169297-84-1Relevant articles and documents
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
Fukunaga, Kenji,Sakai, Daiki,Watanabe, Kazutoshi,Nakayama, Kazuki,Kohara, Toshiyuki,Tanaka, Hiroshi,Sunada, Shinji,Nabeno, Mika,Okamoto, Masako,Saito, Ken-Ichi,Eguchi, Jun-Ichi,Mori, Akiko,Tanaka, Shinji,Inazawa, Keiko,Horikawa, Takashi
, p. 1086 - 1091 (2015/02/19)
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.
3-(Imidazolyl)-2-alkoxypropanoic acids
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, (2008/06/13)
Compounds according to formula (I) wherein n is 0-3, R1 is optionally substituted C1-6 alkyl, C2-6 alkenyl, or C2-6 alkynyl, Heterocycle, Aromatic heterocycle, Aryl or hydrogen and R2, R3, R4, R5, R6, R7, R8 and R9 are each independently selected from hydrogen and optionally substituted C1-6 alkyl, or R5 and R8 are an alkylene chain, are novel. They are useful in the treatment of thrombotic conditions and other pathologies associated with fibrin deposition.
Stereoselective Synthesis of Novel Methylene Ether Dipeptide Isosteres
Norman, Bryan H.,Kroin, Julian S.
, p. 4151 - 4154 (2007/10/02)
We have developed a versatile new synthesis of the Ψ pseudopeptides from N-protected 5-substituted morpholin-3-ones.This approach focuses on a stereoselective alkylation of the morpholin-3-ones.The resulting alkylation products were used in the synt
