Search Results - "Favreau, Leonard"

Design and Validation of Bicyclic Iminopyrimidinones As Beta Amyloid Cleaving Enzyme‑1 (BACE1) Inhibitors: Conformational Constraint to Favor a Bioactive Conformation by Mandal, Mihirbaran, Zhu, Zhaoning, Cumming, Jared N, Liu, Xiaoxiang, Strickland, Corey, Mazzola, Robert D, Caldwell, John P, Leach, Prescott, Grzelak, Michael, Hyde, Lynn, Zhang, Qi, Terracina, Giuseppe, Zhang, Lili, Chen, Xia, Kuvelkar, Reshma, Kennedy, Matthew E, Favreau, Leonard, Cox, Kathleen, Orth, Peter, Buevich, Alexei, Voigt, Johannes, Wang, Hongwu, Kazakevich, Irina, McKittrick, Brian A, Greenlee, William, Parker, Eric M, Stamford, Andrew W

“…On the basis of our observation that the biaryl substituent of iminopyrimidinone 7 must be in a pseudoaxial conformation to occupy the contiguous S1–S3…”
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Supercritical fluid chromatography/tandem mass spectrometric method for analysis of pharmaceutical compounds in metabolic stability samples by Hsieh, Yunsheng, Favreau, Leonard, Schwerdt, John, Cheng, K.-C.

“…Packed-column supercritical fluid chromatography (pSFC) coupled to an atmospheric pressure chemical ionization (APCI) source and a tandem mass spectrometer…”
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Inhibition of CYP3A4 in a Rapid Microtiter Plate Assay Using Recombinant Enzyme and in Human Liver Microsomes Using Conventional Substrates by NOMEIR, Amin A, RUEGG, Charles, SHOEMAKER, Matthew, FAVREAU, Leonard V, PALAMANDA, Jairam R, SILBER, Paul, LIN, Chin-Chung

“…Cytochrome P450 inhibition studies are performed in the pharmaceutical industry in the discovery stage to screen candidates that may have the potential for…”
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Validation of a rapid microtiter plate assay to conduct cytochrome P450 2D6 enzyme inhibition studies by Palamanda, Jairam R, Favreau, Leonard, Lin, Chin-chung, Nomeir, Amin A

“…Cytochrome P450 (CYP) inhibition studies are often performed on new chemical entities during the drug discovery stage. However, advances in combinatorial…”
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Stereochemical dynamics of aliphatic hydroxylation by cytochrome P-450 by White, Ronald E, Miller, John P, Favreau, Leonard V, Bhattacharyya, Apares

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Structure based design of iminohydantoin BACE1 inhibitors: Identification of an orally available, centrally active BACE1 inhibitor by Cumming, Jared N., Smith, Elizabeth M., Wang, Lingyan, Misiaszek, Jeffrey, Durkin, James, Pan, Jianping, Iserloh, Ulrich, Wu, Yusheng, Zhu, Zhaoning, Strickland, Corey, Voigt, Johannes, Chen, Xia, Kennedy, Matthew E., Kuvelkar, Reshma, Hyde, Lynn A., Cox, Kathleen, Favreau, Leonard, Czarniecki, Michael F., Greenlee, William J., McKittrick, Brian A., Parker, Eric M., Stamford, Andrew W.

“…From an initial lead 1, a structure-based design approach led to identification of a novel, high-affinity iminohydantoin BACE1 inhibitor that lowers…”
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Discovery of Cyclic Acylguanidines as Highly Potent and Selective β-Site Amyloid Cleaving Enzyme (BACE) Inhibitors: Part IInhibitor Design and Validation by Zhu, Zhaoning, Sun, Zhong-Yue, Ye, Yuanzan, Voigt, Johannes, Strickland, Corey, Smith, Elizabeth M, Cumming, Jared, Wang, Lingyan, Wong, Jesse, Wang, Yu-Sen, Wyss, Daniel F, Chen, Xia, Kuvelkar, Reshma, Kennedy, Matthew E, Favreau, Leonard, Parker, Eric, McKittrick, Brian A, Stamford, Andrew, Czarniecki, Michael, Greenlee, William, Hunter, John C

