1245708-05-7Relevant academic research and scientific papers
Development of novel benzomorpholine class of diacylglycerol acyltransferase i inhibitors
Zhou, Gang,Zorn, Nicolas,Ting, Pauline,Aslanian, Robert,Lin, Mingxiang,Cook, John,Lachowicz, Jean,Lin, Albert,Smith, Michelle,Hwa, Joyce,Van Heek, Margaret,Walker, Scott
, p. 544 - 549 (2014/06/09)
Diacylglycerol acyltransferase 1 (DGAT1) presents itself as a potential therapeutic target for obesity and diabetes for its important role in triglyceride biosynthesis. Herein we report the rational design of a novel class of DGAT1 inhibitors featuring a
DERIVATIVES OF OXADIAZOLE AND PYRIDAZINE, THEIR PREPARATION AND THEIR APPLICATION IN THERAPEUTICS
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, (2013/06/05)
The invention relates to compounds of formula (I): in which: n is equal to 0 or 1; D represents an oxygen atom or a bond; W represents a nitrogen atom or a —CH— group; X1 represents a nitrogen atom or a —CH═CH— group; X2 represents an oxygen atom or a nitrogen atom; X3 represents an oxygen atom or a nitrogen atom; one of X1, X2, X3 being other than a nitrogen atom, X2 and X3 not being an oxygen atom at the same time; R1, R2 are absent or represent, (i) independently of one another, a hydrogen atom or a (C1-C4)alkyl group, (ii) R1 and R2 may form, with the carbon atom to which they are attached, a —(C3-C10)cycloalkyl- group; Y represents a —(C3-C10)cycloalkyl-, aryl or aryloxy group, said groups being optionally substituted with one or more substituents chosen from a halogen atom or a (C1-C6)alkoxy group; Z1 is absent or represents an —NH— function; Z2 and Z3 are as defined in the description. The invention also relates to a process for preparing compounds of formula (I), compositions containing them and their application in therapeutics.
Thiadiazoles as new inhibitors of diacylglycerol acyltransferase type 1
Mougenot, Patrick,Namane, Claudie,Fett, Eykmar,Camy, Florence,Dadji-Fa?hun, Rommel,Langot, Gwladys,Monseau, Catherine,Onofri, Bénédicte,Pacquet, Franois,Pascal, Cécile,Crespin, Olivier,Ben-Hassine, Majdi,Ragot, Jean-Luc,Van-Pham, Thao,Philippo, Christophe,Chatelain-Egger, Florence,Péron, Philippe,Le Bail, Jean-Christophe,Guillot, Etienne,Chamiot-Clerc, Philippe,Chabanaud, Marie-Aude,Pruniaux, Marie-Pierre,Schmidt, Friedemann,Venier, Olivier,Nicola?, Eric,Viviani, Fabrice
, p. 2497 - 2502 (2012/05/05)
A novel class of DGAT1 inhibitors containing a thiadiazole core has been discovered. Chemical optimization lead to inhibitors of human DGAT1 with an appropriate ADME profile and that show in vivo activity in target tissues.
