Discovery of BMS-986339, a Pharmacologically Differentiated Farnesoid X Receptor Agonist for the Treatment of Nonalcoholic Steatohepatitis
Nara, Susheel J., Jogi, Srinivas, Cheruku, Srinivas, Kandhasamy, Sarkunam, Jaipuri, Firoz, Kathi, Pavan Kalyan, Reddy, Subba, Sarodaya, Sanket, Cook, Erica M., Wang, Tao, Sitkoff, Doree, Rossi, Karen A., Ruzanov, Max, Kiefer, Susan E., Khan, Javed A., Gao, Mian, Reddy, Satyanarayana, Sivaprasad LVJ, Sankara, Sane, Ramola, Mosure, Kathy, Zhuo, Xiaoliang, Cao, Gary G., Ziegler, Milinda, Azzara, Anthony, Krupinski, John, Soars, Matthew G., Ellsworth, Bruce A., Wacker, Dean A.
Published in Journal of medicinal chemistry (14.07.2022)
Published in Journal of medicinal chemistry (14.07.2022)
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Journal Article
Discovery of 5‑Chloro-4-((1-(5-chloropyrimidin-2-yl)piperidin-4-yl)oxy)-1-(2-fluoro-4-(methylsulfonyl)phenyl)pyridin-2(1H)‑one (BMS-903452), an Antidiabetic Clinical Candidate Targeting GPR119
Wacker, Dean A, Wang, Ying, Broekema, Matthias, Rossi, Karen, O’Connor, Steven, Hong, Zhenqiu, Wu, Ginger, Malmstrom, Sarah E, Hung, Chen-Pin, LaMarre, Linda, Chimalakonda, Anjaneya, Zhang, Lisa, Xin, Li, Cai, Hong, Chu, Cuixia, Boehm, Stephanie, Zalaznick, Jacob, Ponticiello, Randolph, Sereda, Larisa, Han, Song-Ping, Zebo, Rachel, Zinker, Bradley, Luk, Chiuwa Emily, Wong, Richard, Everlof, Gerry, Li, Yi-Xin, Wu, Chunyu K, Lee, Michelle, Griffen, Steven, Miller, Keith J, Krupinski, John, Robl, Jeffrey A
Published in Journal of medicinal chemistry (25.09.2014)
Published in Journal of medicinal chemistry (25.09.2014)
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Journal Article
Discovery of BMS-986318, a Potent Nonbile Acid FXR Agonist for the Treatment of Nonalcoholic Steatohepatitis
Carpenter, Joseph, Wu, Gang, Wang, Ying, Cook, Erica M, Wang, Tao, Sitkoff, Doree, Rossi, Karen A, Mosure, Kathy, Zhuo, Xiaoliang, Cao, Gary G, Ziegler, Milinda, Azzara, Anthony V, Krupinski, Jack, Soars, Matthew G, Ellsworth, Bruce Alan, Wacker, Dean A
Published in ACS medicinal chemistry letters (09.09.2021)
Published in ACS medicinal chemistry letters (09.09.2021)
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Journal Article
Utilization of an Active Site Mutant Receptor for the Identification of Potent and Selective Atypical 5‑HT2C Receptor Agonists
Carpenter, Joseph, Wang, Ying, Wu, Gang, Feng, Jianxin, Ye, Xiang-Yang, Morales, Christian L, Broekema, Matthias, Rossi, Karen A, Miller, Keith J, Murphy, Brian J, Wu, Ginger, Malmstrom, Sarah E, Azzara, Anthony V, Sher, Philip M, Fevig, John M, Alt, Andrew, Bertekap, Robert L, Cullen, Mary Jane, Harper, Timothy M, Foster, Kimberly, Luk, Emily, Xiang, Qian, Grubb, Mary F, Robl, Jeffrey A, Wacker, Dean A
Published in Journal of medicinal chemistry (27.07.2017)
Published in Journal of medicinal chemistry (27.07.2017)
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Journal Article
Synthesis and structure–activity relationship of dihydrobenzofuran derivatives as novel human GPR119 agonists
Ye, Xiang-Yang, Morales, Christian L., Wang, Ying, Rossi, Karen A., Malmstrom, Sarah E., Abousleiman, Mojgan, Sereda, Larisa, Apedo, Atsu, Robl, Jeffrey A., Miller, Keith J., Krupinski, John, Wacker, Dean A.
