1374150-56-7

Upstream product

• 74-96-4 ethyl bromide 
• 82104-74-3 1-oxo-1,3-dihydro-isobenzofuran-5-carbonitrile 
• 75-03-6 ethyl iodide 

Downstream Products

• 1374150-03-4 N-{2-[5-(2-amino-pyrimidin-5-yl)-1-tert-butyl-1H-benzoimidazol-2-yl]-4-cyano-benzoyl}-methanesulfonamide 
• 1374150-00-1 2-[5-(2-amino-pyrimidin-5-yl)-1-tert-butyl-1H-benzoimidazol-2-yl]-4-cyano-N-cyano-benzamide 
• 1374150-59-0 C₂₃H₂₀N₆O₂ 
• 1374149-97-9 2-[5-(2-amino-pyrimidin-5-yl)-1-tert-butyl-1H-benzoimidazol-2-yl]-N-methyl-4-(2H-tetrazol-5-yl)-benzamide 
• 1374150-58-9 C₂₅H₂₄N₆O₂ 
• 1374149-92-4 2-[5-(2-amino-pyrimidin-5-yl)-1-tert-butyl-1H-benzoimidazol-2-yl]-4-cyano-N-methyl-benzamide 
• 1374150-57-8 C₁₁H₉NO₃ 

Relevant academic research and scientific papers

Tunable pH-sensitive 2-carboxybenzyl phosphoramidate cleavable linkers

We previously described a pH-sensitive phosphoramidate linker scaffold that can be tuned to release amine-containing drugs at various pH values. In these previous studies it was determined that the tunability of this linker was dependent upon the proximity of an acidic group (e.g., carboxylic acid or pyridinium). In this study, we confirmed that the tunability of pH-triggered amine-release was also dependent upon the pKa of the proximal acidic group. A series of 2-carboxybenzyl phosphoramidates was prepared in which the pKa of the proximal benzoic acid was predictably attenuated by substituents on the benzoate ring consistent with their σ-values.

CC-90009: A Cereblon E3 Ligase Modulating Drug That Promotes Selective Degradation of GSPT1 for the Treatment of Acute Myeloid Leukemia

Acute myeloid leukemia (AML) is marked by significant unmet clinical need due to both poor survival and high relapse rates where long-term disease control for most patients with relapsed or refractory AML remain dismal. Inspired to bring novel therapeutic options to these patients, we envisioned protein degradation as a potential therapeutic approach for the treatment of AML. Following this course, we discovered and pioneered a novel mechanism of action which culminated in the discovery of CC-90009. CC-90009 represents a novel protein degrader and the first cereblon E3 ligase modulating drug to enter clinical development that specifically targets GSPT1 (G1 to S phase transition 1) for proteasomal degradation. This manuscript briefly summarizes the mechanism of action, scientific rationale, medicinal chemistry, pharmacokinetic properties, and efficacy data for CC-90009, which is currently in phase 1 clinical development.

BENZIMIDAZOLE INHIBITORS OF LEUKOTRIENE PRODUCTION

The present invention relates to compounds of formula IA and IB and pharmaceutically acceptable salts thereof, wherein R1-R7 are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds,