26304-51-8Relevant articles and documents
β-nitroacrylates as useful building blocks for the synthesis of alkyl indole-2-carboxylates
Palmieri, Alessandro,Gabrielli, Serena,Maggi, Raimondo,Ballini, Roberto
, p. 128 - 132 (2014)
Polyfunctionalized alkyl indole 2-carboxylates can be easily synthesized starting form β-nitroacrylates and o-bromoanilines through an addition-elimination process followed by an intramolecular palladium-catalyzed Heck reaction. Georg Thieme Verlag Stuttg
5-MEMBERED HETEROCYCLE FUSED WITH [3,4-D]PYRIDAZINONE, AND MANUFACTURING METHOD, PHARMACEUTICAL COMPOSITION, AND APPLICATION THEREOF
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Paragraph 0098; 0099, (2019/04/29)
The present invention provides a compound comprising a 5-membered heterocycle fused with a pyridazinone, wherein the compound is used as an FGFR kinase inhibitor, and a manufacturing method and application thereof. The invention specifically provides a co
Development of indole sulfonamides as cannabinoid receptor negative allosteric modulators
Greig, Iain R.,Baillie, Gemma L.,Abdelrahman, Mostafa,Trembleau, Laurent,Ross, Ruth A.
, p. 4403 - 4407 (2016/08/25)
Existing CB1 negative allosteric modulators (NAMs) fall into a limited range of structural classes. In spite of the theoretical potential of CB1 NAMs, published in vivo studies have generally not been able to demonstrate the expected therapeutically-relevant CB1-mediated effects. Thus, a greater range of molecular tools are required to allow definitive elucidation of the effects of CB1 allosteric modulation. In this study, we show a novel series of indole sulfonamides. Compounds 5e and 6c (ABD1075) had potencies of 4 and 3?nM respectively, and showed good oral exposure and CNS penetration, making them highly versatile tools for investigating the therapeutic potential of allosteric modulation of the cannabinoid system.