A Dipolar Cycloaddition Reaction To Access 6‑Methyl-4,5,6,7-tetrahydro‑1H‑[1,2,3]­triazolo[4,5‑c]­pyridines Enables the Discovery Synthesis and Preclinical Profiling of a P2X7 Anta... von Chrovian, Christa C, Soyode-Johnson, Akinola, Peterson, Alexander A, Gelin, Christine F, Deng, Xiaohu, Dvorak, Curt A, Carruthers, Nicholas I, Lord, Brian, Fraser, Ian, Aluisio, Leah, Coe, Kevin J, Scott, Brian, Koudriakova, Tatiana, Schoetens, Freddy, Sepassi, Kia, Gallacher, David J, Bhattacharya, Anindya, Letavic, Michael A

Volltext

Blockade of Orexin-1 Receptors Attenuates Orexin-2 Receptor Antagonism-Induced Sleep Promotion in the Rat von Dugovic, Christine, Shelton, Jonathan E, Aluisio, Leah E, Fraser, Ian C, Jiang, Xiaohui, Sutton, Steven W, Bonaventure, Pascal, Yun, Sujin, Li, Xiaorong, Lord, Brian, Dvorak, Curt A, Carruthers, Nicholas I, Lovenberg, Timothy W

Volltext

Discovery of a Series of Substituted 1H‑((1,2,3-Triazol-4-yl)methoxy)pyrimidines as Brain Penetrants and Potent GluN2B-Selective Negative Allosteric Modulators von Gelin, Christine F., Stenne, Brice, Coate, Heather, Hiscox, Afton, Soyode-Johnson, Akinola, Wall, Jessica L., Lord, Brian, Schoellerman, Jeffrey, Coe, Kevin J., Wang, Kai, Alcázar, Jesus, Chrovian, Christa C., Dvorak, Curt A., Carruthers, Nicholas I., Koudriakova, Tatiana, Balana, Bartosz, Letavic, Michael A.

Volltext

Discovery and SAR studies of 2-alkyl-3-phenyl-2,4,5,6,7,8-hexahydropyrazolo[3,4-d]azepines as 5-HT7/2 inhibitors leading to the identification of a clinical candidate von Dvorak, Curt A., Rudolph, Dale A., Nepomuceno, Diane, Dvorak, Lisa, Lord, Brian, Fraser, Ian, Bonaventure, Pascal, Lovenberg, Timothy, Carruthers, Nicholas I.

Volltext

Discovery of a Series of Substituted 1 H -((1,2,3-Triazol-4-yl)methoxy)pyrimidines as Brain Penetrants and Potent GluN2B-Selective Negative Allosteric Modulators von Gelin, Christine F, Stenne, Brice, Coate, Heather, Hiscox, Afton, Soyode-Johnson, Akinola, Wall, Jessica L, Lord, Brian, Schoellerman, Jeffrey, Coe, Kevin J, Wang, Kai, Alcázar, Jesus, Chrovian, Christa C, Dvorak, Curt A, Carruthers, Nicholas I, Koudriakova, Tatiana, Balana, Bartosz, Letavic, Michael A

Volltext

4‑Methyl-6,7-dihydro‑4H‑triazolo[4,5‑c]­pyridine-Based P2X7 Receptor Antagonists: Optimization of Pharmacokinetic Properties Leading to the Identification of a Clinical Candidate... von Letavic, Michael A, Savall, Brad M, Allison, Brett D, Aluisio, Leah, Andres, Jose Ignacio, De Angelis, Meri, Ao, Hong, Beauchamp, Derek A, Bonaventure, Pascal, Bryant, Stewart, Carruthers, Nicholas I, Ceusters, Marc, Coe, Kevin J, Dvorak, Curt A, Fraser, Ian C, Gelin, Christine F, Koudriakova, Tatiana, Liang, Jimmy, Lord, Brian, Lovenberg, Timothy W, Otieno, Monicah A, Schoetens, Freddy, Swanson, Devin M, Wang, Qi, Wickenden, Alan D, Bhattacharya, Anindya

Volltext

Translational evaluation of JNJ-18038683, a 5-hydroxytryptamine type 7 receptor antagonist, on rapid eye movement sleep and in major depressive disorder von Bonaventure, Pascal, Dugovic, Christine, Kramer, Michelle, De Boer, Peter, Singh, Jaskaran, Wilson, Sue, Bertelsen, Kirk, Di, Jianing, Shelton, Jonathan, Aluisio, Leah, Dvorak, Lisa, Fraser, Ian, Lord, Brian, Nepomuceno, Diane, Ahnaou, Abdellah, Drinkenburg, Wilhelmus, Chai, Wenying, Dvorak, Curt, Sands, Steve, Carruthers, Nicholas, Lovenberg, Timothy W

Volltext

Re-evaluation of Adrenocorticotropic Hormone and Melanocyte Stimulating Hormone Activation of GPR139 in Vitro von Nepomuceno, Diane, Kuei, Chester, Dvorak, Curt, Lovenberg, Timothy, Liu, Changlu, Bonaventure, Pascal

