The present invention relates to Pyrazolopyrimidinone compounds as PDE5 inhibitors with better IC50 value, good in vivo efficacy and PK profile and a process for the preparation thereof. The present invention covers the pyrazolo pyrimidinone based compounds that have been designed, synthesized and screened for PDE5 inhibitory activity and its PDE5 inhibitory potential is provided in this invention. These designer compounds have shown nanomolar potency when screened for PDE5 inhibitory activity and also shown better in vivo efficacy. These compounds can be used in the treatment of male erectile dysfunction or in the treatment of impotence.
本发明涉及作为PDE5
抑制剂的
吡唑嘧啶酮化合物,具有更好的IC50值、良好的体内有效性和PK特性,以及其制备方法。本发明涵盖基于
吡唑嘧啶酮的化合物,这些化合物已经被设计、合成和筛选用于PDE5抑制活性,其PDE5抑制潜力在本发明中提供。这些设计的化合物在筛选PDE5抑制活性时表现出纳摩尔级的效力,并且在体内表现出更好的有效性。这些化合物可以用于治疗男性勃起功能障碍或阳痿的治疗。