20173-49-3Relevant articles and documents
IMPROVED METHODS, KITS, COMPOSITIONS AND DOSING REGIMENS FOR THE USE OF HETEROCYCLIC INHIBITORS OF ERK1 AND ERK2
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Page/Page column 125, (2021/05/07)
The present application provides improved compositions, methods, kits and dosing regimens for the use of heterocyclic compounds and pharmaceutically acceptable salts, prodrugs, solvates, hydrates, or stereoisomers thereof. These compositions, methods, kit
C-H Pyridonation of (Hetero-)Arenes by Pyridinium Radical Cations
Hillenbrand, Julius,Ham, Won Seok,Ritter, Tobias
supporting information, p. 5363 - 5367 (2019/09/06)
Pyridones are important heteroaromatic scaffolds found in natural products and pharmaceuticals and are, therefore, of major interest in organic synthetic chemistry. Here we report the first C-H pyridonation of unactivated (hetero-)arenes, providing a methodology to directly access N-aryl-2- and 4-pyridones. Generation of pyridinium radical cations through single-electron reduction allows for the synthesis of pyridones on structurally complex molecules.
2-hydroxy-4-amino-5-picoline heterocyclic compounds
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Paragraph 0025-0029, (2017/01/23)
The invention discloses a 2-hydroxy-4-amino-5-methylpyridine heterocyclic compound which can be used as an intermediate for synthesizing an omeprazole compound. The invention further discloses a synthesis method of a 2-hydroxy-4-amino-5-methylpyridine heterocyclic compound. The synthesis method comprises four steps of synthesis of 2-chloro-5-methylpyridine nitrogen oxide, synthesis of 2-chloro-4-nitro-5-methylpyridine nitrogen oxide, synthesis of 2-chloro-4-amino-5-methylpyridine and synthesis of 2-hydroxy-4-amino-5-methylpyridine. The synthesis method of the 2-hydroxy-4-amino-5-methylpyridine heterocyclic compound disclosed by the invention is simple, reaction raw materials are low in price, and a synthesis route is environment-friendly.
HETEROCYCLIC INHIBITORS OF ERK1 AND ERK2 AND THEIR USE IN THE TREATMENT OF CANCER
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Paragraph 0530-0531, (2017/01/02)
The present application provides novel heterocyclic compounds and pharmaceutically acceptable salts thereof. Also provided are methods for preparing these compounds. These compounds are useful for inhibiting ERK1/2. By administering to a patient in need a
Fluorescence polarization for the evaluation of small-molecule inhibitors of PCAF BRD/Tat-AcK50 association
Hu, Ping,Wang, Xinghui,Zhang, Baiqun,Zhang, Shuai,Wang, Qiang,Wang, Zhiyong
supporting information, p. 928 - 931 (2014/05/20)
A fluorescence polarization competitive assay was developed to efficiently screen and evaluate inhibitors of PCAF bromodomain/Tat-AcK50 protein-peptide interaction. A series of pyridine 1-oxide derivatives were synthesized and evaluated. Some of the novel
NOVEL 6-ARYLAMINO PYRIDONE SULFONAMIDES AND 6-ARYLAMINO PYRAZINONE SULFONAMIDES AS MEK INHIBITORS
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Page/Page column 50-51, (2010/12/31)
The invention provides novel substituted 6-arylamino pyridone sulfonamides and 6 arylamino pyrazinone sulfonamides represented by Formula I, or a pharmaceutically acceptable salt, solvate, polymorph, ester, tautomer or prodrug thereof, and a composition comprising these compounds. The compounds provided can be used as inhibitors of MEK and are useful in the treatment of inflammatory diseases, cancer and other hyperproliferative diseases. The invention further provides a method of treatment for inflammatory diseases, cancer and other hyperproliferative diseases in mammals, especially humans
Synthesis of heteroaryl-fused pyrazoles as P38 kinase inhibitors
Abbot, Sarah C.,Billedeau, Roland J.,Dewdney, Nolan J.,Gabriel, Tobias,Goldstein, David M.,McCaleb, Kristen L.,Soth, Michael,Trejo-Martin, Teresa Alejandra,Zecic, Hasim
experimental part, p. 2811 - 2826 (2010/04/25)
The synthesis of pyrazolo-pyridine, pyrimidine, pyrazine and pyridazine heterocycles is described. In addition, we report the utilization of 2,4-difluorophenoxide as a leaving group, to facilitate formation of the desired pyrazole adducts.
Probing integrin selectivity: rational design of highly active and selective ligands for the α5β1 and αvβ3 integrin receptor
Heckmann, Dominik,Meyer, Axel,Marinelli, Luciana,Zahn, Grit,Stragies, Roland,Kessler, Horst
, p. 3571 - 3574 (2008/03/12)
(Chemical Equation Presented) Try and fit in: A strategy for the rational design of α5β1 ligands for the purpose of lead generation and biochemical studies on integrin selectivity is based α5β1 homology modeling. Ligand 1 can bind α5β1 with activities in
FUSED PYRAZOLE AS p38 MAP KINASE INHIBITORS
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Page/Page column 43, (2008/06/13)
Fused pyrazoles effective as p38 MAP kinase inhibitors, methods of making the compounds, and methods of using the compounds for treatment of p38 MAP kinase-mediated diseases.
PYRIDINE DERIVATIVES AND THEIR USE AS MEDICAMENTS FOR TREATING DISEASES RELATED TO MCH RECEPTOR
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Page/Page column 54, (2010/10/20)
The present invention encompasses novel substituted pyridine compounds of Formula (I), which act as MCH receptor antagonists. These compositions and pharmaceutical compositions thereof are useful in the prophylaxis or treatment of improving memory function, sleeping and arousal, anxiety, depression, mood disorders, seizure, obesity, diabetes, appetite and eating disorders, cardiovascular disease, hypertension, dyslipidemia, myocardial infarction, binge eating disorders including bulimia, anorexia, mental disorders including manic depression, schizophrenia, delirium, dementia, stress, cognitive disorders, attention deficit disorder, substance abuse disorders and dyskinesias including Parkinson's disease, epilepsy, and addiction.