- PREPARATION OF 2-CHLORO-1-(2-CHLOROTHIAZOL-5-YL)ETHANONE
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The present invention relates to a process for the preparation 2-chloro-1-(2-chlorothiazol-5-yl)ethanone.
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Page/Page column 13; 15
(2021/04/10)
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- Second generation of thiazolylmannosides, FimH antagonists for E. coli-induced Crohn's disease
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The anti-adhesive strategy, consisting of disrupting bacterial attachment to the host cells, is widely explored as an alternative to antibiotic therapies. Recently, thiazolylmannosides (TazMans) have been identified as strong anti-adhesives of E. coli strains implied in the gut inflammation of patients with Crohn's disease. In this work, we developed a second generation of TazMans with improved chemical stability. The anomeric nitrogen was substituted by short linkers and the compounds were assessed against the bacterial adhesin FimH and the clinically isolated LF82 E. coli strain in four in vitro assays. The results obtained on the FimH adhesin alone and the whole bacteria enabled the identification of a candidate for further in vivo evaluations.
- Chalopin,Alvarez Dorta,Sivignon,Caudan,Dumych,Bilyy,Deniaud,Barnich,Bouckaert,Gouin
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p. 3913 - 3925
(2016/05/19)
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- Utilization of a nitrogen-sulfur nonbonding interaction in the design of new 2-aminothiazol-5-yl-pyrimidines as p38α MAP kinase inhibitors
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The design, synthesis, and structure-activity relationships (SAR) of a series of 2-aminothiazol-5-yl-pyrimidines as novel p38α MAP kinase inhibitors are described. These efforts led to the identification of 41 as a potent p38α inhibitor that utilizes a un
- Lin, Shuqun,Wrobleski, Stephen T.,Hynes Jr., John,Pitt, Sidney,Zhang, Rosemary,Fan, Yi,Doweyko, Arthur M.,Kish, Kevin F.,Sack, John S.,Malley, Mary F.,Kiefer, Susan E.,Newitt, John A.,McKinnon, Murray,Trzaskos, James,Barrish, Joel C.,Dodd, John H.,Schieven, Gary L.,Leftheris, Katerina
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scheme or table
p. 5864 - 5868
(2010/11/18)
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- Thiazole-diamides as potent γ-secretase inhibitors
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The thiazole-diamide series (1) has been identified as highly potent γ-secretase inhibitors. Several representative compounds showed IC50 values of 3H]-2a, are d
- Chen, Yuhpyng L.,Cherry, Kevin,Corman, Michael L.,Ebbinghaus, Charles F.,Gamlath, Chandra B.,Liston, Dane,Martin, Barbara-Anne,Oborski, Christine E.,Sahagan, Barbara G.
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p. 5518 - 5522
(2008/03/14)
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- THIAZOLE DERIVATIVES AND USE THEREOF
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The present invention is related to thiazole derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.
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Page/Page column 79
(2008/06/13)
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