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Items: 1 to 50 of 157

1.

Benzothiazole-based compounds as potent endothelial lipase inhibitors.

Meng W, Adam LP, Behnia K, Zhao L, Yang R, Kopcho LM, Locke GA, Taylor DS, Yin X, Wexler RR, Finlay H.

Bioorg Med Chem Lett. 2019 Oct 15;29(20):126673. doi: 10.1016/j.bmcl.2019.126673. Epub 2019 Sep 6.

PMID:
31519373
2.

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.

Bioorg Med Chem Lett. 2019 Oct 1;29(19):126604. doi: 10.1016/j.bmcl.2019.08.008. Epub 2019 Aug 16.

PMID:
31445854
3.

Corrigendum to "Identification of substituted benzothiazole sulfones as potent and selective inhibitors of endothelial lipase" [Bioorg. Med. Chem. Lett. 29 (2019) 1918-1921].

Kim SH, Johnson JA, Jiang J, Parkhurst B, Phillips M, Pi Z, Qiao JX, Tora G, Ye Chen A, Liu E, Yin X, Yang R, Zhao L, Taylor DS, Basso M, Behnia K, Onorato J, Chen XQ, Abell LM, Lu H, Locke G, Caporuscio C, Adam LP, Gordon D, Wexler RR, Finlay HJ.

Bioorg Med Chem Lett. 2019 Sep 1;29(17):2525. doi: 10.1016/j.bmcl.2019.07.032. Epub 2019 Jul 25. No abstract available.

PMID:
31353296
4.

Discovery of Potent Protease-Activated Receptor 4 Antagonists with in Vivo Antithrombotic Efficacy.

Miller MM, Banville J, Friends TJ, Gagnon M, Hangeland JJ, Lavallée JF, Martel A, O'Grady H, Rémillard R, Ruediger E, Tremblay F, Posy SL, Allegretto NJ, Guarino VR, Harden DG, Harper TW, Hartl K, Josephs J, Malmstrom S, Watson C, Yang Y, Zhang G, Wong P, Yang J, Bouvier M, Seiffert DA, Wexler RR, Lawrence RM, Priestley ES, Marinier A.

J Med Chem. 2019 Aug 22;62(16):7400-7416. doi: 10.1021/acs.jmedchem.9b00186. Epub 2019 Aug 5.

PMID:
31246024
5.

Discovery of a Lead Triphenylethanamine Cholesterol Ester Transfer Protein (CETP) Inhibitor.

Finlay HJ, Jiang J, Rampulla R, Salvati ME, Qiao JX, Wang TC, Lawrence RM, Harikrishnan LS, Kamau MG, Taylor DS, Chen AYA, Yin X, Huang CS, Chang M, Chen XQ, Sleph PG, Xu C, Li J, Levesque P, Adam LP, Wexler RR.

ACS Med Chem Lett. 2019 May 6;10(6):911-916. doi: 10.1021/acsmedchemlett.9b00086. eCollection 2019 Jun 13.

PMID:
31223447
6.

Identification of substituted benzothiazole sulfones as potent and selective inhibitors of endothelial lipase.

Kim SH, Johnson JA, Jiang J, Parkhurst B, Phillips M, Pi Z, Qiao JX, Tora G, Ye Chen A, Liu E, Yin X, Yang R, Zhao L, Taylor DS, Basso M, Behnia K, Onorato J, Chen XQ, Abell LM, Lu H, Locke G, Caporuscio C, Adam LP, Gordon D, Wexler RR, Finlay HJ.

Bioorg Med Chem Lett. 2019 Aug 1;29(15):1918-1921. doi: 10.1016/j.bmcl.2019.05.048. Epub 2019 May 25. Erratum in: Bioorg Med Chem Lett. 2019 Sep 1;29(17):2525.

PMID:
31176700
7.

Sulfonylated Benzothiazoles as Inhibitors of Endothelial Lipase.

Johnson JA, Tora G, Pi Z, Phillips M, Yin X, Yang R, Zhao L, Chen AY, Taylor DS, Basso M, Rose A, Behnia K, Onorato J, Chen XQ, Abell LM, Lu H, Locke G, Caporuscio C, Galella M, Adam LP, Gordon D, Wexler RR, Finlay HJ.

