LY3372689
Names
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
Identifiers
3D model (JSmol)
  • InChI=1S/C16H22FN5O3S/c1-9-6-12(24-8-14-19-11(3)25-21-14)4-5-22(9)7-13-15(17)20-16(26-13)18-10(2)23/h9,12H,4-8H2,1-3H3,(H,18,20,23)
    Key: FRVXHWNHGWUTQO-UHFFFAOYSA-N
  • CC(NC1=NC(F)=C(CN2CC[C@H](OCC3=NOC(C)=N3)C[C@@H]2C)S1)=O
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

  1. ↑ "LY3372689". www.alzforum.org.
  2. ↑ Shcherbinin, Sergey; Kielbasa, William; Dubois, Susan; Lowe, Stephen L; Phipps, Krista M; Tseng, James; Kevin, Donnelly B; Natanegara, Fanni; Warner, Susan; Dreyfus, Nicolas; Lindsay-Scott, Peter; Hawk, Mai Khanh; McDonald, Nicholas; Zhang, Xiaoyu; Gilmore, Julie A; Biglan, Kevin; Mergott, Dustin J; Russell, David; Gunn, Roger N; Constantinescu, Cristian; Nuthall, Hugh Norman; Collins, Emily C (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. S2CID 227501893.
  3. ↑ "Assessment of Safety, Tolerability, and Efficacy of LY3372689 in Early Symptomatic Alzheimer's Disease". clinicaltrials.gov. 22 March 2022. Retrieved 31 March 2022.
  4. ↑ "A Study of LY3372689 to Assess the Safety, Tolerability, and Efficacy in Participants With Alzheimer's Disease". Retrieved 31 March 2022.
  5. ↑ Krietsch Boerner, Leigh (25 March 2022). "Hybrid meeting divulges structures of drug candidates". Chemical & Engineering News. ISSN 0009-2347.
  6. ↑ 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". Retrieved 31 March 2022.


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