23230-39-9Relevant articles and documents
Design, synthesis and biological evaluation of novel benzoylimidazole derivatives as RAF and histone deacetylases dual inhibitors
Chen, Xin,Gong, Guoliang,Chen, Xinyang,Song, Ruihu,Duan, Mei,Qiao, Ruizhi,Jiao, Yu,Qi, Jianzhao,Chen, Yadong,Zhu, Yong
, p. 1116 - 1122 (2019)
In recent studies, combinations of histone deacetylases (HDACs) inhibitor with kinase inhibitor showed additive and synergistic effects. BRafV600E as an attractive target in many diseases treatments has been studied extensively. Herein, we pres
IMIDAZOLE DERIVATIVES AND THEIR USE AS MODULATORS OF CYCLIN DEPENDENT KINASES
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Page/Page column 111-112, (2010/11/17)
The invention provides compounds of the formula (I): and salts, tautomers, solvates and N-oxides thereof; wherein Q is CH or N; X is N, N+-O- or CR3; Y is N, N+-O- or CR3a; R1 and R2 are independently selected from hydrogen and various substituents as defined in the claims; or R1 and R2 together with the atoms to which they are attached, link to form an optionally substituted carbocyclic or heterocyclic aromatic or non-aromatic ring of 4 to 7 members; R3 is selected from hydrogen and various substituents; and R3a is selected from hydrogen and various substituents as defined in the claims. Also provided are pharmaceutical compositions containing the compounds of formula (I), processes for making the compounds and the medical uses of the compounds. The compounds of formula (I) have activity as inhibitors of CDK kinases and are useful in the treatment of inter alia proliferative diseases such as cancers.
Structure-activity studies on 4-substituted-2-anilinopyrimidine corticotropin releasing factor (CRF) antagonists
Gilligan, Paul J.,He, Liqi,Culp, Steven,Fitzgerald, Lawrence,Tam, S.William,Wong, Y.Nancy
, p. 2321 - 2328 (2007/10/03)
Structure-activity studies around the 4-position of 2-anilinopyrimidine corticotropin releasing factor (CRF) antagonists suggest that there is a large lipophilic cavity in the rat CRF receptor, which can accommodate a wide variety of substituents at this position in contrast to the steric constraints observed for other positions on the 2-anilinopyrimidine core. The chemical syntheses and biological activities of 2-anilinopyrimidine CRF antagonists with carbon-linked substituents at the 4-position are reported. Significant improvements in rat pharmacokinetic parameters were achieved relative to those for the lead structure. While the lead compound 1 (rCRF K(i) = 44 nM) afforded no detectable rat plasma levels after intraperitoneal (ip) or oral (po) dosing, compounds 3-3 (rCRF K(i) = 16 nM) and 3-4 (rCRF K(i) = 59 nM) gave high rat plasma levels at 30 mg/kg (ip, po) (C(max) = 1389 nM and 8581 nM (ip) respectively; C(max) = 113 nM and 988 nM (po), respectively). Furthermore 3-3 and 3-4 had superior bioavailabilities at these doses (59 and 46% (ip), respectively; 2 and 10% (po), respectively). (C) 1999 DuPont Pharmaceuticals Company.