78531-45-0Relevant academic research and scientific papers
Novel pH-sensitive cationic lipids with linear ortho ester linkers for gene delivery
Chen, Haigang,Zhang, Huizhen,Thor, Der,Rahimian, Roshanak,Guo, Xin
, p. 159 - 172 (2012)
In an effort to develop pH-sensitive lipoplexes for efficient gene delivery, we report three novel cationic lipids containing a linear ortho ester linker that conjugates either the headgroup (Type I) or one hydrocarbon chain (Type II) with the rest of the lipid molecule. The cationic lipids carry either an iodide or a chloride counterion. Compared to our previously reported cyclic ortho ester linker, the linear ortho ester linker facilitated the construction of cationic liposomes and lipoplexes with different helper lipids. The chloride counterion not only facilitated the hydration of the lipid films during liposome construction, but also enhanced the hydrolysis of the ortho ester linker in the lipoplexes. After incubation at endosomal pH 5.5, the Type I lipoplexes aggregated and destabilized the endosome-mimicking model liposomes, but not the Type II lipoplexes. The helper lipids (DOPE or cholesterol) of the lipoplexes enhanced the pH-sensitivity of the Type I lipoplexes. In CV-1 cells (monkey kidney fibroblast), the Type I ortho ester-based lipoplexes, especially those with the chloride counterion, significantly improved the gene transfection efficiency, in some cases by more than 100 fold, compared to their pH-insensitive counterparts consisting of DOTAP. The gene transfection efficiency of the ortho ester-based lipoplexes was well correlated with their rate of aggregation and membrane destabilization in response to the endosomal pH 5.5.
COMPOUNDS, COMPOSITIONS AND METHODS FOR STABILIZING TRANSTHYRETIN AND INHIBITING TRANSTHYRETIN MISFOLDING
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Paragraph 0559-0562, (2021/08/06)
Provided herein are compounds having activity against TTR related conditions, and pharmaceutically accepted salts and solvates thereof. Also provided are methods of using the compounds for inhibiting and preventing TTR aggregation and/or amyloid formation in the peripheral nerves, kidney, cardiac tissue, eye and CNS, and of treating a subject with peripheral TTR amyloidosis.
5-dimethylamino-1, 3-dioxane-2-ketone as well as preparation method and application thereof
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Paragraph 0022-0025; 0027; 0029; 0031-0033, (2019/03/29)
The invention discloses 5-dimethylamino-1, 3-dioxane-2-ketone as well as a preparation method and the application thereof. The structural formula of the 5-dimethylamino-1, 3-dioxane-2-ketone is as shown in the formula (I). The 5-dimethylamino-1, 3-dioxane-2-ketone can be copolymerized with a cyclic carbonate monomer and a lactone monomer further, so as to prepare a functional aliphatic polycarbonate and poly(ester-carbonic ester) copolymer. A tertiary amino on a side chain of the polymer carries positive charges under a physiological condition and can be used for killing pathogenic bacteria with negative charges. Therefore, the polymer is a good antibacterial biological material. The 5-dimethylamino-1, 3-dioxane-2-ketone is simple in preparation process and has higher application value.
FREE-STANDING NON-FOULING POLYMERS, THEIR COMPOSITIONS, AND RELATED MONOMERS
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Page/Page column 51, (2017/01/23)
Free-standing non-fouling polymers and polymeric compositions, monomers and macromonomers for making the polymers and polymeric compositions, objects made from the polymers and polymeric compositions, and methods for making and using the polymers and polymeric compositions.
2 - N, N - dimethyl - 1, 3 - diazido-propane and its preparation method
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Paragraph 0024; 0027-0030, (2017/11/17)
The invention relates to N,N-dimethyl-1,3-diazidopropane and a preparation method thereof, belongs to the field of high-energy nitrogen-containing compounds and provides the structure formula of the N,N-dimethyl-1,3-diazidopropane. The preparation method of the N,N-dimethyl-1,3-diazidopropane is that 2-amino-1, 3-dihydroxy propane, formaldehyde, formic acid, thionyl chloride and sodium azide are taken as raw materials, firstly the 2-amino-1, 3-dihydroxy propane and the formaldehyde generate N, N-dimethyl-1, 3- dihydroxypropane in a formic acid system, the intermediate reacts with the thionyl chloride to generate N, N-dimethyl-1, 3-2-dichloromethane hydrochloride, and the N, N-dimethyl-1, 3-2-dichloromethane hydrochloride reacts with sodium azide to obtain a finished product of the N,N-dimethyl-1,3-diazidopropane. According to the N,N-dimethyl-1,3-diazidopropane and the preparation method thereof, the raw material cost is low, the operation method is simple and convenient, the product yield is high, besides, the N,N-dimethyl-1,3-diazidopropane can solve the problems that toxicity of liquid propellant methylhydrazine is large and the firing time of N,N-Dimethylazidoethylamine is long and has a good market application prospect.
COMPOUNDS FOR INHIBITING CELL PROLIFERATION IN EGFR-DRIVEN CANCERS
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Page/Page column 72-73, (2013/12/03)
The invention features compounds, pharmaceutical compositions and methods for treating patients who have an EGFR-driven cancer of Formula (I), wherein the variables are as defined herein.
Cationic and polycationic amphiphiles, reactives containing the same and their use
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, (2008/06/13)
PCT No. PCT/EP96/02541 Sec. 371 Date Dec. 5, 1997 Sec. 102(e) Date Dec. 5, 1997 PCT Filed Jun. 12, 1996 PCT Pub. No. WO97/00241 PCT Pub. Date Jan. 3, 1997The invention concerns new cationic or polycationic amphiphiles which are capable of forming aggregates with macromolecules, in particular with DNA or RNA, and it concerns their delivery into prokaryotic or eukaryotic cells. Compounds with spermyl-dioleoyloxypropyl structure have proven to be particularly preferable.
Process for the preparation of serinol and of serinol derivatives, and products obtained therefrom
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, (2008/06/13)
A method for the synthesis of serinol and serinol derivatives substituted at the nitrogen atoms by reacting a lower 1,3-dialkoxy-isopropyl halide with ammonia or an amine to form a 1,3-dialkoxy-isopropylamine and then removing the ether groups by heating with a hydrogen halide acid. The method allows the production of serinol and serinol derivatives using inexpensive starting materials in a simple manner and obtaining a high purity product which is free of interfering isomers. Novel compounds obtained by the method which are useful as pharmaceutical intermediates, X-ray contrasting agents and cytostatic or psychopharmacological drugs are also disclosed.
