恭喜中国医学科学院医药生物技术研究所李卓荣获国家专利权
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龙图腾网恭喜中国医学科学院医药生物技术研究所申请的专利一组环状多肽化合物及其制备方法和应用获国家发明授权专利权,本发明授权专利权由国家知识产权局授予,授权公告号为:CN114874293B 。
龙图腾网通过国家知识产权局官网在2025-05-23发布的发明授权授权公告中获悉:该发明授权的专利申请号/专利号为:202210611460.2,技术领域涉及:C07K7/60;该发明授权一组环状多肽化合物及其制备方法和应用是由李卓荣;杨鹤显;崔阿龙;易红;耿晶设计研发完成,并于2022-05-27向国家知识产权局提交的专利申请。
本一组环状多肽化合物及其制备方法和应用在说明书摘要公布了:本发明公开了一组环状多肽化合物及其制备方法和应用。所述的环状多肽化合物具有如通式Ⅰ所示的结构。所述的环状多肽化合物的制备方法包括以下步骤:1经保护的碱性氨基酸Fmoc‑AA‑OP侧链游离氨基和卤代树脂反应得到Fmoc‑AA‑OP‑树脂;2Fmoc‑AA‑OP‑树脂逐一偶联得到线性多肽‑树脂;3线性多肽‑树脂选择性脱除保护基、固相环合得到环状多肽‑树脂;4环状多肽‑树脂经酸解、乙醚沉淀得环状多肽粗品;5环状多肽粗品经纯化和或转盐,冻干得环状多肽化合物纯品。实验证明,本发明的环状多肽化合物的抗菌活性与抗菌谱均较天然产物八肽菌素有显著改善,本发明的提出为抗菌药物的开发应用提供了新的技术手段。
本发明授权一组环状多肽化合物及其制备方法和应用在权利要求书中公布了:1.环状多肽化合物或其可药用盐,其特征在于,所述的环状多肽化合物选自以下组成的组:HX-1R-3-羟基癸酰基-D-Dab-环2-8[Dab-Dab-D-Leu-Thr-Dab-Dab-Thr] HX-2S-6-甲基辛酰基-D-Dab-环2-8[Dab-Dab-D-Leu-Leu-Dab-Dab-Leu] HX-6S-3-羟基癸酰基-D-Dab-环2-8[Dab-Dab-D-Leu-Leu-Dab-Dab-Leu] HX-8R-3-羟基癸酰基-D-Dab-环2-8[Dab-Dab-D-Leu-Leu-Dab-Dab-Thr] HX-10R-3-羟基癸酰基-D-Dab-环2-8[Dab-Dab-D-Phe-Thr-Dab-Dab-Leu] HX-12R-3-羟基癸酰基-D-Dab-环2-8[Dab-Dab-D-Leu-Thr-Dab-Dab-Leu] HX-13R-3-羟基癸酰基-D-Dab-环2-8[Dab-Dab-D-Phe-Thr-Dab-Dab-Thr] HX-15正壬酰基-D-Dab-环2-8[Dab-Dab-D-Leu-Leu-Dab-Dab-Leu] HX-16丁二酸单1-甲基丁基酯-D-Dab-环2-8[Dab-Dab-D-Leu-Leu-Dab-Dab-Thr] HX-18R-3-羟基癸酰基-Dab-环2-8[Dab-Dab-D-Leu-Leu-Dab-Dab-Leu] HX-19R-3-羟基癸酰基-Dab-D-Dab-环3-9[Dab-Dab-D-Leu-Phe-Dab-Dab-Leu] HX-20R-3-羟基癸酰基-D-Ser-D-Dab-环3-9[Dab-Dab-D-Leu-Phe-Dab-Dab-Leu] HX-24正癸酰基-D-Dab-环2-8[Dab-Dab-D-Leu-Bip-Dab-Dab-Thr] HX-25正癸酰基-D-Dab-环2-8[Dab-Dab-D-Bip-Leu-Dab-Dab-Thr] HX-26正癸酰基-D-Dab-环2-8[Dab-Dab-D-Chg-Leu-Dab-Dab-Thr] HX-27正癸酰基-D-Dab-环2-8[Dab-Dab-D-Leu-octyl-Gly-Dab-Dab-Thr] HX-30苯己酰基-D-Dab-环2-8[Dab-Dab-D-Leu-Leu-Dab-Dab-Thr] HX-317,7-二甲基辛酰基-D-Dab-环2-8[Dab-Dab-D-Leu-Leu-Dab-Dab-Thr] HX-32正癸酰基-D-Dap-环2-8[Dab-Dab-D-Leu-Leu-Dab-Dab-Thr] HX-33正癸酰基-D-Orn-环2-8[Dab-Dab-D-Leu-Leu-Dab-Dab-Thr] HX-38正癸酰基-D