- SULFONAMIDE DERIVATIVE AND PHARMACEUTICAL USE THEREOF
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Provided is a sulfonamide derivative represented by the following general formula (1) and having an α4 integrin inhibitory effect with high selectivity with a low effect on α4β1 and a high effect on α4β7, or a pharmaceutically acceptable salt thereof (in the general formula (1), A, B, D, E, R41, and a to h are as described in the description).
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Paragraph 0283; 0284; 0285
(2016/09/26)
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- SULFONAMIDE DERIVATIVE AND MEDICINAL USE THEREOF
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Provided are sulfonamide derivatives of a specific chemical structure in which a sulfonamide group having, as a substituent, a phenyl group or a heterocyclic group having a hetero atom(s) as a constituent element(s) is present at its terminal, and pharmaceutically acceptable salts thereof. These compounds are novel compounds having excellent α4 integrin-inhibitory action.
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Paragraph 1531-1532
(2015/02/25)
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- Discovery and in vivo evaluation of alcohol-containing benzothiazoles as potent dual-targeting bacterial DNA supercoiling inhibitors
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A series of dual-targeting, alcohol-containing benzothiazoles has been identified with superior antibacterial activity and drug-like properties. Early lead benzothiazoles containing carboxylic acid moieties showed efficacy in a well-established in vivo model, but inferior drug-like properties demanded modifications of functionality capable of demonstrating superior efficacy. Eliminating the acid group in favor of hydrophilic alcohol moieties at C 5, as well as incorporating solubilizing groups at the C7 position of the core ring provided potent, broad-spectrum Gram-positive antibacterial activity, lower protein binding, and markedly improved efficacy in vivo.
- Palmer, James T.,Axford, Lorraine C.,Barker, Stephanie,Bennett, James M.,Blair, Michael,Collins, Ian,Davies, David T.,Ford, Leigh,Gannon, Carlie T.,Lancett, Paul,Logan, Alastair,Lunniss, Christopher J.,Morton, Craig J.,Offermann, Daniel A.,Pitt, Gary R.W.,Rao, B. Narasinga,Singh, Amit K.,Shukla, Tarun,Srivastava, Anil,Stokes, Neil R.,Thomaides-Brears, Helena B.,Yadav, Anju,Haydon, David J.
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p. 4215 - 4222
(2014/10/15)
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- Antibacterial Compounds
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The present invention provides a compound of the following formula, salts, racemates, diastereomers, enantiomers, esters, carbamates, phosphates, sulfates, deuterated forms and prodrugs thereof. Also provided is the use of these compounds as antibacterials, compositions comprising them and processes for their manufacture.
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Paragraph 0596
(2013/10/07)
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- Hydroxymethylations of aryl halides by Pd-catalyzed cross-couplings with (benzoyloxy)methylzinc iodide - Scope and limitations of the reaction
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Palladium-catalyzed cross-coupling reactions of (benzoyloxymethyl)zinc iodide with diverse (het)aryl halides leading to (benzoyloxymethyl)(het)arenes were studied to define the scope of this reaction. It has been found that this reaction is only applicable for electron-deficient aryl halides and the most efficient it is for 2-halopyridines and 4-halopyrimidines. Deprotection of the intermediates gives (hydroxymethyl)pyridines and -pyrimidines in high yields. Georg Thieme Verlag Stuttgart.
- Hasník, Zbyněk,?ilhár, Peter,Hocek, Michal
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p. 543 - 546
(2008/12/22)
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