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In response to a recent article that was posted online on November 6, 2012 entitled “Leucine-rich repeat kinase 2 inhibitors: a patent review (2006 – 2011)” (doi:10.1517/13543776.2012.729041).
The authors appear to claim that they were the first to discover compound 11 and that Genentech/Roche discovered 11 in a parallel effort. However, the patent and non-patent literature clearly shows that Genentech/Roche was the first to discover compound 11 and that the Gray group found it later.
On page 4 of the article, the authors present a misleading chronology of the discovery and reporting of compound 11. The Genentech/Roche patent Citation[1] (Reference 48 in this patent review) was published in December of 2011 and clearly exemplifies compound 11 as Example 3. Because the compound was made before the provisional filing date of June 4, 2010, this clearly shows that this patent was the first disclosure of compound 11.
The first disclosure of compound 11 in the non-patent literature was in the publication by Chen et al. Citation[2] (Reference 50 in patent review). This article was received by J. Med. Chem. on March 31, 2012, and first published online on May 16, 2012. This publication appeared online six days before the publication by Choi et al. Citation[3]. (Reference 47 in patent review) was received by ACS Med. Chem. Lett. (May 22, 2012). The Choi article was first published online on June 18, 2012.
Furthermore, the current article misrepresents the authorship of Reference 50 in the text as “Hu et al.” rather than the correct “Chen et al.” The authors also do not make reference anywhere in the text to compound 12 (Figure 6) as this compound has clearly been shown to have a superior LRRK2 activity and ADME profile in comparison to compound 11 Citation[4].
Declaration of interest
The author of this letter is an employee of Genentech, Inc. The author declares no other conflict of interest and has received no payment in preparation of this correspondence.
Bibliography
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- Chen H, Chan BK, Drummond J, Discovery of selective LRRK2 inhibitors guided by computational analysis and molecular modeling. J Med Chem 2012;55:5536-45
- Choi HG, Zhang J, Deng X, Brain penetrant LRRK2 inhibitor. ACS Med. Chem Lett 2012;3:658-62
- Estrada AA, Liu X, Baker-Glenn C Discovery of highly potent, selective, and brain-penetrable leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitors. J Med Chem 2012; 55:9416-9433