Raising high-density lipoprotein in humans through inhibition of cholesteryl ester transfer protein: an initial multidose study of torcetrapib

…, RT Wester, JA Williams, ME Perlman… - … , and vascular biology, 2004 - Am Heart Assoc
Objective— The ability of the potent cholesteryl ester transfer protein (CETP) inhibitor
torcetrapib (CP-529,414) to raise high-density lipoprotein cholesterol (HDL-C) levels in healthy …

Direct measurements of the dissociation-rate constant for inhibitor-enzyme complexes via the T1ρ and T2 (CPMG) methods

DG Davis, ME Perlman, RE London - Journal of Magnetic Resonance …, 1994 - Elsevier
The unimolecular dissociation rate constant, k −1 , for the inhibitor-enzyme complex
tubercidin-Escherichia coli purine nucleoside phosphorylase (PNPase) has been determined …

Mechanism of preconditioning. Ionic alterations.

C Steenbergen, ME Perlman, RE London… - Circulation …, 1993 - Am Heart Assoc
The mechanism by which preconditioning (brief intermittent periods of ischemia and reflow)
improves recovery of function and reduces enzyme release after a subsequent 30-minute …

Development of a self-emulsifying formulation that reduces the food effect for torcetrapib

ME Perlman, SB Murdande, MJ Gumkowski… - International journal of …, 2008 - Elsevier
Torcetrapib is a highly lipophilic (ClogP=7.45) and water insoluble cholesteryl ester transfer
protein (CETP) inhibitor developed for the treatment of atherosclerosis. Self-emulsifying drug …

Design, Synthesis, and Pharmacological Evaluation of Conformationally Constrained Analogues of N,N'-Diaryl- and N-Aryl-N-aralkylguanidines as Potent Inhibitors of …

MC Maillard, ME Perlman, O Amitay… - Journal of medicinal …, 1998 - ACS Publications
In the present investigation, the rationale for the design, synthesis, and biological evaluation
of potent inhibitors of neuronal Na + channels is described. N,N‘-Diaryl- and N-aryl-N-…

Nucleosides. 133. Synthesis of 5-alkenyl-1-(2-deoxy-2-fluoro-. beta.-D-arabinofuranosyl) cytosines and related pyrimidine nucleosides as potential antiviral agents

ME Perlman, KA Watanabe, RF Schinazi… - Journal of medicinal …, 1985 - ACS Publications
The synthesis of l-(2-deoxy-2-fluoro-dD-arabinofuranosyl) cytosines with a halovinyl (8 and
9) or vinyl (10) substituent at C-5 was accomplished from the corresponding 5-iodo (FIAC, 1) …

Synthesis and Pharmacological Evaluation of N,N'-Diarylguanidines as Potent Sodium Channel Blockers and Anticonvulsant Agents

NL Reddy, W Fan, SS Magar, ME Perlman… - Journal of medicinal …, 1998 - ACS Publications
Synthesis and structure−activity relationships (SAR) are described for a series of N,N‘-diarylguanidines
related to N-acenaphth-5-yl-N‘-(4-methoxynaphth-1-yl)guanidine (3) as …

Synthesis and binding characteristics of N-(1-naphthyl)-N′-(3-[125I]-iodophenyl)-N′-methylguanidine ([125I]-CNS 1261): a potential SPECT agent for imaging …

…, K Kodama, SS Magar, ME Perlman… - Nuclear medicine and …, 2000 - Elsevier
N-(1-Naphthyl)-N′-(3-[ 125 I]-iodophenyl)-N′-methylguanidine ([ 125 I]-CNS 1261) was
synthesized as a potential radioligand to image N-methyl-D-aspartate (NMDA) receptor …

Relaxation-matrix analysis of the transferred nuclear Overhauser effect for finite exchange rates

RE London, ME Perlman, DG Davis - Journal of Magnetic Resonance …, 1992 - Elsevier
A matrix formalism is developed for calculations of time-dependent nuclear Overhauser
effects in systems undergoing chemical exchange, and the analysis is applied to the …

Development and scale-up of a crystallization process to improve an API's physiochemical and bulk powder properties

…, C Mitchell, G Morris, ME Perlman… - … Process Research & …, 2018 - ACS Publications
A revised crystallization process for TAK-117, a selective PI3Kα inhibitor currently in Phase
1b clinical trials, was developed that greatly improved the overall purity, recovery, and …