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Anticancer agent

A technology of anticancer agents and compounds, which can be used in antitumor drugs, peptide/protein components, drug combinations, etc., and can solve problems such as inability to exert anticancer effects.

Pending Publication Date: 2020-10-30
OSAKA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Therefore, when Ubenimex is applied to solid cancers such as hepatocellular carcinoma, if it is not used at a concentration hundreds of times higher than the blood concentration obtained in the clinical treatment of acute leukemia, it will not be able to exert an effective anticancer effect. Effect

Method used

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Examples

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Embodiment

[0109] Hereinafter, although this invention is demonstrated in detail based on an Example, this invention is not limited to these Examples.

Synthetic example 1

[0110] Synthesis Example 1. Synthesis of PEG-b-Plys(Ube)20

[0111] A compound comprising a chain structure was synthesized in the following manner by making 20% ​​of lysine residues of a block copolymer of polyethylene glycol and polylysine (PEG-b-Plys) The amino group on the side chain is connected with the carboxyl group of Ubenimex through an amide bond. Specifically, the synthetic figure 2 A and figure 2 A compound of n=8 in the structural formula shown in B.

Synthetic example 1-1

[0112] Synthesis Example 1-1. Synthesis of PEG-b-Plys

[0113] 1.1 g of polyethylene glycol (PEG) having a methoxy group at one end and an amino group at the other end (average molecular weight: 10000) was taken and dissolved in 10 mL of dimethyl sulfoxide. Dissolve 1.3 g of N-(4-(2,5-dioxo-4-oxazolidinyl)butyl)-2,2,2-trifluoroacetamide (Lys(TFA)-NCA) in 10 mL of dimethyl sulfoxide. The resulting two solutions were combined under an atmosphere of argon and stirred overnight at room temperature. Next, the reaction solution was poured into excess diethyl ether so that the product was precipitated again and recovered, and dried under reduced pressure. The obtained white powder was dissolved in 100 mL of a mixed solution of methanol / 1M aqueous NaOH (9 / 1 [v / v]), and stirred overnight at 35°C. The pH of the reaction solution was neutralized to 1-2 with hydrochloric acid. Dialysis was further performed, and a white powder (1.1 g, yield 61%) was obtained by freeze-drying.

[01...

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Abstract

The problem addressed by the present invention is to provide a technique for improving the anticancer effect of ubenimex, especially the anticancer effect on solid cancers. The problem is solved by acompound containing a chain-form structure obtained by linking a plurality of ubenimex to a chain-form polymer.

Description

technical field [0001] The present invention relates to anticancer agents and the like. Background technique [0002] Ubenimex is known to activate immunity by binding to CD13 / APN present on the cell membrane of macrophages, and is a drug used for remission maintenance therapy of acute leukemia in adults. In addition, in recent years, it has also been reported that ubenimex also inhibits the activity of CD13 / APN in several solid cancers. [0003] However, if ubenimex is not administered at a very high concentration compared to the case of acute leukemia, it cannot exert an effective anticancer effect on solid cancer. IC of Ubenimex on Hepatocellular Carcinoma Cell Lines (HuH7, PLC) 30 , 394.8 μg / ml for HuH7 and 498.8 μg / ml for PLC (Non-Patent Document 1). On the other hand, the dosage for the above-mentioned acute leukemia is 30 mg orally administered once a day, and the maximum blood drug concentration obtained by this is 2.21 μg / ml. Therefore, when Ubenimex is applied ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K19/00A61K38/05A61K45/06A61K47/60A61K47/64A61P35/00
CPCA61K47/42A61K47/60A61P35/00C07K14/001A61K45/06A61K31/513A61K31/704A61K33/243A61K47/645C12N9/99A61K38/00A61K9/0019C07K5/0202A61K2300/00A61K47/64
Inventor 森正树石井秀始今野雅允江口英利原口直绍俊山礼志西山伸宏武元宏泰
Owner OSAKA UNIV
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