Chemistry:LY3372689
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| IUPAC name
N-[4-fluoro-5-[[2-methyl-4-[(5-methyl-1,2,4-oxadiazol-3-yl)methoxy]piperidin-1-yl]methyl]-1,3-thiazol-2-yl]acetamide
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| Identifiers | |
3D model (JSmol)
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PubChem CID
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| Properties | |
| C16H22FN5O3S | |
| Molar mass | 383.44 g·mol−1 |
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa). | |
| Infobox references | |
LY3372689 is a drug candidate molecule under investigation to treat Alzheimer's disease. It targets the enzyme O-GlcNAcase.[1] Its result is to reduce formation of tau protein tangles.
A molecule containing radioactive fluorine was used with a PET scan to show that LY3372689 binds in the human brain.[2]
Eli Lilly and Company is recruiting subjects for a clinical trial.[3] Some hospitals in Australia: St Vincent's Hospital, Sydney Hornsby Ku-Ring-Gai Hospital, The Prince Charles Hospital, The Queen Elizabeth Hospital, Adelaide, Box Hill Hospital, and Delmont Private Hospital are involved.[4] Results of the trial are expected by June 2024.[5]
Chemical
The molecule contains three rings: thiazole, piperidine and oxadiazole. Other functional groups included are an ether, acetamide, and a fluoride.[6]
References
- ↑ "LY3372689". https://www.alzforum.org/therapeutics/ly3372689.
- ↑ Shcherbinin, Sergey; Kielbasa, William; Dubois, Susan; Lowe, Stephen L; Phipps, Krista M; Tseng, James; Kevin, Donnelly B; Natanegara, Fanni et al. (December 2020). "Brain target occupancy of LY3372689, an inhibitor of the O-GlcNAcase (OGA) enzyme: Translation from rat to human: Neuroimaging / evaluating treatments". Alzheimer's & Dementia 16 (S4). doi:10.1002/alz.040558.
- ↑ "Assessment of Safety, Tolerability, and Efficacy of LY3372689 in Early Symptomatic Alzheimer's Disease". clinicaltrials.gov. 22 March 2022. https://clinicaltrials.gov/ct2/show/NCT05063539.
- ↑ "A Study of LY3372689 to Assess the Safety, Tolerability, and Efficacy in Participants With Alzheimer's Disease". https://www.australianclinicaltrials.gov.au/anzctr/trial/NCT05063539.
- ↑ Krietsch Boerner, Leigh (25 March 2022). "Hybrid meeting divulges structures of drug candidates". Chemical & Engineering News. ISSN 0009-2347. https://cen.acs.org/acs-news/acs-meeting-news/Hybrid-meeting-divulges-structures-drug-candidates/100/web/2022/03.
- ↑ Dreyfus, Nicolas Jacques Francois; Lindsay-Scott, Peter James (2 August 2018). "N-[4-Fluoro-5-[[(2S,4S)-2-Methyl-4-[(5-Methyl-1,2,4-Oxadiazol-3-Yl)methoxy-1-Piperidyl]methyl]thiazol-2-Yl]acetamide as Oga Inhibitor"] (in en). https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2018140299&_cid=P12-L1ERBN-23050-1.
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