Ergoline-Derived Inverse Agonists of the Human H3 Receptor for the Treatment of Narcolepsy
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.
Published in ChemMedChem (01.08.2014)
Published in ChemMedChem (01.08.2014)
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Harrison, David, Billinton, Andy, Bock, Mark G., Doedens, John R., Gabel, Christopher A., Holloway, M. Katharine, Porter, Roderick A., Reader, Valerie, Scanlon, Jane, Schooley, Kenneth, Watt, Alan P.
Published in Journal of medicinal chemistry (09.11.2023)
Published in Journal of medicinal chemistry (09.11.2023)
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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
Doedens, John R., Diamond, Christine, Harrison, David, Bock, Mark G., Clarke, Nicholas, Watt, Alan P., Gabel, Christopher A.
Published in Biochemical pharmacology (01.09.2024)
Published in Biochemical pharmacology (01.09.2024)
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Cover Picture: Ergoline-Derived Inverse Agonists of the Human H3 Receptor for the Treatment of Narcolepsy (ChemMedChem 8/2014)
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.
Published in ChemMedChem (01.08.2014)
Published in ChemMedChem (01.08.2014)
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Target Cell Activation of a Structurally Novel NOD-Like Receptor Pyrin Domain-Containing Protein 3 Inhibitor NT-0796 Enhances Potency
Smolak, Pamela, Nguyen, MyTrang, Diamond, Christine, Wescott, Heather, Doedens, John R, Schooley, Kenneth, Snouwaert, John N, Bock, Mark G, Harrison, David, Watt, Alan P, Koller, Beverly H, Gabel, Christopher A
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Published in The Journal of pharmacology and experimental therapeutics (15.02.2024)
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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
Published in Journal of the American Chemical Society (25.06.2003)
Published in Journal of the American Chemical Society (25.06.2003)
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Discovery and Optimization of Triazolopyrimidinone Derivatives as Selective NLRP3 Inflammasome Inhibitors
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.
Published in ACS medicinal chemistry letters (11.08.2022)
Published in ACS medicinal chemistry letters (11.08.2022)
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The Discovery of LML134, a Histamine H3 Receptor Inverse Agonist for the Clinical Treatment of Excessive Sleep Disorders
Troxler, Thomas, Feuerbach, Dominik, Zhang, Xuechun, Yang, Charles R., Lagu, Bharat, Perrone, Mark, Wang, Tie‐Lin, Briner, Karin, Bock, Mark G., Auberson, Yves P.
Published in ChemMedChem (03.07.2019)
Published in ChemMedChem (03.07.2019)
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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 Indane Aryl Sulfonamides
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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3‑Alkoxy-pyrrolo[1,2‑b]pyrazolines as Selective Androgen Receptor Modulators with Ideal Physicochemical Properties for Transdermal Administration
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
Published in Journal of medicinal chemistry (11.09.2014)
Published in Journal of medicinal chemistry (11.09.2014)
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Generation and Characterization of a Human Bradykinin Receptor B1 Transgenic Rat as a Pharmacodynamic Model
Hess, J Fred, Ransom, Richard W, Zeng, Zhizhen, Chang, Raymond S L, Hey, Patricia J, Warren, Lee, Harrell, Charles M, Murphy, Kathryn L, Chen, Tsing-Bau, Miller, Patricia J, Lis, Edward, Reiss, Duane, Gibson, Raymond E, Markowitz, M Kristine, DiPardo, Robert M, Su, Dai-Shi, Bock, Mark G, Gould, Robert J, Pettibone, Douglas J
Published in The Journal of pharmacology and experimental therapeutics (01.08.2004)
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Discovery of 1,4-Substituted Piperidines as Potent and Selective Inhibitors of T-Type Calcium Channels
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
Published in Journal of medicinal chemistry (23.10.2008)
Published in Journal of medicinal chemistry (23.10.2008)
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From Ergolines to Indoles: Improved Inhibitors of the Human H3 Receptor for the Treatment of Narcolepsy
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.
Published in ChemMedChem (01.02.2015)
Published in ChemMedChem (01.02.2015)
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Amiloride derived inhibitors of acid-sensing ion channel-3 (ASIC3)
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.
Published in Bioorganic & medicinal chemistry letters (01.05.2009)
Published in Bioorganic & medicinal chemistry letters (01.05.2009)
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Discovery and expanded SAR of 4,4-disubstituted quinazolin-2-ones as potent T-type calcium channel antagonists
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.
Published in Bioorganic & medicinal chemistry letters (01.09.2010)
Published in Bioorganic & medicinal chemistry letters (01.09.2010)
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Bradykinin B1 receptor antagonists : An α-hydroxy amide with an improved metabolism profile
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
Published in Bioorganic & medicinal chemistry letters (15.09.2008)
Published in Bioorganic & medicinal chemistry letters (15.09.2008)
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Development of Orally Bioavailable and CNS Penetrant Biphenylaminocyclopropane Carboxamide Bradykinin B1 Receptor Antagonists
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.
Published in Journal of medicinal chemistry (25.01.2007)
Published in Journal of medicinal chemistry (25.01.2007)
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Indazole derivatives as novel bradykinin B1 receptor antagonists
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
Published in Bioorganic & medicinal chemistry letters (01.12.2010)
Published in Bioorganic & medicinal chemistry letters (01.12.2010)
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