Discovery of highly potent and efficacious MC4R agonists with spiroindane N-Me-1,2,4-triazole privileged structures for the treatment of obesity von He, Shuwen, Ye, Zhixiong, Dobbelaar, Peter H., Bakshi, Raman K., Hong, Qingmei, Dellureficio, James P., Sebhat, Iyassu K., Guo, Liangqin, Liu, Jian, Jian, Tianying, Lai, Yingjie, Franklin, Christopher L., Reibarkh, Mikhail, Holmes, Mark A., Weinberg, David H., MacNeil, Tanya, Tang, Rui, Tamvakopoulos, Constantin, Peng, Qianping, Miller, Randy R., Stearns, Ralph A., Chen, Howard Y., Chen, Airu S., Strack, Alison M., Fong, Tung M., Wyvratt, Matthew J., Nargund, Ravi P.

Volltext

Synthesis and SAR of derivatives based on 2-biarylethylimidazole as bombesin receptor subtype-3 (BRS-3) agonists for the treatment of obesity von Liu, Jian, He, Shuwen, Jian, Tianying, Dobbelaar, Peter H., Sebhat, Iyassu K., Lin, Linus S., Goodman, Allan, Guo, Cheng, Guzzo, Peter R., Hadden, Mark, Henderson, Alan J., Pattamana, Kevin, Ruenz, Megan, Sargent, Bruce J, Swenson, Brian, Yet, Larry, Tamvakopoulos, Constantin, Peng, Qianping, Pan, Jie, Kan, Yanqing, Palyha, Oksana, Kelly, Theresa M., Guan, Xiao-Ming, Howard, Andrew D., Marsh, Donald J., Metzger, Joseph M., Reitman, Marc L., Wyvratt, Matthew J., Nargund, Ravi P.

Volltext

Discovery of substituted biphenyl imidazoles as potent, bioavailable bombesin receptor subtype-3 agonists von He, Shuwen, Dobbelaar, Peter H., Liu, Jian, Jian, Tianying, Sebhat, Iyassu K., Lin, Linus S., Goodman, Allan, Guo, Cheng, Guzzo, Peter R., Hadden, Mark, Henderson, Alan J., Ruenz, Megan, Sargent, Bruce J., Yet, Larry, Kelly, Theresa M., Palyha, Oksana, Kan, Yanqing, Pan, Jie, Chen, Howard, Marsh, Donald J., Shearman, Lauren P., Strack, Alison M., Metzger, Joseph M., Feighner, Scott D., Tan, Carina, Howard, Andrew D., Tamvakopoulos, Constantin, Peng, Qianping, Guan, Xiao-Ming, Reitman, Marc L., Patchett, Arthur A., Wyvratt, Matthew J., Nargund, Ravi P.

Volltext

Discovery of a spiroindane based compound as a potent, selective, orally bioavailable melanocortin subtype-4 receptor agonist von He, Shuwen, Ye, Zhixiong, Dobbelaar, Peter H., Sebhat, Iyassu K., Guo, Liangqin, Liu, Jian, Jian, Tianying, Lai, Yingjie, Franklin, Christopher L., Bakshi, Raman K., Dellureficio, James P., Hong, Qingmei, Tsou, Nancy N., Ball, Richard G., Cashen, Doreen E., Martin, William J., Weinberg, David H., MacNeil, Tanya, Tang, Rui, Tamvakopoulos, Constantin, Peng, Qianping, Miller, Randy R., Stearns, Ralph A., Chen, Howard Y., Chen, Airu S., Strack, Alison M., Fong, Tung M., MacIntyre, D. Euan, Wyvratt, Matthew J., Nargund, Ravi P.

Volltext

Spiroindane based amides as potent and selective MC4R agonists for the treatment of obesity von He, Shuwen, Ye, Zhixiong, Dobbelaar, Peter H., Sebhat, Iyassu K., Guo, Liangqin, Liu, Jian, Jian, Tianying, Lai, Yingjie, Franklin, Christopher L., Bakshi, Raman K., Dellureficio, James P., Hong, Qingmei, Weinberg, David H., MacNeil, Tanya, Tang, Rui, Strack, Alison M., Tamvakopoulos, Constantin, Peng, Qianping, Miller, Randy R., Stearns, Ralph A., Chen, Howard Y., Chen, Airu S., Fong, Tung M., Wyvratt, Matthew J., Nargund, Ravi P.

