570398-18-4Relevant articles and documents
Deuterated Vistusertib compound and use thereof
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Paragraph 0089-0095, (2019/11/14)
The invention discloses a compound shown in a formula (I) (please see the specification for the formula I) or an optical isomer of the compound, a pharmaceutically acceptable salt, an aquo-complex ora solvate, wherein, R1-R29 is respectively and independe
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.
5-CHLORO-2-DIFLUOROMETHOXYPHENYL PYRAZOLOPYRIMIDINE COMPOUNDS, COMPOSITIONS AND METHODS OF USE THEREOF
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Paragraph 0895, (2015/12/05)
Compounds of Formula (00A) and methods of use as Janus kinase inhibitors are described herein.
A facile synthetic route to diazepinone derivatives via ring closing metathesis and its application for human cytidine deaminase inhibitors
Kim, Minkyoung,Gajulapati, Kondaji,Kim, Chorong,Jung, Hwa Young,Goo, Jail,Lee, Kyeong,Kaur, Navneet,Kang, Hyo Jin,Chung, Sang J.,Choi, Yongseok
supporting information, p. 11443 - 11445 (2013/01/15)
A variety of diazepinone derivatives were prepared from α-amino acids and amino alcohols by a new synthetic methodology based on ring closing metathesis as a key step. The diazepinones were coupled with ribose derivatives to afford novel diazepinone nucleosides. Among them, (4R)-1-ribosyl-4-methyl-3, 4-dihydro-1H-1,3-diazepin-2(7H)-one (3) showed a potent inhibitory effect (Ki = 145.97 ± 4.87 nM) against human cytidine deaminase.
INHIBITORS OF JANUS KINASES
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Page/Page column 123-124, (2009/01/23)
The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2) and PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3 TYK2 and PDK1 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer.
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.