cas 204521-63-1, Nε-PalMitoyl-L-glutaMic Acid γ-SucciniMidyl-α-tert-butyl Ester

Articles about 204521-63-1Total 8 be found

AN IMPROVED PROCESS FOR PREPARATION OF LIRAGLUTIDE
The present invention relates to an improved process for the preparation of Liraglutide. The present invention further related an improved process for the preparation of substantially pure material having a purity of greater than or equal to 99.5% by HPLC.
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(2021/07/02)

IMPROVED PROCESSES FOR THE PREPARATION OF PEPTIDE INTERMEDIATES/MODIFIERS
The present application relates to improved processes for the preparation of peptide intermediates/modifier compounds of Formula (I) and their use in the synthesis of peptide derivatives. The present application further provides the compound of Formula I with high chemical purity of >98% and chiral purity of >99% and its use to make pharmaceutical peptide like Liraglutide.
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(2020/10/21)

Novel GLP-1 Analogues
The present disclosure pertains to novel Glucagon like Peptide-1 (GLP-1) (7-37) analogs having an amino acid sequence with Leu or Ile at the C-terminal. The new analogs are potent GLP-1 agonists with reduced adverse effect and improved duration of action. The present disclosure further relates to acylated derivatives of the new analogs which have further improved potency and duration of action and are suitable for oral administration. The analogs of present disclosure may be useful in treatment of diabetes and obesity.
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(2019/10/20)

Preparation method of high-purity liraglutide side chain
The invention discloses a preparation method of a high-purity liraglutide side chain, palmitic acid, N-hydroxysuccinimide and N, N'-diisopropylcarbodiimide are used as starting materials to react to obtain Palmitoyl-OSu, Palmitoyl-Glu-OtBu, Liraglutide side chain crude product Palmitoyl-Glu (OSu)-OtBu in sequence; the reaction solution is filtered, the obtained filtrate is washed with an acidic aqueous solution, and an organic phase is concentrated the until being dry; the organic phase is recrystallized by using an alkane and a fatty alcohol or a mixed solvent of the alkane and the fatty alcohol to obtain the high-purity liraglutide side chain. The method for preparing the high-purity liraglutide side chain is simple to operate, the synthesis period is short, the cost is low, the after-treatment is easy, the product purity can reach 99.41%, and the method can effectively remove HOSU, DIU, tetradecanoic acid impurities, L5-S2 and octadecanoic acid impurities and other unknown impurities, and is beneficial to large-scale production.
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(2019/07/04)

INSULIN DIMER-INCRETIN CONJUGATES
Insulin dimers conjugated to peptides having at least one incretin activity are disclosed.
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(2017/12/15)

INSULIN-INCRETIN CONJUGATES
Insulin-incretin conjugates comprising a peptide having agonist activity at the glucagon-like 1 (GLP-1) receptor, the glucagon (GCG) receptor, and/or the gastric inhibitory protein (GIP) receptor conjugated to an insulin molecule having agonist activity at the insulin receptor and use of the conjugates for treatment of metabolic diseases, for example, Type 2 diabetes, are described.
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(2017/10/11)

Innovative chemical synthesis and conformational hints on the lipopeptide liraglutide
Liraglutide is a new generation lipopeptide drug used for the treatment of type II diabetes. In this work, we describe new approaches for its preparation fully by chemical methods. The key step of these strategies is the synthesis in solution of the Lys/γ-Glu building block, Fmoc-Lys-(Pal-γ-Glu-OtBu)-OH, in which Lys and Glu residues are linked through their side chains and γ-Glu is Nα-palmitoylated. This dipeptide derivative is then inserted into the peptide sequence on solid phase. As liraglutide is obtained with great purity and high yield, our approach can be particularly attractive for an industrial production. We also report here the results of a circular dichroism conformational analysis in a membrane mimetic environment that offers new insights into the mechanism of action of liraglutide. Copyright
Guryanov, Ivan,Bondesan, Alex,Visentini, Dario,Orlandin, Andrea,Biondi, Barbara,Toniolo, Claudio,Formaggio, Fernando,Ricci, Antonio,Zanon, Jacopo,Cabri, Walter
p. 471 - 479
(2016/10/12)

GLP-2 COMPOUNDS, FORMULATIONS, AND USES THEREOF
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.
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(2008/06/13)