807618-13-9Relevant academic research and scientific papers
Structure-Guided Discovery of Aminoquinazolines as Brain-Penetrant and Selective LRRK2 Inhibitors
Acton, John J.,Adpressa, Donovon,Ardolino, Michael J.,Bennett, David Jonathan,Chau, Ryan W.,Ciaccio, Paul J.,Dimauro, Erin F.,Faltus, Robert,Fell, Matthew J.,Fuller, Peter H.,Gulati, Anmol,Hegde, Laxminarayan G.,Johnson, Rebecca E.,Kattar, Solomon D.,Kennedy, Matthew E.,Keylor, Mitchell H.,Lesburg, Charles A.,Lin, Shishi,Liu, Ping,Margrey, Kaila A.,McMinn, Spencer E.,Morriello, Gregori J.,Neelamkavil, Santhosh,Nogle, Lisa,Otte, Karin M.,Palte, Rachel L.,Piesvaux, Jennifer,Pio, Barbara,Poremba, Kelsey E.,Simov, Vladimir,Su, Jing,Wood, Harold B.,Woodhouse, Janice D.,Xiong, Tina,Yan, Xin,Zarate, Cayetana
supporting information, p. 838 - 856 (2022/01/20)
The leucine-rich repeat kinase 2 (LRRK2) protein has been genetically and functionally linked to Parkinson's disease (PD), a disabling and progressive neurodegenerative disorder whose current therapies are limited in scope and efficacy. In this report, we
N-(HETEROARYL) QUINAZOLIN-2-AMINE DERIVATIVES AS LRRK2 INHIBITORS, PHARMACEUTICAL COMPOSITIONS, AND USES THEREOF
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Page/Page column 47, (2021/04/30)
The present invention is directed to substituted certain N-(heteroaryl)quinazolin-2-amine derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein J, R3, and R4, are as defined herein, which are potent inhib
HETEROCYCLIC GLP-1 AGONISTS
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Page/Page column 141, (2021/11/06)
This disclosure relates to GLP-1 agonists of Formula (I): including pharmaceutically acceptable salts and solvates thereof, and pharmaceutical compositions including the same.
TRPML MODULATORS
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Paragraph 0480, (2021/06/26)
The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.
HETEROARYL COMPOUNDS FOR TREATING HUNTINGTON'S DISEASE
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Page/Page column 214, (2020/01/24)
The present description relates to compounds, forms, and pharmaceutical compositions thereof and methods of using such compounds, forms, or compositions thereof for treating or ameliorating Huntington's disease. In particular, the present description relates to substituted benzothiazole compounds of Formula (I) or (II), forms and pharmaceutical compositions thereof and methods of using such compounds, forms, or compositions thereof for treating or ameliorating Huntington's disease.
SHMT INHIBITORS AND USES THEREOF
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, (2018/06/30)
The present invention provides compounds, compositions thereof, and methods of using the same.
COMPOUNDS FOR TREATING HUNTINGTON'S DISEASE
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Page/Page column 90; 107; 108, (2019/01/06)
The present description relates to compounds, forms, and pharmaceutical compositions thereof and methods of using such compounds, forms, or compositions thereof for treating or ameliorating Huntington's disease. In particular, the present description relates to substituted bicyclic heteroaryl compounds of Formula (I), forms and pharmaceutical compositions thereof and methods of using such compounds, forms, or compositions thereof for treating or ameliorating Huntington's disease.
A preparation method of the midbody color Switzerland for Nepal
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Paragraph 0015; 0016, (2017/08/24)
The invention relates to a preparation method of ceritinib. The preparation method comprises the following steps: (1) reacting metal powder with N-t-butyloxycarboryl-4 iodine piperidine with a structural formula of SR-1 to generate a metal coupling agent with a structural formula of SR-2; (2) performing a coupling reaction on the metal coupling agent SR-2 and 1-bromo-5-isopropoxy-2-methyl-4-nitrobenzene to generate a compound SR-3; (3) performing hydrogenation reduction on the compound SR-3, and removing BOC amino protection to generate the ceritinib SR-4. According to the invention, a novel preparation method of the ceritinib is developed. The synthetic route is very short; the yield is high; raw materials can be easily obtained and are low in cost; reaction conditions are very mild and easy to control; therefore, the preparation method is suitable for large-scale industrial production.
5-[3-[PIPERIDIN-1-YL]-3-OXO-PROPYL]-IMIDAZOLIDINE-2,4-DIONE DERIVATIVES AS ADAMTS 4 AND 5 INHIBITORS FOR TREATING E.G. OSTEOARTHRITIS
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Paragraph 0209; 0210, (2018/01/15)
The present invention discloses 5-[3-[piperazin-l-yl]-3-oxo-propyl]-imidazolidine-2,4-dione derivatives according to Formula (I), wherein R1, R2, R3a, R3b, R6a, R6b, the subscript n and Cy are as defined herein. The present invention relates to compounds inhibiting ADAMTS 4 and 5 for the prophylaxis or treatment of inflammatory diseases or diseases involving degradation of cartilage or disruption of cartilage homeostasis, such as e.g. osteoarthritis.
Discovery of Phosphodiesterase 10A (PDE10A) PET Tracer AMG 580 to Support Clinical Studies
Hu, Essa,Chen, Ning,Kunz, Roxanne K.,Hwang, Dah-Ren,Michelsen, Klaus,Davis, Carl,Ma, Ji,Shi, Jianxia,Lester-Zeiner, Dianna,Hungate, Randall,Treanor, James,Chen, Hang,Allen, Jennifer R.
supporting information, p. 719 - 723 (2016/07/26)
We report the discovery of PDE10A PET tracer AMG 580 developed to support proof of concept studies with PDE10A inhibitors in the clinic. To find a tracer with higher binding potential (BPND) in NHP than our previously reported tracer 1, we implemented a surface plasmon resonance assay to measure the binding off-rate to identify candidates with slower washout rate in vivo. Five candidates (2-6) from two structurally distinct scaffolds were identified that possessed both the in vitro characteristics that would favor central penetration and the structural features necessary for PET isotope radiolabeling. Two cinnolines (2, 3) and one keto-benzimidazole (5) exhibited PDE10A target specificity and brain uptake comparable to or better than 1 in the in vivo LC-MS/MS kinetics distribution study in SD rats. In NHP PET imaging study, [18F]-5 produced a significantly improved BPND of 3.1 and was nominated as PDE10A PET tracer clinical candidate for further studies.
