Edelinontrine

Image may be NSFW.
Clik here to view.

Image may be NSFW.
Clik here to view.

Image may be NSFW.
Clik here to view.

Edelinontrine

CRD740, PF04447943, cas 1082744-20-4

6-[(3S,4S)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl]-1-(oxan-4-yl)-5H-pyrazolo[3,4-d]pyrimidin-4-one

• 7N969W8Y4O
• 6-((3S,4S)-4-Methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl)-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo(3,4-d)pyrimidin-4-one
• 6-[(3S,4S)-4-METHYL-1-(PYRIMIDIN-2-YLMETHYL)PYRROLIDIN-3-YL]-1-(OXAN-4-YL)-5H-PYRAZOLO[3,4-D]PYRIMIDIN-4-ONE
• 6-((3S,4S)-4-Methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl)-1-(tetrahydro-2H-pyran-4-yl)-1H-pyrazolo[3,4-d]pyrimidin-4(5H)-one

Edelinontrine (PF-04447943) is a potent inhibitor of human recombinant PDE9A (IC₅₀=12 nM) with >78-fold selectivity, respectively, over other PDE family members (IC₅₀>1000 nM).

Image may be NSFW.
Clik here to view.

PF-04447943 is a potent, selective brain penetrant PDE9 inhibitor (Ki of 2.8, 4.5 and 18 nM) for human, rhesus and rat recombinant PDE9 respectively and high selectivity for PDE9 versus PDEs1-8 and 10-11. PF-04447943 was being developed by Pfizer for the treatment of cognitive disorders. PF-04447943 attenuates a scopolamine-induced deficit in a novel rodent attention task. PF-04447943 enhances synaptic plasticity and cognitive function in rodents. PF-04447943 has completed Phase II clinical trials in subjects with mild to moderate AD in 2013 but this research was discontinued. Pfizer completes a phase I trial in Sickle cell anaemia.

SCHEME

SUDECHAIN

Image may be NSFW.
Clik here to view.

MAIN

Image may be NSFW.
Clik here to view.

Patent

WO2023114995  PFIZER

https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2023114995&_cid=P20-MB07JE-44537-1

PAPER

Journal of Medicinal Chemistry (2012), 55(21), 9045-9054 

PATENT

WO2008139293

https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2008139293&_cid=P20-MB07LY-46583-1

EXAMPLE 111

6-[(3S,4S)-4-methyl-1-(pyrimidin-2-ylmethyl)pyiτolidin-3-yl]-1-αetrahydro-2H- pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one

Image may be NSFW.
Clik here to view.

///////Edelinontrine, CRD740, PF04447943, CRD 740, PF 04447943, PHASE 1