Selective Inhibitors of G2019S-LRRK2 Kinase Activity
Garofalo, Albert W, Bright, Jessica, De Lombaert, Stéphane, Toda, Alyssa M. A, Zobel, Kerry, Andreotti, Daniele, Beato, Claudia, Bernardi, Silvia, Budassi, Federica, Caberlotto, Laura, Gao, Peng, Griffante, Cristiana, Liu, Xinying, Mengatto, Luisa, Migliore, Marco, Sabbatini, Fabio Maria, Sava, Anna, Serra, Elena, Vincetti, Paolo, Zhang, Mingliang, Carlisle, Holly J
Published in Journal of medicinal chemistry (10.12.2020)
Published in Journal of medicinal chemistry (10.12.2020)
Get full text
Journal Article
Optimization of spirocyclic proline tryptophan hydroxylase-1 inhibitors
Goldberg, Daniel R., De Lombaert, Stéphane, Aiello, Robert, Bourassa, Patricia, Barucci, Nicole, Zhang, Qing, Paralkar, Vishwas, Stein, Adam J., Holt, Melissa, Valentine, Jim, Zavadoski, William
Published in Bioorganic & medicinal chemistry letters (01.02.2017)
Published in Bioorganic & medicinal chemistry letters (01.02.2017)
Get full text
Journal Article
Discovery of spirocyclic proline tryptophan hydroxylase-1 inhibitors
Goldberg, Daniel R., De Lombaert, Stéphane, Aiello, Robert, Bourassa, Patricia, Barucci, Nicole, Zhang, Qing, Paralkar, Vishwas, Valentine, James, Zavadoski, William
Published in Bioorganic & medicinal chemistry letters (15.02.2016)
Published in Bioorganic & medicinal chemistry letters (15.02.2016)
Get full text
Journal Article
Synthesis, SAR, and Series Evolution of Novel Oxadiazole-Containing 5‑Lipoxygenase Activating Protein Inhibitors: Discovery of 2‑[4-(3-{(R)‑1-[4-(2-Amino-pyrimidin-5-yl)-phenyl]-1-cyclopropyl-ethyl}-[1,2,4]oxadiazol-5-yl)-pyrazol-1-yl]‑N,N‑dimethyl-acetamide (BI 665915)
Takahashi, Hidenori, Riether, Doris, Bartolozzi, Alessandra, Bosanac, Todd, Berger, Valentina, Binetti, Ralph, Broadwater, John, Chen, Zhidong, Crux, Rebecca, De Lombaert, Stéphane, Dave, Rajvee, Dines, Jonathon A, Fadra-Khan, Tazmeen, Flegg, Adam, Garrigou, Michael, Hao, Ming-Hong, Huber, John, Hutzler, J. Matthew, Kerr, Steven, Kotey, Adrian, Liu, Weimin, Lo, Ho Yin, Loke, Pui Leng, Mahaney, Paige E, Morwick, Tina M, Napier, Spencer, Olague, Alan, Pack, Edward, Padyana, Anil K, Thomson, David S, Tye, Heather, Wu, Lifen, Zindell, Renee M, Abeywardane, Asitha, Simpson, Thomas
Published in Journal of medicinal chemistry (26.02.2015)
Published in Journal of medicinal chemistry (26.02.2015)
Get full text
Journal Article
Discovery of Potent, Selective Chymase Inhibitors via Fragment Linking Strategies
Taylor, Steven J, Padyana, Anil K, Abeywardane, Asitha, Liang, Shuang, Hao, Ming-Hong, De Lombaert, Stéphane, Proudfoot, John, Farmer, Bennett S, Li, Xiang, Collins, Brandon, Martin, Leslie, Albaugh, Daniel R, Hill-Drzewi, Melissa, Pullen, Steven S, Takahashi, Hidenori
Published in Journal of medicinal chemistry (13.06.2013)
Published in Journal of medicinal chemistry (13.06.2013)
Get full text
Journal Article
Structure-Based Optimization of Arylamides as Inhibitors of Soluble Epoxide Hydrolase
Eldrup, Anne B, Soleymanzadeh, Fariba, Taylor, Steven J, Muegge, Ingo, Farrow, Neil A, Joseph, David, McKellop, Keith, Man, Chuk C, Kukulka, Alison, De Lombaert, Stéphane
Published in Journal of medicinal chemistry (08.10.2009)
Published in Journal of medicinal chemistry (08.10.2009)
Get full text
Journal Article
Identification of a Potent Sodium Hydrogen Exchanger Isoform 1 (NHE1) Inhibitor with a Suitable Profile for Chronic Dosing and Demonstrated Cardioprotective Effects in a Preclinical Model of Myocardial Infarction in the Rat
