103235-15-0Relevant academic research and scientific papers
Intestinally targeted diacylglycerol acyltransferase 1 (DGAT1) inhibitors robustly suppress postprandial triglycerides
Serrano-Wu, Michael H.,Coppola, Gary M.,Gong, Yongjin,Neubert, Alan D.,Chatelain, Ricardo,Clairmont, Kevin B.,Commerford, Renee,Cosker, Theresa,Daniels, Thomas,Hou, Ying,Jain, Monish,Juedes, Marlene,Li, Lisha,Mullarkey, Tara,Rocheford, Erik,Sung, Moo Je,Tyler, Andrew,Yang, Qing,Yoon, Taeyoung,Hubbard, Brian K.
, p. 411 - 415 (2012/07/03)
High DGAT1 expression levels in the small intestine highlight the critical role this enzyme plays in nutrient absorption. Identification of inhibitors which predominantly inhibit DGAT1 in the gut is an attractive drug discovery strategy with anticipated benefits of reduced systemic toxicity. In this report we describe our discovery and optimization of DGAT1 inhibitors whose plasma exposure is minimized by the action of transporters, including the P-glycoprotein transporter. The impact of this unique absorption profile on efficacy in rat and dog efficacy models is presented.
OXADIAZOLE- AND OXAZOLE-SUBSTITUTED BENZIMIDAZOLE- AND INDOLE-DERIVATIVES AS DGAT1 INHIBITORS
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Page/Page column 104, (2009/05/29)
The present invention provides oxadiazolyl- substituted benzimidazole- and idole-derivates that are useful for treating conditions or disorders associated with DGAT1 activity in animals, particularly humans.
Herbicidal cyclohexane-1,3-dione derivatives
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, (2008/06/13)
The invention concerns novel compounds of the formula I STR1 wherein: m is an integer selected from 1 to 4; n is zero or an integer selected from 1 to 4; X are selected from halogen, nitro, cyano, alkyl, substituted alkyl, hydroxy, alkoxy, alkylthio, sulfamoyl, substituted sulfamoyl, amino, substituted amino, the group --(CH2)p C(=A)Z in which p is zero or one A is oxygen or sulfur, and Z is hydrogen, hydroxy, alkoxy, alkylthio, alkyl, substituted alkyl, amino or substituted amino, the group --NHC(=B)NR7 R8 in which B is oxygen or sulfur and R7 and R8 are hydrogen or alkyl; R1 is selected from hydrogen, acyl and an inorganic or organic cation; R2 is selected from alkyl, substituted alkyl, alkenyl, haloalkenyl, alkynyl and haloalkynyl; R3 is selected from alkyl, fluoroalkyl, alkenyl, alkynyl, and phenyl; and R4 is selected from hydrogen, halogen, alkyl, cyano and alkoxycarbonyl. The compounds of the invention show herbicidal properties and plant growth regulating properties and in further embodiments the invention provides processes for the preparation of compounds of formula I, intermediates useful in the preparation of the compounds of formula I, compositions containing as active ingredient a compound of formula I, and herbicidal and plant growth regulating processes utilizing compounds of formula I.
