67643-67-8Relevant academic research and scientific papers
Comparison of flow and batch polymerization processes for production of vinyl ether terpolymers for use in the delivery of siRNA
Nyrop, Jason L.,Soheili, Arash,Xiang, Rong,Meng, Fanyu,Waldman, Jacob H.,Jia, Xiujuan,Parmar, Rubina Giarre,Thuronyi, Benjamin W.,Williams, J. Michael,Dimichele, Lisa,Journet, Michel,Howell, Bonnie J.,Mao, Bing,Davies, Ian W.,Colletti, Steven L.,Sepp-Lorenzino, Laura,Guidry, Erin N.
, p. 1119 - 1129 (2014)
Synthetic polymers represent a modifiable class of materials that can serve as adjuvants to address challenges in numerous biomedical and medicinal chemistry applications including the delivery of siRNA. Polymer-based therapeutics offer unique challenges in both synthesis and characterization as compared to small molecule therapeutics. The ability to control the structure of the polymer is critical in creating a therapeutic. Reported herein, are batch and flow polymerization processes to produce amphiphilic terpolymers through a Lewis acid BF3OEt2-catalyzed polymerization. These processes focus on controlling reaction variables, which affect polymer structure in this rapid, exothermic, nonliving cationic polymerization. In addition to analytical characterization of the polymers, the in vivo activity of the polymer-siRNA conjugates is also highlighted - demonstrating that the method of synthesis does affect the in vivo activity of the resulting polymer conjugate. 2014 Wiley Periodicals, Inc. J. Polym. Sci., Part A: Polym. Chem. 2014, 52, 1119-1129 The ability to control the character of the polymer structure in terms of size and monomer incorporation is critical for polymeric biomaterials to move into the clinic. Two scaleable and reproducible processes to prepare amphiphilic terpolymers through a cationic polymerization for use in siRNA delivery are reported. The polymer-siRNA conjugates derived from polymers produced using these two methods are characterized in vivo, illustrating that control over the method of polymer synthesis can affect the polymer produced. Copyright
COMPOSITIONS FOR TARGETED DELIVERY OF SIRNA
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Paragraph 0120, (2016/03/05)
The present invention is directed compositions for targeted delivery of RNA interference (RNAi) polynucleotides to hepatocytes in vivo. Targeted RNAi polynucleotides are administered together with co-targeted delivery polymers. Delivery polymers provide m
Galactose cluster-pharmacokinetic modulator targeting moiety for siRNA
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Page/Page column 27, (2016/02/29)
The present invention is directed compositions for targeted delivery of RNA interference (RNAi) polynucleotides to cell in vivo. The pharmacokinetic modulator improve in vivo targeting compared to the targeting ligand alone. Targeting ligand-pharmacokinet
Compositions for Targeted Delivery of siRNA
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, (2011/09/16)
The present invention is directed compositions for targeted delivery of RNA interference (RNAi) polynucleotides to hepatocytes in vivo. Targeted RNAi polynucleotides are administered together with co-targeted delivery polymers. Delivery polymers provide m
Polyconjugates for In Vivo Delivery of Polynucleotides
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Page/Page column 17, (2008/12/06)
The present invention is directed to compounds, compositions, and methods useful for delivering polynucleotides or other cell-impermeable molecules to mammalian cells. Described are polyconjugates systems that incorporate targeting, anti-opsonization, anti-aggregation, and transfection activities into small biocompatible in vivo delivery vehicles. The use of multiple reversible linkages connecting component parts provides for physiologically responsive activity modulation.
Polyvinylethers for delivery of polynucleotides to mammalian cells
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, (2008/06/13)
A class of polymers for delivery of polynucleotides to cells in described. More specifically, amphiphilic polyvinylethers and compositions containing amphiphilic polyvinylethers are described.
Reversible attachment of a membrane active polymer to a polynucleotide
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, (2008/06/13)
Described is a process for delivering a biologically active compound to a cell by reversibly linking the compound to a membrane active polymer. In particular, polymer-polynucleotide conjugates are described. Methods for reversibly modifying the polymers to decrease cellular toxicity and improve efficacy are provided.
Acetals as New 2′-O-Protecting Functions for the Synthesis of Oligoribonucleotides: Synthesis of Uridine Building Blocks and Evaluation of Their Relative Acid Stability
Matysiak, Stefan,Fitznar, Hans-Peter,Schnell, Ralf,Pfleiderer, Wolfgang
, p. 1545 - 1566 (2007/10/03)
A broad variety of new acyclic vinyl ethers (see 6-41) have been synthesized via the vinyl-interchange reaction of ethyl vinyl ether at room temperature using mercury(II) trifluoroacetate as a highly efficient catalyst. The appropriate vinyl ethers were r
Photochemistry of N-Alk-4-enyl and N-Alk-5-enyl-phthalimides: Two Different Types of Cyclization Reaction
Maruyama, Kazuhiro,Ogawa, Takuji,Kubo, Yasuo,Araki, Takeo
, p. 2025 - 2032 (2007/10/02)
Photochemical reactions of N-alk-4- and -5-enylphthalimides (1a-e) have been investigated.In the photolyses of acetonitrile solutions of (1a-e), intramolecular cyclization reactions accompanying C(=O)-N bond cleavage to give (2a-e) were generally predominant, together with intramolecular hydrogen abstraction in some cases.Photolyses of cis- and trans-N-hex-4-enylphthalimides in acetonitrile solution showed stereospecific cyclization reactions; irridiation of cis-(1e) gave cis-(2e) and that of trans-(1e) gave trans-(2e) selectively with low conversion.In methanol (1d), which has a vinyl ether moiety, gave different types of cyclization product: namely, (8a) and (9a), methanol-incorporated products probably resulting from an intramolecular electron transfer process.
