131747-45-0Relevant academic research and scientific papers
Aminopyridyloxypyrazole derivative and preparation method and application thereof
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Paragraph 0075; 0170-0176, (2021/05/19)
The invention relates to an aminopyridyloxypyrazole derivative and a preparation method and application thereof. The structure of the aminopyridyloxypyrazole derivative is shown as a formula (I). The invention provides a brand-new aminopyridyloxypyrazole derivative which has obvious effects of inhibiting TGF [beta] R1 (ALK5) kinase activity and treating cancer or fibrosis related diseases, and the preparation method of the derivative is simple and easy to operate.
ANALOGS OF 2-PRALIDOXIME AS ANTIDOTES AGAINST ORGANOPHOSPHORUS NERVE AGENTS
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, (2020/02/23)
Provided herein are compounds useful in treating exposure to an organophosphorus compound, such as a nerve agent, pesticide, or, generally, an acetylcholinesterase inhibitor, such as sarin. Compositions, e.g. pharmaceutical compositions or dosage forms, comprising the compounds also are provided herein. Methods of treating a patient exposed to a nerve agent, pesticide, or, generally, an acetylcholinesterase inhibitor, e.g., an organophosphorus compound, such as sarin, also are provided.
INHIBITORS OF PLASMA KALLIKREIN AND USES THEREOF
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, (2019/09/30)
The present invention provides compounds and compositions thereof which are useful as inhibitors of plasma kallikrein and which exhibit desirable characteristics for the same.
Synthesis method of 2-pyridylaldehyde derivative
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Paragraph 0067-0068; 0072-0073; 0076-0083, (2018/09/28)
The invention relates to the field of medical intermediates, in particular to a synthesis method of 2-pyridylaldehyde derivative. A synthesis path shown in the formula 1 is adopted, wherein X can be Cl or Br or CF3. Cheap starting raw materials are adopted, the use of hazardous materials which have large toxicity and are easily explosive is avoided, the cost of the product is greatly lowered, popularization and industrialized production are facilitated, and the synthesis method has the advantages of being low in cost, easy to operate, high in yield, easy to industrialize and the like. The formula 1 is shown in the description.
ALK KINASE INHIBITOR, AND PREPARATION METHOD AND USE THEREOF
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Paragraph 0201; 0202; 0203, (2017/04/18)
An ALK kinase inhibitor compound as represented by Formula I, pharmaceutical composition containing the compound, and preparation method and use thereof in the preparation of drugs serving as an ALK inhibitor for treating cancer.
Solvent polarity and oxygen sensitivity, rather than viscosity, determine lifetimes of biaryl-sensitised terbium luminescence
Walter, Edward R. H.,Williams, J. A. Gareth,Parker, David
supporting information, p. 13344 - 13347 (2017/12/26)
In a macrocyclic terbium complex incorporating a biaryl sensitiser, the observed variation of emission lifetime is shown to be determined by the solubility of oxygen in the solvent system and the relative energy of the chromophore excited state, rather than any dependence on solvent viscosity.
MODULATORS OF METHYL MODIFYING ENZYMES, COMPOSITIONS AND USES THEREOF
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, (2016/09/22)
Provided are novel compounds of Formula (I): and pharmaceutically acceptable salts thereof, which are useful for treating a variety of diseases, disorders or conditions, associated with methyl modifying enzymes. Also provided are pharmaceutical compositions comprising the novel compounds of Formula (I), pharmaceutically acceptable salts thereof, and methods for their use in treating one or more diseases, disorders or conditions, associated with methyl modifying enzymes.
BENZENESULFONAMIDES USEFUL AS SODIUM CHANNEL INHIBITORS
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, (2015/12/17)
The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to a new sulfonamide Nav1.7 inhibitors of formula (I), or a pharmaceutically acceptable salt thereof, wherein X, R1, R2, R3a, R3b and R4 are as defined in the description. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.
Anchoring a molecular iron catalyst to solar-responsive WO3 improves the rate and selectivity of photoelectrochemical water oxidation
Klepser, Benjamin M.,Bartlett, Bart M.
, p. 1694 - 1697 (2014/03/21)
Molecular catalysts help overcome the kinetic limitations of water oxidation and generally result in faster rates for water oxidation than do heterogeneous catalysts. However, molecular catalysts typically function in the dark and therefore require sacrificial oxidants such as Ce4+ or S2O82- to provide the driving force for the reaction. In this Communication, covalently anchoring a phosphonate-derivatized complex, Fe(tebppmcn)Cl2 (1), to WO3 removes the need for a sacrificial oxidant and increases the rate of photoelectrochemical water oxidation on WO3 by 60%. The dual-action catalyst, 1-WO3, also gives rise to increased selectivity for water oxidation in pH 3 Na 2SO4 (56% on bare WO3, 79% on 1-WO 3). This approach provides promising alternative routes for solar water oxidation.
Human carbonic anhydrase II as host protein for the creation of artificial metalloenzymes: The asymmetric transfer hydrogenation of imines
Monnard, Fabien W.,Nogueira, Elisa S.,Heinisch, Tillmann,Schirmer, Tilman,Ward, Thomas R.
, p. 3269 - 3274 (2013/07/26)
In the presence of human carbonic anhydrase II, aryl-sulfonamide-bearing IrCp* pianostool complexes catalyze the asymmetric transfer hydrogenation of imines. Critical cofactor-protein interactions revealed by the X-ray structure of [(η5-Cp*)Ir(pico 4)Cl] 9 WT hCA II were genetically optimized to improve the catalytic performance of the artificial metalloenzyme (68% ee, kcat/KM 6.11 × 10 -3 min-1 mM-1).