“…A number of novel amidine containing heterocycles were designed to reproduce the unique interaction pattern, revealed by X-ray crystallography, between the…”
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Structure-Based Design of an Iminoheterocyclic β‑Site Amyloid Precursor Protein Cleaving Enzyme (BACE) Inhibitor that Lowers Central Aβ in Nonhuman Primates by Mandal, Mihirbaran, Wu, Yusheng, Misiaszek, Jeffrey, Li, Guoqing, Buevich, Alexei, Caldwell, John P, Liu, Xiaoxiang, Mazzola, Robert D, Orth, Peter, Strickland, Corey, Voigt, Johannes, Wang, Hongwu, Zhu, Zhaoning, Chen, Xia, Grzelak, Michael, Hyde, Lynn A, Kuvelkar, Reshma, Leach, Prescott T, Terracina, Giuseppe, Zhang, Lili, Zhang, Qi, Michener, Maria S, Smith, Brad, Cox, Kathleen, Grotz, Diane, Favreau, Leonard, Mitra, Kaushik, Kazakevich, Irina, McKittrick, Brian A, Greenlee, William, Kennedy, Matthew E, Parker, Eric M, Cumming, Jared N, Stamford, Andrew W

“…We describe successful efforts to optimize the in vivo profile and address off-target liabilities of a series of BACE1 inhibitors represented by 6 that…”
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Overcoming Time-Dependent Inhibition (TDI) of Cytochrome P450 3A4 (CYP3A4) Resulting from Bioactivation of a Fluoropyrimidine Moiety by Mandal, Mihirbaran, Mitra, Kaushik, Grotz, Diane, Lin, Xinjie, Palamanda, Jairam, Kumari, Pramila, Buevich, Alexei, Caldwell, John P, Chen, Xia, Cox, Kathleen, Favreau, Leonard, Hyde, Lynn, Kennedy, Matthew E, Kuvelkar, Reshma, Liu, Xiaoxiang, Mazzola, Robert D, Parker, Eric, Rindgen, Diane, Sherer, Edward, Wang, Hongwu, Zhu, Zhaoning, Stamford, Andrew W, Cumming, Jared N

“…Herein we describe structure–activity relationship (SAR) and metabolite identification (Met-ID) studies that provided insight into the origin of time-dependent…”
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Mechanism-Based Inactivation of CYP2D6 by 5-Fluoro-2-[4-[(2-phenyl-1H-imidazol-5-yl)methyl]-1-piperazinyl]pyrimidine by PALAMANDA, Jairam R, CASCIANO, Christopher N, NORTON, Laura A, CLEMENT, Robert P, FAVREAU, Leonard V, LIN, Chin-Chung, NOMEIR, Amin A

“…SCH 66712 [5-fluoro-2-[4-[(2-phenyl-1 H -imidazol-5-yl)methyl]-1-piperazinyl]pyrimidine] caused a time- and NADPH-dependent loss of CYP2D6 activity. The…”
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Effect of heparin and heparin fractions on platelet aggregation by Salzman, E W, Rosenberg, R D, Smith, M H, Lindon, J N, Favreau, L

“…Porcine intestinal mucosal heparin induced aggregation of platelets in citrated platelet-rich plasma and enhanced platelet aggregation and serotonin secretion…”
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Improved Reliability of the Rapid Microtiter Plate Assay Using Recombinant Enzyme in Predicting CYP2D6 Inhibition in Human Liver Microsomes by FAVREAU, L. V, PALAMANDA, J. R, LIN, C.-C, NOMEIR, A. A

“…A higher throughput method of screening for the inhibition of recombinant CYP2D6 using a microtiter plate (MTP) assay was evaluated using 62 new chemical…”
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Discovery of an Orally Available, Brain Penetrant BACE1 Inhibitor That Affords Robust CNS Aβ Reduction by Stamford, Andrew W, Scott, Jack D, Li, Sarah W, Babu, Suresh, Tadesse, Dawit, Hunter, Rachael, Wu, Yusheng, Misiaszek, Jeffrey, Cumming, Jared N, Gilbert, Eric J, Huang, Chunli, McKittrick, Brian A, Hong, Liwu, Guo, Tao, Zhu, Zhaoning, Strickland, Corey, Orth, Peter, Voigt, Johannes H, Kennedy, Matthew E, Chen, Xia, Kuvelkar, Reshma, Hodgson, Robert, Hyde, Lynn A, Cox, Kathleen, Favreau, Leonard, Parker, Eric M, Greenlee, William J

