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参考文献:与苯并[c]菲啶骨架的一步合成进入等位和有效的抗癌氮杂环
标题:与苯并[c]菲啶骨架的一步合成进入等位和有效的抗癌氮杂环
摘要:描述了一种通用的一步式两组分环化反应,可构建新的四环氮杂环.将邻甲基甲基戊烯腈成分与醛缩合,以访问一个由大量不同取代的环系统组成的库.通过改变环内氮原子在邻位的位置,可以很容易地修饰杂环核-甲基戊烯甲腈底物.导致缩合的亲核攻击方式可以由氮原子位置引起的分子中不同的电子密度分布来触发.考虑到这一点,存在电子偏好,其导致以吡啶并菲咯啉或相应的吡啶并氮杂咔唑为主要产物.我们证明了某些合成杂环具有很高的抗肿瘤潜力,这在很大程度上取决于通过醛组分引入的取代模式.内环氮原子的位置和数量在所研究化合物的细胞毒性方面起着重要作用.
Doi:10.1002/chem.201600308
专利信息
专利号:US-2005124683-A1
优先权日:2003-09-17
标 题:HIV protease inhibitors, compositions containing the same, their pharmaceutical uses and materials for their synthesis
发明人:ALEGRIA LARRY A; CANAN-KOCH STACIE S; DRESS KLAUS R; HUANG BUWEN; KUMPF ROBERT A; LEWIS KATHLEEN K; MATTHEWS JEAN J; SAKATA SYLVIE K; VIRGIL SCOTT C
权利人:AGOURON PHARMA
摘要:The present invention relates to a series of chemical compounds useful as Human Immunodeficiency Virus (HIV) protease inhibitors and to the use of such compounds as antiviral agents. The invention further relates to pharmaceutical compositions containing such antiviral agents, and their uses and materials for their synthesis
专利号:US-7179918-B2
优先权日:2001-06-11
标 题:HIV protease inhibitors, compositions containing the same, their pharmaceutical uses and materials for their synthesis
发明人:CANAN KOCH STACIE S; ALEXANDER THERESE N; BURKE BENJAMIN J; JEWELL TANYA M; KUCERA DAVID J; LINTON MARIA ANGELICA; MITCHELL JR LENNERT J; REICH SIEGFRIED H; SKALITZKY DONALD J; TATLOCK JOHN H; VARNEY MICHAEL D; VIRGIL SCOTT C; WEBBER STEPHEN E; WORLAND STEPHEN T; BARVIAN MARK; BOLTON GARY; BOYER JR FREDERICK EARL; MACHAK JEFFREY J; HOLLER TOD; MURPHY SEAN T; MELNICK MICHAEL; JOSYULA VARA PRASAD
权利人:AGOURON PHARMA
摘要:Compounds of the formula: n nwhere the formula variables are as defined herein, are disclosed that advantageously inhibit or block the biological activity of the HIV protease. These compounds, as well as pharmaceutical compositions containing these compounds, are useful for treating patients or hosts infected with the HIV virus. Intermediates and synthetic methods for preparing such compounds are also described.
专利号:US-7094909-B2
优先权日:2001-06-11
标 题 :HIV protease inhibitors, compositions containing the same, their pharmaceutical uses and materials for their synthesis
发明人:KUCERA DAVID JOHN; SCOTT ROBERT WILLIAM
权利人:AGOURON PHARMA
摘要:The present invention concerns processes for preparing compounds of formula (I-H), or a prodrug, pharmaceutically active metabolite, or pharmaceutically active salt or solvate thereof, n nwhich are useful as inhibitors of the HIV protease enzyme.