1197294-80-6Relevant articles and documents
COMPOUNDS AND USES THEREOF
-
Page/Page column 274; 275, (2021/08/06)
The present disclosure features compounds and methods useful for the treatment of BAF complex-related disorders.
Discovery of 7-(3-(piperazin-1-yl)phenyl)pyrrolo[2,1-f][1,2,4]triazin-4-amine derivatives as highly potent and selective PI3Kδ inhibitors
Qin, Lan-Ying,Ruan, Zheming,Cherney, Robert J.,Dhar, T.G. Murali,Neels, James,Weigelt, Carolyn A.,Sack, John S.,Srivastava, Anurag S.,Cornelius, Lyndon A.M.,Tino, Joseph A.,Stefanski, Kevin,Gu, Xiaomei,Xie, Jenny,Susulic, Vojkan,Yang, Xiaoxia,Yarde-Chinn, Melissa,Skala, Stacey,Bosnius, Ruth,Goldstein, Christine,Davies, Paul,Ruepp, Stefan,Salter-Cid, Luisa,Bhide, Rajeev S.,Poss, Michael A.
, p. 855 - 861 (2017/02/10)
As demonstrated in preclinical animal models, the disruption of PI3Kδ expression or its activity leads to a decrease in inflammatory and immune responses. Therefore, inhibition of PI3Kδ may provide an alternative treatment for autoimmune diseases, such as RA, SLE, and respiratory ailments. Herein, we disclose the identification of 7-(3-(piperazin-1-yl)phenyl)pyrrolo[2,1-f][1,2,4]triazin-4-amine derivatives as highly potent, selective and orally bioavailable PI3Kδ inhibitors. The lead compound demonstrated efficacy in an in vivo mouse KLH model.
Highly potent aminopyridines as Syk kinase inhibitors
Castillo, Marcos,Forns, Pilar,Erra, Montse,Mir, Marta,Lopez, Manel,Maldonado, Monica,Orellana, Adelina,Carreno, Cristina,Ramis, Isabel,Miralpeix, Montserrat,Vidal, Bernat
scheme or table, p. 5419 - 5423 (2012/09/22)
A novel class of potent Syk inhibitors has been developed from rational design. Highly potent aminopyridine derivatives bearing a 4-trifluoromethyl-2- pyridyl motif and represented by compound 13b IC50: 0.6 nM were identified. Substitution by a 2-pyrazinyl motif and SAR expansion in position 4 of the central core provided diverse potent non-cytotoxic Syk inhibitors showing nanomolar activity inhibiting human mast cell line LAD2 degranulation.