959122-10-2Relevant articles and documents
Process development of a diacyl glycerolacyltransferase-1 inhibitor
Ravn, Matthew M.,Wagaw, Seble H.,Engstrom, Kenneth M.,Mei, Jianzhang,Kotecki, Brian,Souers, Andrew J.,Kym, Philip R.,Judd, Andrew S.,Zhao, Gang
, p. 417 - 424 (2011/04/22)
A synthesis of a selective diacyl glycerolacyltransferase-1 (DGAT-1) inhibitor, 1, is described. The synthesis illustrates a diketone Favorskii reaction on 9 in place of the more common ketoester variant for generation of the dicarboxycyclopentane core, t
Inhibitors of diacylglycerol O-acyltransferase type 1 enzyme
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Page/Page column 17, (2008/06/13)
The present invention relates to compounds of formula (I). wherein R1, R2, R3, R4, R5, R6, m, n, p and q are defined herein Pharmaceutical compositions and methods for treating DGAT-1 relat
Validation of diacyl glycerolacyltransferase I as a novel target for the treatment of obesity and dyslipidemia using a potent and selective small molecule inhibitor
Zhao, Gang,Souers, Andrew J.,Voorbach, Martin,Falls, H. Doug,Droz, Brian,Brodjian, Sevan,Yau, Yi Lau,Iyengar, Rajesh R.,Gao, Ju,Judd, Andrew S.,Wagaw, Seble H.,Ravn, Matthew M.,Engstrom, Kenneth M.,Lynch, John K.,Mulhern, Mathew M.,Freeman, Jennifer,Dayton, Brian D.,Wang, Xiaojun,Grihalde, Nelson,Fry, Dennis,Beno, David W. A.,Marsh, Kennan C.,Su,Diaz, Gilbert J.,Collins, Christine A.,Sham, Hing,Reilly, Regina M.,Brune, Michael E.,Kym, Philip R.
, p. 380 - 383 (2008/09/17)
A highly potent and selective DGAT-1 inhibitor was identified and used in rodent models of obesity and postprandial chylomicron excursion to validate DGAT-1 inhibition as a novel approach for the treatment of metabolic diseases. Specifically, compound 4a conferred weight loss and a reduction in liver triglycerides when dosed chronically in DIO mice and depleted serum triglycerides following a lipid challenge in a dose-dependent manner, thus, reproducing major phenotypical characteristics of DGAT-1-/- mice.
INHIBITORS OF DIACYLGLYCEROL O-ACYLTRANSFERASE TYPE 1 ENZYME
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Page/Page column 69, (2010/11/29)
The present invention relates to compounds of formula (I) wherein R1, R3, X, Q, Z, A, D, m, and n are defined herein. Pharmaceutical compositions and methods for treating DGAT-1 related diseases or conditions are also disclosed.