“…Inhibition of BACE1 to prevent brain Aβ peptide formation is a potential disease-modifying approach to the treatment of Alzheimer’s disease. Despite over a…”
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Discovery of potent iminoheterocycle BACE1 inhibitors by Caldwell, John P., Mazzola, Robert D., Durkin, James, Chen, Joseph, Chen, Xia, Favreau, Leonard, Kennedy, Matthew, Kuvelkar, Reshma, Lee, Julie, McHugh, Nansie, McKittrick, Brian, Orth, Peter, Stamford, Andrew, Strickland, Corey, Voigt, Johannes, Wang, Liyang, Zhang, Lili, Zhang, Qi, Zhu, Zhaoning

“…The synthesis of a series of iminoheterocycles and their structure–activity relationships (SAR) as inhibitors of the aspartyl protease BACE1 will be detailed…”
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Dopamine D1/D5 Receptor Antagonists with Improved Pharmacokinetics:  Design, Synthesis, and Biological Evaluation of Phenol Bioisosteric Analogues of Benzazepine D1/D5 Antagonists by Wu, Wen-Lian, Burnett, Duane A, Spring, Richard, Greenlee, William J, Smith, Michelle, Favreau, Leonard, Fawzi, Ahmad, Zhang, Hongtao, Lachowicz, Jean E

“…Benzazepines 1 and 2 (SCH 23390 and SCH 39166, respectively) are two classical benzazepine D1/D5 antagonists, with K i values 1.4 and 1.2 nM, respectively…”
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Piperazine sulfonamide BACE1 inhibitors: Design, synthesis, and in vivo characterization by Cumming, Jared, Babu, Suresh, Huang, Ying, Carrol, Carolyn, Chen, Xia, Favreau, Leonard, Greenlee, William, Guo, Tao, Kennedy, Matthew, Kuvelkar, Reshma, Le, Thuy, Li, Guoqing, McHugh, Nansie, Orth, Peter, Ozgur, Lynne, Parker, Eric, Saionz, Kurt, Stamford, Andrew, Strickland, Corey, Tadesse, Dawit, Voigt, Johannes, Zhang, Lili, Zhang, Qi

“…Design and optimization of a novel series of piperazine sulfonamide inhibitors of BACE1 are described, with an emphasis on SAR of the non-prime side and S2′…”
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Dopamine D 1 /D 5 Receptor Antagonists with Improved Pharmacokinetics:  Design, Synthesis, and Biological Evaluation of Phenol Bioisosteric Analogues of Benzazepine D 1 /D 5 Antagonists by Wu, Wen-Lian, Burnett, Duane A., Spring, Richard, Greenlee, William J., Smith, Michelle, Favreau, Leonard, Fawzi, Ahmad, Zhang, Hongtao, Lachowicz, Jean E.

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Discovery of Cyclic Acylguanidines as Highly Potent and Selective β-Site Amyloid Cleaving Enzyme (BACE) Inhibitors: Part I–Inhibitor Design and Validation by Zhu, Zhaoning, Sun, Zhong-Yue, Ye, Yuanzan, Voigt, Johannes, Strickland, Corey, Smith, Elizabeth M., Cumming, Jared, Wang, Lingyan, Wong, Jesse, Wang, Yu-Sen, Wyss, Daniel F., Chen, Xia, Kuvelkar, Reshma, Kennedy, Matthew E., Favreau, Leonard, Parker, Eric, McKittrick, Brian A., Stamford, Andrew, Czarniecki, Michael, Greenlee, William, Hunter, John C.

“…A number of novel amidine containing heterocycles were designed to reproduce the unique interaction pattern, revealed by X-ray crystallography, between the…”
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The Rat Quinone Reductase Antioxidant Response Element by Favreau, Leonard V., Pickett, Cecil B.

“…The antioxidant response element (ARE) found in the 5′-flanking region of the rat quinone reductase gene has been further characterized by mutational and…”
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Discovery of amide and heteroaryl isosteres as carbamate replacements in a series of orally active γ-secretase inhibitors by McBriar, Mark D., Clader, John W., Chu, Inhou, Del Vecchio, Robert A., Favreau, Leonard, Greenlee, William J., Hyde, Lynn A., Nomeir, Amin A., Parker, Eric M., Pissarnitski, Dmitri A., Song, Lixin, Zhang, Lili, Zhao, Zhiqiang

“…The design of amide and heteroaryl amide isosteres as replacements for the carbamate substructure in previously disclosed 2,6-disubstituted piperidine…”
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