📜N-苄氧羰基-L-脯氨酸置于palladium On Activated Charcoal N-羟基-7-氮杂苯并三氮唑,氢气,1-(3-二甲基氨基丙基)-3-乙基碳二亚胺体系中,用 甲醇,N,N-二甲基甲酰胺 用作溶剂,化学反应生成N,N-二甲基吡咯烷-2-甲酰胺 参考文献:Structure-activity Relationships Of The Peptide Deformylase Inhibitor Bb-3497: Modification Of The P2' And P3' Side Chains 标题:Structure-activity Relationships Of The Peptide Deformylase Inhibitor Bb-3497: Modification Of The P2' And P3' Side Chains 摘要:Structural Modifications To The Peptide Deformylase Inhibitor Bb-3497 Are Described. In This Paper,We Describe The Initial Sar Around This Lead For Modifications To Both The P2' And P3' Side Chains. Enzyme Inhibition And Antibacterial Activity Data Revealed That A Variety Of Substituents Are Tolerated At The P2' And P3' Positions Of The Inhibitor Backbone. The Data From This Study Highlights The Potential For Modification At The P2' And P3' Positions To Optimise The Physicochemical Properties. (C) 2003 Elsevier Ltd. All Rights Reserved. Doi:10.1016/s0960-894X(03)00533-X
专利号:US-6906046-B2 优先权日:2000-12-22 标题 :Pharmaceutical uses and synthesis of benzobicyclooctanes 发明人:JACKSON RANDY W; DARWISH IHAB; BAUGHMAN TED A; HOWBERT J JEFFRY 权利人:CELLTECH R & D INC 摘要:Benzobicyclooctane compounds, their use in inhibiting cellular events involving TNF-α and IL-8, and in the treatment of inflammation events in general; a combinatorial library of diverse bicyclooctanes and process for their synthesis as a library and as individual compounds.
专利号:US-8338620-B2 优先权日:2007-04-03 标 题:Methods for the production of C-8 lactam lactone compounds 发明人:SEDELMEIER GOTTFRIED 权利人:SEDELMEIER GOTTFRIED; NOVARTIS AG 摘要:The invention related to a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, especially renin inhibitors, such as Aliskiren, the invention relates to a process for the manufacture of a compound of the formula I, n nor a salt thereof, wherein R1 as well as Act are as defined in the specification, and processes of manufacturing this compound as well as intermediates in this process.
专利号:US-6797820-B2 优先权日:1999-12-17 标 题:Succinate compounds, compositions and methods of use and preparation 发明人:PATEL DINESH; JACOBS JEFFREY W; JAIN RAKESH; NI ZHI-JIE; YUAN ZHENGYU 权利人:VICURON PHARM INC 摘要:Novel hydroxamic acid compounds are disclosed. These hydroxamates inhibit peptidyl deformylase (PDF), an enzyme present in prokaryotes. The hydroxymates are useful as antimicrobials and antibiotics. The compounds of the invention display selective inhibition of peptidyl deformylase versus other metalloproteinases such as matrix metalloproteinases (MMPs). Methods of synthesis and of use of the compounds are also disclosed.
专利号:US-2003069305-A1 优先权日:2000-12-22 标题:Pharmaceutical uses and synthesis of benzobicyclooctanes
专利号:WO-02051851-A2 优先权日:2000-12-22 标题:Pharmaceutical uses and synthesis of benzobicyclooctanes
专利号:RU-2198879-C2 优先权日:1996-09-25 标题:Derivatives of quinazoline, methods of their synthesis, pharmaceutical compositions comprising thereof, method of attainment of antiangiogenic effect and/or effect of blood vessel permeability reduction in warm-blooded animal