503860-53-5

Usage

Uses

Used in Research Laboratories:
[4,4'-Bipyrimidin]-6(1H)-one,2,3-dihydro-1-me is used as a reagent in various chemical reactions for its unique structure and properties.
Used in Pharmaceutical Applications:
[4,4'-Bipyrimidin]-6(1H)-one,2,3-dihydro-1-me is used as a potential central nervous system depressant and sedative for its potential therapeutic uses.

Upstream product

• 64210-67-9 ethyl 3-oxo-3-(pyrimidin-4-yl)propanoate 
• 1093114-82-9 C₉H₁₀N₂O₃ 
• 598-52-7 1-(methyl)-thiourea 
• 2450-08-0 methyl pyrimidine-4-carboxylate 
• 3438-46-8 4-Methylpyrimidine 
• 31462-59-6 pyrimidine-4-carboxylic acid 

Downstream Products

• 503860-54-6 2-chloro-3-methyl-6-(pyrimidin-4-yl)-pyrimidine-4-one 
• 503860-57-9 UDA-680 

Relevant academic research and scientific papers

Discovery of Novel Tacrine-Pyrimidone Hybrids as Potent Dual AChE/GSK-3 Inhibitors for the Treatment of Alzheimer's Disease

Based on a multitarget strategy, a series of novel tacrine-pyrimidone hybrids were identified for the potential treatment of Alzheimer's disease (AD). Biological evaluation results demonstrated that these hybrids exhibited significant inhibitory activities toward acetylcholinesterase (AChE) and glycogen synthase kinase 3 (GSK-3). The optimal compound 27g possessed excellent dual AChE/GSK-3 inhibition both in terms of potency and equilibrium (AChE: IC50 = 51.1 nM; GSK-3β: IC50 = 89.3 nM) and displayed significant amelioration on cognitive deficits in scopolamine-induced amnesia mice and efficient reduction against phosphorylation of tau protein on Ser-199 and Ser-396 sites in glyceraldehyde (GA)-stimulated differentiated SH-SY5Y cells. Furthermore, compound 27g exhibited eligible pharmacokinetic properties, good kinase selectivity, and moderate neuroprotection against GA-induced reduction in cell viability and neurite damage in SH-SY5Y-derived neurons. The multifunctional profiles of compound 27g suggest that it deserves further investigation as a promising lead for the prospective treatment of AD.

2-(2-Phenylmorpholin-4-yl)pyrimidin-4(3H)-ones; A new class of potent, selective and orally active glycogen synthase kinase-3β inhibitors

A series of 2-(2-phenylmorpholin-4-yl)pyrimidin-4(3H)-ones was synthesized and examined for their inhibitory activity against glycogen synthase kinase-3β (GSK-3β). We found 21, 29 and 30 to possess potent in vitro GSK-3β inhibitory activity with good in vitro PK profiles. 21 demonstrated significant decrease of tau phosphorylation after oral administration in mice and excellent PK profiles.

3-[1,4]OXAZEPANE-4-PYRIMIDONE DERIVATIVES

A compound represented by the formula (I) or a pharmaceutically acceptable salt thereof: wherein Z represents nitrogen atom, C-F or the like; R1 represents a C1-C3 alkyl group; Y represents oxygen atom or N-R7; R2, R3, R4, R5, R6 and R7 each independently represents hydrogen atom, a C1-C6 alkyl group, or a group represented by the formula (II): which is used for preventive and/or therapeutic treatment of a disease caused by tau protein kinase 1 hyperactivity such as a neurodegenerative diseases (e.g. Alzheimer disease).

3-METHYL-2- ( (2S) -2- (4- (3-METHYL-L, 2, 4-0XADIAZ0L-5-YL) PHENYL) MORPHOLINO) -6- (PYRIMIDIN-4-YL) PYRIMIDIN-4 (3H) -ONE AS TAU PROTEIN KINASE INHIBITOR

A compound represented by the formula (I) or a pharmaceutically acceptable salt thereof: which is used for preventive and/or therapeutic treatment of a disease caused by abnormal activity of tau protein kinase 1 such as a neurodegenerative diseases (e.g.

6-PYRIMIDINYL-PYRIMID-2-ONE DERIVATIVE

A compound represented by the formula (I) or a pharmaceutically acceptable salt thereof: which is used for preventive and/or therapeutic treatment of a disease caused by abnormal activity of tau protein kinase 1 such as a neurodegenerative diseases (e.g.

PYRIMIDONE COMPOUNDS AS GSK-3 INHIBITORS

The invention relates to pyrimidone derivatives I having activity as GSK-3 inhibitors. The invention further relates to pharmaceutical compositions comprising such derivatives and uses thereof in treating certain disorders. Formula (I):

INTERMEDIATE COMPOUND FOR SYNTHESIZING PHARMACEUTICAL AGENT AND PRODUCTION METHOD THEREOF

The present invention relates to a production method of an optically active morpholine compound represented by the formula 10, which includes the following steps: wherein each symbol is as defined in the specification. The present invention also relates t

2, 3, 6-TRISUBSTITUTED-4-PYRIMIDONE DERIVATIVES

A pyrimidone derivative having tau protein kinase 1 inhibitory activity which is represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof; useful for prventive and/or therapeutic treatment of diseass such as neurodegenerative diseases (e.g. Alzheimer disease); wherein Q represents CH or nitrogen atom; R represents a C1-C12 alkyl group; the ring of Formula (I): represents piperazine ring or piperidine ring; each X independently represents a C1-C8 alkyl group, an optionally partially hydrogenated C6-C10 aryl ring, an indan ring or the like; m represents an integer of 1 to 3; each Y independently represents a halogen atom, a hydroxy group, a cyano group, a C1-C6 alkyl group or the like; n represents an integer of 0 to 8; when X and Y or two Y groups are attached on the same carbon atom, they may combine to each other to form a C2-C6 alkylene group.

3-SUBSTITUTED-4-PYRIMIDONE DERIVATIVES

A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof useful as a tau protein kinase 1 inhibitor:wherein X represents CH or nitrogen atom; R1 represents a C?1#191-C?12#191 alkyl group wh

Substituted pyrimidinyl-2-(diaza-bicyclo-alkyl)-pyrimidone derivatives

The invention relates to a 2-(diaza-bicyclo-alkyl)-pyrimidone derivative represented by formula (I) or a salt thereof: wherein:R1 represents a hydrogen atom, a C1-6 alkyl group or a halogen atom;R2 represents a hydrogen atom, a C1-6