Volltext

Discovery of potent, selective, and orally bioavailable 3H-spiro[isobenzofuran-1,4'-piperidine] based melanocortin subtype-4 receptor agonists von LIANGQIN GUO, ZHIXIONG YE, TSOU, Nancy N, BALL, Richard G, WEINBERG, David H, MACNEIL, Tanya, RUI TANG, TAMVAKOPOULOS, Constantin, QIANPING PENG, CHEN, Howard Y, CHEN, Airu S, MARTIN, William J, JIAN LIU, EUAN MACINTYRE, D, STRACK, Alison M, FONG, Tung M, WYVRATT, Matthew J, NARGUND, Ravi P, SHUWEN HE, BAKSHI, Raman K, SEBHAT, Iyassu K, DOBBELAAR, Peter H, QINGMEI HONG, TIANYING JIAN, DELLUREFICIO, James P

Volltext

Synthesis and Antibacterial Activity of a Novel Class of 4‘-Substituted 16-Membered Ring Macrolides Derived from Tylosin von Phan, Ly T, Jian, Tianying, Chen, Zhigang, Qiu, Yao-Ling, Wang, Zhaolin, Beach, Theresa, Polemeropoulos, Alex, Or, Yat Sun

Volltext

Optimization of privileged structures for selective and potent melanocortin subtype-4 receptor ligands von Hong, Qingmei, Bakshi, Raman K., Dellureficio, James, He, Shuwen, Ye, Zhixiong, Dobbelaar, Peter H., Sebhat, Iyassu K., Guo, Liangqin, Liu, Jian, Jian, Tianying, Tang, Rui, Kalyani, Rubana N., MacNeil, Tanya, Vongs, Aurawan, Rosenblum, Charles I., Weinberg, David H., Peng, Qingping, Tamvakopoulos, Constantin, Miller, Randy R., Stearns, Ralph A., Cashen, Doreen, Martin, Willian J., Chen, Airu S., Metzger, Joseph M., Chen, Howard Y., Strack, Allison M., Fong, Tung M., Maclntyre, Euan, Van der Ploeg, Lex H.T., Wyvratt, Matthew J., Nargund, Ravi P.

Volltext

Synthesis of novel 4′-substituted 16-membered ring macrolide antibiotics derived from leucomycins von Wang, Zhaolin, Jian, Tianying, Phan, Ly T., Or, Yat Sun

Volltext

Accelerating the discovery of DGAT1 inhibitors through the application of parallel medicinal chemistry (PMC) von Yu, Yang, Wu, Zhicai, Shi, Zhi-Cai, He, Shuwen, Lai, Zhong, Cernak, Timothy A., Vachal, Petr, Liu, Min, Liu, Jian, Hong, Qingmei, Jian, Tianying, Guiadeen, Deodial, Krikorian, Arto, Sperbeck, Donald M., Verras, Andreas, Sonatore, Lisa M., Murphy, Beth A., Wiltsie, Judyann, Chung, Christine C., Gorski, Judith N., Liu, Jinqi, Xiao, Jianying, Wolff, Michael, Tong, Sharon X., Madeira, Maria, Karanam, Bindhu V., Shen, Dong-Ming, Balkovec, James M., De Vita, Robert J., Pinto, Shirly, Nargund, Ravi P.

