19075-53-7Relevant academic research and scientific papers
PPAR (peroxisome proliferator-activated receptor) agonist and application thereof to treatment of senile dementia and other diseases
-
, (2018/07/30)
The invention relates to a compound, namely a gamma-subtype peroxisome proliferator-activated receptor (PPAR) agonist. In addition, the invention discloses a medicinal component and a preparation containing the compound and application of such the gamma-subtype PPAR agonist.
SELECTIVE HDAC6 INHIBITORS AND USES THEREOF
-
Page/Page column 19; 20, (2016/08/10)
The present invention relates to selective Histone deacetylase 6 (HDAC6) inhibitors and compositions containing the same. Methods of treating diseases and conditions wherein inhibition of HDAC6 provides a benefit, like a cell proliferative disease, an aut
Synthesis of benzothiophene-based hydroxamic acids as potent and selective HDAC6 inhibitors
De Vreese, Rob,Van Steen, Nicholas,Verhaeghe, Tom,Desmet, Tom,Bougarne, Nadia,De Bosscher, Karolien,Benoy, Veronick,Haeck, Wanda,Van Den Bosch, Ludo,D'Hooghe, Matthias
supporting information, p. 9868 - 9871 (2015/06/16)
A small library of 3-[(4-hydroxycarbamoylphenyl)aminomethyl]benzothiophenes was prepared and assessed as a novel class of HDAC6 inhibitors, leading to the identification of three representatives as potent and selective HDAC6 inhibitors. Further tests with
Potent BRAF kinase inhibitors based on 2,4,5-trisubstituted imidazole with naphthyl and benzothiophene 4-substituents
Niculescu-Duvaz, Dan,Niculescu-Duvaz, Ion,Suijkerbuijk, Bart M.J.M.,Ménard, Delphine,Zambon, Alfonso,Davies, Lawrence,Pons, Jean-Francois,Whittaker, Steven,Marais, Richard,Springer, Caroline J.
, p. 1284 - 1304 (2013/03/14)
The RAS-RAF-MEK-ERK pathway is hyperactivated in 30% of human cancers. BRAF is a serine-threonine kinase, belonging to this pathway that is mutated with high frequency in human melanoma and other cancers thus BRAF is an important therapeutic target in melanoma. We have designed inhibitors of BRAF based on 2,4,5-trisubstituted imidazoles with naphthyl and benzothiophene-4-substituents. Two compounds were discovered to be potent BRAF inhibitors: 1-(6-{2-[4-(2-dimethylamino-ethoxy)phenyl]-5-(pyridin-4-yl)-1H-imidazol-4-yl} benzo[b]thiophen-3-yl)-2,2,2-trifluoroethanol (1i) with BRAF IC50 = 190 nM and with cellular GI50 = 2100 nM, and 6-{2-[4-(2- dimethylamino-ethoxy)-phenyl]-5-pyridin-4-yl-3H-imidazol-4-yl}-naphthalen-1-ol (1q) with IC50 = 9 nM and GI50 = 220 nM.
Pharmaceutical compounds
-
, (2008/06/13)
This invention relates to compounds of formula (I) where R1 to R12, —W—V—, —X—Y—, m and n have the values defined in claim 1, their preparation and use as pharmaceuticals.