Huber, John D, Bentzien, Jörg, Boyer, Stephen J, Burke, Jennifer, De Lombaert, Stéphane, Eickmeier, Christian, Guo, Xin, Haist, James V, Hickey, Eugene R, Kaplita, Paul, Karmazyn, Morris, Kemper, Raymond, Kennedy, Charles A, Kirrane, Thomas, Madwed, Jeffrey B, Mainolfi, Elizabeth, Nagaraja, Nelamangara, Soleymanzadeh, Fariba, Swinamer, Alan, Eldrup, Anne B
Published in Journal of medicinal chemistry (23.08.2012)
Published in Journal of medicinal chemistry (23.08.2012)
Get full text
Journal Article
Discovery of Novel 6,6-Heterocycles as Transient Receptor Potential Vanilloid (TRPV1) Antagonists
Blum, Charles A, Caldwell, Timothy, Zheng, Xiaozhang, Bakthavatchalam, Rajagopal, Capitosti, Scott, Brielmann, Harry, De Lombaert, Stéphane, Kershaw, Mark T, Matson, David, Krause, James E, Cortright, Daniel, Crandall, Marci, Martin, William J, Murphy, Beth Ann, Boyce, Susan, Jones, A. Brian, Mason, Glenn, Rycroft, Wayne, Perrett, Helen, Conley, Rachael, Burnaby-Davies, Nicola, Chenard, Bertrand L, Hodgetts, Kevin J
Published in Journal of medicinal chemistry (22.04.2010)
Published in Journal of medicinal chemistry (22.04.2010)
Get full text
Journal Article
Design and synthesis of substituted nicotinamides as inhibitors of soluble epoxide hydrolase
Taylor, Steven J., Soleymanzadeh, Fariba, Eldrup, Anne B., Farrow, Neil A., Muegge, Ingo, Kukulka, Alison, Kabcenell, Alisa K., Lombaert, Stephane De
Published in Bioorganic & medicinal chemistry letters (15.10.2009)
Published in Bioorganic & medicinal chemistry letters (15.10.2009)
Get full text
Journal Article
Tryptophan hydroxylase 1 Inhibition Impacts Pulmonary Vascular Remodeling in Two Rat Models of Pulmonary Hypertension
Aiello, Robert J, Bourassa, Patricia-Ann, Zhang, Qing, Dubins, Jeffrey, Goldberg, Daniel R, De Lombaert, Stéphane, Humbert, Marc, Guignabert, Christophe, Cavasin, Maria A, McKinsey, Timothy A, Paralkar, Vishwas
Published in The Journal of pharmacology and experimental therapeutics (01.02.2017)
Published in The Journal of pharmacology and experimental therapeutics (01.02.2017)
Get full text
Journal Article
The design, synthesis and structure–activity relationships of 1-aryl-4-aminoalkylisoquinolines: A novel series of CRF-1 receptor antagonists
Yoon, Taeyoung, De Lombaert, Stéphane, Brodbeck, Robbin, Gulianello, Michael, Chandrasekhar, Jayaraman, Horvath, Raymond F., Ge, Ping, Kershaw, Mark T., Krause, James E., Kehne, John, Hoffman, Diane, Doller, Darío, Hodgetts, Kevin J.
Published in Bioorganic & medicinal chemistry (01.02.2008)
Published in Bioorganic & medicinal chemistry (01.02.2008)
Get full text
Journal Article
Discovery of acyl guanidine tryptophan hydroxylase-1 inhibitors
Goldberg, Daniel R., De Lombaert, Stéphane, Aiello, Robert, Bourassa, Patricia, Barucci, Nicole, Zhang, Qing, Paralkar, Vishwas, Stein, Adam J., Valentine, Jim, Zavadoski, William
Published in Bioorganic & medicinal chemistry letters (15.06.2016)
Published in Bioorganic & medicinal chemistry letters (15.06.2016)
Get full text
Journal Article
Discovery and evaluation of pyrazolo[1,5- a]pyrimidines as neuropeptide Y1 receptor antagonists
Griffith, David A., Hargrove, Diane M., Maurer, Tristan S., Blum, Charles A., De Lombaert, Stéphane, Inthavongsay, John K., Klade, Lee E., Mack, Christine M., Rose, Colin R., Sanders, Martin J., Carpino, Philip A.
