366445-82-1Relevant articles and documents
2,4- DIARYL-SUBSTITUTED [1,8] NAPHTHYRIDINES AS KINASE INHIBITORS FOR USE AGAINST CANCER
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Page/Page column 118, (2012/01/14)
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
ISOQUINOLINE DERIVATIVES
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Page/Page column 36-37, (2008/06/13)
The invention relates to isoquinoline derivatives having the general Formula (I) wherein X is O, S or NH; Y is OH or NH2; m is 0, 1 or 2; n is 1 or 2; R1 is H, when Y is NH2; or R1 is H, (C1-4)alkyl or halogen, when Y is OH; R2 and R3 are independently H, (C1-4)alkyl or halogen; R is H or (C1-6)alkyl, optionally substituted with OH, (C1-4)- alkyloxy, (C1-4)alkyloxycarbonyl, (C3-7)cycloalkyl, which may optionally comprise a heteroatom selected from O and S, (C6-10)aryl, (C6-10)aryloxy or a 5- or 6-membered heteroaryl group comprising 1-3 heteroatoms independently selected from O, N and S, each aryl or heteroaryl group being optionally substituted with 1-3 substituents independently selected from (C1-4)alkyl, (C1-4)alkyloxy, (C1-4)alkylsulfonyl and halogen; or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same as well as to the use of the isoquinoline derivatives in the treatment of ROCK-I related disorders such as hypertension, atherosclerosis and glaucoma.
Identification of novel and potent isoquinoline aminooxazole-based IMPDH inhibitors
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)
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.