发明名称 Process for the preparation of new pyridinones inhibiting HIV reverse transcriptase
摘要 The present invention relates to a process for preparation of new pyridinones which inhibit the reverse transcriptase of HIV, and are useful for the prevention or treatment of HIV infection and in the treatment of AIDS, in the form of compounds, pharmaceutically acceptable salts or ingredients for pharmaceutical compositions, with or without other antiviral agents, anti-infectious agents, immunomodulators, antibiotics or vaccines. The methods for the treatment of AIDS and methods for the prevention and treatment of HIV infection are also described. The compounds now prepared have for example the formula (III): <IMAGE> in which n is 1-4; R1 is, for example, C1-8 alkyl; R2 is, for example, H, methyl or ethyl; R3 is H or C1-8 alkyl; the circle included in the formula is aryl or heterocyclyl, substituted or unsubstituted. The process consists, for example, in condensing the compound 1: <IMAGE> with the compound 2: <IMAGE> by means of alkylation, so as to give rise to a compound of formula III.
申请公布号 PT98003(A) 申请公布日期 1993.08.31
申请号 PT19910098003 申请日期 1991.06.17
申请人 MERCK & CO., INC. 发明人 JACOB M. HOFFMAN;CLARENCE S. ROONEY;WALFRED S. SAARI;JOHN S. WAI;THERESA M. WILLIAMS;DONA L. BAMBERGER;JAMES H. JONES
分类号 A61K31/44;C07D;C07D213/64;C07D213/76;C07D401/06;C07D401/12;(IPC1-7):C07D213/64 主分类号 A61K31/44
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