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12 results on '"Rooney, Suzanne"'

1. Discovery of 12 (BMS-986172) as a Highly Potent MGAT2 Inhibitor that Achieved Targeted Efficacious Exposures at a Low Human Dose for the Treatment of Metabolic Disorders

Author

Meng, Wei, primary, Brigance, Robert, additional, Mignone, James, additional, Negash, Lidet, additional, Zhao, Guohua, additional, Ahmad, Saleem, additional, Wang, Wei, additional, Moore, Fang, additional, Ye, Xiang-Yang, additional, Sun, Jung-Hui, additional, Mathur, Arvind, additional, Li, Yi-Xin, additional, Azzara, Anthony, additional, Ma, Zhengping, additional, Chu, Ching-Hsuen, additional, Cullen, Mary Jane, additional, Rooney, Suzanne, additional, Harvey, Susan, additional, Kopcho, Lisa, additional, Abell, Lynn, additional, O’Malley, Kevin, additional, Keim, William, additional, Dierks, Elizabeth A., additional, Chang, Shu, additional, Foster, Kimberly A., additional, Harden, David, additional, Dabros, Marta, additional, Goti, Vineet, additional, De Oliveira, Claudia, additional, Krishna, Gopal, additional, Pelleymounter, Mary Ann, additional, Whaley, Jean, additional, Robl, Jeffrey A., additional, Cheng, Dong, additional, and Devasthale, Pratik, additional

Published
2023
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2. Discovery of 12(BMS-986172) as a Highly Potent MGAT2 Inhibitor that Achieved Targeted Efficacious Exposures at a Low Human Dose for the Treatment of Metabolic Disorders

Author

Meng, Wei, Brigance, Robert, Mignone, James, Negash, Lidet, Zhao, Guohua, Ahmad, Saleem, Wang, Wei, Moore, Fang, Ye, Xiang-Yang, Sun, Jung-Hui, Mathur, Arvind, Li, Yi-Xin, Azzara, Anthony, Ma, Zhengping, Chu, Ching-Hsuen, Cullen, Mary Jane, Rooney, Suzanne, Harvey, Susan, Kopcho, Lisa, Abell, Lynn, O’Malley, Kevin, Keim, William, Dierks, Elizabeth A., Chang, Shu, Foster, Kimberly A., Harden, David, Dabros, Marta, Goti, Vineet, De Oliveira, Claudia, Krishna, Gopal, Pelleymounter, Mary Ann, Whaley, Jean, Robl, Jeffrey A., Cheng, Dong, and Devasthale, Pratik

Abstract

A series of dihydropyridinone (DHP) compounds was prepared and evaluated for MGAT2 activity. The efforts led to the identification of novel tetrazolones with potent MGAT2 inhibitory activity and favorable in vitroprofiles. Further tests of select analogues in mouse models revealed significant reduction in food intake and body weight. Subsequent studies in MGAT2 knockout mice with the lead candidate 12(BMS-986172) showed on-target- and mechanism-based pharmacology. Moreover, its favorable pharmacokinetic (PK) profile and the lack of species variability in the glucuronidation potential resulted in a greater confidence level in the projection of a low dose for achieving targeted efficacious exposures in humans. Consistent with these projections, PK data from a phase 1 trial confirmed that targeted efficacious exposures could be achieved at a low dose in humans, which supported compound 12as our second and potentially superior development candidate for the treatment of various metabolic disorders.

Published
2023
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3. Screening Hit to Clinical Candidate: Discovery of BMS-963272, a Potent, Selective MGAT2 Inhibitor for the Treatment of Metabolic Disorders

Author

Turdi, Huji, primary, Chao, Hannguang, additional, Hangeland, Jon J., additional, Ahmad, Saleem, additional, Meng, Wei, additional, Brigance, Robert, additional, Zhao, Guohua, additional, Wang, Wei, additional, Moore, Fang, additional, Ye, Xiang-Yang, additional, Mathur, Arvind, additional, Hou, Xiaoping, additional, Kempson, James, additional, Wu, Dauh-Rurng, additional, Li, Yi-Xin, additional, Azzara, Anthony V., additional, Ma, Zhengping, additional, Chu, Ching-Hsuen, additional, Chen, Luping, additional, Cullen, Mary Jane, additional, Rooney, Suzanne, additional, Harvey, Susan, additional, Kopcho, Lisa, additional, Panemangelor, Reshma, additional, Abell, Lynn, additional, O’Malley, Kevin, additional, Keim, William J., additional, Dierks, Elizabeth, additional, Chang, Shu, additional, Foster, Kimberly, additional, Apedo, Atsu, additional, Harden, David, additional, Dabros, Marta, additional, Gao, Qi, additional, Pelleymounter, Mary Ann, additional, Whaley, Jean M., additional, Robl, Jeffrey A., additional, Cheng, Dong, additional, Lawrence, R. Michael, additional, and Devasthale, Pratik, additional

