神经激肽-1 受体拮抗剂：全面专利调查。
Neurokinin-1 receptor antagonists: a comprehensive patent survey.
机构信息
Millennium: The Takeda Oncology Company, Cambridge, MA 02139, USA.
出版信息
Expert Opin Ther Pat. 2010 Aug;20(8):1019-45. doi: 10.1517/13543776.2010.495121.
IMPORTANCE OF THE FIELD
Substance P is involved in mediating a number of biological effects such as emesis, pain, inflammation, bronchoconstriction, antitumor activity, and regulation of gastrointestinal and CNS function by binding to the neurokinin-1 (NK1) receptor. Antagonists of this receptor have the potential to be useful in the treatment of various disease conditions.
AREAS COVERED IN THIS REVIEW
More than 300 patents have been filed by nearly 20 companies and 2 academic institutions in the past 2 decades. This review provides an overview of the patenting activity in the NK1 antagonist field over the last 20 years.
WHAT THE READER WILL GAIN
Chemically diverse non-peptide NK1 receptor antagonists have been identified since the discovery of CP-96,345 by Pfizer in 1991. Representative examples of patented ligands and their biological activities are presented in a company-wise approach.
TAKE HOME MESSAGE
The NK1 receptor research has led to the clinical introduction of aprepitant in 2003 and its water soluble injectable form, fosaprepitant dimeglumine, in 2009 by Merck for the prevention of postoperative nausea and vomiting and for inhibiting chemotherapy-induced nausea and vomiting. In addition, maropitant citrate received approval in 2007 for veterinary use.
重要性领域
P 物质参与介导多种生物效应，如呕吐、疼痛、炎症、支气管收缩、抗肿瘤活性以及胃肠道和中枢神经系统功能的调节，其通过与神经激肽-1（NK1）受体结合发挥作用。该受体的拮抗剂有可能在治疗各种疾病方面发挥作用。
涵盖领域
在过去的 20 年中，近 20 家公司和 2 所学术机构已提交了超过 300 项专利。这篇综述概述了过去 20 年中 NK1 拮抗剂领域的专利活动情况。
读者受益
自辉瑞（Pfizer）公司于 1991 年发现 CP-96,345 以来，已经发现了化学结构多样的非肽 NK1 受体拮抗剂。以公司为基础的方式展示了已获专利的配体及其生物学活性的代表性实例。
结论
NK1 受体研究导致默克（Merck）公司于 2003 年推出阿瑞匹坦（aprepitant），用于预防术后恶心和呕吐以及抑制化疗引起的恶心和呕吐，其水溶性注射用福沙匹坦二甲葡胺（fosaprepitant dimeglumine）于 2009 年推出，此外，柠檬酸马罗匹坦于 2007 年获准兽用。
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