200267-65-8Relevant academic research and scientific papers
Thiazolinone unsubstituted quinolines
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Page/Page column 16, (2010/02/15)
Thiazolinone quinoline derivatives having no substitution on the quinoline ring active as CDK1 inhibitors which are useful as anti-proliferation agents such as for treating solid tumors.
Azaindole thiazolinones
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Page/Page column 18, (2010/10/20)
Azaindole thiazolinone derivatives which demonstrate CDK1 and CDK2 antiproliferative activities and are useful as anti-cancer agents.
Fused purine derivatives
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, (2008/06/13)
A condensed purine derivative represented by Formula (I): wherein X—Y—Z represents R1N—C═O or N═C—W, R2 represents a hydrogen atom, a substituted or unsubstituted lower alkyl group, a substituted or unsubstituted aralkyl group, a substituted or unsubstituted aryl group, a substituted or unsubstituted aromatic heterocyclic group, a substituted or unsubstituted alicyclic heterocyclic group or the like, n represents an integer of from 0 to 3, V1 represents a hydrogen atom, a substituted or unsubstituted lower alkyl group, a substituted or unsubstituted aralkyl group, a substituted or unsubstituted aryl group, or a substituted or unsubstituted aromatic heterocyclic group, V2 represents a substituted lower alkyl group or a substituted or unsubstituted aromatic heterocyclic group, and when V1 represents a hydrogen atom, a lower alkyl group, a substituted or unsubstituted aralkyl group, or a substituted or unsubstituted aryl group, and for example, X—Y—Z represents R1aN—C═O and R2 represents a substituted lower alkyl group, a substituted or unsubstituted aralkyl group, a substituted or unsubstituted alicyclic heterocyclic group, a halogen atom, a lower alkylthio group, —NR7R8, —CO2H, a lower alkoxycarbonyl group, —COHal, —CONR9R10 or —CHO, V2 may represent a lower alkyl group, a substituted or unsubstituted aralkyl group, or a substituted or unsubstituted aryl group; or a pharmacologically acceptable salt thereof.
Remedies for diabetes
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, (2008/06/13)
A medicament for the therapeutic treatment of diabetes which comprises as an active ingredient a compound represented by the general formula (I): wherein R1represents a hydrogen atom, a lower alkyl group, a substituted or unsubstituted aryl gro
Tricyclic erythromycin derivatives
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, (2008/06/13)
Compounds, or pharmaceutically acceptable salts and esters thereof, of the formula: wherein A, B, D and E, R1, R2, and Z are specifically defined, having antibacterial activity, pharmaceutical compositions containing said compounds, treatment of bacterial infections with such compositions, and processes for the preparation of the compounds.
Benzoxazolamines and Benzothiazolamines: Potent, Enantioselective Inhibitors of Leukotriene Biosynthesis with a Novel Mechanism of Action
Lazer, Edward S.,Miao, Clara K.,Wong, Hin-Chor,Sorcek, Ronald,Spero, Denice M.,et al.
, p. 913 - 923 (2007/10/02)
A series of benzoxazolamine and benzothiazolamine analogs that inhibit leukotriene (LT) biosynthesis are described.The initial lead, (S)-N-(benzothiazol-2-yl)phenylalanine ethyl ester (5a), was discovered in a screening program for inhibition of Ca-ionophore-A23187-induced LTB4 release in human polymorphonuclear leukocytes (IC50 0.23 μM).Through structural modification, it was determined that hydrophobic substituents in the 5-position and replacement of the phenyl ring of phenylalanine with a cyclohexyl group greatly enhance potency.Several ester bioisosteres that retain potency and enantiomeric selectivity are described.Lead optimization culminated in (S)-N--5-methyl-2-benzoxazolamine (43b), IC50 0.001 μM.The compounds described are not inhibitors of 5-lipoxygenase but, rather, act at the level of arachidonic acid release.
