申请人:Aventis Pharma Deutschland GmbH
公开号:US06162819A1
公开(公告)日:2000-12-19
The present invention relates to pyrazole derivatives of the formula I, their preparation and their use in pharmaceuticals: ##STR1## in which X, R.sup.1, R.sup.1a, R.sup.2, R.sup.3, R.sup.4 and n are as defined in the claims, which are useful pharmaceutically active compounds for the therapy and prophylaxis of illnesses, for example of cardiovascular diseases such as hypertension, angina pectoris, cardiac insufficiency, thromboses or atherosclerosis. The compounds of the formula I are capable of modulating the body's production of cyclic guanosine monophosphate "cGMP" and are generally suitable for the therapy and prophylaxis of illnesses which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for preparing compounds of the formula 1, to their use for the therapy and prophylaxis of the abovementioned illnesses and for preparing pharmaceuticals for this purpose, and also to pharmaceutical preparations which comprise the compounds of the formula I.
本发明涉及式I的吡唑衍生物,其制备及其在药物中的应用:##STR1## 其中X,R.sup.1,R.sup.1a,R.sup.2,R.sup.3,R.sup.4和n如索引中所定义,它们是有用的药用活性化合物,用于治疗和预防疾病,例如心血管疾病,如高血压,心绞痛,心力衰竭,血栓或动脉粥样硬化。式I的化合物能够调节体内环鸟苷酸单磷酸鸟苷“cGMP”的产生,并通常适用于与扰乱cGMP平衡相关的疾病的治疗和预防。该发明还涉及制备式1的化合物的方法,它们用于治疗和预防上述疾病,以及用于为此目的制备药物,以及包含式I化合物的药物制剂。