Search Results - "LIANGQIN GUO"

Discovery of Potent and Orally Available Bicyclo[1.1.1]pentane-Derived Indoleamine-2,3-dioxygenase 1 (IDO1) Inhibitors by Pu, Qinglin, Zhang, Hongjun, Guo, Liangqin, Cheng, Mangeng, Doty, Amy C, Ferguson, Heidi, Fradera, Xavier, Lesburg, Charles A, McGowan, Meredeth A, Miller, J. Richard, Geda, Prasanthi, Song, Xuelei, Otte, Karin, Sciammetta, Nunzio, Solban, Nicolas, Yu, Wensheng, Sloman, David L, Zhou, Hua, Lammens, Alfred, Neumann, Lars, Bennett, David Jonathan, Pasternak, Alexander, Han, Yongxin

“…Indoleamine-2,3-dioxygenase 1 (IDO1) inhibition and its combination with immune checkpoint inhibitors like pembrolizumab have drawn considerable attention from…”
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Estrogen receptor ligands. Part 16: 2-Aryl indoles as highly subtype selective ligands for ERα by Dykstra, Kevin D., Guo, Liangqin, Birzin, Elizabeth T., Chan, Wanda, Yang, Yi Tien, Hayes, Edward C., DaSilva, Carolyn A., Pai, Lee-Yuh, Mosley, Ralph T., Kraker, Bryan, Fitzgerald, Paula M.D., DiNinno, Frank, Rohrer, Susan P., Schaeffer, James M., Hammond, Milton L.

“…A novel class of indole ligands for estrogen receptor α have been discovered which exhibit potent affinity and high selectivity. Substitution of the…”
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Discovery of highly potent and efficacious MC4R agonists with spiroindane N-Me-1,2,4-triazole privileged structures for the treatment of obesity by 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.

“…We report an SAR study of MC4R analogs containing spiroindane heterocyclic privileged structures. Compound 26 with N-Me-1,2,4-triazole moiety possesses…”
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Discovery of a piperazine urea based compound as a potent, selective, orally bioavailable melanocortin subtype-4 receptor partial agonist by Hong, Qingmei, Bakshi, Raman K., Palucki, Brenda L., Park, Min K., Ye, Zhixiong, He, Shuwen, Pollard, Patrick G., Sebhat, Iyassu K., Liu, Jian, Guo, Liangqin, 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.

“…We report the discovery of piperazine urea based compound 1, a potent, selective, orally bioavailable melanocortin subtype-4 receptor partial agonist. Compound…”
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Discovery of a spiroindane based compound as a potent, selective, orally bioavailable melanocortin subtype-4 receptor agonist by 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.

“…We report the design, synthesis and properties of spiroindane based compound 1, a potent, selective, orally bioavailable, non-peptide melanocortin subtype-4…”
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Spiroindane based amides as potent and selective MC4R agonists for the treatment of obesity by 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.

“…We report a series of potent and selective MC4R agonists based on spiroindane amide privileged structures for potential treatments of obesity. Among the…”
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Discovery of potent, selective, and orally bioavailable 3H-spiro[isobenzofuran-1,4'-piperidine] based melanocortin subtype-4 receptor agonists by 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

“…Design, synthesis, and SAR of a series of 3H-spiro[isobenzofuran-1,4'-piperidine] based compounds as potent, selective and orally bioavailable melanocortin…”
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Synthesis and SAR of potent and orally bioavailable tert-butylpyrrolidine archetype derived melanocortin subtype-4 receptor modulators by Guo, Liangqin, Ye, Zhixiong, Ujjainwalla, Feroze, Sings, Heather L., Sebhat, Iyassu K., Huber, John, Weinberg, David H., Tang, Rui, MacNeil, Tanya, Tamvakopoulos, Constantin, Peng, Qianping, MacIntyre, Euan, van der Ploeg, Lex H.T., Goulet, Mark T., Wyvratt, Matthew J., Nargund, Ravi P.

“…Discovery of a series of tert-butyl pyrrolidine derived, potent and orally bioavailable melanocortin receptor subtype-4 (MC4R) selective modulators is…”
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Discovery of 3,5-bis(trifluoromethyl)benzyl l-arylglycinamide based potent CCR2 antagonists by Yang, Lihu, Zhou, Changyou, Guo, Liangqin, Morriello, Gregori, Butora, Gabor, Pasternak, Alexander, Parsons, William H., Mills, Sander G., MacCoss, Malcolm, Vicario, Pasquale P., Zweerink, Hans, Ayala, Julia M., Goyal, Shefali, Hanlon, William A., Cascieri, Margaret A., Springer, Marty S.

