CAS: 106612-94-6; (5S,11S,14S,17S,20S,23S,26S,29S,32S,35S,38S,41S,44S,50S,53S,56S,59S,62S,65S,68S,71S,74S,77S,80S,86S)-20-((1H-Indol-3-yl)Methyl)-86-((S)-2-((S)-2-Amino-3-(1H-Imidazol-5-yl)Propanamido)Propanamido)-44-(3-Amino-3-Oxopropyl)-11,35-Bis(4-Aminobutyl)-29,77-Dibenzyl-26-((S)-Sec-Butyl)-32,50-Bis(2-Carboxyethyl)-68-(Carboxymethyl)-5-(3-Guanidinopropyl)-56-(4-Hydroxybenzyl)-74,80-Bis((R)-1-Hydroxyethyl)-59,62,71-Tris(Hydroxymethyl)-17,53-Diisobutyl-14,65-Diisopropyl-23,38,41-Trimethyl-4,7,10,13,16,19,22,25,28,31,34,37,40,43,46,49,52,55,58,61,64,67,70,73,76,79,82,85-Octacosaoxo-3,6,9,12,15,18,21,24,27,30,33,36,39,42,45,48,51,54,57,60,63,66,69,72,75,78,81,84-Octacosaazanonaoctacontanedioic Acid

专利信息

专利号:US-2019177392-A1
优先权日:2014-09-23
标 题 :Synthesis of glp-1 peptides
发明人：PENIAS NAVON SHARON; NAVEH SHIRLY; VASILEIOU ZOI; BARLOS KONSTANTINOS
权利人:NOVETIDE LTD
摘要:Disclosed are processes for the synthesis of GLP-1 peptides, such as liraglutide and semaglutide, and a process for purifying liraglutide.

专利号:US-10005720-B2
优先权日:2013-04-05
标题:Compounds useful for the treatment of metabolic disorders and synthesis of the same
发明人：SEXTON JONATHAN Z; BRENMAN JAY E; MUSSO DAVID L
权利人:NORTH CAROLINA CENTRAL UNIV; UNIV NORTH CAROLINA CHAPEL HILL
摘要:The present invention provides compounds of Formula (I): wherein variables X, Y, Z and R1 are as described herein. Some of the compounds described herein are glutamate dehydrogenase activators. The invention is also directed to pharmaceutical compositions comprising these compounds, uses of these compounds and compositions in the treatment of metabolic disorders as well as synthesis of the compounds.

专利号:US-11518794-B2
优先权日:2016-08-19
标 题:Synthesis method for liraglutide with low racemate impurity
发明人：FU YUQING; MA HONGJI; LI XINYU; ZHANG LIXIANG; ZHI QIN; WU LIFEN; LIU ZICHENG
权利人:SHENZHEN JYMED TECH CO LTD
摘要:A synthesis method for low-racemization impurity liraglutide comprises the following steps: performing synthesis to obtain a propeptide, coupling 2 to 5 peptides comprising Thr-Phe on the propeptide by using a solid-phase synthesis method; further, performing solid-phase synthesis to obtain a liraglutide resin; the liraglutide resin is cracked after modification, or the liraglutide resin is directly cracked, purified and frozen dry, so as to obtain the liraglutide. The provided liraglutide synthesis method effectively restrains or reduces the generation of racemization impurity D-Thr 5 highly similar to a product property, which facilitates the purification of the coarse liraglutide, and the high yield of the liraglutide is ensured, thereby greatly reducing production costs; during the synthesis of the liraglutide, the syntheses between dipeptide fragments, tripeptide fragments, the tetrapeptide fragments and pentapeptide fragments and the Gly-resin or the syntheses between the combination of the dipeptide fragments, the tripeptide fragments, the tetrapeptide fragments and pentapeptide fragments and the Gly resin can be carried out at the same time, and accordingly the synthesis time is shortened to some extent.

专利号:US-8227571-B2
优先权日:2007-12-11
标题 :Insulinotropic peptide synthesis using solid and solution phase combination techniques
发明人：CHEN LIN; HAN YEUN-KWEI; ROBERTS CHRISTOPHER R
权利人:CHEN LIN; HAN YEUN-KWEI; ROBERTS CHRISTOPHER R; ROCHE PALO ALTO LLC
摘要:The present invention relates to the preparation of insulinotropic peptides that are synthesized using a solid and solution phase (“hybridâ€?) approach. Generally, the approach includes synthesizing three different peptide intermediate fragments using solid phase chemistry. Solution phase chemistry is then used to add additional amino acid material to the third fragment which is then coupled to the second fragment and then the first fragment in solution. Alternatively, a different second fragment is coupled to the first fragment in the solid phase. Then, solution phase chemistry is then used to add additional amino acid material to a different third fragment. Subsequently, this different third fragment is coupled to the coupled first and different second fragment in the solution phase. The use of a pseudoproline in one of the fragments eases solid phase synthesis of that fragment and also eases subsequent solution phase coupling of this fragment to the other fragments. The present invention is very useful for forming insulinotropic peptides such as GLP-1(7-36) and its natural and non-natural counteparts.

专利号:WO-2025128985-A1
优先权日:2023-12-14
标题 :Sulfoxide and sulfone derivatives of thiocarbazates as synthons for azapeptides synthesis and process of using same
发明人：AL-ABED YOUSEF
权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH
摘要:Provided for herein are sulfoxide and sulfone derivatives of thiocarbazates that have the formula (I): wherein A, R, R 1 , R 2 , and n are defined herein. The compounds may be used as synthons in the synthesis of azaeptides and other aza- amino acid conjugates.

专利号:US-10344069-B2
优先权日:2014-10-31
标 题:Process for the preparation of liraglutide
发明人：VADLAMANI SURESH KUMAR; DAGADU PATIL NILESH; SHAFEE MOHAMMED ABDUL; PATIL SANJAY DEVIDAS; AGASALADINNI NAGANA GOUD
权利人:AURO PEPTIDES LTD; VADLAMANI SURESH KUMAR; DAGADU PATIL NILESH; SHAFEE MOHAMMED ABDUL; PATIL SANJAY DEVIDAS; AGASALADINNI NAGANA GOUD
摘要:The present invention relates to a process for the preparation of Liraglutide, which comprises: a) synthesis of suitable fragments (protected) by solid phase peptide synthesis; b) coupling of the suitable fragments on solid support; c) concurrently cleaving the protected peptide from the solid support and de-protecting the peptide; d) purification of Liraglutide (crude) on reverse phase HPLC; e) isolating pure Liraglutide.