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    • 8. 发明授权
    • Pyrimidine derivatives and processes for the preparation thereof
    • 嘧啶衍生物及其制备方法
    • US06352993B1
    • 2002-03-05
    • US09381814
    • 1999-09-24
    • Jong Wook LeeBong Yong LeeChang Seop KimSeung Kyu LeeKeun Seog SongSong Jin LeeWoo Jeon ShimMan Soon Hwang
    • Jong Wook LeeBong Yong LeeChang Seop KimSeung Kyu LeeKeun Seog SongSong Jin LeeWoo Jeon ShimMan Soon Hwang
    • C07D40104
    • C07D401/04C07D401/14C07D417/14
    • 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.
    • 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。