214759-65-6Relevant articles and documents
Discovery of G2019S-Selective Leucine Rich Repeat Protein Kinase 2 inhibitors with in vivo efficacy
Fitch, William L.,Gajera, Chandresh R.,Lam, Grace,Le?niak, Robert K.,Montine, Thomas J.,Nguyen, Khanh C.,Nichols, R. Jeremy,Schonemann, Marcus,Smith, Mark,Zhao, Jing
supporting information, (2022/01/08)
Mutations in the Leucine Rich Repeat Protein Kinase 2 gene (LRRK2) are the most common genetic causes of Parkinson's Disease (PD). The G2019S mutation is the most common inherited LRRK2 mutation, occurs in the kinase domain, and results in increased kinase activity. We report the discovery and development of compound 38, an indazole-based, G2019S-selective (>2000-fold vs. WT) LRRK2 inhibitor capable of entering rodent brain (Kp = 0.5) and selectively inhibiting G2019S-LRRK2. The compounds disclosed herein present a starting point for further development of brain penetrant G2019S selective inhibitors that hopefully reduce lung phenotype side-effects and pave the way to providing a precision medicine for people with PD who carry the G2019S mutation.
HETEROTETRACYCLIC COMPOUNDS AS TPO MIMETICS
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Page/Page column 32, (2009/04/24)
The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated TPO activity, particularly diseases or disorders that involve thrombocytopenia.
BICYCLIC COMPOUNDS HAVING BRADYKININ RECEPTORS AFFINITY AND PHARMACEUTICAL COMPOSITIONS THEREOF
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Page 127, (2008/06/13)
Selected compounds are effective for treatment of pain and diseases, such as inflammation mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and