09/15/21 News Simple exploration of 5908-62-3

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A self-immolative gamma-aminopropylsulfonate linker was investigated for use in the development of prodrugs that are reactive to various chemical or biological stimuli. To demonstrate their utility, a leucine-conjugated prodrug of 5-chloroquinolin-8-ol (5-Cl-8-HQ), which is a potent inhibitor against aminopeptidase from Aeromonas proteolytica (AAP), was synthesized. The sulfonate prodrug was considerably stable under physiological conditions, with only enzyme-mediated hydrolysis of leucine triggering the subsequent intramolecular cyclization to simultaneously release 5-Cl-8-HQ and form gamma-sultam. It was also confirmed that this gamma-aminopropylsulfonate linker was applicable for prodrugs of not only 8-HQ derivatives but also other drugs bearing a phenolic hydroxy group.

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The invention provides an inner sulfonamide compounds and their preparation method. The invention of the specific method is catalyst C, sulfonamide B, oxidizing agent D reaction in an organic solvent is added, after the separation and purification, to obtain an internal sulfonamide compound E, […] detection after the reaction is finished, then adding the oxidizing agent after the reaction F, inlet separation and purification, to obtain in the sulfonyl imide compound G. The method the catalyst needed is cheap and easy to obtain, low toxicity of the iron complex. When using the sulfonamide H when, through according to the above method after the reaction, and then adding the other additional oxidizing agent F under the condition of, one-pot synthesis in the realization of the sulfonyl imide compound. In the preparation of the sulfonamide and in the sulfonyl imide compound widely used in pharmaceutical chemistry, materials chemistry and the field of organic synthesis. (by machine translation)

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This application relates to compounds of Formula (I) or pharmaceutically acceptable salts or stereoisomers thereof, which modulate the activity of adenosine receptors, such as subtypes A2A and A2B receptors, and are useful in the treatment of diseases related to the activity of adenosine receptors including, for example, cancer, inflammatory diseases, cardiovascular diseases, and neurodegenerative diseases.

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The present invention provides novel compounds having general formula (I), wherein R1 to R4, A, W, Q and Y are as described herein, compositions including the compounds and methods of using the compounds.

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The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.

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A convenient, general, and high yielding Pd-catalyzed cross-coupling of methanesulfonamide with aryl bromides and chlorides is reported. The use of this method eliminates concern over genotoxic impurities that can arise when an aniline is reacted with methanesulfonyl chloride. The application of this method to the synthesis of dofetilide is also reported.

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The invention is directed to 5,6-dihydro-lH-pyridin-2-one compounds and pharmaceutical compositions containing such compounds that are useful in treating infections by hepatitis C virus.

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The invention relates to a compound of formula (I) wherein R1 to R4 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.

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A room-temperature, copper-catalyzed amination of primary benzylic C?H bonds with primary and secondary sulfonamides is described. The reaction is applicable to the coupling of a range of primary and secondary benzylic hydrocarbons with a diverse set of sulfonamides and is tolerant of substitution on both coupling partners. Factors which influence the selectivity of C?H functionalization between primary and secondary sites are examined.

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The present invention provides a compound of formula (I) or a pharmaceutically acceptable derivative, salt or prodrug thereof. The present invention further provides a method of treatment or prophylaxis of a viral infection in a subject comprising administering to said subject an effective amount of a compound of formula (I) or a pharmaceutically acceptable derivative, salt or prodrug thereof. Pharmaceutical compositions comprising a compound of formula (I) are also provided.

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