,  Woo Jeon Shim ,  Man Soon Hwang

    Inventor： Jong Wook Lee ,  Bong Yong Lee ,  Chang Seop Kim ,  Seung Kyu Lee ,  Keun Seog Song ,  Song Jin Lee ,  Woo Jeon Shim ,  Man Soon Hwang

    IPC: C07D40104

    CPC classification number: C07D401/04 ,  C07D401/14 ,  C07D417/14

    Abstract: The present invention relates to novel pyrimidine derivatives of formula (I) or pharmaceutically acceptable salts thereof which possess an excellent anti-secretory activity, pharmaceutical compositions containing the same as an active ingredient, their novel intermediates, and processes for the preparation thereof wherein: when A is piperidin-1-yl or —NH—B, wherein B is C3-C4 alkyl, C3-C4 alkenyl, C3-C7 cycloalkyl, C1-C3 alkoxyethyl, phenylethl which may be substituted or unsubstituted, 3-trifluoromethylphenylmethyl, 1-naphthylmethyl, 4-methylthiazol-2-yl or 4-phenylthiazol-2-yl, R1 is hydrogen or methyl; and R2, R3, R4 and R5 are hydrogen; or when A is a group of formula (II); when R1 is hydroxymethyl or C1-C3 alkoxymethyl, R2, R3, R4, R5 and R6 are hydrogen; and R7 is hydrogen or halogen; or when R1 is hydrogen or methyl, R7 is hydrogen or halogen; and one or two of R2, R3, R4, R5 and R6 is hydroxy, methoxy, or a group of formula (III) wherein Z is C1-C4 alkyl, substituted or unsubstituted C1-C4 alkenyl, cyloalkyl, benzyloxyalkyl, alkoxycarbonylalkyl, morpholinomethyl, piperidinomethyl, 4-substituted-piperazinomethyl, substituted or unsubstituted phenyl, naphthyl, substituted or unsubstituted benzyl, thiophen-2-yl-methyl, 1-substituted-pyrrolidin-2-yl or —CHR8NHR9, wherein R8 is hydrogen, methyl, isopropyl, benzyl, benzyloxymethyl, methylthioethyl, benzyloxycarbonylmethyl, carbamolymethyl, carbamoylethyl, or 1-benzylimidazol-4-ylmethyl and R9 is hydrogen or t-butoxycarbonyl; and the others are hydrogen or methyl.

    Abstract translation: 本发明涉及具有优异抗分泌活性的式（I）的新颖的嘧啶衍生物或其药学上可接受的盐，其含有与活性成分相同的药物组合物，其新颖的中间体及其制备方法，其中： A是哌啶-1-基或-NH-B，其中B是C 3 -C 4烷基，C 3 -C 4烯基，C 3 -C 7环烷基，C 1 -C 3烷氧基乙基，可以被取代或未取代的苯乙基，3-三氟甲基苯基甲基， 萘基甲基，4-甲基噻唑-2-基或4-苯基噻唑-2-基，R 1是氢或甲基; R2，R3，R4和R5是氢; 或当A为式（II）的基团时; 当R 1是羟甲基或C 1 -C 3烷氧基甲基时，R 2，R 3，R 4，R 5和R 6是氢; 并且R 7是氢或卤素; 或当R 1为氢或甲基时，R 7为氢或卤素; R 2，R 3，R 4，R 5和R 6中的一个或两个是羟基，甲氧基或其中Z是C 1 -C 4烷基，取代或未取代的C 1 -C 4烯基，环烷基，苄氧基烷基，烷氧基羰基烷基，吗啉代甲基 ，哌啶基甲基，4-取代的哌嗪基甲基，取代或未取代的苯基，萘基，取代或未取代的苄基，噻吩-2-基 - 甲基，1-取代的吡咯烷-2-基或-CHR8NHR9，其中R8是氢，甲基， 苄基，苄氧基甲基，甲硫基乙基，苄氧基羰基甲基，氨基甲酰基，氨基甲酰基乙基或1-苄基咪唑-4-基甲基，R9为氢或叔丁氧基羰基; 其他的是氢或甲基。

Patent Agency Ranking