Published in Bioorganic & medicinal chemistry letters (01.06.2014)
Published in Bioorganic & medicinal chemistry letters (01.06.2014)
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Journal Article
Utilization of an Active Site Mutant Receptor for the Identification of Potent and Selective Atypical 5-HT 2C Receptor Agonists
Carpenter, Joseph, Wang, Ying, Wu, Gang, Feng, Jianxin, Ye, Xiang-Yang, Morales, Christian L, Broekema, Matthias, Rossi, Karen A, Miller, Keith J, Murphy, Brian J, Wu, Ginger, Malmstrom, Sarah E, Azzara, Anthony V, Sher, Philip M, Fevig, John M, Alt, Andrew, Bertekap, Jr, Robert L, Cullen, Mary Jane, Harper, Timothy M, Foster, Kimberly, Luk, Emily, Xiang, Qian, Grubb, Mary F, Robl, Jeffrey A, Wacker, Dean A
Published in Journal of medicinal chemistry (27.07.2017)
Published in Journal of medicinal chemistry (27.07.2017)
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Journal Article
Position 5.46 of the Serotonin 5-HT2A Receptor Contributes to a Species-Dependent Variation for the 5-HT2C Agonist (R)-9-Ethyl-1,3,4,10b-tetrahydro-7-trifluoromethylpyrazino[2,1-a]isoindol-6(2H)-one: Impact on Selectivity and Toxicological Evaluation
Miller, Keith J, Wu, Ginger Y, Varnes, Jeffrey G, Levesque, Paul, Li, Julia, Li, Danshi, Robl, Jeffrey A, Rossi, Karen A, Wacker, Dean A
Published in Molecular pharmacology (01.12.2009)
Published in Molecular pharmacology (01.12.2009)
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Journal Article
Discovery of (R)-9-Ethyl-1,3,4,10b-tetrahydro-7-trifluoromethylpyrazino[2,1-a]isoindol- 6(2H)-one, a Selective, Orally Active Agonist of the 5-HT2C Receptor
Wacker, Dean A, Varnes, Jeffrey G, Malmstrom, Sarah E, Cao, Xueying, Hung, Chen-Pin, Ung, Thao, Wu, Ginger, Zhang, Ge, Zuvich, Eva, Thomas, Michael A, Keim, William J, Cullen, Mary Jane, Rohrbach, Kenneth W, Qu, Qinling, Narayanan, Rangaraj, Rossi, Karen, Janovitz, Evan, Lehman-McKeeman, Lois, Malley, Mary F, Devenny, James, Pelleymounter, Mary Ann, Miller, Keith J, Robl, Jeffrey A
Published in Journal of medicinal chemistry (22.03.2007)
Published in Journal of medicinal chemistry (22.03.2007)
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Journal Article
Structure–activity relationship and pharmacokinetic profile of 5-ketopyrazole factor Xa inhibitors
Varnes, Jeffrey G., Wacker, Dean A., Pinto, Donald J.P., Orwat, Michael J., Theroff, Jay P., Wells, Brian, Galemo, Robert A., Luettgen, Joseph M., Knabb, Robert M., Bai, Steven, He, Kan, Lam, Patrick Y.S., Wexler, Ruth R.
Published in Bioorganic & medicinal chemistry (15.01.2008)
Published in Bioorganic & medicinal chemistry (15.01.2008)
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Journal Article
Discovery of CC Chemokine Receptor-3 (CCR3) Antagonists with Picomolar Potency
De Lucca, George V, Kim, Ui Tae, Vargo, Brian J, Duncia, John V, Santella, Joseph B, Gardner, Daniel S, Zheng, Changsheng, Liauw, Ann, Wang, Zhang, Emmett, George, Wacker, Dean A, Welch, Patricia K, Covington, Maryanne, Stowell, Nicole C, Wadman, Eric A, Das, Anuk M, Davies, Paul, Yeleswaram, Swamy, Graden, Danielle M, Solomon, Kimberly A, Newton, Robert C, Trainor, George L, Decicco, Carl P, Ko, Soo. S
Published in Journal of medicinal chemistry (24.03.2005)
Published in Journal of medicinal chemistry (24.03.2005)
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Journal Article
Design, structure–activity relationship, and pharmacokinetic profile of pyrazole-based indoline factor Xa inhibitors
Varnes, Jeffrey G., Wacker, Dean A., Jacobson, Irina C., Quan, Mimi L., Ellis, Christopher D., Rossi, Karen A., He, Ming Y., Luettgen, Joseph M., Knabb, Robert M., Bai, Steven, He, Kan, Lam, Patrick Y.S., Wexler, Ruth R.
