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Use of renin inhibitors for the prevention or treatment of diastolic dysfunction or diastolic heart failure

机译:肾素抑制剂在预防或治疗舒张功能障碍或舒张性心力衰竭中的用途

摘要

Pharmaceutical composition comprising a renin inhibitor, or a pharmaceutically acceptable salt thereof, in combination with (i) an ACE inhibitor, or a pharmaceutically acceptable salt thereof; or (ii) an angiotensin II receptor blocker, or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable carrier; for use in the treatment of diastolic dysfunction or cardiac-diastolic insufficiency, in which the renin inhibitor is selected from the group consisting of RO 66-1132, RO 66-1168 and a compound of formula (III) in which R1 is halogen , C1-6 halogenoalkyl, C1-6 alkoxy-C1-6 alkyloxy or C1-6 alkoxy-C1-6 alkyl; R2 is halogen, C1-4 alkyl or C1-4 alkoxy; R3 and R4 are independently branched C3-6 alkyl; and R 5 is cycloalkyl, C 1-6 alkyl, C 1-6 hydroxyalkyl, C 1-6 alkoxy-C 1-6 alkyl, C 1-6 alkanoyloxy-C 1-6 alkyl, C 1-6 aminoalkyl, C 1-6 alkylamino-C 1-6 alkyl, C1-6 dialkylamino-C1-6 alkyl, C1-6 alkanoylamino-C1-6 alkyl, HO (O) C-C1-6 alkyl, C1-6 alkyl-O- (O) C-C1-6 alkyl, H2N- C (O) -C 1-6 alkyl, C 1-6 alkyl-HN-C (O) -C 1-6 alkyl or (C 1-6 alkyl) 2N-C (O) -C 1-6 alkyl; or in each case a pharmaceutically acceptable salt thereof, with the proviso that, when the composition comprises (ii) an angiotensin II receptor blocker or a pharmaceutically acceptable salt thereof, it does not comprise a neutral endopeptidase (NEP) inhibitor, or a pharmaceutically acceptable salt thereof.
机译:药物组合物,其包含肾素抑制剂或其药学上可接受的盐,与(i)ACE抑制剂或其药学上可接受的盐组合; (ii)血管紧张素II受体阻断剂或其药学上可接受的盐;或和药学上可接受的载体;用于治疗舒张功能障碍或心脏舒张功能不全,其中肾素抑制剂选自RO 66-1132,RO 66-1168和其中R1为卤素,C1的式(III)化合物-6个卤代烷基,C 1-6烷氧基-C 1-6烷氧基或C 1-6烷氧基-C 1-6烷基; R2是卤素,C1-4烷基或C1-4烷氧基; R3和R4独立地为支链C3-6烷基; R 5为环烷基,C 1-6烷基,C 1-6羟烷基,C 1-6烷氧基-C 1-6烷基,C 1-6烷酰氧基-C 1-6烷基,C 1-6氨基烷基,C 1 -6烷基氨基-C 1-6烷基,C1-6二烷基氨基-C1-6烷基,C1-6烷酰基氨基-C1-6烷基,HO(O)C-C1-6烷基,C1-6烷基-O-(O )C-C1-6烷基,H2N-C(O)-C 1-6烷基,C 1-6烷基-HN-C(O)-C 1-6烷基或(C 1-6烷基)2N-C (O)-C 1-6烷基;或其每种情况下的药学上可接受的盐,条件是当组合物包含(ii)血管紧张素II受体阻滞剂或其药学上可接受的盐时,它不包含中性内肽酶(NEP)抑制剂或药学上可接受的盐其盐。

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