-Dab-环2-8[Orn-Dab-D-Leu-Leu-Dab-Dab-Thr] HX-39正癸酰基-D-Dab-环2-8[Dab-Dab-D-Phe4-tBu-Leu-Dab-Dab-Thr] HX-40正癸酰基-D-Dab-环2-8[Dab-Dab-D-Phe4-Cl-Leu-Dab-Dab-Thr] HX-41正辛酰基-D-Dab-环2-8[Dab-Dab-D-Leu-Phe-Dab-Dab-Leu] HX-42正壬酰基-D-Dab-环2-8[Dab-Dab-D-Leu-Phe-Dab-Dab-Leu] HX-45正癸酰基-D-Dab-环2-8[Dab-Dab-D-Phe-Bip-Dab-Dab-Thr] HX-46正癸酰基-D-Dab-环2-8[Dab-Dab-D-Leu-Trp-Dab-Dab-Leu] HX-47正癸酰基-D-Dab-环2-8[Dab-Dab-D-Phe-Bip-Dab-Dab-Leu] HX-48正癸酰基-D-Dab-环2-8[Dab-Dab-D-Phe-Phe-Dab-Dab-Leu] HX-50正癸酰基-D-Dab-环2-8[Dab-Dab-D-Leu-Phe-Dab-Dab-Phe] HX-51正癸酰基-D-Dab-环2-8[Dab-Dab-D-Leu-Phe4-Me-Dab-Dab-Leu] HX-52正癸酰基-D-Dab-环2-8[Dab-Dab-D-Leu-Phe4-OMe-Dab-Dab-Leu] HX-53正癸酰基-D-Dab-环2-8[Dab-Dab-D-Phe3-Cl-Leu-Dab-Dab-Thr] HX-55正癸酰基-D-Dab-环2-8[Dab-Dab-D-Phe2-Cl-Leu-Dab-Dab-Thr] HX-56正癸酰基-D-Dab-环2-8[Dab-Dab-D-Phe3,4-DiCl-Leu-Dab-Dab-Thr] HX-57正癸酰基-D-Dab-环2-8[Dab-Dab-D-Phe4-Me-Leu-Dab-Dab-Thr] HX-60正癸酰基-D-Dab-环2-8[Dab-Dab-D-Leu-Leu-Dab-Dab-Val] HX-61正癸酰基-D-Dab-环2-8[Dab-Dab-D-Leu-Leu-Dab-Dab-Nva] HX-62正癸酰基-D-Dab-环2-8[Dab-Dab-D-Leu-Leu-Dab-Dab-Ile] HX-63正癸酰基-D-Dab-环2-8[Dab-Dab-D-Val-Leu-Dab-Dab-Thr] HX-64正癸酰基-D-Dab-环2-8[Dab-Dab-D-Nva-Leu-Dab-Dab-Thr] HX-65正癸酰基-D-Dab-环2-8[Dab-Dab-D-Ile-Leu-Dab-Dab-Thr] HX-66正癸酰基-D-Dab-环2-8[Dab-Dab-D-Leu-Val-Dab-Dab-Thr] HX-67正癸酰基-D-Dab-环2-8[Dab-Dab-D-Leu-Nva-Dab-Dab-Thr] HX-68正癸酰基-D-Dab-环2-8[Dab-Dab-D-Leu-Ile-Dab-Dab-Thr] HX-69R-3-羟基-6-甲基庚酰基-D-Dab-环2-8[Dab-Dab-D-Leu-Leu-Dab-Dab-Thr] HX-70R-2-羟基癸酰基-D-Dab-环2-8[Dab-Dab-D-Leu-Leu-Dab-Dab-Thr] HX-719-羟基壬酰基-D-Dab-环2-8[Dab-Dab-D-Leu-Leu-Dab-Dab-Thr] HX-723R,6S-3-羟基-6-甲基辛酰基-D-Dab-环2-8[Dab-Dab-D-Leu-Leu-Dab-Dab-Thr] HX-77R-3-羟基癸酰基-D-Arg-环2-8[Dab-Dab-D-Leu-Leu-Dab-Dab-Leu] HX-78R-3-羟基癸酰基-D-3-胍基丙氨酸-环2-8[Dab-Dab-D-Leu-Leu-Dab-Dab-Leu]
如需购买、转让、实施、许可或投资类似专利技术,可联系本专利的申请人或专利权人中国医学科学院医药生物技术研究所,其通讯地址为:100050 北京市东城区天坛西里1号;或者联系龙图腾网官方客服,联系龙图腾网可拨打电话0551-65771310或微信搜索“龙图腾网”。
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