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-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-10112976-B2 优先权日:2014-06-30 标 题:Process for the production of D-arginyl-2,6-dimethyl-L-tyrosyl-L-lysyl-L-phenylalaninamide 发明人:ZHAO XINJUN; ZHENG MINYU; YU XIAOZHONG; GAO HANRONG; CORNILLE FABRICE 权利人:FLAMMA SPA 摘要:The invention relates to a process for solution-phase synthesis of D-Arginyl-2,6-dimethyl-L-tyrosyl-L-lysyl-L-phenylalaninamide, an active ingredient used for both common and rare diseases including a mitochondrial targeted therapy for ischemia reperfusion injury.
专利号:US-11440881-B2 优先权日:2019-05-09 标题 :Thiosemicarbazates and uses thereof 发明人:AL-ABED YOUSEF; ALTITI AHMAD 权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH 摘要:Thioesters, thiocarbamates, thiocarbazates, semithiocarbazates, peptides, aza-amino acid conjugates, and azapeptides; and a chemoselective and site-specific functionalization protocol of protected thiocarbazates and semithiocarbazates are described. The protocol features the use of Mitsunobu reaction to alkylate specifically the nitrogen atom close to the acylthiol moiety with alcohols to produce protected mono-substituted thiocarbazates that can be stored for months, activated under mild conditions at low temperature using halonium reagents and integrated orthogonally to make substituted semicarbazides that can be used, e.g., as synthons in synthesis of aza-amino acid conjugates, azapeptides and other peptidomimetics. Methods for preparing and using ureases, carbazides, semicarbazides, beta-peptides, azapeptides, and other peptidomimetics and azapeptide conjugates, and uses of ureases, carbazides, semicarbazides, beta-peptides, azapeptides in drug discovery, diagnosis, inhibition, prevention and treatment of diseases are also described.
[参考文献]: Fujita Y, Et Al. Studies On The Structure-Activity Relationship Of 2',6'-Dimethyl-L-Tyrosine (Dmt) Derivatives: Bioactivity Profile Of H-Dmt-Nh-Ch(3). Bioorg Med Chem Lett. 2005 Feb 1;15(3):599-602.
合成参考文献
摘要:Andersson, C.-M.; Andersson, M., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 3, 8. 参考文献:10.1159/000093046 摘要:Ioja E, Tóth G, Benyhe S, Tourwe D, Péter A, Tömböly C, Borsodi A. Opioid receptor binding characteristics and structure-activity studies of novel tetrapeptides in the TIPP (Tyr-Tic-Phe-Phe) series. Neurosignals. 2005;14(6):317–28. doi: 10.1159/000093046. 参考文献:10.1124/jpet.103.060061 摘要:Jinsmaa Y, Okada Y, Tsuda Y, Shiotani K, Sasaki Y, Ambo A, Bryant SD, Lazarus LH. Novel 2′,6′-Dimethyl-l-Tyrosine-Containing Pyrazinone Opioid Mimetic μ-Agonists with Potent Antinociceptive Activity in Mice. The Journal of Pharmacology and Experimental Therapeutics. 2004 Apr;309(1):432–8. doi: 10.1124/jpet.103.060061. 参考文献:10.1248/cpb.47.1506 摘要:Sasaki Y, Suto T, Ambo A, Ouchi H, Yamamoto Y. Biological properties of opioid peptides replacing Tyr at position 1 by 2,6-dimethyl-Tyr. Chem Pharm Bull (Tokyo). 1999 Oct;47(10):1506–9. doi: 10.1248/cpb.47.1506. 参考文献:10.1021/jm060369k 摘要:Lu Y, Lum TK, Leow Augustine YW, Weltrowska G, Nguyen TM, Lemieux C, Chung NN, Schiller PW. Replacement of the N-terminal tyrosine residue in opioid peptides with 3-(2,6-dimethyl-4-carbamoylphenyl)propanoic acid (Dcp) results in novel opioid antagonists. J Med Chem. 2006 Aug 24;49(17):5382–5. doi: 10.1021/jm060369k.