527-62-8Relevant academic research and scientific papers
BENZIMIDAZOLE COMPOUNDS
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Page/Page column 79-80, (2008/12/05)
There is provided a compound of the formula (1) wherein R1 is an optionally substituted C1-10 alkyl; R2 is H, or a C1-6 alkyl which may be substituted with 1 to 3 substituents; R3 is a 5- or 6-membered aromatic group which may be substituted with 1 to 5 substituents, wherein the 5- or 6-membered aromatic group may be fused with a 5- or 6- membered ring which may be substituted with 1 to 3 C1-6 alkyls; R4 is a hydrogen, a halogen, a hydroxy, a cyano, a C1-6 alkyl or a C1-6 alkoxy; Z is -O-, -S-, -SO-, -SO2-, or - NR5- wherein R5 is a hydrogen or a C1-6 alkyl; or a salt thereof or a prodrug thereof, which have CRF receptor antagonist activity and use thereof.
Regulatory molecules for the 5-HT3 receptor ion channel gating system
Yoshida, Satoshi,Watanabe, Takashi,Sato, Yasuo
, p. 3515 - 3523 (2008/02/07)
Substituted benzoxazole derivatives which possess a nitrogen-containing heterocycle at C2 are selective partial agonists of the 5-HT3 receptor. Alteration of substituents on the benzoxazole nucleus affords both agonist-like and antagonist-like compounds, and uniquely modifies the function of the 5-HT3 receptor ion channel gating system. SAR and corroborative computational docking study for these partial agonists successfully explained structure and function of the 5-HT3 receptor.
Pyrazolopyrimidines as therapeutic agents
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, (2008/06/13)
The present invention is directed to pyrazolopyrimidine derivatives of formula (I) wherein the substituents are defined herein, which are useful as kinase inhibitors and as such are useful for affecting angiogenesis and diseases and conditions associated with angiogenesis.
Oxamide inhibitors of plasminogen activator inhibitor-1
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Page/Page column 12, (2010/02/11)
Methods of treating disorders associated with elevated levels of PAI-1 are disclosed comprising administering to a patient in need thereof a therapeutically effective amount of at least one compound of formula at least one compound of formula (I), or a pharmaceutically-acceptable salt, prodrug, stereoismer or solvate thereof, wherein: A is aryl or heteroaryl, X is O or S, and R1-R9 and R18 are defined herein. The invention also pertains to pharmaceutical compositions and compounds within the scope of formula (I) as well as medicaments and articles of manufacture comprising compounds of formula (I).
Pyrazolopyrimidines as therapeutic agents
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, (2008/06/13)
The present invention provides compounds of Formula I, including pharmaceutically acceptable salts and/or prodrugs thereof, where G, R2, and R3 are defined as described herein.
A new intramolecular migration of the imino group of O-arylketoximes to the aryl group under the Beckmann condition
Kikugawa, Yasuo,Tsuji, Chiho,Miyazawa, Etsuko,Sakamoto, Takeshi
, p. 2337 - 2339 (2007/10/03)
ZrCl4-mediated decomposition of O-arylketoximes in benzene leads to regioselective intramolecular migration of the imino group from the oxygen to the ortho position of the aryl group via electron-deficient nitrogen intermediates.
IL-8 RECEPTOR ANTAGONISTS
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, (2008/06/13)
The present invention relates to novel compounds and a novel use of phenyl ureas in the treatment of disease states mediated by the chemokine Interleukin-8 (IL-8).
IL-8 RECEPTOR ANTAGONISTS
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, (2008/06/13)
This invention relates to the novel use of phenyl ureas in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).
Novel inhibitors of bacterial two-component systems with gram positive antibacterial activity: Pharmacophore identification based on the screening hit closantel
Hlasta, Dennis J.,Demers, James P.,Foleno, Barbara D.,Fraga-Spano, Stephanie A.,Guan, Jihua,Hilliard, Jamese J.,Macielag, Mark J.,Ohemeng, Kwasi A.,Sheppard, Cheryl M.,Sui, Zhihua,Webb, Glenda C.,Weidner-Wells, Michele A.,Werblood, Harvey,Barrett, John F.
, p. 1923 - 1928 (2007/10/03)
This SAR study has shown that the salicylanilide is the pharmacophore for inhibition of the bacterial two-component system. Hydrophobic substituents improve the potency of inhibitors in this series; however, hydrophobicity is not the sole determinant for inhibition; structural and electronic requirements also exist. Closantel (1) was found to inhibit a two- component system and to have antibacterial activity against drug resistant S. aureus and E. faecium.
Benzoxazole derivatives as novel 5-HT3 receptor partial agonists in the gut
Sato, Yasuo,Yamada, Megumi,Yoshida, Satoshi,Soneda, Tomoko,Ishikawa, Midori,Nizato, Tetsutaro,Suzuki, Kokichi,Konno, Fukio
, p. 3015 - 3021 (2007/10/03)
A series of benzoxazoles with a nitrogen-containing heterocyclic substituent at the 2-position was prepared and evaluated for 5-HT3 partial agonist activity on isolated guinea pig ileum. The nature of the substituent at the 5-position of the benzoxazole ring affected the potency for the 5-HTs receptor, and the 5-chloro derivatives showed increased potency and lowered intrinsic activity. 5-Chloro-7-methyl-2-(4-methyl-1- homopiperazinyl)benzoxazole (6v) exhibited a high binding affinity in the same range as that of the 5-HT3 antagonist granisetron, and its intrinsic activity was 12% of that of 5-HT. Compound 6v inhibited 5-HT-evoked diarrhea but did not prolong the transition time of glass beads in the normal distal colon even at a dose of 100 times the ED50 for diarrhea inhibition in mice. Compounds of this type are expected to be effective for the treatment of irritable bowel syndrome without the side effect of constipation.
