Ethyl 4-Amino-3-Chlorobenzoate Acetate置于sodium Hydroxide体系中,用 甲醇 用作溶剂,化学反应 3.0H,反应生成3-氯-4-氨基苯甲酸 参考文献:Drug Evolution Concept In Drug Design: 1. Hybridization Method 标题:Drug Evolution Concept In Drug Design: 1. Hybridization Method 摘要:A Novel Concept,"Drug Evolution",Is Proposed To Develop Chemical Libraries That Have A High Probability Of Finding Drugs Or Drug Candidates. It Converts Biological Evolution Into Chemical Evolution. In This Paper,We Present "Hybridization" Drug Evolution,Which Is The Equivalent Of Sexual Recombination Of Parental Genomes In Biological Evolution. The Hybridization Essentially Shuffles The Building Blocks Of The Parent Drugs And Ought To Drug(S); No Drug Evolution Can Otherwise occur. We Hybridized Two Drugs,Benzocaine And Metoclopramide And Generated 16 Molecules That Include The Parent Drugs,Four Known Drugs,And Two Molecules Whose Therapeutic Activities Are Reported. The Unusually High Number Of Drugs And Drug Candidates In The Library Encourages High Expectations Of Finding New Drug(S) Or Drug Candidate(S) Within The Remaining Eight Compounds. Interestingly,The Therapeutic Applications Of The Eight Drugs Or Drug Candidates In The Library Are Fairly Diverse As 38 Therapeutic Applications And 25 Molecular Targets Are Counted. Therefore,The Library Fits As A General Chemical Library For Unspecified Therapeutic Activities. The Hybridization Of Other Two Drugs,Aspirin And Cresotamide,Is Also Described To Demonstrate The Generality Of The Method. Doi:10.1021/jm049637+
专利号:US-10005720-B2 优先权日:2013-04-05 标题:Compounds useful for the treatment of metabolic disorders and synthesis of the same 发明人:SEXTON JONATHAN Z; BRENMAN JAY E; MUSSO DAVID L 权利人:NORTH CAROLINA CENTRAL UNIV; UNIV NORTH CAROLINA CHAPEL HILL 摘要:The present invention provides compounds of Formula (I): wherein variables X, Y, Z and R1 are as described herein. Some of the compounds described herein are glutamate dehydrogenase activators. The invention is also directed to pharmaceutical compositions comprising these compounds, uses of these compounds and compositions in the treatment of metabolic disorders as well as synthesis of the compounds.
专利号:US-2018370905-A1 优先权日:2013-04-05 标题:Compounds Useful for the Treatment of Metabolic Disorders and Synthesis of the Same
专利号:US-2025259704-A1 优先权日:2022-06-24 标 题:Systems and methods for cell-free iterative site saturation mutagenesis and its application for the directed evolution of enzymes catalyzing unnatural reactions 发明人:JEWETT MICAHEL C; BOGART JONATHAN W; LANDWEHR GRANT M; Karim Ashty Stephen 权利人:UNIV NORTHWESTERN 摘要:Disclosed are methods, compositions, systems, and protein compounds for the directed evolution of enzymes and proteins. The method comprising generating variant protein with a desired functionality, comprising one or more DNA expression templates comprising nucleic acid sequences encoding a variant protein, expressing the variant protein using cell-free protein synthesis; and analyzing one or more parameters associated with the variant protein.
专利号:US-8003785-B2 优先权日:2008-06-18 标 题 :Halo-substituted pyrimidodiazepines 发明人:CAI JIANPING; CHEN SHAOQING; CHU XIN-JIE; LUK KIN-CHUN; MISCHKE STEVEN GREGORY; SUN HONGMAO; WOVKULICH PETER MICHAEL 权利人:TAKEDA PHARMACEUTICAL 摘要:The present invention provides PLK1 inhibitor compounds of formula I: n nuseful in the treatment or control of cell proliferative disorders, particularly oncological disorders. These compounds and formulations containing such compounds may be useful in the treatment or control of solid tumors, such as, for example, breast, colon, lung and prostate tumors and other oncological diseases such as non-Hodgkin's lymphomas. Also provided are intermediate compounds useful in the synthesis of compounds of formula I.
专利号:EP-2402011-A1 优先权日:2004-08-25 标题:Intermediates in the synthesis of S-triazolyl alpha-mercaptoacetanildes as inhibitors of HIV reverse transcriptase
专利号:US-2016046560-A1 优先权日:2013-04-05 标题 :Compounds useful for the treatment of metabolic disorders and synthesis of the same
[参考文献]: Tomasz Frczek, Et Al. Searching For Novel Scaffold Of Triazole Non-Nucleoside Inhibitors Of Hiv-1 Reverse Transcriptase. J Enzyme Inhib Med Chem. 2016;31(3):481-9.
合成参考文献
参考文献:10.1016/s0891-5849(96)00486-8 摘要:She Z, Mays DC, Sagone, Jr AL, Davis WB. Aminobenzoic Acid Compounds as HOCl Traps for Activated Neutrophils. Free Radical Biology and Medicine. 1997;22(6):989–98. doi: 10.1016/s0891-5849(96)00486-8.