Published in Bioorganic & medicinal chemistry (01.12.2007)
Published in Bioorganic & medicinal chemistry (01.12.2007)
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Journal Article
From rigid cyclic templates to conformationally stabilized acyclic scaffolds. Part I: The discovery of CCR3 antagonist development candidate BMS-639623 with picomolar inhibition potency against eosinophil chemotaxis
Santella, Joseph B., Gardner, Daniel S., Yao, Wenqing, Shi, Chongsheng, Reddy, Prabhakar, Tebben, Andrew J., DeLucca, George V., Wacker, Dean A., Watson, Paul S., Welch, Patricia K., Wadman, Eric A., Davies, Paul, Solomon, Kimberly A., Graden, Dani M., Yeleswaram, Swamy, Mandlekar, Sandhya, Kariv, Ilona, Decicco, Carl P., Ko, Soo S., Carter, Percy H., Duncia, John V.
Published in Bioorganic & medicinal chemistry letters (15.01.2008)
Published in Bioorganic & medicinal chemistry letters (15.01.2008)
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CC chemokine receptor-3 (CCR3) antagonists: Improving the selectivity of DPC168 by reducing central ring lipophilicity
Pruitt, James R., Batt, Douglas G., Wacker, Dean A., Bostrom, Lori L., Booker, Shon K., McLaughlin, Erin, Houghton, Gregory C., Varnes, Jeffrey G., Christ, David D., Covington, Maryanne, Das, Anuk M., Davies, Paul, Graden, Danielle, Kariv, Ilona, Orlovsky, Yevgeniya, Stowell, Nicole C., Vaddi, Krishna G., Wadman, Eric A., Welch, Patricia K., Yeleswaram, Swamy, Solomon, Kimberly A., Newton, Robert C., Decicco, Carl P., Carter, Percy H., Ko, Soo S.
Published in Bioorganic & medicinal chemistry letters (01.06.2007)
Published in Bioorganic & medicinal chemistry letters (01.06.2007)
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Journal Article
Discovery of N-propylurea 3-benzylpiperidines as selective CC chemokine receptor-3 (CCR3) antagonists
Varnes, Jeffrey G, Gardner, Daniel S, Santella, Joseph B, Duncia, John V, Estrella, Melissa, Watson, Paul S, Clark, Cheryl M, Ko, Soo S, Welch, Patricia, Covington, Maryanne, Stowell, Nicole, Wadman, Eric, Davies, Paul, Solomon, Kimberley, Newton, Robert C, Trainor, George L, Decicco, Carl P, Wacker, Dean A
Published in Bioorganic & medicinal chemistry letters (05.04.2004)
Published in Bioorganic & medicinal chemistry letters (05.04.2004)
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Journal Article
CCR3 antagonists: a potential new therapy for the treatment of asthma. Discovery and structure–activity relationships
Wacker, Dean A, Santella, III, Joseph B, Gardner, Daniel S, Varnes, Jeffrey G, Estrella, Melissa, DeLucca, George V, Ko, Soo S, Tanabe, Keiichi, Watson, Paul S, Welch, Patricia K, Covington, Maryanne, Stowell, Nicole C, Wadman, Eric A, Davies, Paul, Solomon, Kimberly A, Newton, Robert C, Trainor, George L, Friedman, Steven M, Decicco, Carl P, Duncia, John V
Published in Bioorganic & medicinal chemistry letters (08.07.2002)
Published in Bioorganic & medicinal chemistry letters (08.07.2002)
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Journal Article
N-Arylalkylpiperidine urea derivatives as CC chemokine receptor-3 (CCR3) antagonists
Batt, Douglas G., Houghton, Gregory C., Roderick, John, Santella, Joseph B., Wacker, Dean A., Welch, Patricia K., Orlovsky, Yevgeniya I., Wadman, Eric A., Trzaskos, James M., Davies, Paul, Decicco, Carl P., Carter, Percy H.
Published in Bioorganic & medicinal chemistry letters (01.02.2005)
Published in Bioorganic & medicinal chemistry letters (01.02.2005)
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Efficient preparation of (3S)-3-(4-fluorobenzyl)piperidinium mandelate
Emmett, GC, Cain, GA, Estrella, MJ, Holler, ER, Piecara, JS, Blum, AM, Mical, AJ, Teleha, CA, Wacker, DA
Published in Synthesis (Stuttgart) (05.01.2005)
Published in Synthesis (Stuttgart) (05.01.2005)
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파르네소이드 X 수용체 조정제로서 유용한 치환된 아미드 화합물
NARAYAN RISHIKESH, SARKUNAM KANDHASAMY, THANGAVEL SOODAMANI, NARA SUSHEEL JETHANAND, CHERUKU SRINIVAS, WACKER DEAN A, KATHI PAVAN KALYAN, JAIPURI FIROZ ALI, JOGI SRINIVAS
Year of Publication 28.10.2021
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Year of Publication 28.10.2021
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