首页> 外国专利> ORGANIC AMINE SALTS, AMINO ACIDS SALTS AND COMBRESTATIN A-4 PHOSPHATE AMINO ACID ESTER SALTS FOR MODULATING TUMOR OR METASTASIS PROLIFERATION AND BENIGN VASCULAR PROLIFERATIVE DISORDER GROWTH

ORGANIC AMINE SALTS, AMINO ACIDS SALTS AND COMBRESTATIN A-4 PHOSPHATE AMINO ACID ESTER SALTS FOR MODULATING TUMOR OR METASTASIS PROLIFERATION AND BENIGN VASCULAR PROLIFERATIVE DISORDER GROWTH

机译:有机胺盐,氨基酸盐和COMBRESTATIN A-4磷酸氨基酯盐,可调节肿瘤或转移的增生和良性血管增生性疾病的生长

摘要

FIELD: organic chemistry, medicine, oncology.;SUBSTANCE: invention relates to organic amine salts, amino acid salts and combrestatin A-4 phosphate amino acid ester salts. Invention describes compound of the general formula (I):; wherein one of substitute -OR1 or -OR represents -O-QH+ and another one represents hydroxyl or -O-QH+; Q represents (A) optionally substituted aliphatic organic amine comprising at least one nitrogen atom that in common with proton forms quaternary ammonium cation QH+; (B) amino acid comprising at least two nitrogen atoms wherein one of nitrogen atoms in common with proton forms quaternary ammonium cation QH+; (C) amino acid comprising one or some nitrogen atoms wherein one of nitrogen atoms in common with proton forms quaternary ammonium cation QH+ and wherein, except for, all carboxyl groups of amino acids are in ester form. Also, invention describes pharmaceutical compositions used in modulation of tumor or metastasis proliferation and growth of benign vascular proliferative disorders, using compound of the formula (I) and a method for synthesis of compound of the formula (I). Invention provides preparing new combrestatin A-4 salts showing useful physicochemical properties that enhance solubility of combrestatin A-4.;EFFECT: valuable medicinal properties of compounds and pharmaceutical compositions.;27 cl, 13 dwg, 5 ex
机译:技术领域本发明涉及有机胺盐,氨基酸盐和梳形抑制素A-4磷酸氨基酸酯盐。本发明描述了通式(I)的化合物: 其中之一是-OR 1 或-OR代表-O-QH + ,另一个代表羟基或-O-QH + ; Q代表(A)任选取代的含有至少一个氮原子的脂肪族有机胺,该氮原子与质子共同形成季铵阳离子QH + ; (B)包含至少两个氮原子的氨基酸,其中一个氮原子与质子共同形成季铵阳离子QH + ; (C)包含一个或几个氮原子的氨基酸,其中与质子共有的氮原子之一形成季铵阳离子QH + ,并且其中,除氨基酸以外,所有羧基均为酯形式。另外,本发明还描述了使用式(I)化合物和用于合成式(I)化合物的方法,用于调节肿瘤或转移性增殖和良性血管增生性疾病的生长的药物组合物。本发明提供了制备新的康普瑞汀A-4盐,其显示出有用的理化性质,其增强了康普瑞汀A-4的溶解性。效果:化合物和药物组合物的有价值的药物性质。27 cl,13 dwg,5 ex

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