专利号:US-12351573-B2 优先权日:2019-05-09 标 题:Compounds for use in synthesis of peptidomimetics 发明人:AL-ABED YOUSEF; CHENG KAI FAN 权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH 摘要:Synthesis of O-benzotriazole and O-imidazole synthons are described. Uses of synthons in synthesis of azapeptides and other peptidomimetics, azapeptides and other peptidomimetics synthesized from the synthons and uses of azapeptides and other peptidomimetics are also described.
专利号:US-2023159450-A1 优先权日:2020-05-08 标 题 :Dimers for use in synthesis of peptidomimetics 发明人:AL-ABED YOUSEF; ALTITI AHMAD 权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH 摘要:Dimers for use in synthesis of peptidomimetics are described. Uses of dimers as synthons in synthesis of azapeptides and other peptidomimetics, azapeptides and other peptidomimetics synthesized from the dimers and uses of azapeptides and other peptidomimetics are also described.
专利号:US-7374926-B2 优先权日:2004-12-23 标题 :Enantioconvergent chemoenzymatic synthesis of (R)-γ-amino-β-hydroxybutyric acid ((R)-GABOB) 发明人:KAMAL AHMED; KHANNA GOLLAPALLI B RAMESH; TADIPARTHI KRISHNAJI; RONDLA RAMU 权利人:COUNCIL SCIENT IND RES 摘要:The present invention particularly relates to a chemoenzymatic process for the stereoselective preparation of both enantiomers of 3-hydroxy-4-trityloxy butanenitrile key intermediates for the preparation of (R)-GABOB by lipase mediated kinetic resolution of its racemates and their effective application in the enantioconvergent synthesis of (R)-GABOB.
专利号:US-2020354404-A1 优先权日:2019-05-09 标 题 :Peptidomimetic agents, synthesis and uses thereof 发明人:AL-ABED YOUSEF 权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH 摘要:Compounds for use in synthesis of peptidomimetic agents; synthesis of peptidomimetic agents; peptidomimetic diagnostic and therapeutic agents; and uses of the compounds and peptidomimetic agents in drug discovery, diagnosis, prevention and treatment of diseases are described.
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-5419966-A 优先权日:1991-06-10 标 题 :Solid support for synthesis of 3'-tailed oligonucleotides 发明人:REED MICHAEL W; MEYER JR RICH B; PETRIE CHARLES R; TABONE JOHN C 权利人:MICROPROBE CORP 摘要:A solid support for oligonucleotide synthesis has the structure where CPG represents a controlled pore glass matrix, the wavy line represents a carbon chain covalently linking the NH group with the controlled pore glass matrix, X is 2,2'-dimethoxytrityl or H, and R is alkyl, aryl, arylalkyl, heteroalkyl, or heteroaryl. The dimethoxytrityl group is removed from the solid support by treatment with acid, and the oligonucleotide is built, step-by-step in a conventional synthesizer after attachment of the 3' end of the first oligonucleotide unit to the hydroxyl function connected to the R group.
摘要:S. H. Yalkowsky and G. Zografi, J. Pharm. Sci. 59, 798 (1970). 参考文献:10.1021/jm00149a012 摘要:Krogsgaard-Larsen P, Nielsen L, Falch E, Curtis DR. GABA agonists. Resolution, absolute stereochemistry, and enantioselectivity of (S)-(+)- and (R)-(-)-dihydromuscimol. J Med Chem. 1985 Nov;28(11):1612–7. doi: 10.1021/jm00149a012. 摘要:Melis GB, Mais V, Paoletti AM, Antinori D, de Ruggiero A, Fioretti P. GABAergic control of anterior pituitary function in humans. Adv Biochem Psychopharmacol. 1986;42():219–42. 参考文献:10.1042/bj1020511 摘要:Turner JM, Willetts AJ. Amino ketone formation and aminopropanol-dehydrogenase activity in rat-liver preparations. Biochem J. 1967 Feb;102(2):511–9.