23230-39-9Relevant academic research and scientific papers
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
Carboxyimidazole histone deacetylase inhibitor
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Paragraph 0039; 0040, (2018/06/15)
The invention belongs to the field of medicinal chemistry, and concretely relates to carboxyimidazole histone deacetylase inhibitors, medicine compositions containing the histone deacetylase inhibitors, and a use of the inhibitors in the preparation of medicines for preventing and/or treating histone deacetylase activity out-of-control related diseases, and especially an anticancer use.
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.
Facile synthesis of N-dialkylaminomethyl-substituted heterocycles
Love, Brian E.
, p. 630 - 632 (2007/10/03)
Iminium ions are generated by treatment of aminals with succinic anhydride. These iminium ions are trapped by heterocycles, giving the corresponding N-dialkylamino-methyl-substituted heterocycles, which are easily separated from the succinic acid monoamid
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.
5-(1-(IMIDAZOL)METHYL)-3,3-DISUBSTITUTED-2(3H)FURANONE DERIVATIVES
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, (2008/06/13)
Furanone compounds and compositions having anticholinergic activity are described. The compounds have the formula: STR1 wherein: the dashed line indicates either the 4,5-unsaturated or the 4,5-dihydrofuranone ring;R 1 and R 2 may be the same or different and are hydrogen, thienyl, furanyl, or cycloalkyl (C. sub.3-C 6), benzyl, phenyl, substituted phenyl or substituted benzyl wherein the phenyl or benzyl group may be substituted with halogen, trifluoromethyl, lower alkyl, lower alkoxy or hydroxy;R. sub.3, R 4 and R 5 may be the same or different and are hydrogen, lower alkyl, lower alkyl substituted with a halogen, alkoxy, amino or carboxylic acid group, an alkyl or alkylene bridge between R 4 and R. sub.5 or R 3 and the ring N, trifluoromethyl, nitro, a cycloalkyl group containing 3 to 6 carbons, halogen, benzyl, phenyl, substituted phenyl or substituted benzyl, for which the substituents are the same as those set forth for R 1 and R 2 substituted benzyl or phenyl.R 6 in the dihydrofuranone series is hydrogen or lower alkyl.Also described are the pharmaceutically acceptable quaternary alkyl and acid addition salts of such compounds. The compounds are particularly useful in the treatment of neurogenic bladder disorder and chronic obstructive pulmonary diseases.
Synthesis of 2-Substituted Imidazoles and Benzimidazoles and of 3-Substituted Pyrazoles by Lithiation of N-(Dialkylamino)methyl Heterocycles
Katritzky, Alan R.,Rewcastle, Gordon W.,Fan, Wei-Qiang
, p. 5685 - 5689 (2007/10/02)
The lithiation of N-(dialkylamino)methyl (aminal) derivatives of imidazole, benzimidazole, and pyrazole (themselves readily available from parent heterocycles, formaldehyde, and a secondary amine) occurs smoothly at 2-, 2-, and 5-positions, respectively, upon treatment with n-butyllithium in ether or tetrahydrofuran.Reaction with electrophiles, and subsequent facile acid-catalyzed hydrolysis of the protecting group, provides 2-substituted imidazoles, 2-substituted benzimidazoles, and 3(5)-substituted pyrazoles in good overall yields.