ACS Med Chem Lett. 2018 Nov 21;9(12):1263-1268. doi: 10.1021/acsmedchemlett.8b00424. eCollection 2018 Dec 13.

PMID:
30613337
8.

Potent Triazolopyridine Myeloperoxidase Inhibitors.

Wurtz NR, Viet A, Shaw SA, Dilger A, Valente MN, Khan JA, Jusuf S, Narayanan R, Fernando G, Lo F, Liu X, Locke GA, Kopcho L, Abell LM, Sleph P, Basso M, Zhao L, Wexler RR, Duclos F, Kick EK.

ACS Med Chem Lett. 2018 Nov 1;9(12):1175-1180. doi: 10.1021/acsmedchemlett.8b00308. eCollection 2018 Dec 13.

PMID:
30613322
9.

Discovery and synthesis of tetrahydropyrimidinedione-4-carboxamides as endothelial lipase inhibitors.

Hu CH, Wang TC, Qiao JX, Haque L, Chen AYA, Taylor DS, Ying X, Onorato JM, Galella M, Shen H, Huang CS, Toussaint N, Li YX, Abell L, Adam LP, Gordon D, Wexler RR, Finlay HJ.

Bioorg Med Chem Lett. 2018 Dec 15;28(23-24):3721-3725. doi: 10.1016/j.bmcl.2018.10.022. Epub 2018 Oct 15.

PMID:
30348490
10.

Triazolopyrimidines identified as reversible myeloperoxidase inhibitors.

Duclos F, Abell LM, Harden DG, Pike K, Nowak K, Locke GA, Duke GJ, Liu X, Fernando G, Shaw SA, Vokits BP, Wurtz NR, Viet A, Valente MN, Stachura S, Sleph P, Khan JA, Gao J, Dongre AR, Zhao L, Wexler RR, Gordon DA, Kick EK.

Medchemcomm. 2017 Oct 26;8(11):2093-2099. doi: 10.1039/c7md00268h. eCollection 2017 Nov 1.

11.

PK/PD Disconnect Observed with a Reversible Endothelial Lipase Inhibitor.

Hangeland JJ, Abell LM, Adam LP, Jiang J, Friends TJ, Haque LE, Neels J, Onorato JM, Chen AYA, Taylor DS, Yin X, Harrity TW, Basso MD, Yang R, Sleph PG, Gordon DA, Huang CS, Wexler RR, Finlay HJ, Lawrence RM.

ACS Med Chem Lett. 2018 Jun 15;9(7):673-678. doi: 10.1021/acsmedchemlett.8b00138. eCollection 2018 Jul 12.

12.

Factor XIa Inhibitors as New Anticoagulants.

Quan ML, Pinto DJP, Smallheer JM, Ewing WR, Rossi KA, Luettgen JM, Seiffert DA, Wexler RR.

J Med Chem. 2018 Sep 13;61(17):7425-7447. doi: 10.1021/acs.jmedchem.8b00173. Epub 2018 May 18. Review.

PMID:
29775297
13.

Correction to "Atropisomer Control in Macrocyclic Factor VIIa Inhibitors".

Glunz PW, Mueller L, Cheney DL, Ladziata V, Zou Y, Wurtz NR, Wei A, Wong PC, Wexler RR, Priestley ES.

J Med Chem. 2018 Apr 26;61(8):3752. doi: 10.1021/acs.jmedchem.8b00465. Epub 2018 Apr 5. No abstract available.

PMID:
29620363
14.

Pyridazine and pyridazinone derivatives as potent and selective factor XIa inhibitors.

Hu Z, Wang C, Han W, Rossi KA, Bozarth JM, Wu Y, Sheriff S, Myers JE Jr, Luettgen JM, Seiffert DA, Wexler RR, Quan ML.

Bioorg Med Chem Lett. 2018 Apr 1;28(6):987-992. doi: 10.1016/j.bmcl.2018.02.049. Epub 2018 Feb 27.

PMID:
29501396
15.

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.

