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Targeted protease degradation platform (TED)

A target and ligase technology, applied in the field of targeted protease degradation platform, can solve the problems of insufficient therapeutic window, shedding of super toxins, toxic and side effects, etc.

Pending Publication Date: 2021-10-19
EUBULUS BIOTHERAPEUTICS INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The bottleneck encountered in the development of ADC drugs is that the therapeutic window is not wide enough. In addition to the toxic and side effects caused by the antibody itself, the supertoxin will fall off before reaching the target due to the heterogeneity of the coupling, causing serious toxic and side effects

Method used

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  • Targeted protease degradation platform (TED)
  • Targeted protease degradation platform (TED)
  • Targeted protease degradation platform (TED)

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 11P1

[0425] Example 1.1 Synthesis report of P1-connector b-A1:

Embodiment 111

[0426] Example 1.1.1 Synthesis of compound UBI-1289 (NH 2 -11b-A1)

[0427]

[0428] Step 1: Synthesis of UBI-1289b (V1179-123): UBI-1289a (7.2g, 36.3mmol) was added with 4M HCl / dioxane (25mL) in ice bath to react overnight. Diethyl ether (25 mL) was added to make a slurry, filter and dry to obtain a white solid UBI-1289b (4.4 g, yield 89%).

[0429] Step 2: Synthesis of UBI-1289d (V1179-126): UBI-1289b (4.2g, 31.2mmol) was dissolved in acetonitrile (150mL) and K 2 CO 3 (13g, 93.6mmol) and UBI-1289c (8.8g, 31.2mmol) were heated to 80°C overnight. The reaction solution was filtered and concentrated through a column (dichloromethane / methanol=0%-10%) to obtain the yellow oily product UBI-1289d (5g, yield 56%). LCMS[M+H] + =286.2.

[0430]Step 3: Synthesis of UBI-1289e (V1179-127): UBI-1289d (5 g, 17.5 mmol) was added with 4M HCl / dioxane (10 mL) under ice-cooling for 1 hour at room temperature. The reaction was concentrated to give the product UBI-1289e (7.8 g) as a whit...

Embodiment 12P

[0436] Example 1.2 Synthesis of P1-connector c-A1

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Abstract

The invention relates to a targeted protease degradation platform (TED), and particularly discloses a conjugate of a target molecule-linker-E3 ligase ligand as shown in a formula I, RT-L1-RE3 (formula I), in which RT is a monovalent group of a target molecule; RE3 is a monovalent group of an E3 ligase ligand; L1 is a connector for connecting A and B; and L1 is as shown in the following formula II:-W1-L2-W2-(II).

Description

technical field [0001] The invention belongs to biomedicine, and in particular relates to a targeted protease degradation platform (TED). Background technique [0002] Modern molecular biology regulates the expression level of proteins from three basic levels: firstly, at the DNA level, through gene knockout, thereby inactivating the DNA of the target protein; secondly, at the mRNA level, through small RNA, interacting with the target protein Third, at the protein level, the amount and activity of the target protein can be adjusted by modifying the post-translational target protein, such as methylation, phosphorylation, glycosylation, etc. [0003] In terms of the overall development of drug research and development, both small molecule and large molecule drug forms have their own advantages and disadvantages. For example, the development of small molecule drugs has been facing key challenges such as how to maintain drug concentration in the body and drug resistance. The s...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/68A61P35/00C07D475/00C07D417/14C07D401/14C07D401/04A61K31/454A61K31/496A61K31/519
CPCA61K47/68A61P35/00C07D475/00C07D417/14C07D401/14C07D401/04A61K31/454A61K31/496A61K31/519A61K47/6803C07D487/04Y02P20/55C07D519/00C07D417/06C07D403/04C07D487/14C07D495/14C07D409/14A61K47/64A61K47/55A61K47/551A61K47/545A61K47/595
Inventor 曹小冬王晓磊黄超然
Owner EUBULUS BIOTHERAPEUTICS INC