35604-35-4Relevant articles and documents
Synthesis and multiparametric evaluation of thiadiazoles and oxadiazoles as diacylglycerol acyltransferase type 1 inhibitors
Mougenot, Patrick,Namane, Claudie,Fett, Eykmar,Goumy, Florence,Dadji-Fa?hun, Rommel,Langot, Gwladys,Monseau, Catherine,Onofri, Bénédicte,Pacquet, Fran?ois,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,Ménegotto, Jér?me,Schmidt, Friedemann,Venier, Olivier,Viviani, Fabrice,Nicolai, Eric
, p. 25 - 32 (2015/12/18)
Chemical modulation of a formerly disclosed DGAT-1 inhibitor resulted in the identification of a compound with a suitable profile for preclinical development. Optimisation of solubility is discussed and a PK/PD study is presented.
DERIVATIVES OF OXADIAZOLE AND PYRIDAZINE, THEIR PREPARATION AND THEIR APPLICATION IN THERAPEUTICS
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Page/Page column 27, (2012/02/05)
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.