954133-47-2

Upstream product

• 570398-22-0 (R)-4-(4-methoxybenzyl)-5-methylmorpholin-3-one 
• 86941-39-1 (R,E)-2-((4-methoxybenzylidene)amino)propan-1-ol 
• 123-11-5 4-methoxy-benzaldehyde 
• 570398-17-3 (R)-2-((4-methoxybenzyl)amino)propan-1-ol 
• 1445590-35-1 (R)-2-bromo-N-(1-hydroxypropan-2-yl)-N-(4-methoxybenzyl)acetamide 

Downstream Products

• 953780-78-4 (3R)-3-methylmorpholine hydrochloride 
• 1445589-63-8 methyl ((S)-3-hydroxy-1-((S)-2-(5-(4-(2-((1S,2S)-2-((R)-3-methylmorpholine-4-carbonyl)cyclopentyl)-1H-imidazol-5-yl)-[1,1'-biphenyl]-4-yl)-1H-imidazol-2-yl)pyrrolidin-1-yl)-1-oxopropan-2-yl)carbamate 
• 1445590-34-0 ((1,2-trans)-2-(5-(4-bromophenyl)-1H-imidazol-2-yl)cyclobutyl)((R)-3-methylmorpholino)methanone 
• 1445590-40-8 ((R)-3-methylmorpholino)((1,2-trans)-2-(5-(4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl)-1H-imidazol-2-yl)cyclobutyl)methanone 
• 74572-04-6 (3R)-3-methylmorpholine 
• 1445591-17-2 (1R,2R)-2-((R)-3-methylmorpholine-4-carbonyl)cyclohexanecarboxylic acid 
• 1445590-45-3 ((1R,2R)-2-(5-(4-bromophenyl)-1H-imidazol-2-yl)cyclohexyl)((R)-3-methylmorpholino)methanone 
• 1445590-70-4 ((1S,2S)-2-(5-(4-bromophenyl)-1H-imidazol-2-yl)cyclopentyl)((R)-3-methylmorpholino)methanone 
• 1445590-41-9 ((1R,2R)-2-(5-(4-bromophenyl)-1H-imidazol-2-yl)cyclopentyl)((R)-3-methylmorpholino)methanone 
• 1445590-77-1 ((R)-3-methylmorpholino)((1R,2R)-2-(5-(4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl)-1H-imidazol-2-yl)cyclopentyl)methanone 
• 1445590-83-9 ((7R,8R)-8-(5-(4-bromophenyl)-1H-imidazol-2-yl)-1,4-dithiaspiro[4.4]nonan-7-yl)((R)-3-methylmorpholino)methanone 
• 1445589-06-9 (S)-tert-butyl 2-(5-(4-(2-((1S,2S)-2-((R)-3-methylmorpholine-4-carbonyl)cyclopentyl)-1H-imidazol-5-yl)-[1,1'-biphenyl]-4-yl)-1H-imidazol-2-yl)pyrrolidine-1-carboxylate 
• 1445597-10-3 methyl ((S)-1-((2S,4S)-4-methoxy-2-(5-(4-(2-((1R,2R)-2-((R)-3-methylmorpholine-4-carbonyl)cyclopentyl)-1H-imidazol-5-yl)-[1,1'-biphenyl]-4-yl)-1H-imidazol-2-yl)pyrrolidin-1-yl)-3-methyl-1-oxobutan-2-yl)carbamate 
• 1445590-87-3 ((1R,2R)-2-(5-(4-bromophenyl)-1H-imidazol-2-yl)-4-methoxycyclopentyl)((R)-3-methylmorpholino)methanone 

Relevant academic research and scientific papers

Discovery of novel 2-(alkylmorpholin-4-yl)-6-(3-fluoropyridin-4-yl)-pyrimidin-4(3H)-ones as orally-active GSK-3β inhibitors for Alzheimer's disease

We herein describe the results of further evolution of GSK-3β inhibitors for Alzheimer's disease from our promising compounds with in vivo tau phosphorylation inhibitory activity by oral administration. Introduction of a low alkyl group instead of the phenyl group at the 3-position of the morpholine moiety aiming to improve pharmacokinetic profiles resulted in potent low molecular weight GSK-3β inhibitors with good in vitro pharmacokinetic profiles, which also showed in vivo tau phosphorylation inhibitory activity by oral administration. Effect of the stereochemistry of the alkyl moiety is also discussed using docking models.

NOVEL HEPATITIS C VIRUS INHIBITORS

The invention provides compounds of formula (I): wherein Rings A and A' are independently 5-membered optionally substituted aromatic heterocycles; Q is C(=O)NR1R1' or formula U is C(R4)2, O, S, S(=O)2, C(R4)2C(R4)2, CH2O, OCH2, CH2S, SCH2, CH2S(=O)2, S(=O)CH2 or C=C(Ru )2; X is CH2, CHR12, CR12R12, O, S, S(=O)2 or NRx; m is 0, 1, 2 or 3; n is 0, 1, 2 or 3; the other variables are as defined in the claims, which are of use in the treatment or prophylaxis of hepatitis C virus infection, and related aspects.

2-(CYCLIC AMINO)-PYRIMIDONE DERIVATIVES AS TPK1 INHIBITORS

A compound represented by the formula (I), an optically active isomer thereof, or a pharmaceutical acceptable salt thereof (I) wherein R2 represents a hydrogen or the like; R3 represents methyl group or the like; R20 represents a halogen atom or the like; q represents an integer of 0 to 3; Z represent nitrogen atom, CH, or the like; R4 represents hydrogen or the like; R5 represents hydrogen or the like; R6 represents a substituted alkyloxy and the like; p represents an integer of 0 to 3; X represents bond, CH2, oxygen atom, NH, or the like; any one or more of R5 and R6, R5 and R4, R6 and R4, X and R5, X and R4, X and R6, and R6 and R6 may combine to each other to form a ring, 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).