100058-61-5Relevant articles and documents
5-Alkyl-2-urea-Substituted Pyridines: Identification of Efficacious Glucokinase Activators with Improved Properties
Kohn, Todd J.,Du, Xiaohui,Lai, Sujen,Xiong, Yumei,Komorowski, Renee,Veniant, Murielle,Fu, Zice,Jiao, Xianyun,Pattaropong, Vatee,Chow, David,Cardozo, Mario,Jin, Lixia,Conn, Marion,DeWolf, Walter E.,Kraser, Christopher F.,Hinklin, Ronald J.,Boys, Mark L.,Medina, Julio C.,Houze, Jonathan,Dransfield, Paul,Coward, Peter
, p. 666 - 670 (2016)
Two 1-(4-aryl-5-alkyl-pyridin-2-yl)-3-methylurea glucokinase activators were identified with robust in vivo efficacy. These two compounds possessed higher solubilities than the previously identified triaryl compounds (i.e., AM-2394). Structure-activity re
Discovery of novel selective GPR120 agonists with potent anti-diabetic activity by hybrid design
Sheng, Ren,Yang, Liu,Zhang, Yanchun,Xing, Enming,Shi, Rui,Wen, Xiaoan,Wang, Heyao,Sun, Hongbin
, p. 2599 - 2604 (2018)
GPR120 is an attractive target for the treatment of type 2 diabetes. In this study, a series of biphenyl derivatives were designed, synthesized by hybrid design. The selected compound 6a exhibited potent GPR120 agonist activity (EC50 = 93 nM) and high selectivity over GPR40. The results of oral glucose tolerance test (OGTT) demonstrated that 6a exhibited significant glucose-lowering effect in glucose-loaded ICR male mice. Analysis of the structure–activity relationship is also presented. Compound 6a deserves further biological evaluation and structural modifications.
COMPOUNDS AND USES THEREOF
-
Page/Page column 356, (2021/08/06)
The present disclosure features compounds useful for the treatment of BAF complex-related disorders.
COMPOUND SERVING AS IRAK INHIBITOR
-
Paragraph 0221-0222, (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.
MERTK DEGRADERS AND USES THEREOF
-
Paragraph 00827, (2020/01/31)
The present invention provides compounds, compositions thereof, and methods of using the same.
THIADIAZOLYL DERIVATIVES AS DNA POLYMERASE THETA INHIBITORS
-
Paragraph 0550, (2020/12/11)
Disclosed herein are certain thiadiazolyl derivatives Formula (I): that inhibit DNA Polymerase Theta (Polθ) activity, in particular inhibit Polθ activity by inhibiting ATP dependent helicase domain activity of Polθ. Also, disclosed are pharmaceutical compositions comprising such compounds and methods of treating and/or preventing diseases treatable by inhibition of Polθ such as cancer, including homologous recombination (HR) deficient cancers.
CEREBLON BINDERS FOR THE DEGRADATION OF IKAROS
-
Page/Page column 395, (2019/10/23)
The present invention provides cereblon binders for the degradation of Ikaros or Aiolos by the ubiquitin proteasome pathway along with their use in therapeutic applications as described herein.
PYRAZOLO[1,5a]PYRIMIDINE DERIVATIVES AS IRAK4 MODULATORS
-
Page/Page column 125, (2019/01/10)
Compounds of Formula (I), Formula (II), Formula (III), Formula (IV), Formula (V), Formula (VI), Formula (VII), Formula (VIII), and methods of use as lnterleukin-1 Receptor Associated Kinase (IRAK4) inhibitors are described herein.
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
supporting information, 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.