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HER2 positive tumor targeting compound and composition thereof

A technology of compounds and solvates, applied in the field of compounds for targeted immunotherapy

Inactive Publication Date: 2015-08-26
BIRDIE BIOPHARM INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the strict technical requirements in terms of antibodies, linker molecules, toxin molecules, conjugation, and limited molecules that can bring toxins into the tumor microenvironment, there are still some difficulties in actual clinical research

Method used

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  • HER2 positive tumor targeting compound and composition thereof
  • HER2 positive tumor targeting compound and composition thereof
  • HER2 positive tumor targeting compound and composition thereof

Examples

Experimental program
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preparation example Construction

[0313] Compound preparation

[0314] In general, activated moieties represented by structures of general formula (I) can be prepared using the synthetic steps outlined below. In step (1), 4-chloro-3-nitroquinoline of general formula A and general formula R 1 NH 2 The reaction of amines generates 3-nitroquinolin-4-amines of general formula B. In step 2, 3-nitroquinolin-4-amines of general formula B are reduced to yield quinoline-3-4-diamines of general formula C. In step 3, quinoline-3-4-diamine of general formula C is reacted with carboxylic acid or its equivalent to generate 1H-imidazo[4,5c]quinoline of general formula D.

[0315]

[0316]Alternatively, compounds of general formula (I) can be prepared according to the synthetic methods described in US6,331,539B1, US6,451,810B1, US7,157,452 and US7,301027B2.

[0317] On the other hand, compounds of general formula (Ia) can be prepared by using a linker to connect both the targeting moiety and the activation moiety. T...

Embodiment 1

[0375] Generation of her2-transfected L cell lines

[0376] Reagents: L cells from ATCC (Manassas, VA; Cat No. CRL2648), Her2 / pEZ-Lv105 cDNA purchased from GeneCopoeia, (Cat No. Z2866), glucose DMEM, L-glutamine, Lipofectamine2000 (Invitrogen; Carlsbad, CA ).

[0377] To generate cell lines for screening conjugated trastuzumab, L cells expressing tagged Her2 were generated. The Her2 / pEZ-Lv105 construct was transfected into L cells (the cells were grown in high glucose DMEM + 10% FBS + 2mM L-glutamine) by standard Lipofectamine2000 protocol.

[0378] Binding analysis (FACS analysis)

[0379] To determine the binding capacity of conjugated trastuzumab, FACS analysis was performed on L cells expressing human her2. Briefly, 100 μl of approximately 10 6 L cells with transiently transfected her2 were incubated with varying amounts of trastuzumab-conjugated antibodies, using PBS or secondary antibody alone or irrelevant huIgG as negative controls. After washing, cells were r...

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Abstract

The present invention provides a HER2 positive tumor targeting compound and a composition thereof, and relates to a compound used for the targeting immunotherapy method, and a composition containing the compound. The present invention further relates to applications of the compound in treatment of HER2-positive tumors / cancers.

Description

technical field [0001] The present invention relates to compounds for use in targeted immunotherapy and compositions containing the compounds. The invention also relates to the use of said compounds in the treatment of diseases such as cancer. Background technique [0002] Therapeutic antibodies have been used in clinical applications for more than two decades. At present, there are fifteen kinds of anti-tumor antibody drugs used clinically, these drugs include: Rituxan (1997), Herceptin (1998), Mylotarg (2000), Campath (2001), Zevalin (2002), Bexxer (2003), Avastin ( 2004), Erbitux (2004), Vectibix (2006); Arzerra (2009); Benlysta (2011); Yervoy (2011); Adcetris (2011); Perjeta (2012); and Kadcyla (2013). These antibodies primarily target four molecules: EGFR, Her2, CD20 and VEGF. [0003] In general, therapeutic antibodies kill tumor cells through three mechanisms (Scott AM, Wolchok JD, Old LJ. Antibody therapy of cancer. Nat Rev Cancer. (2012), 12:278-87): (1) Antibody...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K16/28A61K39/395A61P35/00
Inventor 李立新
Owner BIRDIE BIOPHARM INC
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