165682-75-7Relevant academic research and scientific papers
The discovery of potent blockers of the canonical transient receptor channels, TRPC3 and TRPC6, based on an anilino-thiazole pharmacophore
Washburn, David G.,Holt, Dennis A.,Dodson, Jason,McAtee, Jeff J.,Terrell, Lamont R.,Barton, Linda,Manns, Sharada,Waszkiewicz, Anna,Pritchard, Christina,Gillie, Dan J.,Morrow, Dwight M.,Davenport, Elizabeth A.,Lozinskaya, Irina M.,Guss, Jeffrey,Basilla, Jonathan B.,Negron, Lorena Kallal,Klein, Michael,Willette, Robert N.,Fries, Rusty E.,Jensen, Timothy C.,Xu, Xiaoping,Schnackenberg, Christine G.,Marino Jr., Joseph P.
, p. 4979 - 4984 (2013/09/02)
Lead optimization of piperidine amide HTS hits, based on an anilino-thiazole core, led to the identification of analogs which displayed low nanomolar blocking activity at the canonical transient receptor channels 3 and 6 (TRPC3 & 6) based on FLIPR (carbac
SUBSTITUTED THIAZOL-2-YLAMINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS, AND METHODS OF USE AS 11-BETA HSD1 MODULATORS
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Page/Page column 8, (2012/02/06)
The present invention is directed to substituted thiazol-2-ylamine derivatives and pharmaceutically acceptable salts thereof that inhibit 11βHSD1 and that may be useful in the treatment of diseases in which modulation or inhibition of 11βHSD1 is beneficial or where a reduction in intracellular glucorticoid levels is desirable. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases, disorders, or conditions in which modulation or inhibition of 11βHSD1 is beneficial or where a reduction in intracellular glucorticoid levels is desirable.
