专利号:US-2023391818-A1 优先权日:2020-11-05 标 题:Peptide synthesis method for suppressing defect caused by diketopiperazine formation 发明人:NOMURA KENICHI; KAGE MIRAI; TAMIYA MINORU; KANAZAWA JUNICHIRO 权利人:CHUGAI PHARMACEUTICAL CO LTD 摘要:Solid-phase synthesis of a peptide has a problem that a desired elongation reaction is prevented from proceeding by diketopiperazine and a 6-membered diamine skeleton compound formed when a protective group at the N-terminal is removed. The present inventors have found that when in production of a peptide by a solid-phase method, a peptide in which an amino group at the N-terminal is protected with a protective group having an Fmoc skeleton is treated in a specific solvent with a base having a pKa of 23 or more in acetonitrile as a conjugate acid, and a peptide chain is then elongated, it is possible to solve the problem described above.
专利号:WO-2023105497-A1 优先权日:2021-12-10 标题:Synthesis of glp-1 analogues 发明人:GODHA ATUL KASTURCHAND; NARAYANASWAMY SATHYA VANGANUR; BHAGYARAJ ARETI VENKATA; BAVADEKAR ASLAM JAHANGIR; LAKSHMANAPPA RUDRESH; NAGOOR SHEIKSYEDALI; MURUGAN RANJITHKUMAR; GADAKH AMOL VASANTRAO; SAMBASIVAM GANESH 权利人:ANTHEM BIOSCIENCES PVT LTD 摘要:The present invention provides a method of preparation of GLP-1 peptides by using different peptide fragments having amino acid sequences SEQ ID NO:1 (Fragment IG), SEQ ID NO:2 (Fragment SG), Fragment BG, SEQ ID NO:3, and SEQ ID NO:4 5 and combinations thereof. The method of preparation is environmentally benign, simple, straightforward, and efficient and provides the end product in high yield and purity. The purification method of the peptides is also described.
专利号:US-2005192265-A1 优先权日:2003-03-20 标 题:Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting beta-amyloid peptide release and/or its synthesis by use of such compounds 发明人:THOMPSON RICHARD C; WILKIE STEPHEN; STACK DOUGLAS R; VANMETER ELDON E; SHI QING; BRITTON THOMAS C; AUDIA JAMES E; REEL JON K; MABRY THOMAS E; DRESSMAN BRUCE A; CWI CYNTHIA L; HENRY STEVEN S; MCDANIEL STACEY L; STUCKY RUSSELL D; PORTER WARREN J 摘要:Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions that include a compound which inhibits β-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
专利号:US-6906056-B2 优先权日:1998-06-22 标 题:Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds 发明人:THOMPSON RICHARD C; WILKIE STEPHEN; STACK DOUGLAS R; VANMETER ELDON E; SHI QING; BRITTON THOMAS C; AUDIA JAMES E; REEL JON K; MABRY THOMAS E; DRESSMAN BRUCE A; CWI CYNTHIA L; HENRY STEVEN S; MCDANIEL STACEY L; STUCKY RUSSELL D; PORTER WARREN J 权利人:LILLY CO ELI 摘要:Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions that include a compound which inhibits β-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
专利号:US-7390801-B2 优先权日:1996-12-23 标题:Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds 发明人:THORSETT EUGENE D; PLEISS MICHAEL A; LATIMER LEE H; JOHN VARGHESE; FREEDMAN STEPHEN; BRITTON THOMAS C; AUDIA JAMES A; REEL JON K; DRESSMAN BRUCE A; DROSTE JAMES J; HENRY STEVEN S; STUCKY RUSSELL D; PORTER WARREN J 权利人:ATHENA NEUROSCIENCES INC; LILLY CO ELI 摘要:Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits β-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
专利号:WO-0050448-A1 优先权日:1999-02-26 标 题 :A method for controlling an enzymatic reaction by the alpha and beta domains of metallothionein 发明人:VALLEE BERT L; MARET WOLFGANG; FISCHER EDMOND H 权利人:VALLEE BERT L; MARET WOLFGANG; FISCHER EDMOND H 摘要:The present invention relates to the alpha and beta domains of metallothionein and analogs thereof, their synthesis, and methods for controlling in vitro and industrial enzymatic reactions using them. Purified metal-free and metal-containing alpha and beta domains of metallothionein and analogs thereof are provided as described below. A high yield method of synthesis and purification is also provided for the metal-free and metal containing alpha and beta domains of metallothionein and analogs thereof. Finally, methods for controlling in vitro and industrial enzymatic reactions are provided wherein the enzymatic processes are controlled by transfer or removal of a metal cation, to or from an enzyme metal-inhibitory site using the alpha and beta domains of metallothionein and analogs thereof.