64951-06-0Relevant articles and documents
TRICYCLIC PESTICIDAL COMPOUNDS
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Page/Page column 81, (2021/10/22)
The invention relates to compounds of formula (I), wherein the variables are as defined in the specification. It also relates to the use of compounds of formula (I) as an agrochemical pesticide; to pesticidal mixtures comprising compounds of formula (I); and to agrochemical or veterinary compositions comprising compounds of formula (I). Other objects are seed comprising compounds of formula (I); and methods for controlling invertebrate pests, infestation, or infection by invertebrate pests by application of compounds of formula (I).
Efficient Access to Imidazo[1,2- a] pyridines/pyrazines/pyrimidines via Catalyst-Free Annulation Reaction under Microwave Irradiation in Green Solvent
Rao, R. Nishanth,Mm, Balamurali,Maiti, Barnali,Thakuria, Ranjit,Chanda, Kaushik
supporting information, p. 164 - 171 (2018/03/21)
An expeditious catalyst-free heteroannulation reaction for imidazo[1,2-a]pyridines/pyrimidines/pyrazines was developed in green solvent under microwave irradiation. Using H2O-IPA as the reaction medium, various substituted 2-aminopyridines/pyra
Discovery of 6-(Aminomethyl)-5-(2,4-dichlorophenyl)-7-methylimidazo[1,2- α]pyrimidine-2-carboxamides as potent, selective dipeptidyl peptidase-4 (DPP4) inhibitors
Meng, Wei,Brigance, Robert P.,Chao, Hannguang J.,Fura, Aberra,Harrity, Thomas,Marcinkeviciene, Jovita,O'connor, Stephen P.,Tamura, James K.,Xie, Dianlin,Zhang, Yaqun,Klei, Herbert E.,Kish, Kevin,Weigelt, Carolyn A.,Turdi, Huji,Wang, Aiying,Zahler, Robert,Kirby, Mark S.,Hamann, Lawrence G.
experimental part, p. 5620 - 5628 (2010/10/20)
Continued structure-activity relationship (SAR) exploration within our previously disclosed azolopyrimidine containing dipeptidyl peptidase-4 (DPP4) inhibitors led us to focus on an imidazolopyrimidine series in particular. Further study revealed that by replacing the aryl substitution on the imidazole ring with a more polar carboxylic ester or amide, these compounds displayed not only increased DPP4 binding activity but also significantly reduced human ether-à-go-go related gene (hERG) and sodium channel inhibitory activities. Additional incremental adjustment of polarity led to permeable molecules which exhibited favorable pharmacokinetic (PK) profiles in preclinical animal species. The active site binding mode of these compounds was determined by X-ray crystallography as exemplified by amide 24c. A subsequent lead molecule from this series, (+)-6-(aminomethyl)-5-(2,4-dichlorophenyl)-N-(1-ethyl-1H- pyrazol-5-yl)-7-methylimidazo[1,2-a]pyrimidine-2-carboxamide (24s), emerged as a potent, selective DPP4 inhibitor that displayed excellent PK profiles and in vivo efficacy in ob/ob mice.