申请人:Aventis Pharma Deutschland GmbH
公开号:EP1388341A1
公开(公告)日:2004-02-11
The present invention relates to acylamino-substituted heteroaromatic compounds of the formula I,
in which R1, R2, R3, R4 and R5 and X have the meanings indicated in the claims. The compounds of formula I are valuable pharmaceutically active compounds which are useful in the treatment of various disease states including cardiovascular disorders such as atherosclerosis, thrombosis, coronary artery disease, hypertension and cardiac insufficiency. They upregulate the expression of the enzyme endothelial nitric oxide (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 furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.
本发明涉及式 I 的酰氨基取代的杂芳香族化合物、
其中 R1、R2、R3、R4 和 R5 以及 X 具有权利要求中所述的含义。式 I 化合物是有价值的药物活性化合物,可用于治疗各种疾病,包括心血管疾病,如动脉粥样硬化、血栓形成、冠状动脉疾病、高血压和心功能不全。它们能上调内皮一氧化氮(NO)合成酶的表达,可用于需要增加所述酶的表达或提高 NO 水平或使降低的 NO 水平恢复正常的情况。本发明还涉及式 I 化合物的制备工艺、其用途(尤其是作为药物的活性成分)以及包含它们的药物制剂。