Volltext

Benzimidazole-based DGAT1 inhibitors with a [3.1.0] bicyclohexane carboxylic acid moiety von He, Shuwen, Lai, Zhong, Hong, Qingmei, Shang, Jackie, Reibarkh, Mikhail, Kuethe, Jeffrey T., Liu, Jian, Guiadeen, Deodial, Krikorian, Arto D., Cernak, Timothy A., Dykstra, Kevin D., Sperbeck, Donald M., Wu, Zhicai, Yu, Yang, Yang, Ginger X., Jian, Tianying, Verras, Andreas, Sonatore, Lisa M., Wiltsie, Judyann, Chung, Christine C., Murphy, Beth A., Gorski, Judith N., Liu, Jinqi, Xiao, Jianying, Wolff, Michael, Tong, Sharon X., Madeira, Maria, Karanam, Bindhu V., Shen, Dong-Ming, Balkovec, James M., Pinto, Shirly, Nargund, Ravi P., DeVita, Robert J.

Volltext

Regulation of Energy Homeostasis by Bombesin Receptor Subtype-3: Selective Receptor Agonists for the Treatment of Obesity von Guan, Xiao-Ming, Chen, Howard, Dobbelaar, Peter H., Dong, Yan, Fong, Tung M., Gagen, Karen, Gorski, Judith, He, Shuwen, Howard, Andrew D., Jian, Tianying, Jiang, Michael, Kan, Yanqing, Kelly, Theresa M., Kosinski, Jennifer, Lin, Linus S., Liu, Jian, Marsh, Donald J., Metzger, Joseph M., Miller, Randy, Nargund, Ravi P., Palyha, Oksana, Shearman, Lauren, Shen, Zhu, Stearns, Ralph, Strack, Alison M., Stribling, Sloan, Tang, Yui Sing, Wang, Sheng-Ping, White, Amanda, Yu, Hong, Reitman, Marc L.

Volltext

Development of a novel class of potent and selective FIXa inhibitors von Zhang, Ting, Andre, Patrick, Bateman, Thomas J., Chen, Yi-Heng, Desai, Kunal, Ellsworth, Kenneth, Geissler, Wayne M., Guo, Liangqin, Hruza, Alan, Jian, Tianying, Meng, Dongfang, Parker, Dann L., Qian, Xiaoxia, Reichert, Paul, Sherer, Edward C., Shu, Min, Smith, Cameron J., Sonatore, Lisa M., Tschirret-Guth, Richard, Nolting, Andrew F., Orr, Robert, Campeau, Louis-Charles, Araki, Kazuto, Nishimura, Teruyuki, Sakurada, Isao, Wood, Harold B.

Volltext

Development of a novel tricyclic class of potent and selective FIXa inhibitors von Meng, Dongfang, Andre, Patrick, Bateman, Thomas J., Berger, Richard, Chen, Yi-Heng, Desai, Kunal, Dewnani, Sunita, Ellsworth, Kenneth, Feng, Daming, Geissler, Wayne M., Guo, Liangqin, Hruza, Alan, Jian, Tianying, Li, Hong, Metzger, Joe, Parker, Dann L., Reichert, Paul, Sherer, Edward C., Smith, Cameron J., Sonatore, Lisa M., Tschirret-Guth, Richard, Wu, Jane, Xu, Jiayi, Zhang, Ting, Campeau, Louis-Charles, Orr, Robert, Poirier, Marc, McCabe-Dunn, Jamie, Araki, Kazuto, Nishimura, Teruyuki, Sakurada, Isao, Hirabayashi, Tomokazu, Wood, Harold B.

Volltext

SAR exploration at the C-3 position of tetrahydro-β-carboline sstr3 antagonists von He, Shuwen, Dobbelaar, Peter H., Guo, Liangqin, Ye, Zhixiong, Liu, Jian, Jian, Tianying, Truong, Quang, Shah, Shrenik K., Du, Wu, Qi, Hongbo, Bakshi, Raman K., Hong, Qingmei, Dellureficio, James D., Sherer, Edward, Pasternak, Alexander, Feng, Zhe, Reibarkh, Mikhail, Lin, Melissa, Samuel, Koppara, Reddy, Vijay B., Mitelman, Stan, Tong, Sharon X., Chicchi, Gary G., Tsao, Kwei-Lan, Trusca, Dorina, Wu, Margaret, Shao, Qing, Trujillo, Maria E., Fernandez, Guillermo, Nelson, Donald, Bunting, Patricia, Kerr, Janet, Fitzgerald, Patrick, Morissette, Pierre, Volksdorf, Sylvia, Eiermann, George J., Li, Cai, Zhang, Bei B., Howard, Andrew D., Zhou, Yun-Ping, Nargund, Ravi P., Hagmann, William K.

