Mehran F. Moghaddam

TL;DR: It is found that optimization beyond potency of degradation, including degradation efficiency and kinetics, could provide efficacy in a lenalidomide-resistant setting and a series of CELMoDs for the treatment of RRMM.

TL;DR: This Letter describes the discovery of potent, selective, and orally active aminopurine JNK inhibitors and the identification of 1 (CC-930) as a development candidate, which is currently in Phase II clinical trial for IPF.

TL;DR: Replacing liver microsome and hepatocyte assays with S9 assay for high throughput metabolic screening purposes provides the combined benefit of comprehensive and high quality data at a reasonable expense for drug discovery programs.

TL;DR: POM is a promising therapeutic agent for CNS lymphoma with excellent CNS penetration, significant preclinical therapeutic activity, and a major impact on the tumor microenvironment.

TL;DR: SAR studies examining the potency, selectivity, and PK parameters for a series of triazole containing 4,6- or 1,7-disubstituted-3,4-dihydropyrazino[2,3-b]pyrazine-2(1H)-ones resulted in the identification of triAZole containing mTOR kinase inhibitors with improved PK properties.