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Calcium complex of phosphorus contg. ethylenediamine derivs.

A complex and phosphorous technology, applied in phosphorous organic compounds, active ingredients of phosphorous compounds, drug combinations, etc.

Inactive Publication Date: 2007-10-10
SCHERING AG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Therefore, the method of preparation of such pharmaceutical preparations is ultimately unacceptable

Method used

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  • Calcium complex of phosphorus contg. ethylenediamine derivs.
  • Calcium complex of phosphorus contg. ethylenediamine derivs.
  • Calcium complex of phosphorus contg. ethylenediamine derivs.

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Experimental program
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preparation example Construction

[0017] Preparation of compounds according to the invention:

[0018] The complexing agent is converted into a calcium complex (Ca-MS-325) by reaction with calcium hydroxide solution, calcium oxide, calcium carbonate, or calcium bicarbonate. The acidic hydrogen atoms present in the acid groups are replaced, if desired, with inorganic and / or organic bases or amino acids.

[0019] In this case, the neutralization reaction is carried out with the aid of inorganic bases such as sodium, potassium, lithium or calcium (such as hydroxides, carbonates or bicarbonates) and / or organic bases such as primary, secondary and tertiary amines (such as ethanolamine , glucosamine, N-methyl- and N,N-dimethylglucosamine) and basic amino acids (such as lysine, arginine or ornithine).

[0020] Because the calcium complex contains four free acid groups, it is recommended to generate a neutral mixed salt containing both inorganic and organic cations as counterions.

[0021] This can be done, for exam...

Embodiment 1

[0036] Calcium(4-), [[(4R)-4-[bis[(carboxy-.kappa.O)methyl]amino-.kappa.N]-6,9-bis[(carboxy.kappa.O)methyl Base]-1-[(4,4-diphenylcyclohexyl)oxy]-1-hydroxy-2-oxa-6,9-diaza-1-phosphaundecane-11-yl acid -.kappa.N6, .kappa.N9, .kappa.011] 1-oxidato(6-)]-, tetrasodium

[0037] Dissolve 10.0 g (12.88 mmol / 95% content (based on weight)) of MS-325 ligand, 0.954 g (12.88 mmol) of calcium hydroxide, and 1.546 g (38.64 mmol) of sodium hydroxide in 2000 ml of deionized water, then stirred at 95°C for 5 hours. Allow to cool before adding another 0.515 g (12.88 mmol) of sodium hydroxide, filter through a 2[mu] filter, and isolate the title product from the filtrate by lyophilization as a colorless, amorphous powder.

[0038] Yield: 12.40g (quantitative), water content: 10.3%

[0039] Elemental analysis (relative to anhydrous material):

[0040] Calculated: C 45.89 / H 4.43 / N 4.87 / Ca 4.64 / Na 10.65 / P 3.59

[0041] Measured: C 46.01 / H 4.52 / N 4.99 / Ca 4.53 / Na 10.77 / P 3.70

Embodiment 2

[0043] Calcium(4-), [[(4R)-4-[bis[(carboxy-.kappa.O)methyl]amino-.kappa.N]-6,9-bis[(carboxy.kappa.O)methyl Base]-1-[(4,4-diphenylcyclohexyl)oxy]-1-hydroxy-2-oxa-6,9-diaza-1-phosphaundecane-11-yl acid -.kappa.N6, .kappa.N9, .kappa.011]1-oxidato(6-)]-, calcium, disodium

[0044] Dissolve 10.0 g (12.88 mmol / 95% content (by weight)) of MS-325 ligand, 2.578 g (25.76 mmol) of calcium carbonate, and 0.515 g (12.88 mmol) of sodium hydroxide in 2000 ml of deionized water , and then stirred at 95 °C for 5 hours. Allow to cool before adding another 0.515 g (12.88 mmol) of sodium hydroxide, filter through a 2[mu] filter, and isolate the title product from the filtrate by lyophilization as a colorless, amorphous powder.

[0045] Yield: 12.25g (quantitative), water content: 9.8%

[0046] Elemental analysis (relative to anhydrous material):

[0047] Calculated: C 46.21 / H 4.47 / N 4.90 / Ca 9.34 / Na 5.36 / P 3.61

[0048] Measured: C 46.32 / H 4.55 / N 5.00 / Ca 9.22 / Na 5.45 / P 3.73

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Abstract

The invention relates to the calcium complex of[[(4R)-4-[bis[(carboxy-.kappa.O)methyl]amino-.kappa.N]-6,9-bis[(carboxy-.kappa.O)methyl]-1-[(4,4-diphenylcyclohexyl)oxy]-1-hydroxy-2-oxa-6,9-diaza-1-phosphaundecan-11-ylic-acid-.kappa.N6,.kappa.N9,.kappa.011]1-oxidato(6-)]-, tetrahydrogen (MS-325) and its salts, pharmaceutical agents that contain these complexes for the production of agents for the reduction of effects that are caused by heavy metals as well as processes for their production.

Description

technical field [0001] The present invention relates to [[(4R)-4-[bis[(carboxy-.kappa.O)methyl]amino-.kappa.N]-6,9-bis[(carboxy.kappa.O)methyl]- 1-[(4,4-diphenylcyclohexyl)oxy]-1-hydroxy-2-oxa-6,9-diaza-1-phosphaundecane-11-yl acid-.kappa .N6, .kappa.N9, .kappa.011] 1-oxidato(6-)]-, hexahydro and salts thereof, pharmaceutical compositions comprising these complexes, medicaments for reducing effects caused by heavy metals The application in and its preparation method. Background technique [0002] In medicine, coordination compounds are especially suitable for the treatment of heavy metal poisoning, pathological iron excess and the preparation of drugs for imaging diagnosis. [0003] EP 71564 describes, for example, the meglumine salt of the gadolinium(III) complex of diethylenetriaminepentaacetic acid (DTPA) as a contrast agent for NMR-tomography. A formulation containing this complex has been approved globally as the first NMR contrast agent under the trade name Magnevis...

Claims

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Application Information

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IPC IPC(8): C07F9/09A61K49/00A61K31/66A61P39/04C07F9/117C07D295/02A61K49/08A61K51/00C07F9/144
CPCC07F9/117A61K49/103C07F9/091A61P39/02A61P39/04C07F9/09
Inventor 约翰内斯·普拉策克乌尔里希·尼德巴尔京特·米歇尔
Owner SCHERING AG
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