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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Journal Article
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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Journal Article
Structure based design of macrocyclic factor XIa inhibitors: Discovery of cyclic P1 linker moieties with improved oral bioavailability
Clark, Charles G., Rossi, Karen A., Corte, James R., Fang, Tianan, Smallheer, Joanne M., De Lucca, Indawati, Nirschl, David S., Orwat, Michael J., Pinto, Donald J.P., Hu, Zilun, Wang, Yufeng, Yang, Wu, Jeon, Yoon, Ewing, William R., Myers, Joseph E., Sheriff, Steven, Lou, Zhen, Bozarth, Jeffrey M., Wu, Yiming, Rendina, Alan, Harper, Timothy, Zheng, Joanna, Xin, Baomin, Xiang, Qian, Luettgen, Joseph M., Seiffert, Dietmar A., Wexler, Ruth R., Lam, Patrick Y.S.
Published in Bioorganic & medicinal chemistry letters (01.10.2019)
Published in Bioorganic & medicinal chemistry letters (01.10.2019)
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Journal Article
Orally bioavailable pyridine and pyrimidine-based Factor XIa inhibitors: Discovery of the methyl N-phenyl carbamate P2 prime group
Corte, James R., Fang, Tianan, Pinto, Donald J.P., Orwat, Michael J., Rendina, Alan R., Luettgen, Joseph M., Rossi, Karen A., Wei, Anzhi, Ramamurthy, Vidhyashankar, Myers, Joseph E., Sheriff, Steven, Narayanan, Rangaraj, Harper, Timothy W., Zheng, Joanna J., Li, Yi-Xin, Seiffert, Dietmar A., Wexler, Ruth R., Quan, Mimi L.
Published in Bioorganic & medicinal chemistry (15.05.2016)
Published in Bioorganic & medicinal chemistry (15.05.2016)
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Journal Article
Novel phenylalanine derived diamides as Factor XIa inhibitors
Smith, Leon M., Orwat, Michael J., Hu, Zilun, Han, Wei, Wang, Cailan, Rossi, Karen A., Gilligan, Paul J., Pabbisetty, Kumar B., Osuna, Honey, Corte, James R., Rendina, Alan R., Luettgen, Joseph M., Wong, Pancras C., Narayanan, Ranga, Harper, Timothy W., Bozarth, Jeffrey M., Crain, Earl J., Wei, Anzhi, Ramamurthy, Vidhyashankar, Morin, Paul E., Xin, Baomin, Zheng, Joanna, Seiffert, Dietmar A., Quan, Mimi L., Lam, Patrick Y.S., Wexler, Ruth R., Pinto, Donald J.P.
Published in Bioorganic & medicinal chemistry letters (15.01.2016)
Published in Bioorganic & medicinal chemistry letters (15.01.2016)
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Journal Article
Orally bioavailable factor Xa inhibitors containing alpha-substituted gem-dimethyl P4 moieties
Orwat, Michael J., Qiao, Jennifer X., He, Kan, Rendina, Alan R., Luettgen, Joseph M., Rossi, Karen A., Xin, Baomin, Knabb, Robert M., Wexler, Ruth R., Lam, Patrick Y. S., Pinto, Donald J. P.
