首页> 外国专利> drug loading cell penetration molecule, methods to facilitate the absorption of a biologically active compound, to improve the bioavailability of a biologically active drug or compound, to introduce a biologically active drug or compound into a site, to treat an individual, and, composition

drug loading cell penetration molecule, methods to facilitate the absorption of a biologically active compound, to improve the bioavailability of a biologically active drug or compound, to introduce a biologically active drug or compound into a site, to treat an individual, and, composition

机译：药物加载细胞渗透分子，促进生物活性化合物吸收，改善生物活性药物或化合物的生物利用度，将生物活性药物或化合物引入部位，治疗个体的方法以及组合物

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摘要

the invention relates to improvements in drug delivery and the use of cell-penetrating agents (cpas) or cell-penetrating peptides (cpps) that have been stabilized, for example: i) stapling two amino acids to form stapled cpps (staps) or ii) sewing three or more amino acids to form stitched cpp (stips). more particularly a drug loading cell penetration molecule (dccpm) is provided which comprises: a biologically active compound (bac), and a cell penetrating agent (cpa), in which bac and cpa are linked directly or through of a bifunctional ligand (bfl). cpa is a stabilized peptide (cpp) that has an imposed conformation when being stapled to form a stapled peptide (stap) or when being sewn to form a stitched peptide (stip). the stip or stap comprises a crosslink or bridge between at least two amino acids of the peptide and the crosslink or bridge provides a cyclization between at least two amino acids that are not formed by an olefin metathesis. cyclization can be achieved by one or more of: condensation of an aldehyde or ketone with a protected hydrazine or hydrazine; a michael addition of thiol-ene; a disulfide formation; a 1.3 dipolar cyloadload of huisgen; a reaction between an amine and carboxylic acid; a singlet or triplet carbine reaction; or a suzuki or sonogashira coupling.

机译：本发明涉及药物递送的改进和已经稳定的细胞穿透剂（cpas）或细胞穿透肽（cpps）的使用，例如：i）装订两个氨基酸以形成钉合的cpps（staps）或ii ）缝制三个或更多的氨基酸以形成缝合的cpp（针尖）。更特别地，提供了载药细胞渗透分子（dccpm），其包含：生物活性化合物（bac）和细胞渗透剂（cpa），其中bac和cpa直接或通过双功能配体（bfl）连接。。 cpa是一种稳定的肽（cpp），当被缝合以形成缝合肽（stap）或被缝合以形成缝合肽（stip）时具有强加的构象。刀头或针头包括在肽的至少两个氨基酸之间的交联或桥，并且该交联或桥提供了不是由烯烃复分解形成的至少两个氨基酸之间的环化。环化可通过以下一种或多种方法实现：醛或酮与受保护的肼或肼的缩合;迈克尔加成的硫醇烯;二硫化物形成; 1.3惠斯根的偶极重载;胺与羧酸之间的反应;单重或三重卡宾枪反应;或铃木或Sonogashira联轴器。

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公开/公告号BR112019027880A2

专利类型
公开/公告日2020-07-07

原文格式PDF
申请/专利权人 SUTURA THERAPEUTICS LTD;
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申请/专利号BR20191127880
发明设计人 ADAM JAMES REGINALD GADD;KEITH FOSTER;
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申请日2018-06-28
分类号A61K48;A61K47/64;A61P21;
国家 BR
入库时间 2022-08-21 11:18:23

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