Organic Chemistry, Institute of Chemistry, The Hebrew University of Jerusalem, Philadelphia Building 201/205, Edmond J. Safra Campus, Jerusalem 91904, Israel.
Drug Discov Today. 2010 Mar;15(5-6):163-70. doi: 10.1016/j.drudis.2010.01.007. Epub 2010 Jan 29.
Enantiomer patents (ENPTs), constituents of chiral switches, claim single enantiomers of chiral drugs previously claimed as racemates. In this article, the strategy of ENPTs and recent court decisions and trends in case law worldwide are highlighted. ENPTs are challenged frequently (e.g. anticipation, obviousness, double patenting and insufficient disclosure), even though the novelty of enantiomers is not destroyed by the description of racemates. For establishing inventiveness (nonobviousness), the description in ENPTs should include superior pharmacological and/or pharmaceutical properties of enantiomer vis-á-vis racemate, above the expected 2:1 ratio. ENPTs were 'obvious-to-try' (unless taught away) since the mid-1980s. General concern about evergreening by ENPTs is not justified. ENPTs should be evaluated on a case-by-case basis. ENPT litigations are especially susceptible to settlements.
对映异构体专利（ENPT）是手性开关的组成部分，它要求对先前作为外消旋体申报的手性药物的单一对映异构体进行申报。本文重点介绍了 ENPT 的策略以及全球范围内最新的法院判决和判例法趋势。ENPT 经常受到质疑（例如，可预见、明显性、双重专利和披露不足），尽管外消旋体的新颖性不会因对手性药物的描述而被破坏。为了确立发明性（非显而易见性），ENPT 中的描述应该包括对映异构体相对于外消旋体的优越的药理学和/或药物学特性，超过预期的 2:1 比例。自 20 世纪 80 年代中期以来，ENPT 一直是“显而易见的尝试”（除非被教导放弃）。人们普遍担心 ENPT 会导致“常青”，但这种担心是没有根据的。应该逐案评估 ENPT。ENPT 诉讼尤其容易达成和解。