Published in Bioorganic & medicinal chemistry letters (01.08.2014)
Published in Bioorganic & medicinal chemistry letters (01.08.2014)
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Journal Article
RXFP1 수용체 효능제로서의 벤조티아졸, 벤조이속사졸 및 벤조디옥솔 유사체
KUMAR SREEKANTHA RATNA, ORWAT MICHAEL J, SRINIVAS PITANI VEERA VENKATA, HEGDE SUBRAMANYA
Year of Publication 07.08.2024
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Year of Publication 07.08.2024
Patent
Discovery of 1-[3-(Aminomethyl)phenyl]-N-[3-fluoro-2‘-(methylsulfonyl)- [1,1‘-biphenyl]-4-yl]-3-(trifluoromethyl)-1H-pyrazole-5-carboxamide (DPC423), a Highly Potent, Selective, and Orally Bioavailable Inhibitor of Blood Coagulation Factor Xa
Pinto, Donald J. P, Orwat, Michael J, Wang, Shuaige, Fevig, John M, Quan, Mimi L, Amparo, Eugene, Cacciola, Joseph, Rossi, Karen A, Alexander, Richard S, Smallwood, Angela M, Luettgen, Joseph M, Liang, Li, Aungst, Bruce J, Wright, Matthew R, Knabb, Robert M, Wong, Pancras C, Wexler, Ruth R, Lam, Patrick Y. S
Published in Journal of medicinal chemistry (15.02.2001)
Published in Journal of medicinal chemistry (15.02.2001)
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Journal Article
1-[3-Aminobenzisoxazol-5′-yl]-3-trifluoromethyl-6-[2′-(3-( R)-hydroxy- N-pyrrolidinyl)methyl-[1,1′]-biphen-4-yl]-1,4,5,6-tetrahydropyrazolo-[3,4- c]-pyridin-7-one (BMS-740808) a highly potent, selective, efficacious, and orally bioavailable inhibitor of blood coagulation factor Xa
Pinto, Donald J.P., Orwat, Michael J., Quan, Mimi L., Han, Qi, Galemmo, Robert A., Amparo, Eugene, Wells, Brian, Ellis, Christopher, He, Ming Y., Alexander, Richard S., Rossi, Karen A., Smallwood, Angela, Wong, Pancras C., Luettgen, Joseph M., Rendina, Alan R., Knabb, Robert M., Mersinger, Lawrence, Kettner, Charles, Bai, Steven, He, Kan, Wexler, Ruth R., Lam, Patrick Y.S.
Published in Bioorganic & medicinal chemistry letters (01.08.2006)
Published in Bioorganic & medicinal chemistry letters (01.08.2006)
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Journal Article
Structure-Based Design of Novel Guanidine/Benzamidine Mimics: Potent and Orally Bioavailable Factor Xa Inhibitors as Novel Anticoagulants
Lam, Patrick Y. S, Clark, Charles G, Li, Renhua, Pinto, Donald J. P, Orwat, Michael J, Galemmo, Robert A, Fevig, John M, Teleha, Christopher A, Alexander, Richard S, Smallwood, Angela M, Rossi, Karen A, Wright, Matthew R, Bai, Stephen A, He, Kan, Luettgen, Joseph M, Wong, Pancras C, Knabb, Robert M, Wexler, Ruth R
Published in Journal of medicinal chemistry (09.10.2003)
Published in Journal of medicinal chemistry (09.10.2003)
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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
RXFP1 효능제
MATHUR ARVIND, LI JIANQING, CLARKE ADAM JAMES, FRIENDS TODD J, ORWAT MICHAEL J, BARRE DURGA BUCHI RAJU, MYERS MICHAEL C, PINTO DONALD J.P, KUMAR SREEKANTHA RATNA, PABBISETTY KUMAR BALASHANMUGA, SHAW SCOTT A, SMITH II LEON M, SU SHUN, VOKITS BENJAMIN P, POTTURI HIMA KIRAN
Year of Publication 21.06.2024
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Year of Publication 21.06.2024
Patent
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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Journal Article
XIa P2' MACROCYCLES WITH HETROCYCLIC P2' GROUPS AS FACTOR XIA INHIBITORS
SMITH LEON M. II, WEXLER RUTH R, ZHU YEHENG, ORWAT MICHAEL J, PINTO DONALD J. P, DE LUCCA INDAWATI, PABBISETTY KUMAR BALASHANMUGA, FANG TIANAN, WANG YUFENG, DILGER ANDREW K, EWING WILLIAM R, CORTE JAMES R, YANG WU
Year of Publication 06.02.2024
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Year of Publication 06.02.2024
Patent
RXFP1 효능제
MATHUR ARVIND, O'MALLEY DANIEL, LI JIANQING, CLARKE ADAM JAMES, LAWRENCE R. MICHAEL, PASUNOORI LAXMAN, FRIENDS TODD J, ORWAT MICHAEL J, WURTZ NICHOLAS R, BHOGADI VIKRAM, MYERS MICHAEL C, PINTO DONALD J.P, KUMAR SREEKANTHA RATNA, PABBISETTY KUMAR BALASHANMUGA, SHAW SCOTT A, SMITH II LEON M, TORA GEORGE O, SU SHUN, SRINIVAS PITANI VEERA VENKATA, FINLAY HEATHER, HEGDE SUBRAMANYA, BILDER DONNA M, VOKITS BENJAMIN P, POTTURI HIMA KIRAN
Year of Publication 28.06.2024
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Year of Publication 28.06.2024
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