310887-39-9Relevant academic research and scientific papers
HETEROARYL-SUBSTITUTED TRIAZOLES AS APJ RECEPTOR AGONISTS
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Paragraph 0756; 0757, (2018/06/12)
Compounds of Formula (I) and Formula (II), pharmaceutically acceptable salt thereof, stereoisomers of any of the foregoing, or mixtures thereof are agonists of the APJ Receptor and may have use in treating cardiovascular and other conditions. Compounds of Formula I and Formula II have the following structures: where the definitions of the variables are provided herein.
HEPARANASE INHIBITORS AND USE THEREOF
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Paragraph 0188, (2018/07/05)
The invention relates to functionalized quinazoline compounds, pharmaceutical compositions comprising such compounds, and the use of such compounds as heparanase inhibitors for the treatment of diseases or conditions related to heparanse activity.
The optimization of aminooxadiazoles as orally active inhibitors of Cdc7
Harrington, Paul E.,Bourbeau, Matthew P.,Fotsch, Christopher,Frohn, Michael,Pickrell, Alexander J.,Reichelt, Andreas,Sham, Kelvin,Siegmund, Aaron C.,Bailis, Julie M.,Bush, Tammy,Escobar, Sonia,Hickman, Dean,Heller, Scott,Hsieh, Faye,Orf, Jessica N.,Rong, Minqing,San Miguel, Tisha,Tan, Helming,Zalameda, Leeanne,Allen, John G.
, p. 6396 - 6400 (2013/11/19)
A series of aminooxadiazoles was optimized for inhibition of Cdc7. Early lead isoquinoline 1 suffered from modest cell potency (cellular IC50 = 0.71 μM measuring pMCM2), low selectivity against structurally related kinases, and high IV clearance in rats (CL = 18 L/h/kg). Extensive optimization resulted in azaindole 26 (Cdc7 IC50 = 1.1 nM, pMCM2 IC50 = 32 nM) that demonstrated robust lowering of pMCM2 in a mouse pharmacodynamic (PD) model when dosed orally. Modifications to improve the pharmacokinetic profile of this series were guided by trapping experiments with glutathione in rat hepatocytes.
7-AZAINDOLE DERIVATIVES
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Page/Page column 23, (2011/07/29)
Novel 7-azaindole derivatives of the formula (I), in which U, L, R, Y, X1, X2 and X3 have the meanings indicated in Claim 1), are kinase inhibitors and can be used for the treatment of diseases and conditions such as diabe
OXADIAZOLE DERIVATIVES AND THEIR USE AS NICOTINIC ACETYLCHOLINE RECEPTOR MODULATORS
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Page/Page column 52, (2009/07/17)
Oxadiazole derivatives of formula (I) where ring A is a bicyclic or tricyclic system. Claimed compounds are active on nicotinic acetylcholine receptors (nAChRs), and are useful to treat neurological, psychiatric, and gastrointestinal disorders, as well as sepsis and obesity.
Pharmaceutically active compounds
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, (2008/06/13)
The present invention relates to novel compounds which are protein kinase C inhibitors, methods for their preparation, intermediates therefor and pharmaceutical compositions comprising them. More particularly, the present invention relates to compounds of formula (I): wherein: one of Ar1and Ar2is optionally substituted bicyclic heteroaryl or optionally substituted tricyclic heteroaryl and the other is optionally substituted heteroaryl or optionally substituted aryl; X is O or S; and R is H, OH, NH2or C1-6alkyl (itself optionally substituted by amino or hydroxy); or a salt or solvate thereof, or a solvate of a salt thereof; and the use of such compounds in medical therapies.
