Abstract：
UNASSIGNED: Phosphodiesterase 9 (PDE9) has been demonstrated as a potential target for neurological disorders and cardiovascular diseases, such as Alzheimer\'s disease and heart failure. For the last few years, a series of PDE9 inhibitors with structural diversities have been developed and patented by researchers and pharmaceutical companies, providing insights into first-in-class therapies of PDE9 drug candidates.
UNASSIGNED: This review provides an overview of PDE9 inhibitors in patents from 2018 to the present.
UNASSIGNED: Only a few of the current PDE9 inhibitors are highly selective over other PDEs, which limits their application in pharmacological and clinical research. The design and development of highly selective PDE9 inhibitors remain the top priority in future research. The advantages of targeting PDE9 rather than other PDEs in treating neurodegenerative diseases need to be explained thoroughly. Besides, application of PDE9 inhibitor-based combination therapies sheds light on treating diabetes and refractory heart diseases. Finally, PDE9 inhibitors should be further explored in clinical indications beyond neurological disorders and cardiovascular diseases.
UNASSIGNED: This review provides an overview of PDE9 inhibitors in patents from 2018 to the present.
UNASSIGNED: Only a few of the current PDE9 inhibitors are highly selective over other PDEs, which limits their application in pharmacological and clinical research. The design and development of highly selective PDE9 inhibitors remain the top priority in future research. The advantages of targeting PDE9 rather than other PDEs in treating neurodegenerative diseases need to be explained thoroughly. Besides, application of PDE9 inhibitor-based combination therapies sheds light on treating diabetes and refractory heart diseases. Finally, PDE9 inhibitors should be further explored in clinical indications beyond neurological disorders and cardiovascular diseases.
摘要：
■磷酸二酯酶9（PDE9）已被证明是神经系统疾病和心血管疾病的潜在靶标，如阿尔茨海默病和心力衰竭。在过去的几年里，一系列具有结构多样性的PDE9抑制剂已被研究人员和制药公司开发并获得专利，提供对PDE9候选药物的一流治疗的见解。
■这篇综述概述了2018年至今专利中的PDE9抑制剂。
■目前只有少数PDE9抑制剂对其他PDEs具有高度选择性，这限制了它们在药理和临床研究中的应用。高选择性PDE9抑制剂的设计和开发仍是未来研究的重中之重。需要彻底解释靶向PDE9而不是其他PDE在治疗神经退行性疾病中的优势。此外,基于PDE9抑制剂的联合疗法的应用为糖尿病和难治性心脏病的治疗提供了启示。最后,PDE9抑制剂应在神经系统疾病和心血管疾病以外的临床适应症中进一步探索。
■这篇综述概述了2018年至今专利中的PDE9抑制剂。
■目前只有少数PDE9抑制剂对其他PDEs具有高度选择性，这限制了它们在药理和临床研究中的应用。高选择性PDE9抑制剂的设计和开发仍是未来研究的重中之重。需要彻底解释靶向PDE9而不是其他PDE在治疗神经退行性疾病中的优势。此外,基于PDE9抑制剂的联合疗法的应用为糖尿病和难治性心脏病的治疗提供了启示。最后,PDE9抑制剂应在神经系统疾病和心血管疾病以外的临床适应症中进一步探索。
