106976-24-3Relevant articles and documents
DUAL ATM AND DNA-PK INHIBITORS FOR USE IN ANTI-TUMOR THERAPY
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Page/Page column 147, (2019/11/12)
Provided herein are compounds of the Formula (I), (II), and (III), as well as pharmaceutically acceptable salts thereof, wherein the substituents are those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of oncologic diseases.
Novel Fused Arylpyrimidinone Based Allosteric Modulators of the M1 Muscarinic Acetylcholine Receptor
Mistry, Shailesh N.,Lim, Herman,J?rg, Manuela,Capuano, Ben,Christopoulos, Arthur,Lane, J. Robert,Scammells, Peter J.
, p. 647 - 661 (2016/06/01)
Benzoquinazolinone 1 is a positive allosteric modulator (PAM) of the M1 muscarinic acetylcholine receptor (mAChR), which is significantly more potent than the prototypical PAM, 1-(4-methoxybenzyl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (BQCA). In this study, we explored the structural determinants that underlie the activity of 1 as a PAM of the M1 mAChR. We paid particular attention to the importance of the tricyclic scaffold of compound 1, for the activity of the molecule. Complete deletion of the peripheral fused benzene ring caused a significant decrease in affinity and binding cooperativity with acetylcholine (ACh). This loss of affinity was rescued with the addition of either one or two methyl groups in the 7- and/or 8-position of the quinazolin-4(3H)-one core. These results demonstrate that the tricyclic benzo[h]quinazolin-4(3H)-one core could be replaced with a quinazolin-4(3H)-one core and maintain functional affinity. As such, the quinazolin-4(3H)-one core represents a novel scaffold to further explore M1 mAChR PAMs with improved physicochemical properties.
Substituted 4-Amino-Quinazoline Compounds with Metabotropic Glutamate Receptor Regulating Activity and Uses Thereof
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Page/Page column 74, (2009/04/24)
Substituted 4-amino-quinazoline compounds corresponding to formula I methods for their production, pharmaceutical compositions containing these compounds as active agents, and the uses thereof for treating or inhibiting disorders or disease states.