- 2,4-DIARYL - SUBSTITUTED [1,8] NAPHTHYRIDINES AS KINASE INHIBITORS FOR USE AGAINST CANCER
-
The present invention relates to novel [1,8]naphthyridine derivatives of formula (I) and to the use of such compounds in which the inhibition, regulation and/or modulation of signal transduction by ATP consuming proteins like kinases plays a role, particu
- -
-
Paragraph 0522; 0523
(2013/05/08)
-
- 2,4- DIARYL-SUBSTITUTED [1,8] NAPHTHYRIDINES AS KINASE INHIBITORS FOR USE AGAINST CANCER
-
The present invention relates to novel [1,8]naphthyridine derivatives of formula (I) and to the use of such compounds in which the inhibition, regulation and/or modulation of signal transduction by ATP consuming proteins like kinases playsa role, particularly to inhibitors of TGF-beta receptor kinases, and to the use of such compounds for the treatment of kinase-induced diseases, in particular for the treatment of tumors
- -
-
Page/Page column 117
(2012/01/14)
-
- Identification of novel and potent isoquinoline aminooxazole-based IMPDH inhibitors
-
Screening of our in-house compound collection led to the discovery of 5-bromo-6-amino-2-isoquinoline 1 as a weak inhibitor of IMPDH. Subsequent optimization of 1 afforded a series of novel 2-isoquinolinoaminooxazole-based inhibitors, represented by 17, with single-digit nanomolar potency against the enzyme.
- Chen, Ping,Norris, Derek,Haslow, Kristin D.,Dhar, T. G. Murali,Pitts, William J.,Watterson, Scott H.,Cheney, Daniel L.,Bassolino, Donna A.,Fleener, Catherine A.,Rouleau, Katherine A.,Hollenbaugh, Diane L.,Townsend, Robert M.,Barrish, Joel C.,Iwanowicz, Edwin J.
-
p. 1345 - 1348
(2007/10/03)
-