683239-16-9Relevant academic research and scientific papers
Preparation method of long-chain aliphatic dicarboxylic acid mono-tert-butyl ester
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, (2021/07/09)
The invention provides a method for obtaining the long-chain aliphatic dicarboxylic acid mono-tert-butyl ester through monohydrolysis of the long-chain aliphatic dicarboxylic acid di-tert-butyl ester by controlling the reaction conditions of monohydrolysis; and the raw material cost is low, the yield is high, the post-treatment method is simple, and the method is suitable for industrial production.
Engineering of Orally Available, Ultralong-Acting Insulin Analogues: Discovery of OI338 and OI320
Kjeldsen, Thomas B.,Hubálek, Franti?ek,Tagmose, Tina M.,Pridal, Lone,Refsgaard, Hanne H. F.,Porsgaard, Trine,Gram-Nielsen, Sanne,Hovgaard, Lars,Valore, Henrik,Münzel, Martin,Hj?rringgaard, Claudia U.,Jeppesen, Claus Bekker,Manfè, Valentina,Hoeg-Jensen, Thomas,Ludvigsen, Svend,Nielsen, Peter Kresten,Lautrup-Larsen, Inger,Stidsen, Carsten E.,Wulff, Erik M.,Garibay, Patrick W.,Kodra, János T.,Nishimura, Erica,Madsen, Peter
, p. 616 - 628 (2021/01/13)
Recently, the first basal oral insulin (OI338) was shown to provide similar treatment outcomes to insulin glargine in a phase 2a clinical trial. Here, we report the engineering of a novel class of basal oral insulin analogues of which OI338, 10, in this publication, was successfully tested in the phase 2a clinical trial. We found that the introduction of two insulin substitutions, A14E and B25H, was needed to provide increased stability toward proteolysis. Ultralong pharmacokinetic profiles were obtained by attaching an albumin-binding side chain derived from octadecanedioic (C18) or icosanedioic acid (C20) to the lysine in position B29. Crucial for obtaining the ultralong PK profile was also a significant reduction of insulin receptor affinity. Oral bioavailability in dogs indicated that C18-based analogues were superior to C20-based analogues. These studies led to the identification of the two clinical candidates OI338 and OI320 (10 and 24, respectively).
A process for preparing a fatty acid derivative method and its application (by machine translation)
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Paragraph 0155-0158, (2018/04/01)
The invention discloses a method for preparing a fatty acid derivative method and its application. The first method is the long-chain fatty acid and thionyl chloride reaction, to obtain the acyl chloride; acyl chloride of preparing butanol reaction, then remove chlorine group, and get long-chain fatty acid uncle ding zhi; then and N - hydroxysuccinimide reaction, long-chain fatty acid succinimide and high yield butylacrylate; then with the L - glutamic acid - 1 - tert-butyl reaction, to obtain tert-butyl long-chain fatty acyl - L - Glu - OtBu; with the N - hydroxysuccinimide reaction, to obtain tert-butyl long-chain fatty acyl - L - Glu (OSu)- OtBu; finally [...] butyl long-chain fatty acyl - L - Glu (OSu)- OtBu tert-butyl in removing, and get long-chain fatty acid derivatives. The method routes the operation is simple, quality is controllable, is suitable for industrial production, and low cost, simple purification at the same time, suitable for use in the preparation of high purity insulin analogs. (by machine translation)
GLP-2 COMPOUNDS, FORMULATIONS, AND USES THEREOF
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Page/Page column 107, (2008/06/13)
The present invention relates to novel compositions comprising human glucagon-like peptide-2 (GLP-2) peptides, pharmaceutical compositions, and uses of these and other GLP-2 compounds, compositions and formulations, including methods of treating gastrointestinal disorders and increasing nutrient absorption therewith.
GLP-2 compounds, formulations, and uses thereof
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, (2008/06/13)
The present invention relates to novel human glucagon-like peptide-2 (GLP-2) peptides and human glucagon-like peptide-2 derivatives which have a protracted profile of action as well as polynucleotide constructs encoding such peptides, vectors and host cells comprising and expressing the polynucleotide, pharmaceutical compositions, uses and methods of treatment.
