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NEW GASOLINE SALTS OF ACE INHIBITORS, METHOD FOR PRODUCING THEM AND THEIR APPLICATION FOR TREATMENT OF CARDIOVASCULAR DISEASES

机译:ACE抑制剂的新汽油盐,其制备方法及其在心血管疾病中的应用

摘要

1. Salts of ACE inhibitors with N, N'-dibenzylethylenediamine (benzathine) of the general formula: where ACE is an ACE inhibitor molecule, and these salts exist in amorphous and crystalline forms. 2. Perindopril benzatin salt in crystalline polymorphic form A with the following X-ray powder diffraction pattern: 3. Perindopril benzatin salt in crystalline polymorphic form B with the following x-ray powder diffraction pattern: 4. Perindopril benzatin salt in amorphous form. 5. Fosinopril benzatin salt in crystalline form with the following X-ray powder diffraction pattern: 6. Enalapril benzatin salt in crystalline form with the following x-ray powder diffraction pattern: 7. Ramipril benzatin salt in crystalline form with the following X-ray powder diffraction pattern: 8. Cilazapril benzatin salt in crystalline form with the following X-ray powder diffraction pattern: 9. A method for producing benzatine salts of ACE inhibitors of the general formula: by the interaction of two moles of ACE inhibitors with one mole of N, N'-dibenzylethylenediamine. 10. The method of producing benzathine salts in crystalline form according to claim 9, characterized in that during crystallization, water or an organic solvent selected from the group consisting of esters, lower alcohols, ketones, nitriles or ethers, preferably ethyl acetate, acetone, is used as a solvent. , ethanol, acetonitrile and methyl tert-butyl ether. 11. The method for producing the benzathine salts of ACE inhibitors in amorphous form according to claim 9, characterized in that a solution of benzathine salt in water is obtained
机译:1. ACE抑制剂与N,N'-二苄基乙二胺(苯甲硫氨酸)的通式的盐:其中ACE是ACE抑制剂分子,并且这些盐以无定形和结晶形式存在。 2.具有以下X射线粉末衍射图的多晶型A的培哚普利苯甲荆盐:3.具有以下X射线粉末衍射图的结晶多晶型B的培哚普利苯甲荆盐:4.无定形的Perindopril苄金盐。 5.具有以下X射线粉末衍射图的结晶形式的福辛普利苯甲汀盐:6.具有以下X射线粉末衍射图的结晶形式的依那普利苯甲汀盐:7.具有以下X射线的结晶形式的雷米普利苯甲汀盐粉末衍射图:8.具有下列X-射线粉末衍射图的结晶形式的西拉普利苄星盐:9.一种通式为ACE的苯甲酸酯盐的制备方法:通过使两摩尔的ACE抑制剂与一摩尔的相互作用N,N′-二苄基乙二胺。 10.根据权利要求9的结晶形式的苄星盐的制备方法,其特征在于在结晶期间,水或选自酯,低级醇,酮,腈或醚的有机溶剂,优选乙酸乙酯,丙酮,用作溶剂。 ,乙醇,乙腈和甲基叔丁基醚。 11.根据权利要求9的无定形形式的ACE抑制剂的苄星盐的制备方法,其特征在于获得苄星盐在水中的溶液。

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