专利号:US-5936128-A 优先权日:1993-11-19 标题:5,6-dihydropyrone derivatives as protease inhibitors and antiviral agents 发明人:ELLSWORTH EDMUND LEE; LUNNEY ELIZABETH; TAIT BRADLEY DEAN 权利人:WARNER LAMBERT CO 摘要:The present invention relates to novel 5,6-dihydropyrone derivatives and related structures which potently inhibit the HIV aspartyl protease blocking HIV infectivity. The 5,6-dihydropyrone derivatives are useful in the development of therapies for the treatment of bacterial and viral infections and diseases, including AIDS. The present invention is also directed to methods of synthesis of multifunctionalized 5,6-dihydropyrones and of related structures.
专利号:WO-0053577-A9 优先权日:1999-03-12 标 题:Hydrazide inhibitors of hiv-1 integrase 发明人:NEAMATI NOURI; POMMIER YVES; LIN ZHAIWEI; BURKE TERRENCE 权利人:US GOV HEALTH & HUMAN SERV; NEAMATI NOURI; POMMIER YVES; LIN ZHAIWEI; BURKE TERRENCE 摘要:The design, synthesis and antiviral activity of novel mercaptosalicylhydrazides are disclosed, which inhibit human immunodeficiency virus type-1 integrase (HIV-1 IN), an essential enzyme for effective viral replication. Examples of the compounds are N,N'-bis(2-mercaptobenzoyl)hydrazide, N,N'-bis(2,2'-dithiosalicyl)hydrazide, and N,N'-bis(2-mercaptobenzyl)-2,2'-dithiosalicylhydrazide. These compounds are effective against the integrase catalytic core domain, inhibit integrase binding to HIV LTR DNA, and inhibit integrase in preassmbled integrase-DNA complexes. The disclosed mercaptosalicylhydrazides are 300 fold less cytotoxic than other known salicylhydrazides, and exhibit antiviral activity. They are also active in Mg+2-based assays, while integrase inhibition by salicylhydrazides is strictly Mn+2-dependent. The mercaptosalicylhydrazides have no detectable effect on other retroviral targets, including reverse transcriptase, protease, and virus attachment, and exhibit no detectable activity against human topoisomerase I at concentrations that effectively inhibited integrase. The mercaptosalicylhydrazides of the invention are therefore selective inhibitors of HIV-1 integrase, are useful in therapeutic compositions for the treatment of HIV disease, and can also be used to find related antiviral drugs.
专利号:US-2007099919-A1 优先权日:2005-10-06 标题 :Composition and synthesis of new reagents for inhibition of HIV replication
专利号:US-7754773-B2 优先权日:2005-10-06 标 题:Composition and synthesis of new reagents for inhibition of HIV replication 发明人:RANA TARIQ M; STEVENSON MARIO; NATHANS ROBIN SCOTT; CAO HONG; ALI AKBAR 权利人:UNIV MASSACHUSETTS 摘要:The present invention provides compounds and compositions for inhibiting Vif and methods for treating viral infection, e.g., HIV infection.
专利号:US-8088884-B2 优先权日:2007-09-27 标 题 :Multi-armed forms of activated polyoxazoline and methods of synthesis thereof 发明人:HARRIS J MILTON; BENTLEY MICHAEL DAVID; YOON KUNSANG; FANG ZHIHAO 权利人:HARRIS J MILTON; BENTLEY MICHAEL DAVID; YOON KUNSANG; FANG ZHIHAO; SERINA THERAPEUTICS INC 摘要:The present disclosure provides novel POZ-2 derivatives, methods for synthesizing POZ-2 derivatives and intermediates useful in such methods. In one embodiment, the POZ-2 derivative comprises two linear POZ chains of the present disclosure linked directly or indirectly to a branching moiety that contains a functional group for linking the POZ-2 derivative to the target molecule. Target molecule-POZ-2 conjugates are also described. In certain embodiment, the POZ-2 derivatives have low polydispersity values and a decreased amount of impurities produced by unwanted side reactions, such as, but not limited to, chain transfer.
专利号:WO-2007044565-A2 优先权日:2005-10-06 标 题 :Composition and synthesis of new reagents for inhibition of hiv replication