1351759-29-9Relevant articles and documents
Synthesis and Preliminary Evaluation of [11C]GNE-1023 as a Potent PET Probe for Imaging Leucine-Rich Repeat Kinase 2 (LRRK2) in Parkinson's Disease
Chen, Zhen,Shao, Tuo,Gao, Wei,Fu, Hualong,Collier, Thomas Lee,Rong, Jian,Deng, Xiaoyun,Yu, Qingzhen,Zhang, Xiaofei,Davenport, April T.,Daunais, James B.,Wey, Hsiao-Ying,Shao, Yihan,Josephson, Lee,Qiu, Wen-Wei,Liang, Steven
, p. 1580 - 1585 (2019)
Leucine-rich repeat kinase 2 (LRRK2) is a large protein involved in the pathogenesis of Parkinson's disease (PD). It has been demonstrated that PD is mainly conferred by LRRK2 mutations that bring about increased kinase activity. As a consequence, selecti
PHARMACEUTICAL COMPOSITION COMPRISING COMPOUND CAPABLE OF PENETRATING BLOOD-BRAIN BARRIER AS EFFECTIVE INGREDIENT FOR PREVENTING OR TREATING BRAIN CANCER
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Paragraph 0089, (2020/01/22)
Disclosed is a pharmaceutical composition for the prevention or treatment of brain cancer, containing a compound capable of penetrating the blood-brain barrier as an active ingredient, the pharmaceutical composition for the prevention or treatment of brain cancer is capable of efficiently penetrating the blood-brain barrier of the brain to thereby effectively inhibit LRRK2 protein expression, and is thus useful in the prevention or treatment of brain cancer.
Fluorine-18 and carbon-11 labeled radioligands for positron emission tomography (PET) imaging for LRRK2
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Page/Page column 72, (2015/11/16)
A method for positron emission tomography (PET) imaging of LRRK2 in tissue of a subject, the method comprising: administering a compound of formula I, formula II or formula III, or a pharmaceutically acceptable salt thereof to the subject, wherein the com
FLUORINE-18 AND CARBON-11 LABELED RADIOLIGANDS FOR POSITRON EMISSION TOMOGRAPHY (PET) IMAGING FOR LRRK2
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Page/Page column 119, (2013/06/27)
A method for positron emission tomography (PET) imaging of LRRK2 in the tissue of a subject, the method comprising: administering a compound of formula (I), formula (II) or formula (III), or a pharmaceutically acceptable salt thereof to the subject, where
Discovery of selective LRRK2 inhibitors guided by computational analysis and molecular modeling
Chen, Huifen,Chan, Bryan K.,Drummond, Jason,Estrada, Anthony A.,Gunzner-Toste, Janet,Liu, Xingrong,Liu, Yichin,Moffat, John,Shore, Daniel,Sweeney, Zachary K.,Tran, Thuy,Wang, Shumei,Zhao, Guiling,Zhu, Haitao,Burdick, Daniel J.
, p. 5536 - 5545 (2012/08/28)
Mutations in the genetic sequence of leucine-rich repeat kinase 2 (LRRK2) have been linked to increased LRRK2 activity and risk for the development of Parkinson's disease (PD). Potent and selective small molecules capable of inhibiting the kinase activity of LRRK2 will be important tools for establishing a link between the kinase activity of LRRK2 and PD. In the absence of LRRK2 kinase domain crystal structures, a LRRK2 homology model was developed that provided robust guidance in the hit-to-lead optimization of small molecule LRRK2 inhibitors. Through a combination of molecular modeling, sequence analysis, and matched molecular pair (MMP) activity cliff analysis, a potent and selective lead inhibitor was discovered. The selectivity of this compound could be understood using the LRRK2 homology model, and application of this learning to a series of 2,4-diaminopyrimidine inhibitors in a scaffold hopping exercise led to the identification of highly potent and selective LRRK2 inhibitors that were also brain penetrable.
AMINOPYRIMIDINE DERIVATIVES AS LRRK2 INHIBITORS
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Page/Page column 35, (2011/12/14)
Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n. X, R1, R2, R3, R5, R6 and R7 are as defined herein. Also disclosed are methods of making the compound
