- COMPOSITIONS USEFUL FOR TREATING DISORDERS RELATED TO KIT AND PDFGR
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Compounds and compositions useful for treating disorders related to KIT and PDGFR are described herein.
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Paragraph 0229; 0230; 0231
(2017/02/24)
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- Access to a wide range of sultams by cyclodialkylation of α-substituted methanesulfonanilides
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A wide range of five- and six-membered sultams bearing an α-ethoxycarbonyl-α-methyl substituent or an α-aryl group (17 examples) were synthesized by the cyclodialkylation of α-substituted methanesulfonanilides with α,ω-dihaloalkanes in the presence of K2CO3 or under phase-transfer catalysis (PTC) conditions. Upon treatment with K2CO3 in N,N-dimethylformamide (DMF) or NaH in dimethyl sulfoxide (DMSO), N-(2,3-dibromopropyl)-α- toluenesulfonanilides furnished different 1,3-diaryl-2-thia-3-azabicyclo[3.1.0] hexane 2,2-dioxides in good to excellent yields (51-88 %, 16 examples). The 4-methoxyphenyl (PMP) group was easily removed from the sultam nitrogen atom by treatment of the corresponding bicyclic sultams with cerium(IV) ammonium nitrate in acetonitrile (71-84 % yield, 6 examples). The intermolecular cyclodialkylation of α-substituted methanesulfonamides constitutes a simple and efficient route to five- and six-membered sultams with α-ethoxycarbonyl-α-methyl or α-aryl substitution. The intramolecular cyclodialkylation of N-(2,3-dibromopropyl)-α- toluenesulfanilides readily leads to bicyclic sultams bearing a cyclopropane ring. Copyright
- Rassadin, Valentin A.,Grosheva, Daria S.,Arefeva, Irina A.,Tomashevskiy, Aleksandr A.,Sokolov, Victor V.,De Meijere, Armin
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supporting information
p. 5028 - 5037,10
(2020/08/24)
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- Indole cytosolic phospholipase A2 α inhibitors: Discovery and in vitro and in vivo characterization of 4-{3-[5-chloro-2-(2-{[(3,4- dichlorobenzyl)sulfonyl]amino}ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]propyl} benzoic acid, efipladib
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The optimization of a class of indole cPLA2α inhibitors is described herein. The importance of the substituent at C3 and the substitution pattern of the phenylmethane sulfonamide region are highlighted. Optimization of these regions led to the
- McKew, John C.,Lee, Katherine L.,Shen, Marina W. H.,Thakker, Paresh,Foley, Megan A.,Behnke, Mark L.,Hu, Baihua,Sum, Fuk-Wah,Tam, Steve,Hu, Yonghan,Chen, Lihren,Kirincich, Steven J.,Michalak, Ronald,Thomason, Jennifer,Ipek, Manus,Wu, Kun,Wooder, Lane,Ramarao, Manjunath K.,Murphy, Elizabeth A.,Goodwin, Debra G.,Albert, Leo,Xu, Xin,Donahue, Frances,Ku, M. Sherry,Keith, James,Nickerson-Nutter, Cheryl L.,Abraham, William M.,Williams, Cara,Hegen, Martin,Clark, James D.
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experimental part
p. 3388 - 3413
(2009/05/26)
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- NEW PYRIDINE ANALOGUES
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The present invention relates to certain new pyridin analogues of Formula (I) Chemical formula should be inserted here. Please see paper copy Formula (I) to processes for preparing such compounds, to their utility as P2Y12 inhibitors and as anti-trombotic agents etc, their use as medicaments in cardiovascular diseases as well as pharmaceutical compositions containing them.
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Page/Page column 150
(2008/06/13)
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- Amidinophenylmethylsulfonylfluoride
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A new compound amidinophenylmethylsulfonylfluoride is formed and preferably used in the para isomer form as an irreversible inactivator of selected serine proteases.
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- ESTERS OF AROMATIC SULFONIC ACIDS
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Novel esters of aromatic sulfonic acids are disclosed. The specific esters are nitrophenyl p-and m-amidinophenylmethanesulfonate. Also disclosed is a method for specific inactivation of the enzyme, thrombin, employing nitrophenyl p-amidinophenylmethanesul
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