1281832-23-2Relevant academic research and scientific papers
Identification of a novel 2-pyridyl-benzensulfonamide derivative, RQ-00203078, as a selective and orally active TRPM8 antagonist
Ohmi, Masashi,Shishido, Yuji,Inoue, Tadashi,Ando, Kazuo,Fujiuchi, Akiyoshi,Yamada, Akiko,Watanabe, Shuzo,Kawamura, Kiyoshi
, p. 5364 - 5368 (2014)
A novel series of 2-pyridyl-benzensulfonamide derivatives have been identified as selective and orally active TRPM8 antagonists via high throughput screening (HTS). Exploration of the structure-activity relationships of compound 1 has led to the identification of RQ-00203078 (compound 36) as a highly selective, potent and orally available TRPM8 antagonist. RQ-00203078 demonstrated excellent in vivo activity in a dose dependent manner with an ED50 value of 0.65 mg/kg in the icilin-induced wet-dog shakes model in rats after oral administration and may become an important pharmacological tool for fully assessing the potential therapeutic use of the targets activated by cold stimulation.
SULFAMOYL BENZOIC ACID DERIVATIVES AS TRPM8 ANTAGONISTS
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Page/Page column 86, (2010/11/17)
The present invention relates to sulfamoyl benzoic acid derivatives of formula (I) or a pharmaceutically acceptable salt thereof, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders which are mediated via the TRPM8 receptor.
