Coordination complex of diaminocyclohexaneplatinum(II) with block copolymer containing poly(carboxylic acid) segment and antitumor agent comprising the same

A technology of diaminocyclohexane and block copolymers, which can be used in antitumor drugs, platinum-based organic compounds, platinum-group organic compounds, etc. It can solve the problems of high cytotoxicity and achieve high anti-tumor efficacy and excellent stability , the effect of safe use

Inactive Publication Date: 2007-01-03
TOUDAITLO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Furthermore, it is described in Non-Patent Document 6 that compared with the CM-Dex complex, the residual cytotoxic activity against experimental tumor cells exists for a longer period of time in a serum-containing medium, and shows a stronger high cytotoxicity

Method used

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  • Coordination complex of diaminocyclohexaneplatinum(II) with block copolymer containing poly(carboxylic acid) segment and antitumor agent comprising the same
  • Coordination complex of diaminocyclohexaneplatinum(II) with block copolymer containing poly(carboxylic acid) segment and antitumor agent comprising the same
  • Coordination complex of diaminocyclohexaneplatinum(II) with block copolymer containing poly(carboxylic acid) segment and antitumor agent comprising the same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0066] Example 1: Generation of polymer micelles

[0067] The structural formula of the block copolymer used in this example is shown below.

[0068]

[0069] (1.a.) Suspend 19 mg of dichloro(1,2-diaminocyclohexane) platinum(II) (dichloro-DACHPt) in 10 ml of distilled water and mix with 12.3 mg of silver nitrate ([AgNO 3 ] / [dichloro-DACHPt] molar ratio = 1.5). The mixture was kept in the dark at 25°C for 24 hours. After the reaction, silver chloride precipitated out. Next, the reaction mixture was centrifuged at 3000 rpm for 5 minutes to remove the precipitated silver chloride. The Diaquo DACHPt-containing supernatant thus obtained was purified through a 0.22 μm filter.

[0070] (1.b.) 24.4 mg of the block copolymer represented by the above structural formula (hereinafter referred to as PEG-P(Glu) 12-35) was added to 10 ml of the purified supernatant obtained in the above (1.a.) ( The molar ratio of "Diaquo-DACHPt" / [Glu] = 1), wherein the above-mentioned block copolyme...

Embodiment 2

[0072] Example 2: Properties of polymer micelles

[0073] (2.a.) Stability in 10mM PBS

[0074] Using the same block copolymer as used above, the stability of the polymer micelles obtained according to Example 1 (hereinafter referred to as DACHPt micelles) was compared with that of the inner capsule produced as described in Example 1 of the above-mentioned WO02 / 26241A1. Stability of polymer micelles of cisplatin (hereinafter referred to as CDDP micelles).

[0075] CDDP micelles were prepared briefly as follows:

[0076] Cisplatin (CDDP) was dissolved in water (5 mmol / l). The same block copolymer as used in Example 1 above was dissolved in this solution ([CDDP] / [Glu of copolymer]=1.0). It was allowed to react at 37°C for 73 hours. The resulting solution was repeatedly subjected to ultrafiltration (MWCO=100,000) to be purified. The formation of polymer micelles was confirmed by measuring dynamic light scattering (DLS).

[0077] First, the micelle concentration is determine...

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Abstract

Provided is a coordination complex of a block copolymer comprising a poly(ethylene glycol) segment and a poly(carboxylic acid) segment with diaminocyclohexaneplatinum(II). The complex can be effectively used in treatments for tumors, in particular malignant tumors.

Description

technical field [0001] The present invention relates to the coordination complex of diaminocyclohexane platinum (II) and polyethylene glycol-polycarboxylic acid block copolymer and the preparation method of the coordination complex and the coordination complex An antitumor agent containing as an active ingredient. Background technique [0002] Cisplatin, which is a platinum compound, and carboplatin, its analogue (equivalent to a compound in which the dichloro group as the leaving group on cisplatin is replaced by 1,1-cyclobutane dicarboxylate) are particularly effective on reproductive organs Cancer is effective and has been used clinically for a long time. On the other hand, a substituted derivative derived from diaminocyclohexane (hereinafter also referred to as DACH) as two amine groups (or amino ligands) as a cisplatin leaving group [dichlorodiaminocyclohexane Alkane platinum (Dichloro DACHplatm)] has good antitumor activity and is a stable complex. However, since th...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08G81/00A61K47/34A61K47/48A61K9/107A61K45/06
CPCA61K45/06C07F15/0093C08G85/002A61K9/1075A61P35/00C08G81/00C08K3/10B82Y30/00Y02P20/55
Inventor 片冈一则西山伸宏H·卡布拉尔冈崎总一郎
Owner TOUDAITLO LTD
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