Volltext

Substituted Azabicyclo[2.2.1]heptanes as Selective Orexin‑1 Antagonists: Discovery of JNJ-54717793 von Préville, Cathy, Bonaventure, Pascal, Koudriakova, Tatiana, Lord, Brian, Nepomuceno, Diane, Rizzolio, Michele, Mani, Neelakandha, Coe, Kevin J, Ndifor, Anthony, Dugovic, Christine, Dvorak, Curt A, Coate, Heather, Pippel, Daniel J, Fitzgerald, Anne, Allison, Brett, Lovenberg, Timothy W, Carruthers, Nicholas I, Shireman, Brock T

Volltext

Identification and SAR of Glycine Benzamides as Potent Agonists for the GPR139 Receptor von Dvorak, Curt A, Coate, Heather, Nepomuceno, Diane, Wennerholm, Michelle, Kuei, Chester, Lord, Brian, Woody, David, Bonaventure, Pascal, Liu, Changlu, Lovenberg, Timothy, Carruthers, Nicholas I

Volltext

A New Class of Diamine-Based Human Histamine H3 Receptor Antagonists:  4-(Aminoalkoxy)benzylamines von Apodaca, Richard, Dvorak, Curt A, Xiao, Wei, Barbier, Ann J, Boggs, Jamin D, Wilson, Sandy J, Lovenberg, Timothy W, Carruthers, Nicholas I

Volltext

Identification of Hydroxybenzoic Acids as Selective Lactate Receptor (GPR81) Agonists with Antilipolytic Effects von Dvorak, Curt A, Liu, Changlu, Shelton, Jonathan, Kuei, Chester, Sutton, Steven W, Lovenberg, Timothy W, Carruthers, Nicholas I

Volltext

The First Potent and Selective Non-Imidazole Human Histamine H4 Receptor Antagonists von Jablonowski, Jill A, Grice, Cheryl A, Chai, Wenying, Dvorak, Curt A, Venable, Jennifer D, Kwok, Annette K, Ly, Kiev S, Wei, Jianmei, Baker, Sherry M, Desai, Pragnya J, Jiang, Wen, Wilson, Sandy J, Thurmond, Robin L, Karlsson, Lars, Edwards, James P, Lovenberg, Timothy W, Carruthers, Nicholas I

Volltext

Preparation and Biological Evaluation of Indole, Benzimidazole, and Thienopyrrole Piperazine Carboxamides:  Potent Human Histamine H4 Antagonists von Venable, Jennifer D, Cai, Hui, Chai, Wenying, Dvorak, Curt A, Grice, Cheryl A, Jablonowski, Jill A, Shah, Chandra R, Kwok, Annette K, Ly, Kiev S, Pio, Barbara, Wei, Jianmei, Desai, Pragnya J, Jiang, Wen, Nguyen, Steven, Ling, Ping, Wilson, Sandy J, Dunford, Paul J, Thurmond, Robin L, Lovenberg, Timothy W, Karlsson, Lars, Carruthers, Nicholas I, Edwards, James P

Volltext

Chimeric, mutant orexin receptors show key interactions between orexin receptors, peptides and antagonists von Tran, Da-Thao, Bonaventure, Pascal, Hack, Michael, Mirzadegan, Taraneh, Dvorak, Curt, Letavic, Michael, Carruthers, Nicholas, Lovenberg, Timothy, Sutton, Steven W.

Volltext

Diamine-based human histamine H3 receptor antagonists: (4-Aminobutyn-1-yl)benzylamines von DVORAK, Curt A, APODACA, Richard, LOVENBERG, Timothy W, CARRUTHERS, Nicholas I, WEI XIAO, JABLONOWSKI, Jill A, BONAVENTURE, Pascal, DUGOVIC, Christine, SHELTON, Jonathan, LORD, Brian, MILLER, Kirsten, DVORAK, Lisa K

Volltext

Polypharmacology of Small-Molecule Modulators of the 5-Lipoxygenase Activating Protein (FLAP) Observed via a High-throughput Lipidomics Platform von Song, Jiao, Liu, Xuejun, Zhu, Jian, Tootoonchi, Mandana, Keith, John M., Meduna, Steven P., Dvorak, Curt A., Eccles, Wendy, Krawczuk, Paul J., Blevitt, Jonathan M., Wu, Jiejun, Rao, Navin L., Lebsack, Alec D., Milla, Marcos E.

Volltext

The discovery and synthesis of JNJ 31020028, a small molecule antagonist of the Neuropeptide Y Y2 receptor von Swanson, Devin M., Wong, Victoria D., Jablonowski, Jill A., Shah, Chandra, Rudolph, Dale A., Dvorak, Curt A., Seierstad, Mark, Dvorak, Lisa K., Morton, Kirsten, Nepomuceno, Diane, Atack, John R., Bonaventure, Pascal, Lovenberg, Timothy W., Carruthers, Nicholas I.

Volltext

Palladium-Catalyzed Coupling of Pyrazole Triflates with Arylboronic Acids von Dvorak, Curt A, Rudolph, Dale A, Ma, Sandy, Carruthers, Nicholas I

Volltext

Novel tetrahydropyrido[3,2-c]pyrroles as 5-HT7 antagonists von Rudolph, Dale A., Dvorak, Curt A., Dvorak, Lisa, Nepomuceno, Diane, Bonaventure, Pascal, Lovenberg, Timothy W., Carruthers, Nicholas I.

Volltext