The pyrimidine of the 6-replacement of HIV inhibiting

The pyrimidine of the 6-replacement of HIV inhibiting

  • CN 101,573,343 B
  • Filed: 12/28/2007
  • Issued: 02/24/2016
  • Est. Priority Date: 12/29/2006
  • Status: Active Grant
First Claim
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1. with following formula (I) compound, its pharmaceutically acceptable additive salt and stereochemistry heterogeneous forms:



  • In formula (I);

    r1, R2with r3independent is hydrogen;

    r6with r7independent is methyl;

    r4for cyano group;

    r8for-CH=CH-CN;

    X is-NH-;

    r5be (1) pyridyl;

    (2)-CONR 5ar 5b;

    Wherein R 5aindependent is hydrogen or C 1-6alkyl;

    R 5bc 1-6alkoxyl group;

    Or C 1-6alkyl, it is by C 1-6alkoxyl group, halogen, cyano group, pyridyl, furyl replace;

    (3)-CH (OR 5c) R 5d;

    Wherein R 5cbe hydrogen and R 5dit is aryl;

    (4)-CH 2-NR 5er 5f;

    R 5ehydrogen or C 1-6alkyl;

    R 5fc 1-6alkoxyl group;

    C 2-6thiazolinyl;

    C 1-6alkyl, it is replaced by following group;

    hydroxyl, C 1-6alkoxyl group, cyano group, amino, list or two C 1-6alkylamino, C 1-6alkyl-carbonyl-amino, aryl, pyridyl, thienyl, furyl, optionally by two C 1-6dioxolane base, tetrahydrofuran base, morpholinyl, C that alkyl replaces 3-7cycloalkyl;

    Or R 5eand R 5fimidazolyl is formed together with the nitrogen-atoms that they replace;

    Morpholinyl;

    Or optionally by C 1-6the piperazinyl that alkyl replaces;

    (5)-CH 2-O-C 2-6thiazolinyl;

    (6)-CH 2-O-P (=O) (OR 5g) 2;

    Each R 5gc 1-6alkyl;

    (7)-CH 2-O-C(=O)-NH 2

    (8)-C (=O)-R 5d;

    Wherein R 5dit is thiazolyl;

    Wherein each aryl independently for phenyl or by one, two or three be independently selected from separately following substituting group replacement phenyl;

    halogen, hydroxyl, C 1-6alkyl, C 1-6alkoxyl group, cyano group, nitro, trifluoromethyl.

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