36947-69-0Relevant academic research and scientific papers
Imidazole-based pinanamine derivatives: Discovery of dual inhibitors of the wild-type and drug-resistant mutant of the influenza A virus
Dong, Jianghong,Chen, Shengwei,Li, Runfeng,Cui, Wei,Jiang, Haiming,Ling, Yixia,Yang, Zifeng,Hu, Wenhui
, p. 605 - 615 (2015/12/30)
We previously reported potent hit compound 4 inhibiting the wild-type influenza A virus A/HK/68 (H3N2) and A/M2-S31N mutant viruses A/WS/33 (H1N1), with its latter activity quite weak. To further increase its potency, a structure-activity relationship study of a series of imidazole-linked pinanamine derivatives was conducted by modifying the imidazole ring of this compound. Several compounds of this series inhibited the amantadine-sensitive virus at low micromolar concentrations. Among them, 33 was the most potent compound, which was identified as being active on an amantadine-sensitive virus through blocking of the viral M2 ion channel. Furthermore, 33 markedly inhibited the amantadine-resistant virus (IC50 = 3.4 μM) and its activity increased by almost 24-fold compared to initial compound, with its action mechanism being not M2 channel mediated.
Novel Heterocyclic Compounds and Uses Thereof
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Paragraph 0332, (2013/08/28)
New substituted heterocyclic compounds, compositions containing them, and methods of using them for the inhibition of Raf kinase activity are provided. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.
LRRK2 INHIBITORS
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Page/Page column 116-117, (2013/02/28)
Provided herein are compounds that inhibit or partially inhibit the activity of leucine rich repeat kinases. Also provided herein are methods of treatment of CNS disorders comprising administration of inhibitors of leucine rich repeat kinases.
Compounds and Compositions as Protein Kinase Inhibitors
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, (2011/04/14)
The present invention provides compounds of Formula I or II: wherein R1, R1b, R2, R3, R4, R5, R6 and R7 are defined herein. The compounds of Formula (I) or (II) and pharmaceutical compositions thereof are useful for the treatment of B-Raf-associated diseases.
NOVEL HETEROCYCLIC COMPOUNDS AND USES THEROF
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Page/Page column 99, (2009/10/22)
New substituted heterocyclic compounds, compositions containing them, and methods of using them for the inhibition of Raf kinase activity are provided. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.
IMIDAZOLE DERIVATIVE
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Page/Page column 65, (2009/09/05)
A CB2 receptor modulator comprising an imidazole derivative represented by the general formula (I): [wherein, R1 represents optionally substituted lower alkyl or the like; R2 represents optionally substituted cycloalkyl or the like; R3 represents optionally substituted aryl or the like; and n represents an integer of 0 to 3] or a pharmaceutically acceptable salt thereof as an active ingredient, and the like are provided.
An efficient synthesis of 2-arylimidazoles by oxidation of 2-arylimidazolines using activated carbon-O2 system and its application to palladium-catalyzed Mizoroki-Heck reaction
Haneda, Satoshi,Okui, Ayaka,Ueba, Chigusa,Hayashi, Masahiko
, p. 2414 - 2417 (2007/10/03)
Oxidative conversion of 2-substituted imidazoline (dihydroimidazole) to the corresponding imidazole was achieved by an activated carbon-O2 system. Also, the 2-arylimidazolines and 2-arylimidazoles have been found to work as simple ligands in the palladium-catalyzed Mizoroki-Heck reaction.
NOVEL COMPOUNDS
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Page/Page column 32, (2010/02/07)
Compounds of formula (I): are inhibitors of the enzyme Lp-PLA2 and are of use in therapy, in particular for treating atherosclerosis. In Formula (I) R1, R2, R3, R4, R5, R6, X and Y are as d
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.
