Discovery of 1-(4-Methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-4,5,6,7-tetrahydro- 1H-pyrazolo[3,4-c]pyridine-3-carboxamide (Apixaban, BMS-562247), a Highly Potent, Selective, Efficacious, and Orally Bioavailable Inhibitor of Blood Coagulation Factor Xa
Pinto, Donald J. P, Orwat, Michael J, Koch, Stephanie, Rossi, Karen A, Alexander, Richard S, Smallwood, Angela, Wong, Pancras C, Rendina, Alan R, Luettgen, Joseph M, Knabb, Robert M, He, Kan, Xin, Baomin, Wexler, Ruth R, Lam, Patrick Y. S
Published in Journal of medicinal chemistry (01.11.2007)
Published in Journal of medicinal chemistry (01.11.2007)
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Discovery of 1-(3‘-Aminobenzisoxazol-5‘-yl)-3-trifluoromethyl-N-[2-fluoro-4- [(2‘-dimethylaminomethyl)imidazol-1-yl]phenyl]-1H-pyrazole-5-carboxyamide Hydrochloride (Razaxaban), a Highly Potent, Selective, and Orally Bioavailable Factor Xa Inhibitor
Quan, Mimi L, Lam, Patrick Y. S, Han, Qi, Pinto, Donald J. P, He, Ming Y, Li, Renhua, Ellis, Christopher D, Clark, Charles G, Teleha, Christopher A, Sun, Jung-Hui, Alexander, Richard S, Bai, Steve, Luettgen, Joseph M, Knabb, Robert M, Wong, Pancras C, Wexler, Ruth R
Published in Journal of medicinal chemistry (24.03.2005)
Published in Journal of medicinal chemistry (24.03.2005)
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First atroposelective Chan-Lam coupling for the synthesis of C-N linked biaryls
Ishida, Moeka, Adachi, Rina, Kobayashi, Kazuki, Yamamoto, Yukiko, Kawahara, Chinatsu, Yamada, Tsuyoshi, Aoyama, Hiroshi, Kanomata, Kyohei, Akai, Shuji, Lam, Patrick Y. S, Sajiki, Hironao, Ikawa, Takashi
Published in Chemical communications (Cambridge, England) (16.01.2024)
Published in Chemical communications (Cambridge, England) (16.01.2024)
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Preclinical pharmacokinetics and pharmacodynamics of apixaban, a potent and selective factor Xa inhibitor
He, Kan, Luettgen, Joseph M., Zhang, Donglu, He, Bing, Grace, James E., Xin, Baomin, Pinto, Donald J. P., Wong, Pancras C., Knabb, Robert M., Lam, Patrick Y. S., Wexler, Ruth R., Grossman, Scott J.
Published in European journal of drug metabolism and pharmacokinetics (01.09.2011)
Published in European journal of drug metabolism and pharmacokinetics (01.09.2011)
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Reductive Isoxazole Ring Opening of the Anticoagulant Razaxaban Is the Major Metabolic Clearance Pathway in Rats and Dogs
DONGLU ZHANG, RAGHAVAN, Nirmala, SKILES, Gary L, KAN HE, CHEN, Shiang-Yuan, HAIYING ZHANG, MIMI QUAN, LECUREUX, Lloyd, PATRONE, Laura M, LAM, Patrick Y. S, BONACORSI, Samuel J, KNABB, Robert M
Published in Drug metabolism and disposition (01.02.2008)
Published in Drug metabolism and disposition (01.02.2008)
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Hepatoselective Dihydroquinolizinone Bis-acids for HBsAg mRNA Degradation
Hwang, Nicky, Sun, Liren, Noe, Daisy, Lam, Patrick Y. S, Zhou, Tianlun, Block, Timothy M, Du, Yanming
Published in ACS medicinal chemistry letters (08.07.2021)
Published in ACS medicinal chemistry letters (08.07.2021)
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Potent, Orally Bioavailable, and Efficacious Macrocyclic Inhibitors of Factor XIa. Discovery of Pyridine-Based Macrocycles Possessing Phenylazole Carboxamide P1 Groups