“…Extensive SAR of a screening hit resulted in a new series of potent and selective CCR2 receptor antagonists. Systematic modification of a screening lead…”
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Optimization of privileged structures for selective and potent melanocortin subtype-4 receptor ligands by 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.

“…Design, syntheses and structure–activity relationships of piperazine privileged structures containing MC4R agonist compounds 6 were described. The most potent…”
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Synthesis and Biological Activities of Potent Peptidomimetics Selective for Somatostatin Receptor Subtype 2 by Yang, Lihu, Berk, Scott C., Rohrer, Susan P., Mosley, Ralph T., Guo, Liangqin, Underwood, Dennis J., Arison, Byron H., Birzin, Elizabeth T., Hayes, Edward C., Mitra, Sudha W., Parmar, Rupa M., Cheng, Kang, Wu, Tsuei-Ju, Butler, Bridgette S., Foor, Forrest, Pasternak, Alexander, Pan, Yanping, Silva, Maria, Freidinger, Roger M., Smith, Roy G., Chapman, Kevin, Schaeffer, James M., Patchett, Arthur A.

“…A series of nonpeptide somatostatin agonists which bind selectively and with high affinity to somatostatin receptor subtype 2 (sst2) have been synthesized. One…”
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α-Aminothiazole-γ-aminobutanoic amides as potent, small molecule CCR2 receptor antagonists by Zhou, Changyou, Guo, Liangqin, Parsons, William H., Mills, Sander G., MacCoss, Malcolm, Vicario, Pasquale P., Zweerink, Hans, Cascieri, Margaret A., Springer, Martin S., Yang, Lihu

“…A series of racemic and homochiral α-aminothiazole-γ-aminobutyroamides that display high affinities for human and murine CCR2 and functional antagonism by…”
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Pictet-Spengler reaction on solid support by Lihu, Yang, Liangqin, Guo

“…Merrifield resin-bound tryptophan undergoes Pictet-Spengler reaction with aldehydes at ambient temperature to give tetrahydro-β-carbolines in excellent yield…”
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Spiro[1H-indene-1,4‘-piperidine] Derivatives As Potent and Selective Non-Peptide Human Somatostatin Receptor Subtype 2 (sst2) Agonists by Yang, Lihu, Guo, Liangqin, Pasternak, Alexander, Mosley, Ralph, Rohrer, Susan, Birzin, Elizabeth, Foor, Forrest, Cheng, Kang, Schaeffer, James, Patchett, Arthur A

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Hydroformylation and Late-Stage Diversification on Densely Functionalized Cores of Influenza Endonuclease Inhibitors by Emmert, Marion H., Liang, Tao, Hyde, Alan M., Liao, Jennie, Ruhl, Kyle E., Shurtleff, Valerie W., Roecker, Anthony J., Schreier, John, Guo, Liangqin, Zhang, Yonglian, Shao, Guangxin, Guo, Zhiwei, Xiao, Dong

“…This work describes synthetic strategies to access diverse chemical matter in a series of inhibitors of the cap-dependent Flu endonuclease. Our approaches…”
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Nipecotic and iso-nipecotic amides as potent and selective somatostatin subtype-2 receptor agonists by CHANGYOU ZHOU, LIANGQIN GUO, KANG CHENG, SCHAEFFER, James M, PATCHETT, Arthur A, LIHU YANG, MORRIELLO, Greg, PASTERNAK, Alex, PAN, Yanping, ROHRER, Susan P, BIRZIN, Elizebeth T, HUSKEY, Su-Er Wu, JACKS, Tom, SCHLEIM, Klaus D

“…N-Substituted nipecotic and iso-nipecotic amides of beta-methylTrpLys tert-butyl ester were found to be novel, selective and potent agonists of the…”
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Development of a novel class of potent and selective FIXa inhibitors by 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.

“…[Display omitted] Using structure based drug design (SBDD), a novel class of potent coagulation Factor IXa (FIXa) inhibitors was designed and synthesized. High…”
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Development of a novel tricyclic class of potent and selective FIXa inhibitors by 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.

“…[Display omitted] Using structure based drug design, a novel class of potent coagulation factor IXa (FIXa) inhibitors was designed and synthesized. High…”
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SAR exploration at the C-3 position of tetrahydro-β-carboline sstr3 antagonists by 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.

“…MK-4256, a tetrahydro-β-carboline sstr3 antagonist, was discontinued due to a cardiovascular (CV) adverse effect observed in dogs. Additional investigations…”
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Preparation of 3,4-fused -spiro[furan-5(5 H),4′-piperidin]-2-one by Liu, Jian, Jian, Tianying, Guo, Liangqin, Atanasova, Tzvetomira, Nargund, Ravi P.

“…A general method for the preparation of various 3,4-fused-spiro[furan-5(5 H),4′-piperidin]-2-one with high yield is reported. The formation of…”
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