Discovery of Clinical Candidate NT-0796, a Brain-Penetrant and Highly Potent NLRP3 Inflammasome Inhibitor for Neuroinflammatory Disorders von Harrison, David, Billinton, Andy, Bock, Mark G., Doedens, John R., Gabel, Christopher A., Holloway, M. Katharine, Porter, Roderick A., Reader, Valérie, Scanlon, Jane, Schooley, Kenneth, Watt, Alan P.

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The ester-containing prodrug NT-0796 enhances delivery of the NLRP3 inflammasome inhibitor NDT-19795 to monocytic cells expressing carboxylesterase-1 von Doedens, John R., Diamond, Christine, Harrison, David, Bock, Mark G., Clarke, Nicholas, Watt, Alan P., Gabel, Christopher A.

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Tetrabutylammonium Salt Induced Denitration of Nitropyridines:  Synthesis of Fluoro-, Hydroxy-, and Methoxypyridines von Kuduk, Scott D, DiPardo, Robert M, Bock, Mark G

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Ergoline-Derived Inverse Agonists of the Human H3 Receptor for the Treatment of Narcolepsy von Auberson, Yves P., Troxler, Thomas, Zhang, Xuechun, Yang, Charles R., Fendt, Markus, Feuerbach, Dominik, Liu, Yu-Chih, Lagu, Bharat, Lerchner, Andreas, Perrone, Mark, Lei, Lijun, Zhang, Chao, Wang, Chunxiu, Wang, Tie-Lin, Bock, Mark G.

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Discovery and Optimization of Triazolopyrimidinone Derivatives as Selective NLRP3 Inflammasome Inhibitors von Harrison, David, Bock, Mark G., Doedens, John R., Gabel, Christopher A., Holloway, M. Katharine, Lewis, Arwel, Scanlon, Jane, Sharpe, Andrew, Simpson, Iain D., Smolak, Pamela, Wishart, Grant, Watt, Alan P.

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Cover Picture: Ergoline-Derived Inverse Agonists of the Human H3 Receptor for the Treatment of Narcolepsy (ChemMedChem 8/2014) von Auberson, Yves P., Troxler, Thomas, Zhang, Xuechun, Yang, Charles R., Fendt, Markus, Feuerbach, Dominik, Liu, Yu-Chih, Lagu, Bharat, Lerchner, Andreas, Perrone, Mark, Lei, Lijun, Zhang, Chao, Wang, Chunxiu, Wang, Tie-Lin, Bock, Mark G.

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Discovery of a Potent, Non-peptide Bradykinin B1 Receptor Antagonist von Su, Dai-Shi, Markowitz, M. Kristine, DiPardo, Robert M, Murphy, Kathy L, Harrell, C. Meacham, O'Malley, Stacy S, Ransom, Richard W, Chang, Raymond S. L, Ha, Sookhee, Hess, Fred J, Pettibone, Douglas J, Mason, Glenn S, Boyce, Susan, Freidinger, Roger M, Bock, Mark G

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The Discovery of LML134, a Histamine H3 Receptor Inverse Agonist for the Clinical Treatment of Excessive Sleep Disorders von Troxler, Thomas, Feuerbach, Dominik, Zhang, Xuechun, Yang, Charles R., Lagu, Bharat, Perrone, Mark, Wang, Tie‐Lin, Briner, Karin, Bock, Mark G., Auberson, Yves P.

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3‑Alkoxy-pyrrolo[1,2‑b]pyrazolines as Selective Androgen Receptor Modulators with Ideal Physicochemical Properties for Transdermal Administration von Ullrich, Thomas, Sasmal, Sanjita, Boorgu, Venkatesham, Pasagadi, Srinivasu, Cheera, Srisailam, Rajagopalan, Sujatha, Bhumireddy, Archana, Shashikumar, Dhanya, Chelur, Shekar, Belliappa, Charamanna, Pandit, Chetan, Krishnamurthy, Narasimharao, Mukherjee, Subhendu, Ramanathan, Anuradha, Ghadiyaram, Chakshusmathi, Ramachandra, Murali, Santos, Paulo G, Lagu, Bharat, Bock, Mark G, Perrone, Mark H, Weiler, Sven, Keller, Hansjoerg

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Discovery of Potent, Selective, and State-Dependent Na V 1.7 Inhibitors with Robust Oral Efficacy in Pain Models: Structure-Activity Relationship and Optimization of Chroman and In... von Ramdas, Vidya, Talwar, Rashmi, Kanoje, Vijay, Loriya, Rajesh M, Banerjee, Moloy, Patil, Pradeep, Joshi, Advait Arun, Datrange, Laxmikant, Das, Amit Kumar, Walke, Deepak Sahebrao, Kalhapure, Vaibhav, Khan, Talha, Gote, Ganesh, Dhayagude, Usha, Deshpande, Shreyas, Shaikh, Javed, Chaure, Ganesh, Pal, Ravindra R, Parkale, Santosh, Suravase, Sachin, Bhoskar, Smita, Gupta, Rajesh V, Kalia, Anil, Yeshodharan, Rajesh, Azhar, Mahammad, Daler, Jagadeesh, Mali, Vinod, Sharma, Geetika, Kishore, Amitesh, Vyawahare, Rupali, Agarwal, Gautam, Pareek, Himani, Budhe, Sagar, Nayak, Arun, Warude, Dnyaneshwar, Gupta, Praveen Kumar, Joshi, Parag, Joshi, Sneha, Darekar, Sagar, Pandey, Dilip, Wagh, Akshaya, Nigade, Prashant B, Mehta, Maneesh, Patil, Vinod, Modi, Dipak, Pawar, Shashikant, Verma, Mahip, Singh, Minakshi, Das, Sudipto, Gundu, Jayasagar, Nemmani, Kumar, Bock, Mark G, Sharma, Sharad, Bakhle, Dhananjay, Kamboj, Rajender Kumar, Palle, Venkata P

