- IONIZABLE LIPIDS AND NANOPARTICLE COMPOSITIONS THEREOF
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Provided herein are ionizable lipids represented by the Formula (I): or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, R1, R2, R3, R4, R5,R6, m, and n are as defined herein. Also provided herein are lipid nanoparticle (LNP) compositions comprising an ionizable lipid of the invention and a capsid-free, non-viral vector (e.g., ceDNA). These LNPs can be used to deliver a capsid-free, non-viral DNA vector to a target site of interest (e.g., cell, tissue, organ, and the like).
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Page/Page column 90; 116-117
(2021/05/29)
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- Puerarin derivative with high biological activity as well as preparation method and application thereof
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The invention relates to a puerarin derivative as well as a preparation method and application thereof. The puerarin derivative is characterized in that puerarin is used as a raw material; through five-step reaction, a compound 6 is prepared; then, the co
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Paragraph 0061; 0064; 0065; 0066; 0067; 0068
(2019/02/25)
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- Synthesis method of N-methylamine compound
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The invention discloses a synthesis method of an N-methylamine compound. The synthesis method is characterized in that a carbamyl imidazole compound is used as a raw material; a NaBH4/I2 is used for performing backflow in tetrahydrofuran to prepare an N-methyl structure compound. The used reduction system NaBH4/I2 has the advantages of environment-friendly effect, performance stability, high conversion rate and the like. The synthesis method has the beneficial effects that (1) the synthesis method has wide applicability; amine can be used as the raw material; carboxylic acid can also be used as the raw material; (2) the product yield is high and reaches as high as 82 percent; (3) a synthetic agent is simple and can be easily obtained; the cost is low; the process is simple; the reaction conditions are mild; the synthesis method is suitable for industrial production. A concrete reaction formula is shown in the description, wherein R1 and R2 are identical or different atoms or groups, and are respectively and independently selected from one of hydrogen atoms, C1-C20 straight-chain or branch-chain alkane, C5-C10 naphthenic groups, aryl groups and substituted aryl groups; monosubstitution or multi-substitution is performed on aromatic rings of the substituted aryl groups. In addition, KBH4 is also applicable to the reaction.
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Paragraph 0049-0052
(2018/09/08)
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- Synthesis, SAR and pharmacological characterization of novel anthraquinone cation compounds as potential anticancer agents
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Emodin, a natural anthraquinone derivative isolated from Rheum palmatum L., has been demonstrated to exhibit good anti-cancer effect. In this study, a series of novel quaternary ammonium salts of emodin, anthraquinone and anthrone were synthesized and their anticancer activities were tested in vitro. The effects of emodin quaternary ammonium salts on cell viability, apoptosis, intracellular ROS, and mitochondrial membrane potential were investigated in A375, BGC-823, HepG2 and HELF cells. The results demonstrated that compound 4a induced morphological changes and decreased cell viability. Apoptosis triggered by compound 4a was visualized using DAPI staining and Annexin V-FITC/PI staining. Compound 4a-induced apoptosis of A375 cells were showed to be associated with the dissipation of mitochondrial membrane potential (ΔΨm) as a result of the up-regulation of P53 and Caspase-3. When cancer cells were treated with emodin derivative, their ability to generate reactive oxygen species (ROS) rose significantly and the mitochondrial membrane potential decreased. Additionally, confocal microscopy assay confirmed that compound 4a was primarily located in the mitochondria of A375 cells. These results suggested that compound 4a has the potential for use in cancer therapy.
- Zheng, Yanyan,Zhu, Li,Fan, Lulu,Zhao, Wenna,Wang, Jianlong,Hao, Xianxiao,Zhu, Yunhui,Hu, Xiufang,Yuan, Yaofeng,Shao, Jingwei,Wang, Wenfeng
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p. 902 - 913
(2016/10/25)
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- ALKYLAMINOMETHYLATION D'ORGANOMAGNESIENS.
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The organomagnesium compound RMgX is converted, in two steps, into the secondary amine R-CH2-NH-R1 (R1=CH3 or alkyl).
- Yankep, Emmanuel,Kapnang, Henriette,Charles, Georges
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p. 7383 - 7384
(2007/10/02)
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- Competing Hydride Transfer and Ene Reactions in the Aminoalkylation of 1-Alkenes with N,N-Dimethylmethyleniminium Ions. A Literature Correction
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A literature report that N,N-dimethylmethyleniminium ion (2) reacts with propylene and styrene to form unsaturated tertiary amines is shown to be incorrect.The major products are the secondary amines 1-(methylamino)butane and 1-(methylamino)-3-phenylpropane in which N-demethylation has occurred along with the saturation of the alkene.Analogous major products are formed with 1-butene, 1-hexene, 1-octene, 1-dodecene, 1-tetradecene, p-methylstyrene, and m-nitrostyrene as substrates.When the substrates are isobutylene, 2-ethyl-1-hexene, α-methylstyrene, and p-methoxystyrene, the major products are tertiary amines, but the secondary amines are also formed in smaller yields.The small yields of tertiary amines obtained in the cases of styrene and p-methylstyrene were increased by going from solvent acetic acid to acetonitrile and by increasing the branching of the alkyl groups on nitrogen.The internal olefins 5-decene and cyclohexene were far less reactive, giving only 3-4percent of amine products that were mainly tertiary in the former case and secondary in the latter.It is concluded that tertiary amine products are favored by an alkene structure and a solvent that favors the formation of a stable carbenium ion intermediate or a transition state with substantial carbenium ion character upon electrophilic attack of the iminium ion on the alkene.The secondary amine products are favored when a carbenium ion is of low stability and when the β-carbon atom of the olefin and/or the alkyl group attached to nitrogen is sterically unhindered; such hindrance decreases the rate of hydride ion transfer that is believed to occur in the production of secondary amines.
- Cohen, Theodore,Onopchenko, Anatoli
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p. 4531 - 4537
(2007/10/02)
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