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19 results

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Page 1
Structure based design of macrocyclic factor XIa inhibitors: Discovery of cyclic P1 linker moieties with improved oral bioavailability.
Clark CG, Rossi KA, Corte JR, Fang T, Smallheer JM, De Lucca I, Nirschl DS, Orwat MJ, Pinto DJP, Hu Z, Wang Y, Yang W, Jeon Y, Ewing WR, Myers JE Jr, Sheriff S, Lou Z, Bozarth JM, Wu Y, Rendina A, Harper T, Zheng J, Xin B, Xiang Q, Luettgen JM, Seiffert DA, Wexler RR, Lam PYS. Clark CG, et al. Among authors: orwat mj. Bioorg Med Chem Lett. 2019 Oct 1;29(19):126604. doi: 10.1016/j.bmcl.2019.08.008. Epub 2019 Aug 16. Bioorg Med Chem Lett. 2019. PMID: 31445854
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 DJ, Orwat MJ, Koch S, Rossi KA, Alexander RS, Smallwood A, Wong PC, Rendina AR, Luettgen JM, Knabb RM, He K, Xin B, Wexler RR, Lam PY. Pinto DJ, et al. Among authors: orwat mj. J Med Chem. 2007 Nov 1;50(22):5339-56. doi: 10.1021/jm070245n. Epub 2007 Oct 3. J Med Chem. 2007. PMID: 17914785
Novel phenylalanine derived diamides as Factor XIa inhibitors.
Smith LM 2nd, Orwat MJ, Hu Z, Han W, Wang C, Rossi KA, Gilligan PJ, Pabbisetty KB, Osuna H, Corte JR, Rendina AR, Luettgen JM, Wong PC, Narayanan R, Harper TW, Bozarth JM, Crain EJ, Wei A, Ramamurthy V, Morin PE, Xin B, Zheng J, Seiffert DA, Quan ML, Lam PYS, Wexler RR, Pinto DJP. Smith LM 2nd, et al. Among authors: orwat mj. Bioorg Med Chem Lett. 2016 Jan 15;26(2):472-478. doi: 10.1016/j.bmcl.2015.11.089. Epub 2015 Nov 26. Bioorg Med Chem Lett. 2016. PMID: 26704266
Orally bioavailable pyridine and pyrimidine-based Factor XIa inhibitors: Discovery of the methyl N-phenyl carbamate P2 prime group.
Corte JR, Fang T, Pinto DJ, Orwat MJ, Rendina AR, Luettgen JM, Rossi KA, Wei A, Ramamurthy V, Myers JE Jr, Sheriff S, Narayanan R, Harper TW, Zheng JJ, Li YX, Seiffert DA, Wexler RR, Quan ML. Corte JR, et al. Among authors: orwat mj. Bioorg Med Chem. 2016 May 15;24(10):2257-72. doi: 10.1016/j.bmc.2016.03.062. Epub 2016 Apr 1. Bioorg Med Chem. 2016. PMID: 27073051
Discovery of a Parenteral Small Molecule Coagulation Factor XIa Inhibitor Clinical Candidate (BMS-962212).
Pinto DJP, Orwat MJ, Smith LM 2nd, Quan ML, Lam PYS, Rossi KA, Apedo A, Bozarth JM, Wu Y, Zheng JJ, Xin B, Toussaint N, Stetsko P, Gudmundsson O, Maxwell B, Crain EJ, Wong PC, Lou Z, Harper TW, Chacko SA, Myers JE Jr, Sheriff S, Zhang H, Hou X, Mathur A, Seiffert DA, Wexler RR, Luettgen JM, Ewing WR. Pinto DJP, et al. Among authors: orwat mj. J Med Chem. 2017 Dec 14;60(23):9703-9723. doi: 10.1021/acs.jmedchem.7b01171. Epub 2017 Nov 17. J Med Chem. 2017. PMID: 29077405
Structure-based design of novel guanidine/benzamidine mimics: potent and orally bioavailable factor Xa inhibitors as novel anticoagulants.
Lam PY, Clark CG, Li R, Pinto DJ, Orwat MJ, Galemmo RA, Fevig JM, Teleha CA, Alexander RS, Smallwood AM, Rossi KA, Wright MR, Bai SA, He K, Luettgen JM, Wong PC, Knabb RM, Wexler RR. Lam PY, et al. Among authors: orwat mj. J Med Chem. 2003 Oct 9;46(21):4405-18. doi: 10.1021/jm020578e. J Med Chem. 2003. PMID: 14521405
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 DJ, Orwat MJ, Quan ML, Han Q, Galemmo RA Jr, Amparo E, Wells B, Ellis C, He MY, Alexander RS, Rossi KA, Smallwood A, Wong PC, Luettgen JM, Rendina AR, Knabb RM, Mersinger L, Kettner C, Bai S, He K, Wexler RR, Lam PY. Pinto DJ, et al. Among authors: orwat mj. Bioorg Med Chem Lett. 2006 Aug 1;16(15):4141-7. doi: 10.1016/j.bmcl.2006.02.069. Epub 2006 May 30. Bioorg Med Chem Lett. 2006. PMID: 16730984
Discovery of potent, efficacious, and orally bioavailable inhibitors of blood coagulation factor Xa with neutral P1 moieties.
Pinto DJ, Galemmo RA Jr, Quan ML, Orwat MJ, Clark C, Li R, Wells B, Woerner F, Alexander RS, Rossi KA, Smallwood A, Wong PC, Luettgen JM, Rendina AR, Knabb RM, He K, Wexler RR, Lam PY. Pinto DJ, et al. Among authors: orwat mj. Bioorg Med Chem Lett. 2006 Nov 1;16(21):5584-9. doi: 10.1016/j.bmcl.2006.08.027. Epub 2006 Sep 11. Bioorg Med Chem Lett. 2006. PMID: 16963264
19 results