[EN] TARGETED DRUG PHOSPHORYLCHOLINE POLYMER CONJUGATES<br/>[FR] CONJUGUÉS DE POLYMÈRE DE PHOSPHORYLCHOLINE À MÉDICAMENT CIBLÉ
申请人:OLIGASIS
公开号:WO2011075185A1
公开(公告)日:2011-06-23
The present invention provides random copolymers containing phosphorylcholine and one or more functional agents, and methods of preparing such random copolymers.
The invention generally relates to zwitterionic polymers (including zwitterionic copolymers), such as polymethacrylic structures, with pendent functional moieties, such as therapeutic or biologic moieties. More particularly, the invention relates to phosphorylcholine-substituted methacrylic polymers prepared by free radical polymerization and click chemistry, for example, and compositions and products comprising same, as well as related methods and uses of the compositions, for example, as biological or therapeutic agents and in drug delivery thereof.
Radical Dehydroxylative Alkylation of Tertiary Alcohols by Ti Catalysis
作者:Hao Xie、Jiandong Guo、Yu-Quan Wang、Ke Wang、Peng Guo、Pei-Feng Su、Xiaotai Wang、Xing-Zhong Shu
DOI:10.1021/jacs.0c07492
日期:2020.9.30
coupling partners, including allylic carboxylates, aryl and vinyl electrophiles, and primary alkyl chlorides/bromides, making the method complementary to the cross-coupling procedures. The method is highlyselective for the alkylation of tertiary alcohols, leaving secondary/primary alcohols (benzyl alcohols included) and phenols intact. The synthetic utility of the method is highlighted by its 10-gram-scale
醇的脱氧自由基 CC 键形成反应是合成化学中长期存在的挑战,目前的方法依赖于多步骤程序。在此,我们报告了叔醇的直接脱羟基自由基烷基化反应。这一新协议显示了从醇类中生成叔碳自由基的可行性,并为轻松精确地构建全碳四元中心提供了一种方法。该反应在醇和活化烯烃的广泛底物范围内进行。它可以耐受各种亲电偶联伙伴,包括烯丙基羧酸盐、芳基和乙烯基亲电试剂以及伯烷基氯/溴化物,使该方法与交叉偶联程序形成互补。该方法对叔醇的烷基化具有高度选择性,保持仲醇/伯醇(包括苯甲醇)和酚类完好无损。该方法的合成效用因其 10 克规模的反应和复杂分子的后期修饰而突出。实验和 DFT 计算的组合建立了一个合理的机制,暗示通过 Ti 催化的 C-OH 键均裂产生叔碳自由基。
Glycosylated Reversible Addition–Fragmentation Chain Transfer Polymers with Varying Polyethylene Glycol Linkers Produce Different Short Interfering RNA Uptake, Gene Silencing, and Toxicity Profiles
作者:Elizabeth G. L. Williams、Oliver E. Hutt、Tracey M. Hinton、Sophie C. Larnaudie、Tam Le、James M. MacDonald、Pathiraja Gunatillake、San H. Thang、Peter J. Duggan
DOI:10.1021/acs.biomac.7b01168
日期:2017.12.11
Achieving efficient and targeted delivery of short interfering (siRNA) is an important research challenge to overcome to render highly promising siRNA therapies clinically successful. Challenges exist in designing synthetic carriers for these RNAi constructs that provide protection against serum degradation, extended blood retention times, effective cellular uptake through a variety of uptake mechanisms, endosomal escape, and efficient cargo release. These challenges have resulted in a significant body of research and led to many important findings about the chemical composition and structural layout of the delivery vector for optimal gene silencing. The challenge of targeted delivery vectors remains, and strategies to take advantage of nature’s self-selective cellular uptake mechanisms for specific organ cells, such as the liver, have enabled researchers to step closer to achieving this goal. In this work, we report the design, synthesis, and biological evaluation of a novel polymeric delivery vector incorporating galactose moieties to target hepatic cells through clathrin-mediated endocytosis at asialoglycoprotein receptors. An investigation into the density of carbohydrate functionality and its distance from the polymer backbone is conducted using reversible addition–fragmentation chain transfer polymerization and postpolymerization modification.
[EN] DYE COMPOUND, METHOD OF PRODUCING DIPYRROMETHENE METAL COMPLEX COMPOUND, METHOD OF PRODUCING DYE MULTIMER, SUBSTITUTED PYRROLE COMPOUND, COLORED CURABLE COMPOSITION, COLOR FILTER, METHOD OF PRODUCING COLOR FILTER, SOLID-STATE IMAGE SENSOR AND LIQUID<br/>[FR] COMPOSÉ DE COLORANT, PROCÉDÉ DE PRODUCTION D'UN COMPOSÉ À BASE D'UN COMPLEXE MÉTALLIQUE DE DIPYRROMÉTHÈNE, PROCÉDÉ DE PRODUCTION D'UN MULTIMÈRE COLORANT, COMPOSÉ DE PYRROLE SUBSTITUÉ, COMPOSITION COLORÉE DURCISSABLE, FILTRE COULEUR, PROCÉDÉ DE PRODUC
申请人:FUJIFILM CORP
公开号:WO2012011391A1
公开(公告)日:2012-01-26
The invention provides a dye compound having a partial structure represented by the following formula (5): wherein in formula (5), Dye represents a dye structure; G1 represents NR or an oxygen atom; G2 represents a monovalent substituent group having an -Es' value as a steric parameter of 1.5 or more; p represents an integer from 1 to 8; when p is 2 or greater, the two or more structures represented by p may be the same or different from each other; and R represents a hydrogen atom or a monovalent substituent group.