共价药物含有亲电子基团，可以与蛋白质（特别是酶）活性位点的亲核氨基酸发生反应。最近，人们对使用共价药物靶向蛋白质中的非催化氨基酸来调节困难靶点（即靶向共价抑制剂）产生了很大的兴趣。共价化合物包含多种共价反应基团 (CRG)，但 FDA 批准的共价药物中只存在其中的少数 CRG。这篇综述总结了 2020-23 专利格局分析，该分析检查了共价药物发现领域的趋势围绕目标和组织。该分析重点关注提交给世界国际专利组织的专利申请，并根据 FDA 批准的药物中存在的 CRG，使用关键词和结构搜索相结合进行选择。共识别出来自 > 300 个组织的 707 份专利申请，公开了化合物作用于 71 个目标。 5个靶点的专利申请数量占总数量的63%（即BTK、EGFR、FGFR、KRAS和SARS-CoV-2 Mpro）。专利数量最多的组织是学术机构（丹娜法伯癌症研究所）。对于一个靶标 KRAS G12C，新药的发现竞争非常激烈（超过 100 个组织，186 项专利申请）。

Covalent drugs contain electrophilic groups that can react with nucleophilic amino acids located in the active sites of proteins, particularly enzymes. Recently, there has been considerable interest in using covalent drugs to target non-catalytic amino acids in proteins to modulate difficult targets (i.e. targeted covalent inhibitors). Covalent compounds contain a wide variety of covalent reacting groups (CRGs), but only a few of these CRGs are present in FDA-approved covalent drugs.This review summarizes a 2020-23 patent landscape analysis that examined trends in the field of covalent drug discovery around targets and organizations. The analysis focused on patent applications that were submitted to the World International Patent Organization and selected using a combination of keywords and structural searches based on CRGs present in FDA-approved drugs.A total of 707 patent applications from > 300 organizations were identified, disclosing compounds that acted at 71 targets. Patent application counts for five targets accounted for ~ 63% of total counts (i.e. BTK, EGFR, FGFR, KRAS, and SARS-CoV-2 Mpro). The organization with the largest number of patent counts was an academic institution (Dana-Farber Cancer Institute). For one target, KRAS G12C, the discovery of new drugs was highly competitive (>100 organizations, 186 patent applications).