Published in Bioorganic & medicinal chemistry letters (01.05.2011)
Published in Bioorganic & medicinal chemistry letters (01.05.2011)
Get full text
Journal Article
Rapid synthesis of an array of trisubstituted urea-based soluble epoxide hydrolase inhibitors facilitated by a novel solid-phase method
Kowalski, Jennifer A., Swinamer, Alan D., Muegge, Ingo, Eldrup, Anne B., Kukulka, Alison, Cywin, Charles L., De Lombaert, Stéphane
Published in Bioorganic & medicinal chemistry letters (15.06.2010)
Published in Bioorganic & medicinal chemistry letters (15.06.2010)
Get full text
Journal Article
Discovery of N-(1-Ethylpropyl)-[3-methoxy-5-(2-methoxy-4-trifluoromethoxyphenyl)-6-methyl-pyrazin-2-yl]amine 59 (NGD 98−2): An Orally Active Corticotropin Releasing Factor-1 (CRF-1) Receptor Antagonist
Hodgetts, Kevin J, Ge, Ping, Yoon, Taeyoung, Lombaert, Stéphane De, Brodbeck, Robbin, Gulianello, Michael, Kieltyka, Andrzej, Horvath, Raymond F, Kehne, John H, Krause, James E, Maynard, George D, Hoffman, Diane, Lee, Younglim, Fung, Laurence, Doller, Dario
Published in Journal of medicinal chemistry (23.06.2011)
Published in Journal of medicinal chemistry (23.06.2011)
Get full text
Journal Article
Benzimidazolone as potent chymase inhibitor: Modulation of reactive metabolite formation in the hydrophobic (P 1) region
Lo, Ho Yin, Nemoto, Peter A., Kim, Jin Mi, Hao, Ming-Hong, Qian, Kevin C., Farrow, Neil A., Albaugh, Daniel R., Fowler, Danielle M., Schneiderman, Richard D., Michael August, E., Martin, Leslie, Hill-Drzewi, Melissa, Pullen, Steven S., Takahashi, Hidenori, De Lombaert, Stéphane
Published in Bioorganic & medicinal chemistry letters (01.08.2011)
Published in Bioorganic & medicinal chemistry letters (01.08.2011)
Get full text
Journal Article
Discovery of potent inhibitors of interleukin-2 inducible T-cell kinase (ITK) through structure-based drug design
Cook, Brian N., Bentzien, Jörg, White, Andre, Nemoto, Peter A., Wang, Ji, Man, Chuk C., Soleymanzadeh, Fariba, Khine, Hnin Hnin, Kashem, Mohammed A., Kugler, Stanley Z., Wolak, John P., Roth, Gregory P., De Lombaert, Stéphane, Pullen, Steven S., Takahashi, Hidenori
Published in Bioorganic & medicinal chemistry letters (01.02.2009)
Published in Bioorganic & medicinal chemistry letters (01.02.2009)
Get full text
Journal Article
Aminoquinazolines as TRPV1 antagonists: Modulation of drug-like properties through the exploration of 2-position substitution
Blum, Charles A., Zheng, Xiaozhang, Brielmann, Harry, Hodgetts, Kevin J., Bakthavatchalam, Rajagopal, Chandrasekhar, Jayaraman, Krause, James E., Cortright, Daniel, Matson, David, Crandall, Marci, Ngo, Chu K., Fung, Lawrence, Day, Marta, Kershaw, Mark, De Lombaert, Stéphane, Chenard, Bertrand L.
Published in Bioorganic & medicinal chemistry (15.08.2008)
Published in Bioorganic & medicinal chemistry (15.08.2008)
Get full text
Journal Article
Substituted pyrazoles as novel sEH antagonist: Investigation of key binding interactions within the catalytic domain
Lo, Ho Yin, Man, Chuk C., Fleck, Roman W., Farrow, Neil A., Ingraham, Richard H., Kukulka, Alison, Proudfoot, John R., Betageri, Raj, Kirrane, Tom, Patel, Usha, Sharma, Rajiv, Hoermann, Mary Ann, Kabcenell, Alisa, Lombaert, Stéphane De
Published in Bioorganic & medicinal chemistry letters (15.11.2010)
Published in Bioorganic & medicinal chemistry letters (15.11.2010)
Get full text
Journal Article