344338-13-2Relevant articles and documents
COMPOUND SERVING AS IRAK INHIBITOR
-
Paragraph 0153-0154; 0212-0213; 0255-0256, (2021/10/07)
The present disclosure relates a compound as an IRAK inhibitor. Specifically, the present disclosure provides a compound of formula I, or a cis-trans isomer, an optical isomer, a racemate, a pharmaceutically acceptable salt, a prodrug, a deuterated derivative thereof, a hydrate or a solvate thereof. The compounds disclosed herein have potent inhibitory effects on IRAK and thus have therapeutic effect on IRAK-related diseases.
SUBSTITUTED BENZIMIDAZOLES AS PAD4 INHIBITORS
-
Paragraph 00190, (2020/03/02)
The present invention provides compounds of Formula (I): useful as inhibitors of PAD4, compositions thereof, and methods of treating PAD4-related disorders.
Synthesis of Electron-Deficient Heteroaromatic 1,3-Substituted Cyclobutyls via Zinc Insertion/Negishi Coupling Sequence under Batch and Automated Flow Conditions
Tissot, Matthieu,Body, Nathalie,Petit, Sylvain,Claessens, Jehan,Genicot, Christophe,Pasau, Patrick
, p. 8022 - 8025 (2019/01/04)
Synthesis of 1,3-substituted cyclobutyls enabled by zinc insertion into functionalized iodocyclobutyl derivatives followed by Negishi coupling with halo-heteroaromatics is reported. Two distinct sets of conditions were developed; the first involved a two-step batch protocol using activated Rieke zinc, and the second involved a multistep continuous flow process. Both methods showed complementarity and allowed for rapid access to these medicinally relevant motifs, the possibility of scaling up, and automation for library synthesis.