225666-34-2Relevant academic research and scientific papers
Discovery of a new series of potent prostacyclin receptor agonists with in vivo activity in rat
Tran, Thuy-Anh,Shin, Young-Jun,Kramer, Bryan,Choi, Juyi,Zou, Ning,Vallar, Pureza,Martens, Peter,Douglas Boatman,Adams, John W.,Ramirez, Juan,Shi, Yunqing,Morgan, Michael,Unett, David J.,Chang, Steve,Shu, Hsin-Hui,Tung, Shiu-Feng,Semple, Graeme
, p. 1030 - 1035 (2015/02/19)
The design and synthesis of two closely related series of prostacyclin receptor agonist compounds that showed excellent human IP receptor potency and efficacy is described. Compounds from this series showed in vivo activity after SC dosing in the monocrotaline model of PAH in rat.
Pyridazine compounds and compositions containing the same
-
Page column 19, (2008/06/13)
This invention relates to pyridazine derivatives represented by the formula (1): wherein R1represents a (substituted) aryl group, R2represents a phenyl group substituted at 4-position by a lower alkoxyl group or a lower alkylthio group, R3represents a lower alkoxyl group, a halogenated lower alkyl group, a lower cycloalkyl group, a (subsituted) aryl group, a (substituted) aryloxy group, a (substituted) nitrogen-containing heterocyclic ring residue, a (substituted) aminocarbonyl group or a lower alkylcarbonyl group, A represents a single bond, a lower alkylene group or a lower alkenylene group, X represents O or S, and the dashed line indicates that the carbon-carbon bond between the 4-position and the 5-position is a single bond or a double bond, or salts thereof; and also to medicines containing them as effective ingredients. These compounds have excellent inhibitory activity against interleukin-1β production, and are useful as preventives and therapeutics for immune system diseases, inflammatory diseases, ischemic diseases and the like.
Mono- and di-substituted 5,6-diphenyl-3-alkylaminopyridazines active as ACAT inhibitors
Toma, Lucio,Giovannoni, Maria Paola,Dal Piaz, Vittorio,Kwon, Byoung-Mog,Kim, Young-Kook,Gelain, Arianna,Barlocco, Daniela
, p. 39 - 46 (2007/10/03)
A series of mono- or di-para-substituted 5,6-diphenyl-3-alkylaminopyridazines were synthesized and their inhibitory activity against acyl-CoA:cholesterol acyltransferase (ACAT) was tested on the enzyme prepared from rat liver microsomes. The compound which combines a chlorine atom on the 6-phenyl ring and a n-hexylamino chain showed a significant enhancement of activity with respect to the unsubstituted derivative. Attempts to correlate the activity of the compounds to their structural features, also through theoretical calculations, are reported.
