首页> 外国专利> EPOXY-STEROIDAL ALDOSTERONE ANTAGONIST AND ANGIOTENSIN II ANTAGONIST COMBINATION THERAPY FOR TREATMENT OF CONGESTIVE HEART FAILURE.

EPOXY-STEROIDAL ALDOSTERONE ANTAGONIST AND ANGIOTENSIN II ANTAGONIST COMBINATION THERAPY FOR TREATMENT OF CONGESTIVE HEART FAILURE.

机译:环氧-甾体醛固酮拮抗剂和血管紧张素Ⅱ拮抗剂联合治疗栓塞性心力衰竭。

摘要

A combination therapy comprising a therapeutically-effective amount of an epoxy-steroidal aldosterone receptor antagonist and a therapeutically-effective amount of an angiotensin II receptor antagonist is described for treatment of circulatory disorders, including cardiovascular disorders such as hypertension, congestive heart failure, cirrhosis and ascites. Preferred angiotensin II receptor antagonists are those compounds having high potency and bioavailability and which are characterized in having an imidazole or triazole moiety attached to a biphenylmethyl or pyridinyl/phenylmethyl moiety. Preferred epoxy-steroidal aldosterone receptor antagonists are 20-spiroxane steroidal compounds characterized by the presence of 9'alpha', 11'alpha'-substituted epoxy moiety. A preferred combination therapy includes the angiotensin II receptor antagonist 5-[2-[5-[(3,5-dibutyl-1H-1,2,4-triazol-1-yl)methyl]-2-pyridi nyl]phenyl-1H-tetrazole and the aldosterone receptor antagonist epoxymexrenone.
机译:描述了包含治疗有效量的环氧类固醇醛固酮受体拮抗剂和治疗有效量的血管紧张素II受体拮抗剂的联合疗法,其用于治疗循环系统疾病,包括心血管疾病,例如高血压,充血性心力衰竭,肝硬化和腹水。优选的血管紧张素II受体拮抗剂是那些具有高效能和生物利用度的化合物,其特征在于具有与联苯甲基或吡啶基/苯甲基部分连接的咪唑或三唑部分。优选的环氧类固醇醛固酮受体拮抗剂是20-螺氧烷类固醇化合物,其特征在于存在9′α′,11′α′取代的环氧部分。优选的组合疗法包括血管紧张素II受体拮抗剂5- [2- [5-[(3,5-二丁基-1H-1,2,4-三唑-1-基)甲基] -2-吡啶基]苯基- 1H-四唑和醛固酮受体拮抗剂环氧美沙酮。

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