26820-34-8Relevant articles and documents
Discovery and optimization of thienopyridine derivatives as novel urea transporter inhibitors
Zhao, Yan,Li, Min,Li, Bowen,Zhang, Shun,Su, Aoze,Xing, Yongning,Ge, Zemei,Li, Runtao,Yang, Baoxue
, p. 131 - 142 (2019/04/08)
Urea transporters (UTs) play an important role in the urine concentrating mechanism and are recognized as novel targets for developing small molecule inhibitors with salt-sparing diuretic activity. Thienoquinoline derivatives, a class of novel UT-B inhibitors identified by our group, play a significant diuresis in animal model. However, the poor solubility and low bioavailability limited its further development. To overcome these shortcomings, the structure modification of thienoquinoline was carried out in this study, which led to the discovery of novel thienopyridine derivatives as specific urea transporter inhibitors. Further optimization obtained the promising preclinical candidate 8n with not only excellent inhibition effect on urea transporters and diuretic activity on rat model, but also suitable water solubility and Log P value.
PYRIDYL COMPOUND SUITABLE FOR THE TREATMENT OF METABOLIC DISORDERS
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Page/Page column 56, (2015/01/16)
The description relates to a pyridyl compound of Formula 1 wherein A, B, X, R1, R2, R3, R4, R5, R6, and n are as defined in the specification, in all their isotopic forms, stereoisomeric and tautomeric forms and mixtures thereof in all ratios, their pharmaceutically acceptable salts, N-oxides, pharmaceutically acceptable solvates, isosteres and prodrugs thereof, which are useful in treating metabolic disorders related to insulin resistance or hyperglycemia. The description also relates to a process for the manufacture of the pyridyl compound and a pharmaceutical composition containing the pyridyl compound.
NOVEL MICROBIOCIDES
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, (2008/12/08)
Compounds of the formula (I) in which the substituents are as defined in claim 1 are suitable for use as microbiocides.