Imidazoquinolines as Novel Inhibitors of LRRK2 Kinase Activity - ACS

Patent Highlight Cite This: ACS Med. Chem. Lett. XXXX, XXX, XXX−XXX

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Imidazoquinolines as Novel Inhibitors of LRRK2 Kinase Activity Gerard Rosse* Drexel University, Department of Pharmacology and Physiology College of Medicine, New College Building, 245 North 15th Street, Philadelphia, Pennsylvania 19102, United States Key Structures.

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Title. Novel imidazo[4,5-C]quinolone Derivatives as LRRK2 Inhibitors Patent Application Number. WO 2018/163066 A1 Publication Date. September 13, 2018 Priority Application. US 2017−62469756 Priority Date. March 10, 2017 Inventors. Brodney, M. A.; Chappie, T. A.; Chen, J. M.; Coe, J. W.; Coffman, K. J.; Galatsis, P.; Garnsey, M. R.; Helal, C. J.; Henderson, J. L.; Kormos, B. L.; Kurumbail, R. G.; MartinezAlsina, L. A.; Pettersson, M. Y.; Reese, M. R.; Rose, C. R.; Stepan, A. F.; Verhoest, P. R.; Wager, T. T.; Warmus, J. S.; Zhang, Y. Assignee Company. Pfizer Inc., USA Disease Area. Parkinson’s disease, Alzheimer’s disease, Crohn’s disease, Tauopathy Biological Target. Leucin-Rich Repeat Kinase 2 (LRRK2) Summary. Novel imidazoquinoline analogs are claimed for the treatment of diseases associated with LRRK2 such as Crohn’s disease, Alzheimer’s disease, Parkinson’s disease, and cancer.

Received: December 28, 2018

© XXXX American Chemical Society

A

DOI: 10.1021/acsmedchemlett.8b00654 ACS Med. Chem. Lett. XXXX, XXX, XXX−XXX

ACS Medicinal Chemistry Letters

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Biological Assay. The compounds were tested for their ability to modulate LRRK2 kinase activity using Lantha Screen technology. Biological Data. Results of LRRK2 kinase activity:

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AUTHOR INFORMATION

Corresponding Author

*E-mail: [email protected]. ORCID

Gerard Rosse: 0000-0003-1993-3575 Notes

The author declares no competing financial interest.

B

DOI: 10.1021/acsmedchemlett.8b00654 ACS Med. Chem. Lett. XXXX, XXX, XXX−XXX