914074-37-6Relevant articles and documents
Discovery of selective PDE4B inhibitors
Naganuma, Kenji,Omura, Akifumi,Maekawara, Naomi,Saitoh, Masahiro,Ohkawa, Naoto,Kubota, Takashi,Nagumo, Hiromitsu,Kodama, Toshiyuki,Takemura, Masayoshi,Ohtsuka, Yuji,Nakamura, Junji,Tsujita, Ryuichi,Kawasaki, Koh,Yokoi, Hirotsugu,Kawanishi, Masashi
scheme or table, p. 3174 - 3176 (2010/03/24)
In this study the first PDE4B selective inhibitor is described. Optimization of lead 2-arylpyrimidine derivatives afforded a series of potent PDE4B inhibitors with >100-fold selectivity over the PDE4D isozyme. With a good pharmacokinetic profile, a selected compound exhibited potent anti-inflammatory effects in vivo and showed less emesis compared with Cilomilast.
SUBSTITUTED CARBOXAMIDES METHOD FOR PRODUCTION AND USE THEREOF AS TNF-ALPHA RELEASE INHIBITORS
-
, (2010/11/24)
The invention relates to novel agents of formula (I), where R1 = aryl, optionally substituted with C1 to C5 alkyl, C2 to C5 alkenyl, C1 to C5 O-alkyl, aryloxy (O-aryl), C1/
3-Amino-1H-pyrazolopyrimidines and 3-Aminoisothiazolopyrimidines as Precursors of Tricyclic Heteroaromatic Systems Containing a Bridgehead Nitrogen Atom.
Golec, Julian M. C.,Scrowston, Richard M.
, p. 326 - 345 (2007/10/02)
3-Amino-4-methyl-6-phenyl-1H-pyrazolopyrimidine (3a) and 3-amino-4-methyl-6-phenylisothiazolopyrimidine (9a) have been prepared.The former reacts with bromoacetone or 3-bromopentane-2,4-dione, to give tricyclic systems (1a) or (13) containing an extra pyrazole or pyrimidine ring, respectively; in each case the newly formed ring contains a bridgehead nitrogen atom, derived from N-2 of the starting material.With the same reagents, the latter undergoes an interesting ring-opening reaction, for which possible mechanisms are proposed.In contrast, 3-amino-1,2-benzisothiazole does not undergo ring fission under similar conditions, but gives rise to tricyclic compounds containing a bridgehead nitrogen atom.
