专利号:US-9944609-B2 优先权日:2013-03-15 标 题:Formation of N-protected bis-3,6-(4-aminobutyl)-2, 5-diketopiperazine through a cyclic alpha-N-protected amino ester 发明人:FREEMAN JOHN J; PHANSTIEL OTTO; BAY WILLIAM ELLIOT; KRAFT KELLY SULLIVAN 权利人:MANNKIND CORP 摘要:A method for the synthesis of N-protected 3,6-aminoalkyl-2,5-diketopiperazines is provided. The method includes obtaining a cyclic α-N protected active amino ester and adding it to a mixture of an amine catalyst in an organic solvent.
专利号:WO-2019182527-A1 优先权日:2018-03-21 标 题:Methyl jasmonate derivatives as possible drug candidates for use in treatment of cancer 发明人:GUZEL MUSTAFA; OZDATLI SUKRAN; SAVLUG OZGECAN; SUCU BILGESU ONUR 权利人:T C ISTANBUL MEDIPOL UNIV 摘要:The present invention relates to the active methyl jasmonate analogues which are effective on the cancer disease and / or on the mechanisms that constitute the disease, the methods of synthesis of said analogs / derivatives and their use in the treatment of a variety of diseases, particularly for treatment of cancer and cancer-causing diseases.
专利号:US-7071338-B2 优先权日:2002-11-27 标 题 :Process for the synthesis of bis-aryl diamidoxime compounds 发明人:BOYKIN DAVID W; ANBAZHAGAN MARIAPPAN; TIDWELL RICHARD R 权利人:UNIV GEORGIA STATE RES FOUND 摘要:Bis-aryl diamidoxime compounds, such as 2,5-bis [4-hydroxy and 4-O-alkylamidinophenyl] furans, can be prepared from 2,5-bis tri-alkylstannanes via a one step palladium-catalyzed cross reaction. Bis-aryl diamidoxime compounds, such as 2,5-bis [4-hydroxy and 4-O-alkylamidinophenyl]furans, are useful as therapeutic compounds. The disclosed process is scalable, simpler, more economic and more feasible than other presently known methods of preparing 2,5-bis [4-hydroxy and 4-O-alkylamidinophenyl]furans and other bis-aryl diamidoxime compounds.
专利号:US-6849650-B2 优先权日:1998-02-27 标 题:Heterocyclic 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; PORTER WARREN J; NISSEN JEFFREY S; LATIMER LEE H; AUDIA JAMES E; DROSTE JAMES 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:US-6399628-B1 优先权日:1996-11-22 标 题 :N-(aryl/heteroaryl) amino acid esters, pharmaceutical compositions comprising same, and methods for inhibiting alpha- amyloid peptide release and/or its synthesis by use of such compounds 发明人:AUDIA JAMES E; FOLMER BEVERLY K; JOHN VARGHESE; LATIMER LEE H; NISSEN JEFFREY S; REEL JON K; THORSETT EUGENE D; WHITESITT CELIA A 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:EP-0951466-B1 优先权日:1996-12-23 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:WU JING; TUNG JAY S; THORSETT EUGENE D; PLEISS MICHAEL A; NISSEN JEFFREY S; NEITZ JEFFREY; LATIMER LEE H; JOHN VARGHESE; FREEDMAN STEPHEN; BRITTON THOMAS C; AUDIA JAMES E; REEL JON K; MABRY THOMAS E; DRESSMAN BRUCE A; CWI CYNTHIA L; DROSTE JAMES J; HENRY STEVEN S; MCDANIEL STACEY L; SCOTT WILLIAM L; STUCKY RUSSELL D 权利人:ELAN PHARM INC; LILLY CO ELI 摘要:Disclosed are compounds for Formula (I) wherein the substituents are as defined in the claims 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.
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合成参考文献
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