Published
2021
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7. Non-basic azolotriazinone MCHR1 antagonists for the treatment of obesity: An empirical brain-exposures-driven candidate selection for in vivo efficacy studies

Author

Devasthale, Pratik, Wang, Wei, Mignone, James, Renduchintala, Kishore, Radhakrishnan, Sridhar, Dhanapal, Jayanthi, Selvaraj, Jagannath, Kuppusamy, Rajesh, Pelleymounter, Mary Ann, Longhi, Daniel, Huang, Ning, Flynn, Neil, Azzara, Anthony V., Rohrbach, Kenneth, Devenny, James, Rooney, Suzanne, Thomas, Michael, Glick, Susan, Godonis, Helen, Harvey, Susan, Cullen, Mary Jane, Zhang, Hongwei, Caporuscio, Christian, Stetsko, Paul, Grubb, Mary, Huang, Christine, Zhang, Lisa, Freeden, Chris, Murphy, Brian J., Robl, Jeffrey A., and Washburn, William N.

Published
2015
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8. Dihydropyrrolopyrazol-6-one MCHR1 antagonists for the treatment of obesity: Insights on in vivo efficacy from a novel FLIPR assay setup

Author

Devasthale, Pratik, Wang, Wei, Hernandez, Andres S., Moore, Fang, Renduchintala, Kishore, Sridhar, Radhakrishnan, Pelleymounter, Mary Ann, Longhi, Daniel, Huang, Ning, Flynn, Neil, Azzara, Anthony V., Rohrbach, Kenneth, Devenny, James, Rooney, Suzanne, Thomas, Michael, Glick, Susan, Godonis, Helen, Harvey, Susan, Cullen, Mary Jane, Zhang, Hongwei, Caporuscio, Christian, Stetsko, Paul, Grubb, Mary, Huang, Christine, Zhang, Lisa, Freeden, Chris, Li, Yi-Xin, Murphy, Brian J., Robl, Jeffrey A., and Washburn, William N.

Published
2015
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9. Synthesis and Antiobesity Properties of 6-(4-Chlorophenyl)-3-(4-((3,3-difluoro-1-hydroxycyclobutyl)methoxy)-3-methoxyphenyl)thieno[3,2-d]pyrimidin-4(3H)-one (BMS-814580): A Highly Efficacious Melanin Concentrating Hormone Receptor 1 (MCHR1) Inhibitor

Author

Ahmad, Saleem, primary, Washburn, William N., additional, Hernandez, Andres S., additional, Bisaha, Sharon, additional, Ngu, Khehyong, additional, Wang, Wei, additional, Pelleymounter, Mary Ann, additional, Longhi, Daniel, additional, Flynn, Neil, additional, Azzara, Anthony V., additional, Rohrbach, Kenneth, additional, Devenny, James, additional, Rooney, Suzanne, additional, Thomas, Michael, additional, Glick, Susan, additional, Godonis, Helen, additional, Harvey, Susan, additional, Zhang, Hongwei, additional, Gemzik, Brian, additional, Janovitz, Evan B., additional, Huang, Christine, additional, Zhang, Lisa, additional, Robl, Jeffrey A., additional, and Murphy, Brian J., additional

Published
2016
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10. Identification of a Nonbasic Melanin Hormone Receptor 1 Antagonist as an Antiobesity Clinical Candidate

Author

Washburn, William N., primary, Manfredi, Mark, additional, Devasthale, Pratik, additional, Zhao, Guohua, additional, Ahmad, Saleem, additional, Hernandez, Andres, additional, Robl, Jeffrey A., additional, Wang, Wei, additional, Mignone, James, additional, Wang, Zhenghua, additional, Ngu, Khehyong, additional, Pelleymounter, Mary Ann, additional, Longhi, Daniel, additional, Zhao, Rulin, additional, Wang, Bei, additional, Huang, Ning, additional, Flynn, Neil, additional, Azzara, Anthony V., additional, Barrish, Joel C., additional, Rohrbach, Kenneth, additional, Devenny, James J., additional, Rooney, Suzanne, additional, Thomas, Michael, additional, Glick, Susan, additional, Godonis, Helen E., additional, Harvey, Susan J., additional, Cullen, Mary Jane, additional, Zhang, Hongwei, additional, Caporuscio, Christian, additional, Stetsko, Paul, additional, Grubb, Mary, additional, Maxwell, Brad D., additional, Yang, Hong, additional, Apedo, Atsu, additional, Gemzik, Brian, additional, Janovitz, Evan B., additional, Huang, Christine, additional, Zhang, Lisa, additional, Freeden, Chris, additional, and Murphy, Brian J., additional

Published
2014
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