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893440-50-1Relevant academic research and scientific papers
Synthetic method of 2-methoxyl-3-amino-5-pyridineboronic acid pinacol ester and intermediate thereof
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, (2019/04/04)
The invention relates to a synthetic method of 2-methoxyl-3-amino-5-pyridineboronic acid pinacol ester and an intermediate thereof. Specifically, the synthetic method is characterized in that the 2-methoxyl-3-amino-5-pyridineboronic acid pinacol ester is obtained by the steps of taking 2-methoxylnicotinic acid as a starting raw material, halogenating, degrading, deprotecting and coupling. The method disclosed by the invention has the advantages of being short in synthesis route, simple, convenient, low in economic cost and highly suitable for industrial production.
Discovery of Pyridopyrimidinones as Potent and Orally Active Dual Inhibitors of PI3K/mTOR
Yu, Tao,Li, Ning,Wu, Chengde,Guan, Amy,Li, Yi,Peng, Zhengang,He, Miao,Li, Jie,Gong, Zhen,Huang, Lei,Gao, Bo,Hao, Dongling,Sun, Jikui,Pan, Yan,Shen, Liang,Chan, Chichung,Lu, Xiulian,Yuan, Hongyu,Li, Yongguo,Li, Jian,Chen, Shuhui
supporting information, p. 256 - 261 (2018/03/21)
The identification and lead optimization of a series of pyridopyrimidinone derivatives are described as a novel class of efficacious dual PI3K/mTOR inhibitors, resulting in the discovery of 31. Compound 31 exhibited high enzyme activity against PI3K and mTOR, potent suppression of Akt and p70s6k phosphorylation in cell assays, and good pharmacokinetic profile. Furthermore, compound 31 demonstrated in vivo efficacy in a PC-3M tumor xenograft model.
Discovery of Potent, Efficient, and Selective Inhibitors of Phosphoinositide 3-Kinase δ through a Deconstruction and Regrowth Approach
Barton, Nick,Convery, Máire,Cooper, Anthony W. J.,Down, Kenneth,Hamblin, J. Nicole,Inglis, Graham,Peace, Simon,Rowedder, James,Rowland, Paul,Taylor, Jonathan A.,Wellaway, Natalie
supporting information, p. 11061 - 11073 (2019/01/08)
A deconstruction of previously reported phosphoinositide 3-kinase δ (PI3Kδ) inhibitors and subsequent regrowth led to the identification of a privileged fragment for PI3Kδ, which was exploited to deliver a potent, efficient, and selective lead series with a novel binding mode observed in the PI3Kδ crystal structure.
Synthesis and profiling of a 3-aminopyridin-2-one-based kinase targeted fragment library: Identification of 3-amino-5-(pyridin-4-yl)pyridin-2(1H)-one scaffold for monopolar spindle 1 (MPS1) and Aurora kinases inhibition
Fearon, Daren,Westwood, Isaac M.,van Montfort, Rob L.M.,Bayliss, Richard,Jones, Keith,Bavetsias, Vassilios
supporting information, p. 3021 - 3029 (2018/05/25)
Screening a 3-aminopyridin-2-one based fragment library against a 26-kinase panel representative of the human kinome identified 3-amino-5-(1-methyl-1H-pyrazol-4-yl)pyridin-2(1H)-one (2) and 3-amino-5-(pyridin-4-yl)pyridin-2(1H)-one (3) as ligand efficient inhibitors of the mitotic kinase Monopolar Spindle 1 (MPS1) and the Aurora kinase family. These kinases are well recognised as attractive targets for therapeutic intervention for treating cancer. Elucidation of the binding mode of these fragments and their analogues has been carried out by X-ray crystallography. Structural studies have identified key interactions with a conserved lysine residue and have highlighted potential regions of MPS1 which could be targeted to improve activity and selectivity.
Indazole derivatives for use in the treatment of influenza virus infection
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, (2016/06/01)
The present invention is directed to compounds for use in the treatment or prevention of influenza virus infection.
