首页> 外国专利> HETEROARYL SUBSTITUTED AMIDS WITH UNSATURATED OR CYCLIC COMPOUND AND THEIR USE AS PHARMACEUTICALS

HETEROARYL SUBSTITUTED AMIDS WITH UNSATURATED OR CYCLIC COMPOUND AND THEIR USE AS PHARMACEUTICALS

机译:具有不饱和或环状化合物的杂芳基取代的酰胺及其作为药物的用途

摘要

The present invention relates to N-alkylamides of the formula I, in which A, Het, X, R 1 , R 2 and R 3 have the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO) synthase and are valuable pharmacologically active compounds. Specifically, the compounds of the formula I upregulate the expression of the enzyme endothelial NO synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired. The invention further relates to processes for the preparation of compounds of the formula I, to pharmaceutical compositions comprising them, and to the use of compounds of the formula I for the manufacture of a medicament for the stimulation of the expression of endothelial NO synthase or for the treatment of various diseases including cardiovascular disorders such as atherosclerosis, thrombosis, coronary artery disease, hypertension and cardiac insufficiency, for example.
机译:本发明涉及式I的N-烷基酰胺,其中A,Het,X,R 1,R 2和R 3具有权利要求书中指出的含义,其调节内皮型一氧化氮(NO)合酶的转录,并且是有价值的药理活性化合物。具体而言,式I化合物上调了酶内皮NO合酶的表达,并且可以在需要增加所述酶的表达或增加NO水平或使NO水平正常化的条件下使用。本发明进一步涉及制备式I化合物的方法,涉及包含它们的药物组合物,以及式I化合物在制备用于刺激内皮NO合酶表达的药物中的用途或用于例如,治疗各种疾病,包括心血管疾病,例如动脉粥样硬化,血栓形成,冠状动脉疾病,高血压和心脏功能不全。

著录项

  • 公开/公告号AT423777T

    专利类型

  • 公开/公告日2009-03-15

    原文格式PDF

  • 申请/专利权人 SANOFI-AVENTIS;

    申请/专利号AT20060754359T

  • 申请日2006-06-14

  • 分类号C07D401/06;A61K31/4439;A61K31/444;A61P9/08;C07D401/08;C07D401/14;C07D409/14;C07D417/06;

  • 国家 AT

  • 入库时间 2022-08-21 19:24:35

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