940927-35-5Relevant academic research and scientific papers
Discovery of Novel Janus Kinase (JAK) and Histone Deacetylase (HDAC) Dual Inhibitors for the Treatment of Hematological Malignancies
Liang, Xuewu,Zang, Jie,Li, Xiaoyang,Tang, Shuai,Huang, Min,Geng, Meiyu,Chou, C. James,Li, Chunpu,Cao, Yichun,Xu, Wenfang,Liu, Hong,Zhang, Yingjie
, p. 3898 - 3923 (2019/04/25)
Concurrent inhibition of Janus kinase (JAK) and histone deacetylase (HDAC) could potentially improve the efficacy of the HDAC inhibitors in the treatment of cancers and resolve the problem of HDAC inhibitor resistance in some tumors. Here, a novel series
Synthesis of [11C]HG-10-102-01 as a new potential PET agent for imaging of LRRK2 enzyme in Parkinson's disease
Wang, Min,Gao, Mingzhang,Xu, Zhidong,Zheng, Qi-Huang
, p. 1351 - 1355 (2017/03/08)
The reference standard (4-((5-chloro-4-(methylamino)pyrimidin-2-yl)amino)-3-methoxyphenyl)(morpholino)methanone (HG-10-102-01) and its precursor (4-((5-chloro-4-(methylamino)pyrimidin-2-yl)amino)-3-hydroxyphenyl)(morpholino)methanone (desmethyl-HG-10-102-
Fluorine-18 and carbon-11 labeled radioligands for positron emission tomography (PET) imaging for LRRK2
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Page/Page column 71, (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
2-PHENYLAMINOPYRIMIDINE DERIVATIVES AS KINASE LRRK2 MODULATORS FOR THE TREATMENT OF PARKINSON'S DISEASE
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Page/Page column 55, (2013/06/27)
Specific Compounds of formula (I): or pharmaceutically acceptable salts thereof, wherein m, X, R, R2, R3, R, R6 and R7 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with LRRK2 receptor, such as Parkinson's disease.
2-(PHENYL OR PYRID-3-YL) AMINOPYRIMIDINE DERIVATIVES AS KINASE LRRK2 MODULATORS FOR THE TREATMENT OF PARKINSON'S DISEASE
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Page/Page column 45; 46, (2013/06/27)
Compounds of the formula (I), or pharmaceutically acceptable salts thereof, wherein m, n. X, R1, R2, R3, R4 and R5 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with LRRK2 receptor, such as Parkinson's disease.
PYRAZOLE AMINOPYRIMIDINE DERIVATIVES AS LRRK2 MODULATORS
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Page/Page column 35, (2013/11/19)
Pyrazole compounds that are modulators of LRRK2, methods of making the compounds, and methods for using the compounds for treatment of diseases associated with LRRK2 receptor, such as Parkinson's disease.
Brain penetrant LRRK2 inhibitor
Choi, Hwan Geun,Zhang, Jinwei,Deng, Xianming,Hatcher, John M.,Patricelli, Matthew P.,Zhao, Zheng,Alessi, Dario R.,Gray, Nathanael S.
supporting information, p. 658 - 662 (2013/01/14)
Activating mutations in leucine-rich repeat kinase 2 (LRRK2) are present in a subset of Parkinson's disease (PD) patients and may represent an attractive therapeutic target. Here, we report that a 2-anilino-4-methylamino-5- chloropyrimidine, HG-10-102-01
PYRAZOLE AMINOPYRIMIDINE DERIVATIVES AS LRRK2 MODULATORS
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Page/Page column 67, (2012/05/31)
Compounds of the formula (I), or pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3, R4 and R5 are as defined herein. Also disclosed are methods of making the compounds and using the com
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.
experimental part, 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.
