1823-00-3Relevant academic research and scientific papers
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.
OXADIAZOLE COMPOUNDS
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Page/Page column 146, (2015/11/11)
The present invention relates to a compound of formula (I) or (II) or a stereoisomer, enantiomer, racemic, or tautomer thereof, (I) (II) wherein R1,R2,R3,L1,L2,L3,L4,L5 and n, have the same meaning as that defined in the claims and the description. The present invention also relates to compositions, in particular pharmaceuticals, comprising such compounds, and to uses of such compounds and compositions for the prevention and/or treatment of metabolic disorders and/or neurodegenerative diseases, and/or protein misfolding disorders.
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.
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.