Corte, James R, Pinto, Donald J. P, Fang, Tianan, Osuna, Honey, Yang, Wu, Wang, Yufeng, Lai, Amy, Clark, Charles G, Sun, Jung-Hui, Rampulla, Richard, Mathur, Arvind, Kaspady, Mahammed, Neithnadka, Premsai Rai, Li, Yi-Xin Cindy, Rossi, Karen A, Myers, Joseph E, Sheriff, Steven, Lou, Zhen, Harper, Timothy W, Huang, Christine, Zheng, Joanna J, Bozarth, Jeffrey M, Wu, Yiming, Wong, Pancras C, Crain, Earl J, Seiffert, Dietmar A, Luettgen, Joseph M, Lam, Patrick Y. S, Wexler, Ruth R, Ewing, William R
Published in Journal of medicinal chemistry (23.01.2020)
Published in Journal of medicinal chemistry (23.01.2020)
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Discovery of a High Affinity, Orally Bioavailable Macrocyclic FXIa Inhibitor with Antithrombotic Activity in Preclinical Species
Yang, Wu, Wang, Yufeng, Lai, Amy, Clark, Charles G, Corte, James R, Fang, Tianan, Gilligan, Paul J, Jeon, Yoon, Pabbisetty, Kumar B, Rampulla, Richard A, Mathur, Arvind, Kaspady, Mahammed, Neithnadka, Premsai Rai, Arumugam, Arunachalam, Raju, Sivashankaran, Rossi, Karen A, Myers, Joseph E, Sheriff, Steven, Lou, Zhen, Zheng, Joanna J, Chacko, Silvi A, Bozarth, Jeffrey M, Wu, Yiming, Crain, Earl J, Wong, Pancras C, Seiffert, Dietmar A, Luettgen, Joseph M, Lam, Patrick Y. S, Wexler, Ruth R, Ewing, William R
Published in Journal of medicinal chemistry (09.07.2020)
Published in Journal of medicinal chemistry (09.07.2020)
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Discovery of a Parenteral Small Molecule Coagulation Factor XIa Inhibitor Clinical Candidate (BMS-962212)
Pinto, Donald J. P., Orwat, Michael J., Smith, Leon M., Quan, Mimi L., Lam, Patrick Y. S., Rossi, Karen A., Apedo, Atsu, Bozarth, Jeffrey M., Wu, Yiming, Zheng, Joanna J., Xin, Baomin, Toussaint, Nathalie, Stetsko, Paul, Gudmundsson, Olafur, Maxwell, Brad, Crain, Earl J., Wong, Pancras C., Lou, Zhen, Harper, Timothy W., Chacko, Silvi A., Myers, Joseph E., Sheriff, Steven, Zhang, Huiping, Hou, Xiaoping, Mathur, Arvind, Seiffert, Dietmar A., Wexler, Ruth R., Luettgen, Joseph M., Ewing, William R.
Published in Journal of medicinal chemistry (14.12.2017)
Published in Journal of medicinal chemistry (14.12.2017)
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Preparation of 1-(4-methoxyphenyl)-1H-pyrazolo[4,3-d]pyrimidin-7(6H)-ones as potent, selective and bioavailable inhibitors of coagulation factor Xa
FEVIG, John M, CACCIOLA, Joseph, BURIAK, Joseph, ROSSI, Karen A, KNABB, Robert M, LUETTGEN, Joseph M, WONG, Pancras C, BAI, Stephen A, WEXLER, Ruth R, LAM, Patrick Y. S
Published in Bioorganic & medicinal chemistry letters (15.07.2006)
Published in Bioorganic & medicinal chemistry letters (15.07.2006)
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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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Conformationally Constrained ortho-Anilino Diaryl Ureas: Discovery of 1‑(2-(1′-Neopentylspiro[indoline-3,4′-piperidine]-1-yl)phenyl)-3-(4-(trifluoromethoxy)phenyl)urea, a Potent, Selective, and Bioavailable P2Y1 Antagonist
Qiao, Jennifer X, Wang, Tammy C, Ruel, Réjean, Thibeault, Carl, L’Heureux, Alexandre, Schumacher, William A, Spronk, Steven A, Hiebert, Sheldon, Bouthillier, Gilles, Lloyd, John, Pi, Zulan, Schnur, Dora M, Abell, Lynn M, Hua, Ji, Price, Laura A, Liu, Eddie, Wu, Qimin, Steinbacher, Thomas E, Bostwick, Jeffrey S, Chang, Ming, Zheng, Joanna, Gao, Qi, Ma, Baoqing, McDonnell, Patricia A, Huang, Christine S, Rehfuss, Robert, Wexler, Ruth R, Lam, Patrick Y. S