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Discovery of 1,4-Substituted Piperidines as Potent and Selective Inhibitors of T-Type Calcium Channels von Yang, Zhi-Qiang, Barrow, James C, Shipe, William D, Schlegel, Kelly-Ann S, Shu, Youheng, Yang, F. Vivien, Lindsley, Craig W, Rittle, Kenneth E, Bock, Mark G, Hartman, George D, Uebele, Victor N, Nuss, Cindy E, Fox, Steve V, Kraus, Richard L, Doran, Scott M, Connolly, Thomas M, Tang, Cuyue, Ballard, Jeanine E, Kuo, Yuhsin, Adarayan, Emily D, Prueksaritanont, Thomayant, Zrada, Matthew M, Marino, Michael J, Graufelds, Valerie Kuzmick, DiLella, Anthony G, Reynolds, Ian J, Vargas, Hugo M, Bunting, Patricia B, Woltmann, Richard F, Magee, Michael M, Koblan, Kenneth S, Renger, John J

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Amiloride derived inhibitors of acid-sensing ion channel-3 (ASIC3) von Kuduk, Scott D., Di Marco, Christina N., Chang, Ronald K., DiPardo, Robert M., Cook, Sean P., Cato, Matthew J., Jovanovska, Aneta, Urban, Mark O., Leitl, Michael, Spencer, Robert H., Kane, Stefanie A., Bilodeau, Mark T., Hartman, George D., Bock, Mark G.

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From Ergolines to Indoles: Improved Inhibitors of the Human H3 Receptor for the Treatment of Narcolepsy von Auberson, Yves P., Troxler, Thomas, Zhang, Xuechun, Yang, Charles R., Feuerbach, Dominik, Liu, Yu-Chih, Lagu, Bharat, Perrone, Mark, Lei, Lijun, Shen, Xiaoxia, Zhang, Dushan, Wang, Chunxiu, Wang, Tie-Lin, Briner, Karin, Bock, Mark G.

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Discovery and expanded SAR of 4,4-disubstituted quinazolin-2-ones as potent T-type calcium channel antagonists von Schlegel, Kelly-Ann S., Yang, Zhi-Qiang, Reger, Thomas S., Shu, Youheng, Cube, Rowena, Rittle, Kenneth E., Bondiskey, Phung, Bock, Mark G., Hartman, George D., Tang, Cuyue, Ballard, Jeanine, Kuo, Yuhsin, Prueksaritanont, Thomayant, Nuss, Cindy E., Doran, Scott M., Fox, Steven V., Garson, Susan L., Kraus, Richard L., Li, Yuxing, Uebele, Victor N., Renger, John J., Barrow, James C.

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Development of Orally Bioavailable and CNS Penetrant Biphenylaminocyclopropane Carboxamide Bradykinin B1 Receptor Antagonists von Kuduk, Scott D., Di Marco, Christina N., Chang, Ronald K., Wood, Michael R., Schirripa, Kathy M., Kim, June J., Wai, Jenny M. C., DiPardo, Robert M., Murphy, Kathy L., Ransom, Richard W., Harrell, C. Meacham, Reiss, Duane R., Holahan, Marie A., Cook, Jacquelynn, Hess, J. Fred, Sain, Nova, Urban, Mark O., Tang, Cuyue, Prueksaritanont, Thomayant, Pettibone, Douglas J., Bock, Mark G.

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Bradykinin B1 receptor antagonists : An α-hydroxy amide with an improved metabolism profile von KUDUK, Scott D, CHANG, Ronald K, BOCK, Mark G, DIPARDO, Robert M, DI MARCO, Christina N, MURPHY, Kathy L, RANSOM, Richard W, REISS, Duane R, TANG, Cuyue, PRUEKSARITANONT, Thomayant, PETTIBONE, Douglas J

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Bradykinin antagonists: new opportunities von Bock, Mark G, Longmore, Jeanette

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Indazole derivatives as novel bradykinin B1 receptor antagonists von BODMER-NARKEVITCH, Vera, ANTHONY, Neville J, BOCK, Mark G, KUDUK, Scott D, COFRE, Victoria, JOLLY, Samson M, MURPHY, Kathy L, RANSOM, Richard W, REISS, Duane R, CUYUE TANG, PRUEKSARITANONT, Thomayant, PETTIBONE, Douglas J

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Discovery of 4,4-Disubstituted Quinazolin-2-ones as T-Type Calcium Channel Antagonists von Barrow, James C, Rittle, Kenneth E, Reger, Thomas S, Yang, Zhi-Qiang, Bondiskey, Phung, McGaughey, Georgia B, Bock, Mark G, Hartman, George D, Tang, Cuyue, Ballard, Jeanine, Kuo, Yuhsin, Prueksaritanont, Thomayant, Nuss, Cindy E, Doran, Scott M, Fox, Steven V, Garson, Susan L, Kraus, Richard L, Li, Yuxing, Marino, Michael J, Kuzmick Graufelds, Valerie, Uebele, Victor N, Renger, John J

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2,3-Diaminopyridine Bradykinin B1 Receptor Antagonists von Kuduk, Scott D, Ng, Christina, Feng, Dong-Mei, Wai, Jenny M.-C, Chang, Raymond S. L, Harrell, Charles M, Murphy, Kathy L, Ransom, Richard W, Reiss, Duane, Ivarsson, Magnus, Mason, Glenn, Boyce, Susan, Tang, Cuyue, Prueksaritanont, Thomayant, Freidinger, Roger M, Pettibone, Douglas J, Bock, Mark G

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