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Anti-cell-acceptor and anti-tumor-growth drug molecule, preparation method thereof and applications thereof

A kind of use and pharmaceutical technology, applied in the direction of anti-receptor/cell surface antigen/cell surface determinant immunoglobulin, drug combination, pharmaceutical formulation, etc., can solve the problem of unsatisfactory toxicity

Active Publication Date: 2013-10-02
BIO THERA SOLUTIONS LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, its toxicity also makes this class of compounds unsatisfactory in human clinical trials because the side effects are intolerable for many patients (Issel et al., Cancer Treat. Rev. 199-207 (1978))

Method used

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  • Anti-cell-acceptor and anti-tumor-growth drug molecule, preparation method thereof and applications thereof
  • Anti-cell-acceptor and anti-tumor-growth drug molecule, preparation method thereof and applications thereof
  • Anti-cell-acceptor and anti-tumor-growth drug molecule, preparation method thereof and applications thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0249] Esterification of maytansinol (MDC) with Fmoc-N-methyl-L-alanine (synthesis of Fmoc-N-Me-D / L-Ala-MDC)

[0250]

[0251] Weigh maytansinol (0.600g, 1.062mmol), Fmoc-N-methyl-L-alanine (6.911g, 21.24mmol), scandium trifluoromethanesulfonate (0.314g, 0.637mmol) and DMAP (0.389 g, 3.186mmol) was placed in a 250ml Schlenck bottle, dichloromethane (100mL) was added under nitrogen protection, and stirred at -8°C for 0.5 hours. Add DIC (2.949g, 23.37mmol) dropwise, continue to stir the reaction at -8°C for 0.5h, slowly warm up to room temperature, and recover the catalyst by filtration. The filtrate is quenched with dilute hydrochloric acid, extracted with dichloromethane, and then saturated Wash with sodium and saturated brine, dry over anhydrous sodium sulfate, and spin to dry the solvent. Column chromatography (silica gel, 300-400 mesh, CH 2 Cl 2 / MeOH 30:1) gave the diastereomeric mixture Fmoc-N-Me-D / L-Ala-MDC as a white solid (0.8385 g, 90.5% yield). Further column ...

Embodiment 2

[0253] Deprotection of Fmoc-N-Me-D / L-Ala-MDC (synthesis of N-Me-D / L-Ala-MDC)

[0254]

[0255] Dissolve Fmoc-N-Me-D / L-Ala-MDC (0.463g, 0.5307mmol) prepared in Example 1 in acetonitrile (200mL), add piperidine (0.865g, 10.15mmol), stir at room temperature for 4 hours, add water Quenching, extraction with dichloromethane, washing with saturated brine, drying over anhydrous sodium sulfate, rotary evaporation to remove the solvent, and drying to obtain a crude product. It was used in the next reaction without further purification. LC-MS (M+H + ) Calculated value: 650.3, measured value: 650.3. Rt: 3.96min.

Embodiment 3

[0257] Deprotection of Fmoc-N-Me-L-Ala-MDC (synthesis of N-Me-L-Ala-MDC)

[0258]

[0259] Fmoc-N-Me-L-Ala-MDC (0.463g, 0.5307mmol) prepared in Example 1 was dissolved in acetonitrile (200mL), piperidine (0.865g, 10.15mmol) was added, stirred at room temperature for 4 hours, and quenched with water , extracted with dichloromethane, washed with saturated brine, dried over anhydrous sodium sulfate, removed the solvent by rotary evaporation, and dried to obtain a crude product. It was used in the next reaction without further purification. LC-MS (M+H + ) calculated value: 650.3, measured value: 650.3. Rt: 3.96min.

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Abstract

The invention relates to the field of biological medicine technology. Traditional anti-tumor antibodies are partly effective for target-positive patients. Chemotherapy drugs with high toxicity can kill tumor cells in a low concentration, but lack targeting. The invention provides a preparation method for an antibody drug conjugate that is anti-CD20-acceptors and inhibits tumor growth, and applications of the antibody drug conjugate in treating B lymphocyte malignant hyperplasia cancer.

Description

technical field [0001] The invention relates to an antibody-drug conjugate that resists CD20 receptors and inhibits the growth of cancer cells, its preparation method and application. Background technique [0002] So far, CD20 has become the most effective antibody therapeutic target for the treatment of B cell malignant cancer cells. Anti-CD20 has three main types of functional activity: target cell CD20 binding leads to growth inhibition and (nonclassical) apoptosis (referring to direct cell death), complement-dependent cytotoxicity (CDC), and antibody-dependent cytotoxicity (ADCC). ), this cytotoxicity is mediated by cells displaying Fc receptors (FcrR), such as NK cells and macrophages expressing FcrRIIIa. [0003] Rituximab, a class I chimeric IgG1 anti-CD20 antibody, has greatly improved the treatment and management of B-cell malignancies, increasing the median survival of patients with these diseases. Combined with chemotherapy, it can effectively improve the respon...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K16/28A61K31/537A61K47/48A61P35/00A61P29/00A61P37/00A61P35/02A61P19/02A61P37/06A61P3/10A61P1/00
CPCA61K47/6849A61P1/00A61P19/02A61P29/00A61P35/00A61P35/02A61P37/00A61P37/06A61P3/10A61K47/68033
Inventor 秦超孟锐奇谭炳华李胜峰
Owner BIO THERA SOLUTIONS LTD
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