198477-89-3Relevant academic research and scientific papers
Pd-Catalysed direct C(sp2)-H fluorination of aromatic ketones: Concise access to anacetrapib
Wu, Qiuzi,Mao, Yang-Jie,Zhou, Kun,Wang, Shuang,Chen, Lei,Xu, Zhen-Yuan,Lou, Shao-Jie,Xu, Dan-Qian
supporting information, p. 4544 - 4547 (2021/05/17)
The Pd-cataylsed direct ortho-C(sp2)-H fluorination of aromatic ketones has been developed for the first time. The reaction features good regioselectivity and simple operations, constituting an alternative shortcut to access fluorinated ketones. A concise synthesis of anacetrapib has also been achieved by using late-stage C-H fluorination as a key step.
HETEROCYCLIC COMPOUNDS AND USES THEREOF
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Paragraph 0960; 0963; 0964, (2019/04/25)
Heterocyclic compounds as Wee1 inhibitors are provided. The compounds may find use as therapeutic agents for the treatment of diseases and may find particular use in oncology.
Design, Synthesis, and Pharmacological Evaluation of Novel Multisubstituted Pyridin-3-amine Derivatives as Multitargeted Protein Kinase Inhibitors for the Treatment of Non-Small Cell Lung Cancer
Zhu, Wei,Chen, Hui,Wang, Yulan,Wang, Jiang,Peng, Xia,Chen, Xianjie,Gao, Yinglei,Li, Chunpu,He, Yulong,Ai, Jing,Geng, Meiyu,Zheng, Mingyue,Liu, Hong
, p. 6018 - 6035 (2017/08/02)
A novel series of pyridin-3-amine derivatives were designed, synthesized, and evaluated as multitargeted protein kinase inhibitors for the treatment of non-small cell lung cancer (NSCLC). Hit 1 was first disclosed by in silico screening against fibroblast
PYRIDOPYRAZINES AS ANTICANCER AGENTS
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Page/Page column 11-12, (2014/07/22)
The present invention relates to pyridopyrazine derivatives and solvates, hydrates and pharmaceutically acceptable salts thereof, the use of them in the prevention and/or the treatment of cancer diseases, as well as pharmaceutical compositions containing at least one of them as pharmaceutically active agent(s) together with pharmaceutically acceptable carrier, excipient and/or diluents, especially for the prevention and/or treatment of cancer diseases.˙
FUSED AMINODIHYDROPYRIMIDINE DERIVATIVE
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Paragraph 0202; 0203, (2013/08/28)
The present invention provides, for example, the following compound: wherein ring A is a substituted or unsubstituted carbocycle or a substituted or unsubstituted heterocycle, X1—X2═X3 is CR5—CR6═CRs
LONG CHAIN BASE SPHINGOSINE KINASE INHIBITORS
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Paragraph 0311; 0204; 0329, (2013/08/28)
The invention relates to inhibitors of sphingosine kinase enzymatic activity, compounds and pharmaceutical compositions that inhibit sphingosine kinase 1 and sphingosine kinase 2 (SphK1 and SphK2) enzymes and further relates to methods of treating diseases and disorders mediated by sphingosine 1 phosphate activity, comprising administering an effective amount of sphingosine kinase inhibitors.
Maximizing lipophilic efficiency: The use of Free-Wilson analysis in the design of inhibitors of acetyl-CoA carboxylase
Freeman-Cook, Kevin D.,Amor, Paul,Bader, Scott,Buzon, Leanne M.,Coffey, Steven B.,Corbett, Jeffrey W.,Dirico, Kenneth J.,Doran, Shawn D.,Elliott, Richard L.,Esler, William,Guzman-Perez, Angel,Henegar, Kevin E.,Houser, Janet A.,Jones, Christopher S.,Limberakis, Chris,Loomis, Katherine,McPherson, Kirk,Murdande, Sharad,Nelson, Kendra L.,Phillion, Dennis,Pierce, Betsy S.,Song, Wei,Sugarman, Eliot,Tapley, Susan,Tu, Meihua,Zhao, Zhengrong
supporting information; experimental part, p. 935 - 942 (2012/03/11)
This paper describes the design and synthesis of a novel series of dual inhibitors of acetyl-CoA carboxylase 1 and 2 (ACC1 and ACC2). Key findings include the discovery of an initial lead that was modestly potent and subsequent medicinal chemistry optimization with a focus on lipophilic efficiency (LipE) to balance overall druglike properties. Free-Wilson methodology provided a clear breakdown of the contributions of specific structural elements to the overall LipE, a rationale for prioritization of virtual compounds for synthesis, and a highly successful prediction of the LipE of the resulting analogues. Further preclinical assays, including in vivo malonyl-CoA reduction in both rat liver (ACC1) and rat muscle (ACC2), identified an advanced analogue that progressed to regulatory toxicity studies.
1,4 OXAZINES AS BACE1 AND/OR BACE2 INHIBITORS
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Page/Page column 55, (2012/08/07)
The present invention relates to 1,4 Oxazines of formula (I): having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the pre
Oxazine Derivatives and their Use in the Treatment of Neurological Disorders
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Page/Page column 43, (2012/07/14)
The invention relates to novel heterocyclic compounds of the formula in which all of the variables are as defined in the specification, in free form or in salt form, to their preparation, to their medical use and to medicaments comprising them.