Volltext

Preparation of 3,4-fused -spiro[furan-5(5 H),4′-piperidin]-2-one von Liu, Jian, Jian, Tianying, Guo, Liangqin, Atanasova, Tzvetomira, Nargund, Ravi P.

Volltext

Discovery of MK-1421, a Potent, Selective sstr3 Antagonist, as a Development Candidate for Type 2 Diabetes von Shah, Shrenik K, He, Shuwen, Guo, Liangqin, Truong, Quang, Qi, Hongbo, Du, Wu, Lai, Zhong, Liu, Jian, Jian, Tianying, Hong, Qingmei, Dobbelaar, Peter, Ye, Zhixiong, Sherer, Edward, Feng, Zhe, Yu, Yang, Wong, Frederick, Samuel, Koppara, Madiera, Maria, Karanam, Bindhu V, Reddy, Vijay B, Mitelman, Stan, Tong, Sharon X, Chicchi, Gary G, Tsao, Kwei-Lan, Trusca, Dorina, Feng, Yue, Wu, Margaret, Shao, Qing, Trujillo, Maria E, Eiermann, George J, Li, Cai, Pachanski, Michele, Fernandez, Guillermo, Nelson, Donald, Bunting, Patricia, Morissette, Pierre, Volksdorf, Sylvia, Kerr, Janet, Zhang, Bei B, Howard, Andrew D, Zhou, Yun-Ping, Pasternak, Alexander, Nargund, Ravi P, Hagmann, William K

Volltext

Discovery of a Potent and Selective DGAT1 Inhibitor with a Piperidinyl-oxy-cyclohexanecarboxylic Acid Moiety von He, Shuwen, Hong, Qingmei, Lai, Zhong, Yang, David X, Ting, Pauline C, Kuethe, Jeffrey T, Cernak, Timothy A, Dykstra, Kevin D, Sperbeck, Donald M, Wu, Zhicai, Yu, Yang, Yang, Ginger X, Jian, Tianying, Liu, Jian, Guiadeen, Deodial, Krikorian, Arto D, Sonatore, Lisa M, Wiltsie, Judyann, Liu, Jinqi, Gorski, Judith N, Chung, Christine C, Gibson, Jack T, Lisnock, JeanMarie, Xiao, Jianying, Wolff, Michael, Tong, Sharon X, Madeira, Maria, Karanam, Bindhu V, Shen, Dong-Ming, Balkovec, James M, Pinto, Shirly, Nargund, Ravi P, DeVita, Robert J

Volltext

Preparation of 2,3-dihydro-1H-spiro[isoquinoline-4,4′-piperidine] via an N-sulfonyl Pictet–Spengler reaction von Liu, Jian, Jian, Tianying, Sebhat, Iyassu, Nargund, Ravi

Volltext

Investigation of Cardiovascular Effects of Tetrahydro-β-carboline sstr3 antagonists von He, Shuwen, Lai, Zhong, Ye, Zhixiong, Dobbelaar, Peter H, Shah, Shrenik K, Truong, Quang, Du, Wu, Guo, Liangqin, Liu, Jian, Jian, Tianying, Qi, Hongbo, Bakshi, Raman K, Hong, Qingmei, Dellureficio, James, Reibarkh, Mikhail, Samuel, Koppara, Reddy, Vijay B, Mitelman, Stan, Tong, Sharon X, Chicchi, Gary G, Tsao, Kwei-Lan, Trusca, Dorina, Wu, Margaret, Shao, Qing, Trujillo, Maria E, Fernandez, Guillermo, Nelson, Donald, Bunting, Patricia, Kerr, Janet, Fitzgerald, Patrick, Morissette, Pierre, Volksdorf, Sylvia, Eiermann, George J, Li, Cai, Zhang, Bei, Howard, Andrew D, Zhou, Yun-Ping, Nargund, Ravi P, Hagmann, William K

Volltext