Provided is a bicyclic compound having an acetyl-CoA carboxylase inhibitory action. A compound represented by the formula: wherein each symbol is as described in the DESCRIPTION, or a salt thereof has an acetyl-CoA carboxylase inhibitory action, is useful for the prophylaxis or treatment of cancer, inflammatory diseases and the like, and has superior efficacy.
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(2017/12/28)
Synthesis and structure-activity relationship of 4-(1,3-benzothiazol-2-yl)- thiophene-2-sulfonamides as cyclin-dependent kinase 5 (cdk5)/p25 inhibitors
4-(1,3-Benzothiazol-2-yl)thiophene-2-sulfonamide (4a) was found to be a moderately potent inhibitor of cyclin-dependent kinase 5 (cdk5) from a HTS screen. The synthesis and SAR around this hit is described. The X-ray coordinates of ligand 4a with cdk5 are also reported, showing an unusual binding mode to the hinge region via a water molecule.
The present invention provides new compounds of formula (I) as well as a process for their preparation and new intermediates used therein, pharmaceutical formulations containing said therapeutically active compounds and to the use of said active compounds
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Page/Page column 10
(2011/05/05)
Benzothiazole based inhibitors of p38α MAP kinase
Rational design, synthesis, and SAR studies of a novel class of benzothiazole based inhibitors of p38α MAP kinase are described. The issue of metabolic instability associated with vicinal phenyl, benzo[d]thiazol-6-yl oxazoles/imidazoles was addressed by t
Liu, Chunjian,Lin, James,Pitt, Sidney,Zhang, Rosemary F.,Sack, John S.,Kiefer, Susan E.,Kish, Kevin,Doweyko, Arthur M.,Zhang, Hongjian,Marathe, Punit H.,Trzaskos, James,Mckinnon, Murray,Dodd, John H.,Barrish, Joel C.,Schieven, Gary L.,Leftheris, Katerina
p. 1874 - 1879
(2008/12/21)
NOVEL ACETYL-COA CARBOXYLASE (ACC) INHIBITORS AND THEIR USE IN DIABETES, OBESITY AND METABOLIC SYNDROME
The present invention relates to compounds of formula (I) which inhibit acetyl-CoA carboxylase (ACC) and are useful for the prevention or treatment of metabolic syndrome, type II diabetes, obesity, atherosclerosis and cardiovascular diseases in humans.
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Page/Page column 19-20
(2008/06/13)
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