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Use of (R)-ibuprofen methanesulfonamide and salts thereof in the treatment and prevention of rejection reactions of transplanted organs

A technology for isobutyl phenylpropionate methylsulfonamide and organ transplantation, applied in the application field of (R)- ibuprofen methylsulfonamide and its salt in the treatment and prevention of transplanted organ rejection, capable of Address issues such as increased risk of acute rejection

Inactive Publication Date: 2005-01-05
DOMPE SPA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There is no consensus that the combination of delayed recovery of renal function and early rejection is an indicator of poor graft survival and that the presence of delayed recovery of renal function can lead to an increased risk of acute rejection (CarmelliniM et al., Delayed graft function adversely affects one year graft survival of cadaveric renal transplants. Transplant Pro 28, 1: 359-360, 1996)

Method used

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  • Use of (R)-ibuprofen methanesulfonamide and salts thereof in the treatment and prevention of rejection reactions of transplanted organs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Preparation of (R)-isobutylphenylpropionic acid methylsulfonamide

[0031] The suspension of R(-)-2-(4-isobutylphenyl)-propionic acid (R-isobutylphenylpropionic acid, 4g, 0.019mol) and thionyl chloride (7.4mL) was refluxed for 4 hours; Cool naturally at room temperature. Excess thionyl chloride was evaporated in vacuo.

[0032] The residue was washed twice with a few drops of anhydrous dioxane, and the solvent was evaporated in vacuo to remove the last remaining thionyl chloride. 4.66 g (0.019 mol) of a yellow oil, R(-)-2-(4-isobutylphenyl)-propionyl chloride, were obtained, which was dissolved in a few ml of anhydrous tetrahydrofuran (THF).

[0033] In addition, methylsulfonamide (2.3 g, 0.0243 mol) was added to a suspension of potassium tert-butoxide (2.73 g, 0.0244 mol) and anhydrous tetrahydrofuran (28 mL), and the mixture was stirred at room temperature for 30 minutes. Then, R(-)-2-(4-isobutylphenyl)-propionyl chloride (4.66 g, 0.019 mol) obtained above was adde...

Embodiment 2

[0036] Preparation of L(+)-Lysine Salt (DF 1681B) of (R)-Isobutylphenylpropionic Acid Methylsulfonamide

[0037] A solution of L(+)-lysine (129 mg, 0.88 mmol) in water (1.3 mL) was added to R(-)-N-[2-(4-isobutylphenyl)propionyl]-methylsulfonyl A solution of the amide (250 mg, 0.88 mmol) in 1 mL of methanol. The solvent was evaporated and the residue was dissolved in ether (5 mL) and stirred at room temperature overnight. The separated highly hygroscopic crystalline substance was quickly filtered under a nitrogen atmosphere, washed with anhydrous ether on the filter membrane, and vacuum-dried at 50°C for 2 hours to obtain 360 mg of R(-)-N-[2-(4-iso Butylphenyl)propionyl]-methanesulfonamide L(+)-lysine salt, which is a pale yellow powder. [α] D =-17.3 (c=1.15; methanol); 1 H-NMR (D 2 O): δ7.30(dd, 4H, J=8Hz); 3.77(t, 1H, J=7Hz); 3.65(q, 1H, J=7Hz); 3.05(m, 5H); 2.52(d, 2H , J=7Hz); 1.92(m, 2H); 1.75(m, 2H); 1.50(m, 3H), 1.40(d, 3H, J=7Hz), 0.90(6H, d, J=7Hz).

[0038] ...

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Abstract

The use of (R).-ibuprofen methanesulfonamide is described for the preparation of medicaments for the treatment and prevention of functional injury resulting from rejection reactions of transplanted organs. In particular, the use of non-toxic salts of (R)-ibuprofen methanesulfonamide, such as the (L)-lysine salt, is described for the prevention and the treatment of rejection reactions of transplanted kidneys.

Description

technical field [0001] The invention relates to the application of (R)-ibuprofen methylsulfonamide and its non-toxic salt in the preparation of medicines for treating and preventing functional damage caused by rejection of transplanted organs. Background of the invention [0002] Organ transplantation, especially kidney transplantation, has advanced dramatically over the past few decades due to the introduction of improved immunosuppressive regimens, organ preservation, and preoperative and postoperative care. However, there is still considerable room for improvement, especially in improving long-term outcomes. Initial ischemia / reperfusion injury after organ recovery, preservation, and transplantation is associated with subsequent deterioration and graft failure. In kidney transplantation, the transplanted kidney does not recover function immediately, which is called delayed graft function (DGF), and usually requires dialysis within the first week after transplantation. De...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/18A61K31/18A61K31/216A61P9/00A61P9/10A61P13/12A61P37/06
CPCA61K31/216A61P13/12A61P37/06A61P9/00A61P9/10A61K31/192
Inventor R·贝尔蒂尼F·科洛特塔R·诺韦尔里尼
Owner DOMPE SPA
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