- Rapid Synthesis of a Lipocationic Polyester Library via Ring-Opening Polymerization of Functional Valerolactones for Efficacious siRNA Delivery
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The ability to control chemical functionality is an exciting feature of modern polymer science that enables precise design of drug delivery systems. Ring-opening polymerization of functional monomers has emerged as a versatile method to prepare clinically translatable degradable polyesters.1 A variety of functional groups have been introduced into lactones; however, the direct polymerization of tertiary amine functionalized cyclic esters has remained elusive. We report a strategy that enabled the rapid synthesis of >130 lipocationic polyesters directly from functional monomers without protecting groups. These polymers are highly effective for siRNA delivery at low doses in vitro and in vivo.
- Hao, Jing,Kos, Petra,Zhou, Kejin,Miller, Jason B.,Xue, Lian,Yan, Yunfeng,Xiong, Hu,Elkassih, Sussana,Siegwart, Daniel J.
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Read Online
- Preparation method of aliphatic mercaptan
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The invention provides a novel method for preparing (CH3CH2) 2NCH2CH2SH, wherein alkali is added when (CH3CH2) 2NH is recovered, so that the content of impurities in the recovered (CH3CH2) 2NH is reduced, and particularly, the impurities which can influence the synthesis of (CH3CH2) 2NCH2CH2SH in the recovered (CH3CH2) 2NH are removed, so that the recovered (CH3CH2) 2NH can be reused in the production of (CH3CH2) 2NCH2CH2SH.
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Paragraph 0045; 0047; 0049-0053; 0055; 0058; 0060; 0063; ...
(2021/08/28)
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- Preparation method of aliphatic mercaptan
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The invention provides a novel method for preparing (CH3CH2) 2NCH2CH2SH, i.e., the reaction is carried out at a lower temperature, and the reaction is controllable by adopting a manner of dropwise adding materials, so that the safe production is realized.
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Paragraph 0030; 0032-0035; 0037-0039; 0041-0042; 0044; ...
(2021/08/28)
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- Method for producing tiamulin by using diethylaminoethanethiol synthesis liquid
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The invention relates to a chemical synthesis method of a veterinary drug substance, in particular to a method for producing tiamulin by using low-concentration diethylaminoethanethiol. The method comprises the following steps: reacting cyclosulfane with
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Paragraph 0021; 0024; 0027
(2021/12/07)
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- A diethylamino thiol preparation method
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The invention relates to a preparation method for diethylaminoethanethiol. The preparation method comprises firstly putting ethylene sulfide in a sealed reactor, slowly stirring, adding ethene diamine, heating to 30 DEG C-40 DEG C, dropwise adding a sodiu
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Paragraph 0018; 0019; 0020; 0021; 0022; 0023; 0024-0029
(2017/08/25)
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- Microwave-assisted activation and modulator removal in zirconium MOFs for buffer-free CWA hydrolysis
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A novel, facile and efficient method was developed for the activation of acetic acid modulated zirconium MOFs. The protocol involves briefly heating the material in water using microwave irradiation. MOF-808, DUT-84 and UiO-66 were all activated in this manner to remove the modulator and organic solvent from the framework post synthesis, with retention of MOF integrity post activation. The degree of activation was characterised by the use of TGA and NMR. The catalytic activity of the activated MOFs and their non-activated counterparts was investigated for chemical warfare agent (CWA) hydrolysis. Upon activation, an increase in the rate of hydrolysis was observed in the degradation of CWA simulant dimethyl 4-nitrophenyl phosphate (DMNP). MOF-808 and DUT-84 were also screened as catalysts for the hydrolysis of the V-series agent VM, with remarkable half-lives obtained for MOF-808 in the absence of any buffers. Currently employed MOF activation procedures involve the use of additional organic solvents post synthesis; we believe this method to be ideally efficacious for the organic desolvation of zirconium MOFs and removing modulator additives.
