适配器相关激酶 1（AAK1）抑制剂的专利研究综述（2013 年至今）。
A patent review of adaptor associated kinase 1 (AAK1) inhibitors (2013-present).
机构信息
Rega Institute for Medical Research, Laboratory of Medicinal ChemistryKU Leuven, Leuven, Belgium.
Department of Microbiology, Immunology and Transplantation, Rega Institute for Medical Research, Laboratory of Virology and ChemotherapyKU Leuven, Leuven, Belgium.
出版信息
Expert Opin Ther Pat. 2021 Oct;31(10):911-936. doi: 10.1080/13543776.2021.1928637. Epub 2021 May 21.
INTRODUCTION
Adaptor-associated kinase 1 (AAK1) has been proposed as being a promising drug target for the treatment of a variety of neurological and psychiatric disorders, such as schizophrenia, cognitive deficits in schizophrenia, Parkinson's disease, bipolar disorder, Alzheimer's disease and neuropathic pain. More recently, AAK1 was shown to be an essential cellular factor for viral replication and therefore has been pursued as a host target for the development of broad-spectrum antiviral agents.
AREAS COVERED
This review provides an overview of the patented AAK1 inhibitors from 2013 to present.
EXPERT OPINION
The promise of AAK1 as drug target for the treatment of neuropathic pain stimulated the search for AAK1 inhibitors. However, only two companies (i.e. Lexicon Pharmaceuticals and Bristol Myers Squibb) seemed to be active in this field and filed patent applications in the last few years. The most promising congeners showed promising activity in a variety of AAK1-related assays. Moreover, selected compounds were also endowed with activity in various preclinical animal models for neuropathic pain.
简介
衔接激酶 1（AAK1）已被提议作为治疗多种神经和精神疾病的有前途的药物靶点，如精神分裂症、精神分裂症认知缺陷、帕金森病、双相情感障碍、阿尔茨海默病和神经病理性疼痛。最近，AAK1 被证明是病毒复制的必需细胞因子，因此被作为广谱抗病毒药物开发的宿主靶点。
涵盖领域
本文综述了 2013 年至今获得专利的 AAK1 抑制剂。
专家意见
AAK1 作为治疗神经病理性疼痛的药物靶点的前景激发了对 AAK1 抑制剂的研究。然而，似乎只有两家公司（即 Lexicon Pharmaceuticals 和 Bristol Myers Squibb）在这一领域活跃，并在过去几年中提交了专利申请。最有前途的同类物在各种与 AAK1 相关的测定中表现出有希望的活性。此外，选定的化合物在各种用于治疗神经病理性疼痛的临床前动物模型中也具有活性。
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