首页> 外国专利> USING DERIVATIVES OF (-)-(3-TRIHALOMETHYLPHENOXY)-(4-HALOPHENYL)-ACETIC ACID IN TREATMENT OF RESISTANCE TO INSULIN, DIABETES MELLITUS TYPE II, HYPERLIPIDEMIA AND HYPERURICEMIA

USING DERIVATIVES OF (-)-(3-TRIHALOMETHYLPHENOXY)-(4-HALOPHENYL)-ACETIC ACID IN TREATMENT OF RESISTANCE TO INSULIN, DIABETES MELLITUS TYPE II, HYPERLIPIDEMIA AND HYPERURICEMIA

机译:在治疗胰岛素,II型糖尿病,高脂血症和高尿酸血症中使用(-)-(3-三羟甲基苯氧基)-(4-卤代苯基)-乙酸衍生物

摘要

FIELD: organic chemistry, medicine, endocrinology.;SUBSTANCE: invention relates to improved methods for modulation of diabetes mellitus type II in mammal and modulation of resistance to insulin. Methods involve administration to indicated mammal needing in this treatment of (-)-stereoisomer of compound of the formula (I): wherein R is chosen from group including hydroxy-, lower araloxy-, d-(lower)-alkylamino-(lower)-alkoxy-, (lower)-alkylamido-(lower)-alkoxy-, benzamido-(lower)-alkoxy-, ureido-(lower)-alkoxy-, N'-(lower)-alkyl-ureido-(lower)-alkoxy-, carbamoyl-(lower)-alkoxy-, halophenoxy-substituted lower alkoxy-, carbamoyl-substituted phenoxy-group; or R represents hydrolysable ester group; each X represents independently halogen atom; or its pharmaceutically acceptable salt wherein (-)-stereoisomer doesn't comprise conceptually (+)-stereoisomer. Also, invention relates to pharmaceutical compositions comprising (-)-stereoisomer of compound of the formula (I) and wherein compositions show significantly reduced inhibitory effect on activity of cytochrome P-450 2C9 as compared with racemic composition having 0% enantiomeric excess of (-)-stereoisomer.;EFFECT: valuable medicinal properties of compound and pharmaceutical composition, improved preparing methods.;59 cl, 21 dwg, 8 tbl, 18 ex
机译:技术领域本发明涉及在哺乳动物中调节II型糖尿病和调节对胰岛素抵抗的改进方法。方法涉及向需要治疗的式(I)化合物的(-)-立体异构体的指定哺乳动物给药:<图像文件=“ 00000002.GIF” he =“ 38” imgContent =“ undefined” imgFormat =“ GIF” wi =“ 72” />其中R选自羟基,低级芳氧基,d-(低级)-烷基氨基-(低级)-烷氧基-,(低级)-烷基酰胺基-(低级)-烷氧基-,苯甲酰氨基- (低级)-烷氧基-,脲基-(低级)-烷氧基-,N'-(低级)-烷基脲基-(低级)-烷氧基-,氨基甲酰基-(低级)-烷氧基-,卤代苯氧基取代的低级烷氧基-,氨基甲酰基取代的苯氧基;或R代表可水解的酯基;每个X独立地代表卤素原子;或其药学上可接受的盐,其中(-)-立体异构体在概念上不包含(+)-立体异构体。另外,本发明涉及包含式(I)化合物的(-)-立体异构体的药物组合物,其中与0%对映体过量的(-)的外消旋组合物相比,组合物对细胞色素P-450 2C9的活性显示出显着降低的抑制作用。 )-立体异构体;作用:化合物和药物组合物的宝贵药用特性,改进的制备方法; 59 cl,21 dwg,8 tbl,18 ex

著录项

  • 公开/公告号RU2281762C2

    专利类型

  • 公开/公告日2006-08-20

    原文格式PDF

  • 申请/专利权人 METABOLEKS INK.;DIATEKS INK.;

    申请/专利号RU20020100037

  • 发明设计人 LASKI KENNET L. (US);LUO DZHAJN (US);

    申请日2000-06-02

  • 分类号A61K31/192;A61K31/216;A61K31/185;A61K31/165;A61K45/06;A61P3/06;A61P3/10;A61P5/50;A61P9/10;A61P19/06;

  • 国家 RU

  • 入库时间 2022-08-21 21:21:34

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