2016-00-4Relevant academic research and scientific papers
PYRAZOLOPYRIMIDINE DERIVATIVES AND THE COMPOSITIONS AND METHODS OF TREATMENT REGARDING THE SAME
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Paragraph 514; 515, (2018/01/17)
The present disclosure is directed to pyrazolo[1,5-a]pyrimidine compounds of formula (I), pharmaceutical compositions thereof and methods for modulating or activating a Parkin ligase The present disclosure is also directed to methods of treating and/or reducing the incidence of diseases or conditions related to the activation of Parkin ligase. R21, R22, R23, R24 and R25 are as defined herein.
Heterocyclic derivative and pharmaceutical composition comprising the same
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Page/Page column 225; 226, (2016/01/10)
The present invention provides novel compounds having a P2X3 and/or P2X2/3 receptor antagonistic effect. A pharmaceutical composition having a P2X3 and/or P2X2/3 receptor antagonistic effect comprising a compoun
Lewis base catalyzed asymmetric hydrosilylation of α-substituted β-enamino esters: Facile access to enantioenriched β2-amino esters via dynamic kinetic resolution
Shu, Chang,Hu, Xiao-Yan,Li, Shuai-Shuai,Yuan, Wei-Cheng,Zhang, Xiao-Mei
supporting information, p. 1879 - 1882 (2014/08/18)
A chiral Lewis base organocatalyzed asymmetric hydrosilylation of α-substituted β-enamino esters is presented. The reactions proceeded through dynamic kinetic resolution to afford various enantioenriched β2-amino esters with high yields (up to
Substituted 3-benzylcoumarins as allosteric MEK1 inhibitors: Design, synthesis and biological evaluation as antiviral agents
Wang, Chao,Zhang, Hao,Xu, Fengrong,Niu, Yan,Wu, Yun,Wang, Xin,Peng, Yihong,Sun, Jing,Liang, Lei,Xu, Ping
, p. 6057 - 6091 (2013/06/27)
In order to find novel antiviral agents, a series of allosteric MEK1 inhibitors were designed and synthesized. Based on docking results, multiple optimizations were made on the coumarin scaffold. Some of the derivatives showed excellent MEK1 binding affinity in the appropriate enzymatic assays and displayed obvious inhibitory effects on the ERK pathway in a cellular assay. These compounds also significantly inhibited virus (EV71) replication in HEK293 and RD cells. Several compounds showed potential as agents for the treatment of viral infective diseases, with the most potent compound 18 showing an IC 50 value of 54.57 nM in the MEK1 binding assay.
NOVEL HETEROCYCLIC DERIVATIVES AND PHARMACEUTICAL COMPOSITION CONTAINING SAME
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Paragraph 0346; 0347, (2013/06/28)
The present invention provides novel compounds having a P2X3 and/or P2X2/3 receptor antagonistic effect. A pharmaceutical composition having a P2X3 and/or P2X2/3 receptor antagonistic effect comprising a compoun
PYRIMIDINONE COMPOUNDS FOR USE IN THE TREATMENT OF DISEASES OR CONDITIONS MEDIATED BY LP - PLA2
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Page/Page column 39, (2012/06/30)
The present invention relates to novel compounds that inhibit Lp-PLA2 activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease, and/or diabetic macular edema (I).
Synthesis and pharmacological evaluation of thieno[2,3-b]pyridine derivatives as novel c-Src inhibitors
Pevet, Isabelle,Brulé, Cédric,Tizot, André,Gohier, Arnaud,Cruzalegui, Francisco,Boutin, Jean A.,Goldstein, Solo
experimental part, p. 2517 - 2528 (2011/06/11)
Among the recently investigated targets for cancer therapy is the c-Src non-receptor tyrosine kinase. Indeed research around deregulated activity of this enzyme has proven its role in tumor progression, while the beneficial effects of c-Src inhibitors in several pathological models has also been demonstrated. We report here the preparation and pharmacological profile of a novel series of c-Src inhibitors that was elaborated around a 3-amino-thieno[2,3-b]pyridine discovered during an HTS campaign. c-Src enzyme inhibition and c-Src inhibition were investigated in a series of related compounds derived from the initial hit. Molecular modeling as well as X-ray studies on one active compound allowed us to hypothesize on ligand orientation and interactions within the ATP hydrophobic pocket. Design and synthesis of structural analogs then led to new ligands possessing quite efficient enzymatic and c-Src inhibition. The structure-activity elements disclosed in this study shed light on the role played by substituents on the thienopyridine ring as well as the impact of other aromatic moieties in the molecule when interacting with the enzyme.
REGULATION OF PROTEIN SYNTHESIS
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Page/Page column 48, (2010/06/19)
A composition and method for inhibiting proliferation of a tumor cell compared to a non-tumor cell. Also described are methods of screening for a composition that inhibits cap-dependent translation compared to cap-independent translation of proteins
[1,2,4]THIADIAZINE 1,1-DIOXIDE COMPOUNDS
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Page/Page column 61, (2009/12/24)
The invention is directed to [1,2,4]thiadiazine 1,1-dioxide compounds and pharmaceutical compositions containing such compounds that are useful in treating infections by hepatitis C virus.
PROCESS FOR PRODUCING OPTICALLY ACTIVE 3-HYDROXYPROPIONIC ESTER DERIVATIVE
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Page/Page column 9, (2010/02/13)
The present invention is to provide a process for simply producing an optically active 3-hydroxypropionic ester derivative useful as a medicament intermediate from an inexpensive material. More specifically, the present invention is directed to a process for producing an optically active 3-hydroxypropionic ester derivative comprising reacting an acetic ester derivative available at low cost with a base and a formic ester, thereby converting the acetic ester derivative into a 2-formylacetic ester derivative, and thereafter, stereospecifically reducing the formyl group of the derivative by use of an enzymatic source capable of stereoselectively reducing the formyl group of the derivative.