- Kalinovskyy,Cooper,Main,Holder,Blight
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p. 15704 - 15709
(2017/12/02)
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- LIPOCATIONIC POLYMERS AND USES THEREOF
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Polymers produced by ring opening polymerization which comprises an amino group that can be used in compositions to deliver a nucleic acid such as a miRNA or a siRNA. In some embodiments, compositions which comprise the polymers described herein and a nucleic acid are also provided herein. In some embodiments, these compositions are used to silence one or more genes in vivo or treat a disease or disorder.
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Page/Page column 46;47
(2016/07/05)
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- Synthesis technology for N,N-diethylaminoethanethiol
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The invention discloses a synthesis technology for N,N-diethylaminoethanethiol. The synthesis technology includes the steps of pressing ethylene sulfide and diethylamine into a pressure reaction kettle by nitrogen, heating to the temperature of 70 DEG C-9
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Paragraph 0011
(2016/11/21)
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- VARIANTS OF PHOSPHOTRIESTERASE FOR THE HYDROLYSIS AND DETOXIFICATION OF NERVE AGENTS
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Variants of phosphotriesterase have been created that exhibit enhanced hydrolysis of V-type and G-type nerve agents over wild-type phosphotriesterase. V- and G-type nerve agents have an SP and RP enantiomer. The SP enantiomers are more toxic. V-type nerve
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Paragraph 0199
(2016/05/24)
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- Variants of Phosphotriesterase for the Enhanced Detoxification of the Chemical Warfare Agent VR
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The V-type organophosphorus nerve agents are among the most hazardous compounds known. Previous efforts to evolve the bacterial enzyme phosphotriesterase (PTE) for the hydrolytic decontamination of VX resulted in the identification of the variant L7ep-3a,
- Bigley, Andrew N.,Mabanglo, Mark F.,Harvey, Steven P.,Raushel, Frank M.
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p. 5502 - 5512
(2015/09/15)
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- Structure-Activity Relationships among Di- and Tetramine Disulfides Related to Benextramine
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The synthesis and irreversible α-blocking activity in the rat vas deferens of a series of tetra- and diamine disulfides 2-38, structural analogues of benextramine (BHC), are described. All compounds containing a central cystamine moiety displayed an irreversible α-adrenergic blockade at concentrations ranging from 10-4 to 6*10-6 M. Potency was increased in cystamines N,N'-disubstituted with 6-aminohexyl groups, especially when the outer nitrogen atoms bear arylalkyl substituents or are enclosed in a ring. However, N,N,N',N'-tetrasubstituted cystamines were poor blockers. Structural specificity in the outer portion of the tetramine disulfide is low, since many types of substituents gave rise to potent α-blockers. Even replacement of the outer amines with nonbasic ethers or amides was observed to maintain irreversible α-blockade.
- Alvarez, M.,Granados, R.,Mauleon, D.,Rosell, G.,Salas, M.,et al.
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p. 1186 - 1193
(2007/10/02)
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- Pesticidal compositions containing phosphoric esters and divalent sulphur compounds
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Pesticidal composition comprising: a pesticidal, phosphoric ester the molecule of which has at least one alkyl group of 1 to 3 carbon atoms, 0.05 to 10% of an agent stabilizing the said ester against decomposition by protonisation, together with adjuvants characterized in that the stabilizing agent comprises at least one sulphur compound containing per molecule at least one divalent sulphur atom of which one valence is bonded to an atom chosen from sulphur, carbon, nitrogen, hydrogen, and metals capable of giving a salt, the other valence being bonded to an atom chosen from hydrogen, the carbon atom already noted, a second carbon atom, the nitrogen atom already noted, a second nitrogen atom, the metal atom already noted in the case of a metal of valence greater than one, a second atom of metal and oxygen when the first valence is not attached to an atom of hydrogen, the proportion of sulphur calculated with reference to the weight of the sulphur compound being between 5 and 99%. Process for stabilizing a phosphoric ester of which the molecule possesses at least one alkyl group containing 1 to 3 carbon atoms characterized in that there is added to the phosphoric ester or to a mixture which contains it, 0.05 to 10% calculated on the weight of the phosphoric acid ester of an agent capable of stabilizing the said phosphoric ester against protonisation and comprising at least one sulphur compound such as that defined thereupon.
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