首页> 外国专利> Composition, useful to treat e.g. atrial fibrillation, atrial flutter and atrial arrhythmia, comprises at least one beta-blocker and at least one compound of a phenylcarboxylic acid amide derivative

Composition, useful to treat e.g. atrial fibrillation, atrial flutter and atrial arrhythmia, comprises at least one beta-blocker and at least one compound of a phenylcarboxylic acid amide derivative

机译:组合物,可用于治疗例如房颤,房扑和房性心律失常,包括至少一种β-受体阻滞剂和至少一种苯基羧酸酰胺衍生物的化合物

摘要

Composition (I) comprises at least one beta-blocker (A) and at least one compound of a phenylcarboxylic acid amide derivative (Ia or Ib) and their salts. Composition (I) comprises at least one beta-blocker and at least one compound of a phenylcarboxylic acid amide derivative of formula (Ia or Ib) and their salts. [Image] R1 : 3-5C alkyl or quinolinyl; R2 : 1-4C alkyl or cyclopropyl; R3 : phenyl or pyridyl (both optionally substituted by 1-2 of F, Cl, CF 3, OCF 3, 1-3C alkyl or 1-3C alkoxy); A : -C nH 2 n; n : 0-2; R4-R7 : H, F, Cl, CF 3, OCF 3, CN, 1-3C alkyl or 1-3C alkoxy; B : -C mH 2 m-; m : 1 or 2; R8 : 2-3C alkyl, phenyl or pyridyl (where the phenyl and pyridyl are optionally substituted by 1-2 of F, Cl, CF 3, OCF 3, 1-3C alkyl or 1-3C alkoxy); R9 : C(O)OR10 or COR10; R10 : -(C xH 2) x-R11; x : 0-2; and R11 : phenyl optionally substituted by 1-2 of F, Cl, CF 3, OCF 3, 1-3C alkyl or 1-3C alkoxy. Independent claims are also included for: (1) a composition comprising (I), a vehicle/additive and optionally other pharmacologically active compounds; and (2) a product comprising (I) for simultaneous, separate or sequential administration for the therapy or prophylaxis of atrial fibrillation or atrial flutter. ACTIVITY : Antiarrhythmic; Cardiovascular-Gen.; Cardiant; Vasotropic. MECHANISM OF ACTION : Beta-adrenoreceptor blocker; Kv1.5 channel blocker. (Ib) is tested for its kv1.5 channel blocking activity using biological assays. The results showed that the median inhibitory concentration of 2'-(benzyloxycarbonylaminomethyl)biphenyl-2- carboxylic acid 2-(2-pyridyl)ethylamide was 0.7 MicroM.
机译:组合物(I)包含至少一种β-阻滞剂(A)和至少一种苯基羧酸酰胺衍生物(Ia或Ib)及其盐的化合物。组合物(I)包含至少一种β-阻滞剂和至少一种式(Ia或Ib)的苯基羧酸酰胺衍生物及其盐的化合物。 [图像] R1:3-5C烷基或喹啉基; R2:1-4C烷基或环丙基; R3:苯基或吡啶基(两者任选地被F,Cl,CF 3,OCF 3,1-3C烷基或1-3C烷氧基的1-2取代); A:-C nH 2 n; n:0-2; R 4 -R 7:H,F,Cl,CF 3,OCF 3,CN,1-3C烷基或1-3C烷氧基; B:-C mH 2 m-; m:1或2; R8:2-3C烷基,苯基或吡啶基(其中苯基和吡啶基任选地被F,Cl,CF 3,OCF 3,1-3C烷基或1-3C烷氧基中的1-2取代); R9:C(O)OR10或COR10; R10 :-( C xH 2)x-R11; x:0-2; R11:被F,Cl,CF 3,OCF 3,1-3C烷基或1-3C烷氧基中的1-2取代的苯基。还包括以下方面的独立权利要求:(1)一种组合物,其包含(I),媒介物/添加剂和任选的其他药理活性化合物; (2)包含(I)的产品,所述产品用于同时,分开或顺序给药以治疗或预防心房颤动或心房扑动。活动:抗心律失常;心血管创卡迪恩变压的。作用机理:β-肾上腺素受体阻滞剂; Kv1.5频道拦截器。 (b)使用生物测定法测试其kv1.5通道阻断活性。结果表明,2'-(苄氧基羰基氨基甲基)联苯-2-羧酸2-(2-吡啶基)乙酰胺的中位抑制浓度为0.7 MicroM。

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