364794-58-1Relevant articles and documents
TETRAHYDROBENZOFURO[2,3-C]PYRIDINE AND BETA-CARBOLINE COMPOUNDS FOR THE TREATMENT, ALLEVIATION OR PREVENTION OF DISORDERS ASSOCIATED WITH TAU AGGREGATES
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Page/Page column 76, (2019/12/28)
The present invention relates to novel compounds of formula (I) that can be employed in the treatment, alleviation or prevention of a group of disorders and abnormalities associated with Tau (Tubulin associated unit) protein aggregates including, but not limited to, Neurofibrillary Tangles (NFTs), such as Alzheimer's disease (AD).
Inverting Conventional Chemoselectivity in Pd-Catalyzed Amine Arylations with Multiply Halogenated Pyridines
Keylor, Mitchell H.,Niemeyer, Zachary L.,Sigman, Matthew S.,Tan, Kian L.
supporting information, p. 10613 - 10616 (2017/08/15)
A new catalyst system capable of selective chloride functionalization in the Pd-catalyzed amination of 3,2- and 5,2- Br/Cl-pyridines is reported. A reaction optimization strategy employing ligand parametrization led to the identification of 1,1′-bis[bis(dimethylamino)phosphino]ferrocene "DMAPF", a readily available yet previously unutilized diphosphine, as a uniquely effective ligand for this transformation.
Discovery of Pyrazolopyridones as a Novel Class of Gyrase B Inhibitors Using Structure Guided Design
Cross, Jason B.,Zhang, Jing,Yang, Qingyi,Mesleh, Michael F.,Romero, Jan Antoinette C.,Wang, Bin,Bevan, Doug,Poutsiaka, Katherine M.,Epie, Felix,Moy, Terence,Daniel, Anu,Shotwell, Joseph,Chamberlain, Brian,Carter, Nicole,Andersen, Ole,Barker, John,Ryan, M. Dominic,Metcalf, Chester A.,Silverman, Jared,Nguyen, Kien,Lippa, Blaise,Dolle, Roland E.
supporting information, p. 374 - 378 (2016/05/19)
The ATPase subunit of DNA gyrase B is an attractive antibacterial target due to high conservation across bacteria and the essential role it plays in DNA replication. A novel class of pyrazolopyridone inhibitors was discovered by optimizing a fragment screening hit scaffold using structure guided design. These inhibitors show potent Gram-positive antibacterial activity and low resistance incidence against clinically important pathogens.