CAS: 3386-42-3; 2,5-Dichlorophenylisothiocyanate

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CAS号1414781-44-4 1,4-diazabicycl... | CAS号95-82-9 2,5-二氯苯胺 | CAS号594-42-3 全氯甲硫醇 | CAS号463-71-8 硫光气 | CAS号86317-31-9 O-(4-methoxyphe... | CAS号127142-39-6 1-(2,5-dichloro...

📜1,4-Diazabicyclo[2.2.2]octane;(2,5-Dichlorophenyl)Carbamodithioic Acid置于三光气体系中,用 二氯甲烷 用作溶剂,化学反应 5.0H,反应生成2,5-二氯异硫氰酸苯酯
参考文献:Structural Optimization And Structure-activity Relationships Of N2-(4-(4-Methylpiperazin-1-yl)Phenyl)-N8-Phenyl-9H-Purine-2,8-Diamine Derivatives,A New Class Of Reversible Kinase Inhibitors Targeting Both Egfr-Activating And Resistance Mutations
标题:Structural Optimization And Structure-activity Relationships Of N2-(4-(4-Methylpiperazin-1-yl)Phenyl)-N8-Phenyl-9H-Purine-2,8-Diamine Derivatives,A New Class Of Reversible Kinase Inhibitors Targeting Both Egfr-Activating And Resistance Mutations
摘要:This Paper Describe The Structural Optimization Of A Hit Compound,N-2-(4-(4-Methylpiperazin-1-yl)Phenyl)-N-8-Phenyl-9H-Purine-2,8-Diamine (1),Which Is A Reversible Kinase Inhibitor Targeting Both Egfr-Activating And Drug-Resistance (T790M) Mutations But Has Poor Binding Affinity. Structure-Activity Relationship Studies Led To The Identification Of 9-Cyclopentyl-N-2-(4-(4-Methylpiperazin-1-yl)Phenyl)-N-8-Phenyl-9H-Purine-2,8-Diamine (9E) That Exhibits Significant In Vitro Antitumor Potency Against The Non-Small-Cell Lung Cancer (Nsclc) Cell Lines Hcc827 And H1975,Which Harbor Egfr-Activating And Drug-Resistance Mutations,Respectively. Compound 9E Was Further Assessed For Potency And Selectivity In Enzymatic Assays And In Vivo Anti-Nsclc Studies. The Results Indicated That Compound 9E Is A Highly Potent Kinase Inhibitor Against Both Egfr-Activating And Resistance Mutations And Has Good Kinase Spectrum Selectivity Across The Kinome. In Vivo,Oral Administration Of Compound 9E At A Dose Of 5 Mg/kg Caused Rapid And Complete Tumor Regression In A Hcc827 Xenograft Model,And An Oral Dose Of 50 Mg/kg Initiated A Considerable Antitumor Effect In An H1975 Xenograft Model.
Doi:10.1021/jm301365E

专利信息

专利号:US-6376649-B1
优先权日:1998-12-18
标题 :Methods for the synthesis of α- hydroxy-β-amino acid and amide derivatives
发明人：SEMPLE JOSEPH E; LEVY ODILE E
权利人:CORVAS INT INC
摘要:Methods for the synthesis of alpha-hydroxy-beta-amino acid and amide derivatives and alpha-ketoamide derivatives and novel derivatives made by these methods are provided. These methods involve reacting a N-terminally blocked (protected) aminoaldehyde with an isonitrile and a carboxylic acid to give an amino-alpha-acyloxy carboxamide. The acyloxy group may be removed to give the derivative. Alternatively the protecting group is removed and acyl shift occurs to give the derivative. These derivatives are useful in the synthesis of compounds such as peptidyl alpha-ketoamides and alpha-hydroxy-beta-carboxylic acid and amide derivatives. Certain of these compounds have been reported to have activity as inhibitors of proteases, such as serine proteases and cysteine proteases.

专利号:US-6133409-A
优先权日:1996-12-19
标 题:Process for the solid phase synthesis of aldehyde, ketone, oxime, amine, hydroxamic acid and αβ-unsaturated carboxylic acid and aldehyde compounds
发明人：SALVINO JOSEPH M; MORTON GEORGE C; MASON HELEN J; LABAUDINIERE RICHARD F
权利人:AVENTIS PHARM PROD INC
摘要:This invention is directed to a process for the solid phase synthesis of aldehyde, ketone, oxime, amine, hydroxamic acid and alpha , beta -unsaturated carboxylic acid and aldehyde compounds and to polymeric hydroxylamine resin compounds useful therefor.

专利号:US-2017349928-A1
优先权日:2014-12-31
标 题:Methods for activating natural energy metabolism for improving yeast cell-free protein synthesis
发明人：JEWETT MICHAEL CHRISTOPHER; ANDERSON MARK J; STARK JESSICA CAROL; HODGMAN CHARLES ERIC
权利人:UNIV NORTHWESTERN
摘要:Disclosed are compositions, methods, and kits for enhanced synthesis of a biological macromolecule in vitro using cell-free protein synthesis. The compositions, methods, and kits include or utilize: a cell-free extract; a phosphate-free energy source; and a phosphate source, and typically do not include an exogenous nucleoside triphosphate or an exogenous nucleoside diphosphate.

专利号:US-2005186197-A1
优先权日:2002-08-29
标 题:Peptide inhibitors of beta lactamases
发明人：PALZKILL TIMOTHY; HUANG WANZHI
摘要:Peptide inhibitors of β-lactamases have been identified by the synthesis of peptide arrays using synthesis SPOT technology. These peptide inhibitors of β-lactamase have activity against a broad spectrum of β-lactamases and are useful in a variety of applications.

专利号:US-2003180804-A1
优先权日:2001-10-29
标题:Solid phase synthesis of chemical libraries
发明人：PRYOR KENT E; LEWIS RONALD D; BROWN JASON W
权利人:CORVAS INT INC
摘要:The present invention provides compounds and compound libraries that are useful as protease modulators. The compounds and compound libraries are preferably made using the methods of the present invention which utilize peptide synthesis and combinatorial chemistry methods on a solid phase.

专利号:US-7674881-B2
优先权日:2005-10-07
标题:Convergent synthesis of proteins by kinetically controlled ligation
发明人：KENT STEPHEN; PENTELUTE BRAD; BANG DUHEE; JOHNSON ERIK; DUREK THOMAS
权利人:UNIV CHICAGO
摘要:The present invention concerns methods and compositions for synthesizing a polypeptide using kinetically controlled reactions involving fragments of the polypeptide for a fully convergent process. In more specific embodiments, a ligation involves reacting a first peptide having a protected cysteyl group at its N-terminal and a phenylthioester at its C-terminal with a second peptide having a cysteine residue at its N-termini and a thioester at its C-termini to form a ligation product. Subsequent reactions may involve deprotecting the cysteyl group of the resulting ligation product and/or converting the thioester into a thiophenylester.