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CAS号24424-99-5 二碳酸二叔丁酯 | CAS号150-13-0 对氨基苯甲酸 | CAS号110969-44-3 4-((叔丁氧羰基)氨基)苯甲酸乙酯 | CAS号6427-66-3 对叠氮苯甲酸 | CAS号5330-71-2 4-苯基甲氧羰基氨基苯甲酸 | CAS号159217-89-7 N-B°C-4-碘苯胺 | CAS号762-75-4 甲酸叔丁酯 | CAS号89399-17-7 4-氨基-n-乙基苯甲酰胺 | CAS号54977-92-3 4-氨基-N-苄基苯甲酰胺 | CAS号61251-99-8 4-氨基-N-苯乙基苯甲酰胺 | CAS号6331-71-1 4-氨基-N,N-二甲基苯甲酰胺 | CAS号144072-29-7 4-(B°C-氨基)苯甲醇 | CAS号916578-53-5 4-(氯甲基)苯基氨基甲酸叔丁酯 | CAS号478798-20-8 [4-(哌嗪-1-羰基)苯基]... | CAS号51-08-1 4-Amino-N-(2-pi... | CAS号53461-08-8 4-amino-N-[3-(d...

📜对氨基苯甲酸置于氯化亚砜,水,三乙胺,Lithium Hydroxide体系中,用 四氢呋喃,甲醇 作为反应溶剂,化学反应 27.0H,反应生成 N-Boc-4-氨基苯甲酸
参考文献:用于开发有效,可逆和选择性单酰基甘油脂肪酶(magl)抑制剂的4-氯苯甲酰基哌啶衍生物的结构优化
标题:用于开发有效,可逆和选择性单酰基甘油脂肪酶(magl)抑制剂的4-氯苯甲酰基哌啶衍生物的结构优化
摘要:单酰基甘油脂肪酶(magl)抑制剂被认为是各种病理状况(包括几种癌症)的潜在治疗剂.文献中报道了许多magl抑制剂.然而,它们大多数显示出不可逆的作用机理,这引起了重要的副作用.迄今为止,可逆的magl抑制剂的使用仅得到了部分研究,这主要是由于缺乏具有非常好的magl可逆抑制特性的化合物.在这项研究中,我们从显示可逆的magl抑制机制(k I = 8.6μm)的(4-(4-氯苯甲酰基)哌啶-1-基)(4-甲氧基苯基)甲酮(cl6A)铅化合物开始,我们开始对其结构进行优化,我们开发了一种新的高效选择性magl抑制剂(17B,K I = 0.65μm).此外,建模研究表明,该化合物的结合相互作用取代了在magl结合位点复制其h键的结构水分子,从而为开发新的magl抑制剂确定了新的关键锚点.
DOI:10.1021/acs.Jmedchem.6B01459

专利信息

专利号:US-2022356182-A1
优先权日:2009-03-27
标题 :Inhibitors of hepatitis c virus replication
发明人：COBURN CRAIG A; LUDMERER STEVEN W; LIU KUN; WU HAO; SOLL RICHARD; ZHONG BIN; ZHU JIAN
权利人:MERCK SHARP & DOHME
摘要:The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5A inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5A activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.

专利号:US-2004110228-A1
优先权日:2002-04-01
标 题:Combinatorial organic synthesis of unique biologically active compounds
发明人：MCALPINE SHELLI R; TAYLOR RACHEL E; BOLLA MEGAN L; SEGALL ANCA M
摘要:The invention provides a method for making a combinatorial library of cyclic compounds, such as Holliday junction-trapping compounds, comprising the steps of (a) obtaining a plurality of trimers according to the generic structure X 1- X 2- X 3 , wherein X 1 , X 2 and X 3 can be independently any naturally or nonnaturally occurring amino acids or peptidomimetics thereof; (b) optionally coupling a spacer S to the trimer at either end; (c) cyclizing two trimers or trimer-spacer conjugates in a head-to-tail orientation; thereby obtaining a combinatorial library of compounds, wherein the library does not include an unmodifed or naturally occurring Holliday Junction-trapping compounds. The invention additionally provides methods macrocyclic compounds that are synergimycin derivatives.

专利号:US-11053243-B2
优先权日:2009-03-27
标 题:Inhibitors of hepatitis C virus replication
发明人：COBURN CRAIG A; LUDMERER STEVEN W; LIU KUN; WU HAO; SOIL RICHARD; ZHONG BIN; ZHU JIAN
权利人:MERCK SHARP & DOHME
摘要:The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5A inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5A activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.

专利号:US-9090661-B2
优先权日:2009-03-27
标 题:Inhibitors of hepatitis C virus replication
发明人：COBURN CRAIG A; MCCAULEY JOHN A; LUDMERER STEVEN W; LIU KUN; VACCA JOSEPH P; WU HAO; HU BIN; SOLL RICHARD; SUN FEI; WANG XINGHAI; YAN MAN; ZHANG CHENGREN; ZHENG MINGWEI; ZHONG BIN; ZHU JIAN
权利人:MERCK SHARP & DOHME
摘要:The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5A inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5A activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.

专利号:US-2023295613-A1
优先权日:2020-02-14
标 题:Long chain carbon and cyclic amino acids substrates for genetic code reprogramming
发明人：JEWETT MICHAEL C; LEE JOONGOO; MOORE JEFFREY S; SCHWARZ KEVIN J
权利人:UNIV NORTHWESTERN; UNIV ILLINOIS
摘要:Abstract: Disclosed are methods, systems, components, and compositions for synthesis of sequence defined polymers. The methods, systems, components, and compositions may be utilized for incorporating novel substrates that include non-standard amino acid monomers and non-amino acid monomers into sequence defined polymers. As disclosed herein, the novel substrates may be utilized for acylation of tRNA via flexizyme catalyzed reactions. The tRNAs thus acylated with the novel substrates may be utilized in synthesis platforms for incorporating the novel substrates into a sequence defined polymer.

专利号:US-11814621-B2
优先权日:2018-06-01
标题 :Expanding the chemical substrates for genetic code reprogramming
发明人：JEWETT MICHAEL CHRISTOPHER; LEE JOONGOO; MOORE JEFFREY S; SCHWIETER KENNETH E; SCHWARZ KEVIN JEROME
权利人:UNIV NORTHWESTERN; UNIV ILLINOIS
摘要:Disclosed are methods, systems, components, and compositions for synthesis of sequence defined polymers. The methods, systems, components, and compositions may be utilized for incorporating novel substrates that include non-standard amino acid monomers and non-amino acid monomers into sequence defined polymers. As disclosed herein, the novel substrates may be utilized for acylation of tRNA via flexizyme catalyzed reactions. The tRNAs thus acylated with the novel substrates may be utilized in synthesis platforms for incorporating the novel substrates into a sequence defined polymer.