- COMPOUND COMPRISING A NUCLEIC ACID AND A HALF-LIFE EXTENSION MOTIF
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Disclosed herein are compounds including a nucleic acid (A), their preparation, and their use.
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Paragraph 0752; 0757; 0765
(2021/06/04)
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- LIPID-MODIFIED NUCLEIC ACID COMPOUNDS AND METHODS
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Disclosed herein, inter alia, are lipid-modified nucleic acid compounds of the following structure, their preparation, and their use: (I).
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Paragraph 0550; 0555; 0563
(2019/12/25)
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- CARBOXYLATED 2'-AMINO-LNA NUCLEOTIDES AND OLIGONUCLEOTIDES COMPRISING THE SAME
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The invention proves an oligonucleotide comprising one or more carboxylated 2'- amino-LNA nucleotide units. The invention also provides a method of transfecting cells with the oligonucleotide, a method of treating a human or animal by therapy using the oligonucleotide, and a pharmaceutical composition comprising the oligonucleotide.
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Page/Page column 36
(2018/03/09)
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- NMR-based molecular ruler for determining the depth of intercalants within the lipid bilayer. Part III: Studies on keto esters and acids
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The development of "molecular rulers" would allow one to quantitatively locate the penetration depth of intercalants within lipid bilayers. To this end, an attempt was made to correlate the 13C NMR chemical shift of polarizable "reporter" carbons (e.g., carbonyls) of intercalants within DMPC liposomal bilayers - with the polarity it experiences, and with its Angstrom distance from the interface. This requires families of molecules with two "reporter carbons" separated by a known distance, residing at various depths/polarities within the bilayer. For this purpose, two homologous series of dicarbonyl compounds, methyl n-oxooctadecanoates and the corresponding n-oxooctadecanoic acids (n = 4-16), were synthesized. To assist in assignment and detection several homologs in each system were prepared 13C-enriched in both carbonyls. Within each family, the number of carbons and functional groups remains the same, with the only difference being the location of the second ketone carbonyl along the fatty acid chain. Surprisingly, the head groups within each family are not anchored near the lipid-water interface, nor are they even all located at the same depth. Nevertheless, using an iterative best fit analysis of the data points enables one to obtain an exponential curve. The latter gives substantial insight into the correlation between polarity (measured in terms of the Reichardt polarity parameter, ET(30)) and penetration depth into the liposomal bilayer. Still missing from this curve are data points in the moderate polarity range.
- Afri, Michal,Alexenberg, Carmit,Aped, Pinchas,Bodner, Efrat,Cohen, Sarit,Ejgenburg, Michal,Eliyahu, Shlomi,Gilinsky-Sharon, Pessia,Harel, Yifat,Naqqash, Miriam E.,Porat, Hani,Ranz, Ayala,Frimer, Aryeh A.
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p. 105 - 118
(2015/02/19)
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- HUMAN INSULIN ANALOGUE AND ACYLATED DERIVATIVE THEREOF
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The present invention provides a human insulin analogue, an acylated derivative thereof and a physiologically acceptable salt. The present invention further provides a preparation method for the insulin analogue and an application of the insulin analogue as a therapeutic agent, and particularly as a diabetes mellitus therapeutic agent.
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Page/Page column
(2014/11/13)
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- A facile synthesis of long chain acyclic alkanols via Kolbe coupling: 1-Docosanol and 1-triacontanol
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A convenient synthesis of long chain acyclic alkanols viz., 1-docosanol and 1-triacontanol has been devised via Kolbe radical coupling of mono-methyl azelate 2, which has been synthesized from azelaic acid 1. The dimer viz. dimethyl thapsate 3, on Ba(OH)2 hydrolysis affords mono-methyl thapsate 4, which upon mixed Kolbe coupling with appropriate alkanoic acid [CH3(CH)2)nCOOH, n = 6 for 1-docosanol and n = 14 for 1-tri-acontanol] gives the cross coupled products methyl docosanoate 7 and methyl triacontanoate 8 along with the radical dimers dimethyl triacontanedioate 4′ and tetradecane 5′/triacontane 6′ as byproducts. Compounds 7 and 8 on LAH reduction in dry THF yield 1-docosanol 9 and 1- triacontanol 10, respectively in high yields. The mixed anodic coupling has been studied by varying parameters viz. degree of neutralization and molar ratio of compounds 4 and C8/C16 alkanoic acid, current density, anode material etc.
- Yadav, Ashok K.,Singh, Arpita
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p. 1724 - 1726
(2007/10/03)
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- 49. Synthesis of tenuilobine, a bis-polyamine alkaloid from Oncinotis tenuiloba, and its transamidation to isotenuilobine
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From the leaves of Oncinotis tenuiloba STAPF, a novel polyamine alkaloid, tenuilobine (9), was isolated. This paper presents the synthesis of 9, as well as the base-catalyzed Zip reaction of 9, leading to the transamidation product isotenuilobine (10). Th
- Doll, Martin K.-H.,Guggisberg, Armin,Hesse, Manfred
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p. 541 - 547
(2007/10/03)
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