223553-68-2Relevant articles and documents
SUBSTITUTED NAPHTHYRIDINES AND THEIR USE AS MEDICAMENTS
-
Page/Page column 37; 42, (2012/02/06)
The invention relates to new substituted naphthyridines of formula 1, as well as pharmacologically acceptable salts, diastereomers, enantiomers, racemates, hydrates or solvates thereof, wherein R1 is selected from among —O—R3 or —NR3R4,R3 is C1-6-alkyl which is substituted by R5 and R6,R5 is selected from hydrogen, branched or linear C1-6-alkyl, C2-6-alkenyl, —C1-6-alkylen-O—C1-3-alkyl, C1-3-haloalkyl,R6 is ring X wherein n is either 0 or 1, and is a either a single or a double bond andwherein A, B, D and E are each independently from one another selected from CH2, CH, C, N, NH, O or S and wherein ring X is attached to the molecule either via position A, B, D or E, wherein said ring X may optionally be further substituted by one, two or three residues each selected individually from the group consisting of -oxo, hydroxy, —C1-3-alkyl, —C1-3-haloalkyl, —O—C1-3-alkyl, —C1-3-alkanol and halogen,and wherein R4, R2, R7, R8, R9, R10, R11 and Q may have the meanings as given in claim 1, as well as pharmaceutical compositions containing these compounds.
Discovery and SAR of novel [1,6]naphthyridines as potent inhibitors of Spleen Tyrosine Kinase (SYK)
Cywin, Charles L.,Zhao, Bao-Ping,McNeil, Daniel W.,Hrapchak, Matt,Prokopowicz III, Anthony S.,Goldberg, Daniel R.,Morwick, Tina M.,Gao, Amy,Jakes, Scott,Kashem, Mohammed,Magolda, Ronald L.,Soll, Richard M.,Player, Mark R.,Bobko, Mark A.,Rinker, James,DesJarlais, Renee L.,Winters, Michael P.
, p. 1415 - 1418 (2007/10/03)
The discovery of novel 5,7-disubstituted[1,6]naphthyridines as potent inhibitors of Spleen Tyrosine Kinase (SYK) is discussed. The SAR reveals the necessity for a 7-aryl group with preference towards para substitution and that this in combination with 5-aminoalkylamino substituents further improved the potency of the compounds. The initial SAR as well as a survey of the other positions is discussed in detail.