Optimization of Novel Indazoles as Highly Potent and Selective Inhibitors of Phosphoinositide 3-Kinase δ for the Treatment of Respiratory Disease
Down, Kenneth,Amour, Augustin,Baldwin, Ian R.,Cooper, Anthony W.J.,Deakin, Angela M.,Felton, Leigh M.,Guntrip, Stephen B.,Hardy, Charlotte,Harrison, Zo? A.,Jones, Katherine L.,Jones, Paul,Keeling, Suzanne E.,Le, Joelle,Livia, Stefano,Lucas, Fiona,Lunniss, Christopher J.,Parr, Nigel J.,Robinson, Ed,Rowland, Paul,Smith, Sarah,Thomas, Daniel A.,Vitulli, Giovanni,Washio, Yoshiaki,Hamblin, J. Nicole
supporting information, p. 7381 - 7399 (2015/10/05)
Optimization of lead compound 1, through extensive use of structure-based design and a focus on PI3Kδ potency, isoform selectivity, and inhaled PK properties, led to the discovery of clinical candidates 2 (GSK2269557) and 3 (GSK2292767) for the treatment of respiratory indications via inhalation. Compounds 2 and 3 are both highly selective for PI3Kδ over the closely related isoforms and are active in a disease relevant brown Norway rat acute OVA model of Th2-driven lung inflammation.
3-(PYRAZOLYL)-1H-PYRROLO[2,3-b]PYRIDINE DERIVATIVES AS KINASE INHIBITORS
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Page/Page column 43, (2014/01/18)
The present application relates to novel 3-(pyrazolyl)-lH-pyrrolo[2,3-b]pyridine derivatives of formula (I), as protein kinase inhibitors. The invention particularly relates to compounds of formula (I), preparation of compounds and pharmaceutical compositions thereof. The invention further relates to pharmaceutically acceptable salts and compositions comprising the said novel 3-(pyrazolyl)-lH-pyrrolo[2,3-b]pyridine derivatives and their use in the treatment of various disorders.
Discovery of selective small molecule type III phosphatidylinositol 4-kinase alpha (PI4KIIIα) inhibitors as anti hepatitis C (HCV) agents
Leivers, Anna L.,Tallant, Matthew,Shotwell, J. Brad,Dickerson, Scott,Leivers, Martin R.,McDonald, Octerloney B.,Gobel, Jeff,Creech, Katrina L.,Strum, Susan L.,Mathis, Amanda,Rogers, Sabrinia,Moore, Chris B.,Botyanszki, Janos
, p. 2091 - 2106 (2014/04/03)
Hepatitis C virus (HCV) assembles many host cellular proteins into unique membranous replication structures as a prerequisite for viral replication, and PI4KIIIα is an essential component of these replication organelles. RNA interference of PI4KIIIα results in a breakdown of this replication complex and cessation of HCV replication in Huh-7 cells. PI4KIIIα is a lipid kinase that interacts with the HCV nonstructural 5A protein (NS5A) and enriches the HCV replication complex with its product, phosphoinositol 4-phosphate (PI4P). Elevated levels of PI4P at the endoplasmic reticulum have been linked to HCV infection in the liver of HCV infected patients.1 We investigated if small molecule inhibitors of PI4KIIIα could inhibit HCV replication in vitro. The synthesis and structure-activity relationships associated with the biological inhibition of PI4KIIIα and HCV replication are described. These efforts led directly to identification of quinazolinone 28 that displays high selectivity for PI4KIIIα and potently inhibits HCV replication in vitro.
PYRROLOTRIAZINONE DERIVATIVES AS PI3K INHIBITORS
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Page/Page column 85, (2014/05/07)
New pyrrolotriazinone derivatives having the chemical structure of formula (I) are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Phosphoinositide 3-Kinases (PI3Ks).
PYRROLOTRIAZINONE DERIVATIVES AS PI3K INHIBITORS
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Page/Page column 130, (2014/05/07)
New pyrrolotriazinone derivatives having the chemical structure of formula (I), are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Phosphoinositide 3-Kinases (PI3Ks)
