专利号:US-5736535-A 优先权日:1992-04-16 标 题:1-pyrimidinylacetamide compounds which are inhibitors of human leukocyte elastase 发明人:BERNSTEIN PETER ROBERT; EDWARDS PHILIP DUKE; SHAW ANDREW; SHENVI ASHOKKUMAR BHIKKAPPA; THOMAS ROYSTON MARTIN; VEALE CHRIS ALLAN; WARNER PETER; WOLANIN DONALD JOHN 权利人:ZENECA LTD 摘要:The present invention relates to certain novel substituted derivatives which are 1-pyrimidinylacetamide derivatives of formula I, ##STR1## which are inhibitors of human leukocyte elastase (HLE), also known as human neutrophil elastase (HNE), making them useful whenever such inhibition is desired, such as for research tools in pharmacological, diagnostic and related studies and in the treatment of diseases in mammals in which HLE is implicated. The invention also includes intermediates useful in the synthesis of these substituted derivatives, processes for preparing the substituted derivatives, pharmaceutical compositions containing such substituted derivatives and methods for their use.
专利号:US-5254558-A 优先权日:1991-08-15 标 题:Substituted 1,3-diazines as leukocyte elastase inhibitors 发明人:BERNSTEIN PETER R; EDWARDS PHILIP D; THOMAS ROYSTON M; VEALE CHRIS A; WARNER PETER; WOLANIN DONALD J 权利人:ICI PLC 摘要:The present invention relates to certain novel substituted heterocycles which are 1-pyrimidinylacetamide compounds of formula I, set out herein, which are inhibitors of human leukocyte elastase (HLE), also known as human neutrophil elastase (HNE), making them useful whenever such inhibition is desired, such as for research tools in pharmacological, diagnostic and related studies and in the treatment of diseases in mammals in which HLE is implicated. The invention also includes intermediates useful in the synthesis of these substituted heterocycles, processes for preparing the substituted heterocycles, pharmaceutical compositions containing such substituted heterocycles and methods for their use.
专利号:WO-9321213-A1 优先权日:1992-04-16 标题 :Alpha-aminoboronic acid peptides and their use as elastase inhibitors 发明人:BERNSTEIN PETER ROBERT; SHAW ANDREW; SHENVI ASHOKKUMAR BHIKKAPPA; THOMAS ROYSTON MARTIN; WARNER PETER; WOLANIN DONALD JOHN 权利人:ZENECA LTD 摘要:The present invention relates to certain novel heterocyclic derivatives which are 1-pyridylacetamide derivatives of formula (I), set out herein, which are inhibitors of human leukocyte elastase (HLE), also known as human neutrophil elastase (HNE), making them useful whenever such inhibition is desired, such as for research tools in pharmacological, diagnostic and related studies and in the treatment of diseases on mammals in which (HLE) is implicated. The invention also includes intermediates useful in the synthesis of these heterocyclic derivatives, processes for preparing the heterocyclic derivatives, pharmaceutical compositions containing such heterocyclic derivatives and methods for their use.
专利号:US-5721222-A 优先权日:1992-04-16 标 题 :Heterocyclic ketones 发明人:BERNSTEIN PETER ROBERT; SHAW ANDREW; THOMAS ROYSTON MARTIN; VEALE CHRIS ALLAN; WARNER PETER; WOLANIN DONALD JOHN 权利人:ZENECA LTD 摘要:The present invention relates to certain novel heterocyclic ketones which are 1-pyridylacetamide ketones of formula I, set out herein, which are inhibitors of human leukocyte elastase (HLE), also known as human neutrophil elastase (HNE), making them useful whenever such inhibition is desired, such as for research tools in pharmacological, diagnostic and related studies and in the treatment of diseases in mammals in which HLE is implicated. The invention also includes intermediates useful in the synthesis of these heterocyclic ketones, processes for preparing the heterocyclic ketones, pharmaceutical compositions containing such heterocyclic ketones and methods for their use.
专利号:CN-115108962-A 优先权日:2022-08-01 标 题:A kind of method for continuous synthesis of azabicyclic compounds
专利号:US-5441960-A 优先权日:1992-04-16 标题:1-pyrimidinylacetamide human leukocyte elastate inhibitors 发明人:BERNSTEIN PETER R; EDWARDS PHILIP D; SHAW ANDREW; THOMAS ROYSTON M; VEALE CHRIS A; WARNER PETER; WOLANIN DONALD J 权利人:ZENECA LTD 摘要:The present invention relates to certain novel substituted ketones which are 1-pyrimidinylacetamide derivatives of formula I, ##STR1## set out herein, which are inhibitors of human leukocyte elastase (HLE), also known as human neutrophil elastase (HNE), making them useful whenever such inhibition is desired, such as for research tools in pharmacological, diagnostic and related studies and in the treatment of diseases in mammals in which HLE is implicated. The invention also includes intermediates ##STR2## useful in the synthesis of these substituted ketones processes for preparing the substituted ketones pharmaceutical compositions containing such substituted ketones and methods for their use.
参考文献:10.1007/s10870-012-0353-2 摘要:Smith G, Wermuth UD. Cyclic Imide and Open-Chain Amide Carboxylic Acid Derivatives from the Facile Reaction of cis-Cyclohexane-1,2-Dicarboxylic Anhydride with Three Substituted Anilines. Journal of Chemical Crystallography. 2012 Aug 21;42(10):1029–35. doi: 10.1007/s10870-012-0353-2. 参考文献:10.1134/s1070428012060164 摘要:Mironov ME, Shul’ts EE, Shakirov MM, Kharitonov YV, Tolstikov GA. Synthetic transformations of higher terpenoids: XXVIII. Diels-Alder reactions of 16-(trimethylsiloxybutadienyl) labdanoids. Russian Journal of Organic Chemistry. 2012 Jun;48(6):840–50. doi: 10.1134/s1070428012060164. 参考文献:10.1016/s1044-0305(99)00141-5 摘要:Muscat D, Henderickx H, Kwakkenbos G, van Benthem R, de Koster CG, Fokkens R, Nibbering NMM. In-source decay of hyperbranched polyesteramides in matrix-assisted laser desorption/ionization time-of-flight mass spectrometry. Journal of The American Society for Mass Spectrometry. 2000 Mar 01;11(3):218–27. doi: 10.1016/s1044-0305(99)00141-5.