发明名称 AMINO-DERIVATIVES OF OXO- OR HYDROXY-SUBSTITUTED HYDRAZINES, METHOD OF THEIR SYNTHESIS AND PHARMACEUTICAL COMPOSITIONS FOR INHIBITION OF RETROVIRUS PROTEASE
摘要 FIELD: organic chemistry, pharmacy. SUBSTANCE: invention proposes amino-derivatives of oxo- or hydroxy-substituted hydrazines of formulas: XN(R)CH- -<EMI ID=0.476 HE=6 WI=57 TI=CHI>-C(O)Y (IC) and XN(R)CH-<EMI ID=0.477 HE=6 WI=48 TI=CHI>-C(O)Y (ID) where R is H; X is H, (C<SB>1</SB>-C<SB>10</SB>)-aryl-(C<SB>1</SB>-C<SB>6</SB>)-alkoxycarbonyl and others; R is (C<SB>6</SB>-C<SB>10</SB>)-aryl-(C<SB>1</SB>-C<SB>6</SB>)- -alkyl; R is H; R is (C<SB>1</SB>-C<SB>6</SB>)-alkyl, (C<SB>6</SB>-C<SB>10</SB>)-aryl-(C<SB>1</SB>-C<SB>6</SB>)-alkyl and others; R is H; Y is (C<SB>1</SB>-C<SB>6</SB>)-alkyl, (C<SB>1</SB>-C<SB>6</SB>)-alkoxy and others. These compounds are synthesized by interaction of compound of the formula X-NR-<EMI ID=0.478 HE=9 WI=30 TI=CHI> with compound of the formula HN-<EMI ID=0.479 HE=6 WI=18 TI=CHI>-C(O)Y. Compounds (IC) and (ID) can be used in pharmaceutical compositions as an active agent to inhibit retrovirus protease, in part, at acquired immunodeficiency syndrome (AIDS) that gives possibility to use these compounds for treatment of patients with viral HIV-infections. EFFECT: improved method of synthesis, enhanced effectiveness of compounds. 11 cl, 3 tbl, 38 ex
申请公布号 RU2126794(C1) 申请公布日期 1999.02.27
申请号 RU19940040859 申请日期 1993.03.11
申请人 NARKHEKS LIMITED 发明人 DAM'JAN VOJTSEKH GROBEL'NY
分类号 A61K31/13;A61K31/15;A61K31/195;A61K31/24;A61K31/27;A61K31/44;A61K31/4402;A61K31/4418;A61K31/4427;A61K31/47;A61K31/50;A61P31/12;A61P31/18;A61P37/04;C07C243/12;C07C243/14;C07C243/26;C07C243/28;C07C271/20;C07C281/02;C07C323/23;C07C323/60;C07D213/24;C07D213/30;C07D213/81;C07D215/12;C07D215/48;C07D231/54;C07D237/04;C07D237/08;C07D237/26;C07D237/30;C07D401/12 主分类号 A61K31/13
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