316181-82-5Relevant articles and documents
REV-ERB AGONISTS FOR THE TREATMENT OF TH17-MEDIATED INFLAMMATORY DISORDERS
-
Paragraph 00528-00530; 00697-00699, (2022/01/05)
The present disclosure provides compounds of Formula IA and Formula IB and their pharmaceutical compositions as selective agonists of REV-ERB-α: where R1, R2, R3, R4, R5, RX1, RX2, nA, nB, X, Y, and Z are described herein. The compounds are useful in various methods and uses, such as in the treatment of diseases including hyperglycemia, dyslipidemia, atherosclerosis, and autoimmune and inflammatory disorders or diseases, and as cancer therapeutics, such as for the treatment of glioblastoma, hepatocellular carcinoma, and colorectal cancer, and for immune-oncology purposes.
Cascade Reaction to Selectively Synthesize Multifunctional Indole Derivatives by IrIII-Catalyzed C?H Activation
Chai, Xin-Yue,Xu, Hui-Bei,Dong, Lin
supporting information, p. 13123 - 13127 (2021/08/13)
An effective and condition-controlled way to synthesize with high selectivity a variety of functionalized indoles with potent biological properties has been developed. Notably, 2,4-dialkynyl indole products were obtained by direct double C?H bond alkynylation, whereas alkynyl at the C4 position could convert to carbonyl to generate 2-alkynyl-3,4-diacetyl indoles fast and effectively. Additionally, a one-pot relay catalytic reaction led to 2,5-di-alkynyl-3,4-diacetyl indoles when using a carbonyl group as the directing group and by controlling the type and quantity of additives. A possible mechanism was proposed based on many studies including deuterium-exchange experiments, the necessary conditions of product conversion, and the effect of water on the reaction.
Preparation and application of pyrimidinedionoindole and pyridinonoindole compounds
-
Paragraph 0198-0201, (2021/03/05)
The invention relates to a preparation method of a compound containing a pyrimidine-2, 4-diono[5, 4-b]indole skeleton or a pyridine-2-ono[3, 2-d]indole skeleton, and further relates to medical application of the compound serving as a BET Bromo structural domain inhibitor.