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Method of conjugating aminothiol containing molecules to vehicles

A technology of carrier and alkyl, applied in the field of carrier derivatives, can solve the problems that prevent the development of biomolecules, obstacles, difficulties, etc.

Inactive Publication Date: 2008-08-06
AMGEN INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Quantification of these individual entities is generally difficult and sometimes impossible, and technical difficulties combined with insufficient existing tools can greatly hinder, or even completely prevent, the development of such biomolecules

Method used

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  • Method of conjugating aminothiol containing molecules to vehicles
  • Method of conjugating aminothiol containing molecules to vehicles
  • Method of conjugating aminothiol containing molecules to vehicles

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0413] General experiment

[0414] NMR: Proton MR for PEG-containing molecules sees PEG singlet (3.7ppm, relative to DSS's D 2 O). 13 C NMR spectrum see PEG singlet (72.0ppm, D relative to DSS 2 O).

[0415] FTMS data were acquired on a Bruker Q-FTMS operating at a 7tesla. The instrument was calibrated externally with PEG300 / 600 solution, using the standard Francel equation. The error between the calculated mass of each calibration ion and the measured value is less than 1.0ppm. For each spectrum, 512k data points were collected with a detection scan width of 1.25 MHz (86 Da mass cutoff). Time-domain data were not processed before quantitative-mode Fourier transformation.

[0416] GC-MS data were recorded with Hewlett-Packard GC-Ms according to the following parameters:

[0417] Column: J and W DB-XLB capillary column, 30m x 0.25mm x 0.50μΜ, PN1221236.

[0418] method 1:

[0419] Injector parameters: Injector temperature = 250°C; 50:1 split ratio; Helium flow rate = 1...

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Abstract

The present invention relates to a new chemical process that provides novel carrier derivatives as excellent 1,2-aminothiol or 1,3-aminothiol specific reagents for use in For conjugation with unprotected targeting compounds (such as polypeptides, peptides or organic compounds) with or modified to have 1,2-aminothiol or 1,3-aminothiol groups. The invention also relates to methods of using the novel water-soluble polymer derivatives and conjugates thereof.

Description

[0001] This application claims priority to U.S. Application No. (not yet assigned), filed January 23, 2006, and claims the benefit of U.S. Provisional Application No. 60 / 646,685, filed January 24, 2005, which is incorporated by reference to this article. Background of the invention [0002] Recent advances in biotechnology have enabled the large-scale production of biomolecules, such as therapeutic proteins, peptides, antibodies and antibody fragments, which can now be produced on a large scale, enabling a wide range of applications of such biomolecules. Unfortunately, rapid proteolytic degradation of biomolecules, short circulatory half-lives, low solubility, instability during production, storage, or administration, or immunogenicity after administration often limit their applications. Because of the growing interest in the therapeutic and / or diagnostic use of administered biomolecules, various approaches to overcome these drawbacks have been investigated. [0003] One of t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61K38/04C07D513/14A61P29/00C07K7/18A61K47/54
Inventor D·C·德阿米科B·C·小阿斯库
Owner AMGEN INC
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