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:US-2013243770-A1 优先权日:2005-10-14 标 题:Treating diabetes using inhibitors of il-1 发明人:LAU JESPER 权利人:NOVO NORDISK AS 摘要:The present invention describes a method of treating diabetes or metabolic syndrome with a compound that inhibits (a) IL-1, (b) the synthesis of IL-1, or (c) the release of IL-1.
专利号:US-2012282255-A1 优先权日:2011-04-07 标题 :Methods and compositions for the treatment of alcoholism and alcohol dependence 发明人:PLUCINSKI GREG 权利人:PLUCINSKI GREG 摘要:The present invention provides for compositions and methods for treating or preventing addictive and compulsive diseases and disorders, particular alcohol-related diseases and disorders, disclosed herein. The GLP activators of the present invention are effective against various alcohol and drug dependency diseases. In accordance with the invention, the present compositions and methods can be used to intercede upstream or downstream in the signal transduction cascade involved in GLP action to treat various alcohol and drug dependency diseases. In one embodiment, the synthesis or release of endogenous GLP can be stimulated. In another embodiment, the endogenous synthesis or release of another molecule active in the cascade downstream from GLP, (e.g., a molecule produced in response to GLP binding to a receptor), can be stimulated. Accordingly, the methods and compositions of the invention are useful for preventing, treating, diagnosing, or monitoring the progression various alcohol and drug dependency diseases disclosed herein.
专利号:US-9732137-B2 优先权日:2007-12-28 标 题 :Semi-recombinant preparation of GLP-1 analogues 发明人:LAU JESPER FAERGEMAN; ANDERSEN ASSER SLOTH; BLOCH PAW; LAU JESPER; GARIBAY PATRICK WILLIAM; KRUSE THOMAS; NØRBY INGA SIG NIELSEN; JESSEN CLAUS ULRICH; CHRISTENSEN CASPAR; NORRILD JENS CHRISTIAN 权利人:LAU JESPER FAERGEMAN; ANDERSEN ASSER SLOTH; BLOCH PAW; LAU JESPER; GARIBAY PATRICK WILLIAM; KRUSE THOMAS; NØRBY INGA SIG NIELSEN; JESSEN CLAUS ULRICH; CHRISTENSEN CASPAR; NORRILD JENS CHRISTIAN; NOVO NORDISK AS 摘要:A semi-recombinant method for the production of GLP-1 analogues and derivatives with non-proteogenic amino acids in the N-terminal part combining the use of recombinant expression techniques and chemical peptide synthesis.
专利号:RU-2448978-C2 优先权日:2006-06-23 标 题:Synthesis of insulinotropic peptides
专利号:JP-4537495-B2 优先权日:2006-06-23 标 题 :Synthesis of insulinotropic peptides
参考文献:10.1021/jm201150j 摘要:Liu Q, Li N, Yuan Y, Lu H, Wu X, Zhou C, He M, Su H, Zhang M, Wang J, Wang B, Wang Y, Ma D, Ye Y, Weiss HC, Gesing ER, Liao J, Wang MW. Cyclobutane derivatives as novel nonpeptidic small molecule agonists of glucagon-like peptide-1 receptor. J Med Chem. 2012 Jan 12;55(1):250–67. doi: 10.1021/jm201150j.