首页> 外国专利> Use of a compound which is both a beta adrenoreceptor antagonist and a alpha-1 adrenoreceptor antagonist especially carvedilol to treat congestive heart failure either on its own or with an angiotensin converting enzyme inhibitor, diuretic and/or cardiac glycoside

Use of a compound which is both a beta adrenoreceptor antagonist and a alpha-1 adrenoreceptor antagonist especially carvedilol to treat congestive heart failure either on its own or with an angiotensin converting enzyme inhibitor, diuretic and/or cardiac glycoside

机译:既是β肾上腺素受体拮抗剂又是α-1肾上腺素受体拮抗剂,特别是卡维地洛的化合物单独或与血管紧张素转化酶抑制剂,利尿剂和/或强心苷一起治疗充血性心力衰竭的用途

摘要

A compound which is both an b-adrenoreceptor antagonist and a a1-arenoreceptor antagonist is used in the manufacture of a medicament for decreasing mortality resulting from congestive heart failure. The medicament can optionally with a angiotensin converting enzyme inhibitor, a diuretic and a cardiac glycoside. The compound can have the formula I wherein: R1 is H, alkyl, benzoyl or naphthoyl; R2 is H, alkyl, benzyl, phenylethyl or phenylpropyl; R3 is H or alkyl; R4 is H or alkyl or when X is O then R4 and R3 can form a -CH2-O- group; X is a single bond, -CH2-, -O- or -S-; Ar is phenyl, naphthyl, indanyl or tetrahydronaphthyl; R5 and R6 are independently H, F, Cl, Br OH, alkyl, -CONH2-, alkoxy, benzoyloxy, alkylthio or alkylsulphonyl or together form a methylenedioxy or a pharmaceutically acceptable salt thereof.
机译:既是β-肾上腺素受体拮抗剂又是α1-肾上腺素受体拮抗剂的化合物用于制造药物,以降低由充血性心力衰竭引起的死亡率。该药物可以任选地与血管紧张素转化酶抑制剂,利尿剂和强心苷一起使用。该化合物可以具有式I,其中:R 1为H,烷基,苯甲酰基或萘甲酰基; R 2是H,烷基,苄基,苯乙基或苯丙基; R3是H或烷基; R4为H或烷基,或当X为O时,R4和R3可形成-CH2-O-基团; X是单键,-CH 2-,-O-或-S-; Ar是苯基,萘基,茚满基或四氢萘基; R 5和R 6独立地为H,F,Cl,Br OH,烷基,-CONH 2-,烷氧基,苯甲酰氧基,烷硫基或烷基磺酰基,或一起形成亚甲二氧基或其药学上可接受的盐。

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