专利号:US-10676423-B2 优先权日:2017-02-21 标题 :Structure and synthesis of highly fluorinated amino acid derivatives 发明人:WEAVER JIMMIE DEAN; TEEGARDIN KIP ALLEN; ARORA AMANDEEP 权利人:UNIV OKLAHOMA STATE 摘要:Methods of synthesizing polyfluorinated amino acid derivatives are disclosed, along with polyfluorinated amino acid derivatives produced from said methods, as well as compositions containing same. The synthesis methods utilize an oxazolone and a perfluoroarene to produce the polyfluorinated amino acid derivatives.
专利号:US-2010273787-A1 优先权日:2007-11-15 标题:Kynurenine-aminotransferase inhibitors 发明人:SCHWARCZ ROBERT; KAJII YASUSHI; ONO SHIN-ICHIRO 权利人:SCHWARCZ ROBERT; KAJII YASUSHI; ONO SHIN-ICHIRO 摘要:Compounds of formula (I): prodrug derivatives and/or pharmaceutically acceptable salt thereof, selectively inhibit the enzyme kynurenine aminotransferase, thereby reducing the synthesis of kynurenic acid. The compounds are used for the treatment of psychiatric and neurological diseases which benefit from an increase in glutamatergic and/or cholinergic neurotransmission, such as schizophrenia, depression, bipolar illness, anxiety and Alzheimer's disease. Furthermore, the compounds of the invention are useful for stimulating attention, memory and other cognitive processes in normal individuals of any age, including children, adolescents and the elderly. Additionally, the compounds of the invention are also useful for treatment of patients suffering from malaria by preventing parasite gametogenesis and fertility based on reduction of xanthurenic acid formation from its bioprecursor 3-hydroxy kynurenine.
专利号:WO-2006013085-A1 优先权日:2004-08-06 标题 :4-sulfonyl-substituted benzoylalanine derivates useful as kynurenine-aminotransferase inhibitors 发明人:PELLICCIARI ROBERTO; SCHWARCZ ROBERT; GUIDETTI PAOLO 权利人:PELLICCIARI ROBERTO; SCHWARCZ ROBERT; GUIDETTI PAOLO 摘要:The invention relates to compounds of formula (I), in which R, R' and R' are as defined in the disclosure and the pharmaceutically acceptable esters thereof. The compounds of the invention reduce the synthesis of kynurenic acid thus inhibiting the enzyme kynurenine aminotransferase and can be used for the preparation of medicaments for the treatment of those psychiatric and neurological diseases which benefit from an increase in glutamatergic and/or cholinergic neurotransmission, such as depression, bipolar illness, anxiety, Alzheimer's disease. Furthemore, the compounds of the invention are useful for stimulating attention, memory and other cognitive processes in normal individuals of any age, including children, adolescents and the elderly.
专利号:US-2020123099-A1 优先权日:2017-02-21 标题 :Structure and Synthesis of Highly Fluorinated Amino Acid Derivatives
专利号:US-5514694-A 优先权日:1992-09-21 标题 :Peptidyl ketoamides 发明人:POWERS JAMES C; LI ZHAOZHAO; PATIL GIRISH S; CHU DER-LUN 权利人:GEORGIA TECH RES INST 摘要:A novel class of peptide alpha -ketoamides useful for selectively inhibiting serine proteases, selectively inhibiting cysteine proteases, generally inhibiting all serine proteases, and generally inhibiting all cysteine proteases, having the formula Y-CO-AA2-AA1-CO-NH-X. Processes for the synthesis of peptidyl alpha -ketoamide derivatives.
专利号:US-8518885-B2 优先权日:2008-02-06 标题 :Heterocyclic peptide ketoamides 发明人:POWERS JAMES C; GLASS JONATHAN D; OVAT ASLI; LI ZHAOZHAO 权利人:POWERS JAMES C; GLASS JONATHAN D; OVAT ASLI; LI ZHAOZHAO; GEORGIA TECH RES INST; UNIV EMORY 摘要:A novel class of peptide α-ketoamides useful for selectively inhibiting calpains, selectively inhibiting cysteine proteases, and generally inhibiting all cysteine proteases, having the formula M-AA 2 -AA 1 -CO—NH—(CH 2 ) n —R 3 . Processes for the synthesis of peptidyl α-ketoamide derivatives. Compositions and methods for inhibiting cysteine proteases, inhibiting calpains, and treating disease caused by cysteine proteases and calpains are provided.
参考标题:A Step-Economic And One-Pot Access To Chiral Cα-Tetrasubstituted α-Amino Acid Derivatives Via A Bicyclic Imidazole-Catalyzed Direct Enantioselective C-Acylation 作者:Mo Wang,Muxing Zhou,Lu Zhang,Zhenfeng Zhang,Wanbin Zhang 摘要:Cα-Tetrasubstituted α-Amino Acids Are Ubiquitous And Unique Structural Units In Bioactive Natural Products And Pharmaceutical Compounds. The Asymmetric Synthesis Of These Molecules Has Attracted A Lot Of Attention, But A More Efficient Method Is Still Greatly Desired. Here We Describe The First Sequential Four-Step Acylation Reaction For The Efficient Synthesis Of Chiral Cα-Tetrasubstituted α-Amino Acid Derivatives
合成参考文献
参考文献:10.3389/fphar.2011.00031 摘要:McNally K, Cotton R, Loizou GD. A Workflow for Global Sensitivity Analysis of PBPK Models. Front Pharmacol. 2011;2():31.