784150-40-9Relevant articles and documents
The condensed heterocyclic compound such as Bruton kinase inhibitors (by machine translation)
-
, (2018/04/20)
The invention relates to a fused heterocycle derivative and an application, which has a structure shown in a formula 1). The compound with the structure shown in the formula 1) has good inhibition effect to Bruton kinases activity, and median inhibitory concentration is lower than 10mol.L generally.
Identification of Purines and 7-Deazapurines as Potent and Selective Type i Inhibitors of Troponin I-Interacting Kinase (TNNI3K)
Lawhorn, Brian G.,Philp, Joanne,Zhao, Yongdong,Louer, Christopher,Hammond, Marlys,Cheung, Mui,Fries, Harvey,Graves, Alan P.,Shewchuk, Lisa,Wang, Liping,Cottom, Joshua E.,Qi, Hongwei,Zhao, Huizhen,Totoritis, Rachel,Zhang, Guofeng,Schwartz, Benjamin,Li, Hu,Sweitzer, Sharon,Holt, Dennis A.,Gatto, Gregory J.,Kallander, Lara S.
, p. 7431 - 7448 (2015/10/05)
A series of cardiac troponin I-interacting kinase (TNNI3K) inhibitors arising from 3-((9H-purin-6-yl)amino)-N-methyl-benzenesulfonamide (1) is disclosed along with fundamental structure-function relationships that delineate the role of each element of 1 for TNNI3K recognition. An X-ray structure of 1 bound to TNNI3K confirmed its Type I binding mode and is used to rationalize the structure-activity relationship and employed to design potent, selective, and orally bioavailable TNNI3K inhibitors. Identification of the 7-deazapurine heterocycle as a superior template (vs purine) and its elaboration by introduction of C4-benzenesulfonamide and C7- and C8-7-deazapurine substituents produced compounds with substantial improvements in potency (>1000-fold), general kinase selectivity (10-fold improvement), and pharmacokinetic properties (>10-fold increase in poDNAUC). Optimal members of the series have properties suitable for use in in vitro and in vivo experiments aimed at elucidating the role of TNNI3K in cardiac biology and serve as leads for developing novel heart failure medicines.
SUBSTITUTED ETHYNYL HETEROBICYCLIC COMPOUNDS AS TYROSINE KINASE INHIBITORS
-
, (2015/12/11)
The present disclosure provides a compound of formula (I) and the use thereof for the therapeutic treatment of human cancers including B-cell lymphoma and autoimmune diseases such as rheumatoid arthritis, systemic lupus erythematosus, and multiple sclerosis.
COMPOUNDS AND METHODS
-
Page/Page column 64-65, (2011/12/14)
Disclosed are compounds having the Formula (I), wherein X, Y, Z, R1, R2 and R3 are as defined herein, and methods of making and using the same.
Efficient formation of 4,6-disubstituted pyrrolo[2,3-d]pyrimidines: A novel route to TWS119, a glycogen synthase kinase-3β inhibitor
Mayasundari, Anand,Fujii, Naoaki
supporting information; scheme or table, p. 3597 - 3598 (2010/08/19)
A concise synthesis of 4,6-disubstituted pyrrolo[2,3-d]pyrimidines is described. The key step involves the formation of an ether or thioether linkage along with concurrent ring closure in one-pot to yield the desired product in only two steps from a common intermediate. The reaction is chemoselective to incorporate phenol, thiophenol, and thiol. This method enabled efficient production of TWS119, a glycogen synthase kinase-3β inhibitor.
Heterocyclic Compounds Useful as RAF Kinase Inhibitors
-
Page/Page column 27, (2009/01/24)
The present invention provides compounds useful as inhibitors of Raf protein kinase. The present invention also provides compositions thereof, and methods of treating Raf-mediated diseases.