Isaac E Marx

发表

Development of 2-aminooxazoline 3-azaxanthenes as orally efficacious β-secretase inhibitors for the potential treatment of Alzheimer's disease.

S. Hitchcock, A. Cheng, Yuan Cheng, 2015, Bioorganic & medicinal chemistry letters.

The discovery of benzoxazine sulfonamide inhibitors of NaV1.7: Tools that bridge efficacy and target engagement.

R. Fremeau, H. Bregman, M. Chu-Moyer, 2017, Bioorganic & medicinal chemistry letters.

Discovery of Phospholipase D Inhibitors with Improved Drug-like Properties and Central Nervous System Penetrance.

I. Enyedy, M. Kaliszczak, Mark W Kankel, 2022, ACS medicinal chemistry letters.

Utilization of Cyclic Amides as Masked Aldehyde Equivalents in Reductive Amination Reactions.

R. Prince, J. Schulz, B. Hopkins, 2019, The Journal of organic chemistry.

Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency and Pharmacokinetics While Mitigating Metabolic Liabilities.

R. Fremeau, H. Bregman, M. Chu-Moyer, 2017, Journal of Medicinal Chemistry.

Discovery of alpha-amidosulfones as potent and selective agonists of CB2: synthesis, SAR, and pharmacokinetic properties.

S. Hitchcock, A. Cheng, R. Fremeau, 2009, Bioorganic & medicinal chemistry letters.

Discovery and Preclinical Characterization of BIIB091, a Reversible, Selective BTK Inhibitor for the Treatment of Multiple Sclerosis.

M. Mingueneau, J. Lyssikatos, T. Bohnert, 2021, Journal of medicinal chemistry.

Inhibitors of β-site amyloid precursor protein cleaving enzyme (BACE1): identification of (S)-7-(2-fluoropyridin-3-yl)-3-((3-methyloxetan-3-yl)ethynyl)-5'H-spiro[chromeno[2,3-b]pyridine-5,4'-oxazol]-2'-amine (AMG-8718).

R. Wahl, A. Cheng, R. Fremeau, 2014, Journal of medicinal chemistry.

Lead optimization and modulation of hERG activity in a series of aminooxazoline xanthene β-site amyloid precursor protein cleaving enzyme (BACE1) inhibitors.

Xiao Mei Zheng, R. Wahl, A. Cheng, 2014, Journal of medicinal chemistry.

Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency, Pharmacokinetics, and Metabolic Properties to Obtain Atropisomeric Quinolinone (AM-0466) that Affords Robust in Vivo Activity.

Roman Shimanovich, Angel Guzman-Perez, R. Fremeau, 2017, Journal of medicinal chemistry.

Utilizing structure based drug design and metabolic soft spot identification to optimize the in vitro potency and in vivo pharmacokinetic properties leading to the discovery of novel reversible Bruton's tyrosine kinase inhibitors.

Y. Liu, L. Silvian, T. Bohnert, 2021, Bioorganic & medicinal chemistry.

Next‐generation Bruton's tyrosine kinase inhibitor BIIB091 selectively and potently inhibits B cell and Fc receptor signaling and downstream functions in B cells and myeloid cells

M. Mingueneau, Baohong Zhang, S. Belachew, 2021, Clinical & translational immunology.

Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency and Pharmacokinetics to Enable in Vivo Target Engagement.

R. Fremeau, H. Bregman, M. Chu-Moyer, 2016, ACS medicinal chemistry letters.

Discovery and Preclinical Characterization of BIIB129, a Covalent, Selective, and Brain-Penetrant BTK Inhibitor for the Treatment of Multiple Sclerosis

R. Prince, M. Hoemberger, Christopher J. Helal, 2024, Journal of medicinal chemistry.