Published in Journal of medicinal chemistry (27.11.2013)
Published in Journal of medicinal chemistry (27.11.2013)
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Synthesis of Biologically Active Piperidine Metabolites of Clopidogrel: Determination of Structure and Analyte Development
Shaw, Scott A, Balasubramanian, Balu, Bonacorsi, Samuel, Cortes, Janet Caceres, Cao, Kevin, Chen, Bang-Chi, Dai, Jun, Decicco, Carl, Goswami, Animesh, Guo, Zhiwei, Hanson, Ronald, Humphreys, W. Griffith, Lam, Patrick Y. S, Li, Wenying, Mathur, Arvind, Maxwell, Brad D, Michaudel, Quentin, Peng, Li, Pudzianowski, Andrew, Qiu, Feng, Su, Shun, Sun, Dawn, Tymiak, Adrienne A, Vokits, Benjamin P, Wang, Bei, Wexler, Ruth, Wu, Dauh-Rurng, Zhang, Yingru, Zhao, Rulin, Baran, Phil S
Published in Journal of organic chemistry (17.07.2015)
Published in Journal of organic chemistry (17.07.2015)
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Preparation of 1-(3-aminobenzo[d]isoxazol-5-yl)-1H-pyrazolo[4,3-d]pyrimidin-7(6H)-ones as potent, selective, and efficacious inhibitors of coagulation factor Xa
LI, Yun-Long, FEVIG, John M, WEXLER, Ruth R, LAM, Patrick Y. S, CACCIOLA, Joseph, BURIAK, Joseph, ROSSI, Karen A, JONA, Janan, KNABB, Robert M, LUETTGEN, Joseph M, WONG, Pancras C, BAI, Stephen A
Published in Bioorganic & medicinal chemistry letters (01.10.2006)
Published in Bioorganic & medicinal chemistry letters (01.10.2006)
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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
Discovery of potent, efficacious, and orally bioavailable inhibitors of blood coagulation factor Xa with neutral P1 moieties
Pinto, Donald J.P., Galemmo, Robert A., Quan, Mimi L., Orwat, Michael J., Clark, Charles, Li, Renhua, Wells, Brian, Woerner, Francis, Alexander, Richard S., Rossi, Karen A., Smallwood, Angela, Wong, Pancras C., Luettgen, Joseph M., Rendina, Alan R., Knabb, Robert M., He, Kan, Wexler, Ruth R., Lam, Patrick Y.S.
Published in Bioorganic & medicinal chemistry letters (01.11.2006)
Published in Bioorganic & medicinal chemistry letters (01.11.2006)
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Sulfonamidolactam inhibitors of coagulation factor Xa
Smallheer, Joanne M., Wang, Shuaige, Laws, Mia L., Nakajima, Suanne, Hu, Zilun, Han, Wei, Jacobson, Irina, Luettgen, Joseph M., Rossi, Karen A., Rendina, Alan R., Knabb, Robert M., Wexler, Ruth R., Lam, Patrick Y.S., Quan, Mimi L.
Published in Bioorganic & medicinal chemistry (01.04.2008)
Published in Bioorganic & medicinal chemistry (01.04.2008)
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Journal Article
Correction to “Synthesis of Biologically Active Piperidine Metabolites of Clopidogrel: Determination of Structure and Analyte Development”
Shaw, Scott A, Balasubramanian, Balu, Bonacorsi, Samuel, Caceres Cortes, Janet, Cao, Kevin, Chen, Bang-Chi, Dai, Jun, Decicco, Carl, Goswami, Animesh, Guo, Zhiwei, Hanson, Ronald, Humphreys, W. Griffith, Lam, Patrick Y. S, Li, Wenying, Mathur, Arvind, Maxwell, Brad D, Michaudel, Quentin, Peng, Li, Pudzianowski, Andrew, Qiu, Feng, Su, Shun, Sun, Dawn, Tymiak, Adrienne A, Vokits, Benjamin P, Wang, Bei, Wexler, Ruth, Wu, Dauh-Rurng, Zhang, Yingru, Zhao, Rulin, Baran, Phil S
Published in Journal of organic chemistry (18.09.2015)
Published in Journal of organic chemistry (18.09.2015)
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