J Med Chem. 2017 Dec 14;60(23):9703-9723. doi: 10.1021/acs.jmedchem.7b01171. Epub 2017 Nov 17.

PMID:
29077405
16.

Macrocyclic factor XIa inhibitors.

Wang C, Corte JR, Rossi KA, Bozarth JM, Wu Y, Sheriff S, Myers JE Jr, Luettgen JM, Seiffert DA, Wexler RR, Quan ML.

Bioorg Med Chem Lett. 2017 Sep 1;27(17):4056-4060. doi: 10.1016/j.bmcl.2017.07.048. Epub 2017 Jul 25.

PMID:
28780160
17.

Macrocyclic inhibitors of Factor XIa: Discovery of alkyl-substituted macrocyclic amide linkers with improved potency.

Corte JR, Yang W, Fang T, Wang Y, Osuna H, Lai A, Ewing WR, Rossi KA, Myers JE Jr, Sheriff S, Lou Z, Zheng JJ, Harper TW, Bozarth JM, Wu Y, Luettgen JM, Seiffert DA, Quan ML, Wexler RR, Lam PYS.

Bioorg Med Chem Lett. 2017 Aug 15;27(16):3833-3839. doi: 10.1016/j.bmcl.2017.06.058. Epub 2017 Jun 23.

PMID:
28687203
18.

Neutral macrocyclic factor VIIa inhibitors.

Wurtz NR, Parkhurst BL, DeLucca I, Glunz PW, Jiang W, Zhang X, Cheney DL, Bozarth JM, Rendina AR, Wei A, Harper T, Luettgen JM, Wu Y, Wong PC, Seiffert DA, Wexler RR, Priestley ES.

Bioorg Med Chem Lett. 2017 Jun 15;27(12):2650-2654. doi: 10.1016/j.bmcl.2017.04.008. Epub 2017 Apr 19.

PMID:
28460818
19.

Selective IKur Inhibitors for the Potential Treatment of Atrial Fibrillation: Optimization of the Phenyl Quinazoline Series Leading to Clinical Candidate 5-[5-Phenyl-4-(pyridin-2-ylmethylamino)quinazolin-2-yl]pyridine-3-sulfonamide.

Gunaga P, Lloyd J, Mummadi S, Banerjee A, Dhondi NK, Hennan J, Subray V, Jayaram R, Rajugowda N, Umamaheshwar Reddy K, Kumaraguru D, Mandal U, Beldona D, Adisechen AK, Yadav N, Warrier J, Johnson JA, Sale H, Putlur SP, Saxena A, Chimalakonda A, Mandlekar S, Conder M, Xing D, Gupta AK, Gupta A, Rampulla R, Mathur A, Levesque P, Wexler RR, Finlay HJ.

J Med Chem. 2017 May 11;60(9):3795-3803. doi: 10.1021/acs.jmedchem.6b01889. Epub 2017 Apr 28.

PMID:
28418664
20.

Design and Synthesis of Novel Meta-Linked Phenylglycine Macrocyclic FVIIa Inhibitors.

Richter JM, Cheney DL, Bates JA, Wei A, Luettgen JM, Rendina AR, Harper TM, Narayanan R, Wong PC, Seiffert D, Wexler RR, Priestley ES.

ACS Med Chem Lett. 2016 Nov 1;8(1):67-72. doi: 10.1021/acsmedchemlett.6b00375. eCollection 2017 Jan 12.

21.

Structure-Based Design of Macrocyclic Factor XIa Inhibitors: Discovery of the Macrocyclic Amide Linker.

Corte JR, Fang T, Osuna H, Pinto DJ, Rossi KA, Myers JE Jr, Sheriff S, Lou Z, Zheng JJ, Harper TW, Bozarth JM, Wu Y, Luettgen JM, Seiffert DA, Decicco CP, Wexler RR, Quan ML.

J Med Chem. 2017 Feb 9;60(3):1060-1075. doi: 10.1021/acs.jmedchem.6b01460. Epub 2017 Jan 31.

PMID:
28085275
22.

Blockade of protease-activated receptor-4 (PAR4) provides robust antithrombotic activity with low bleeding.

Wong PC, Seiffert D, Bird JE, Watson CA, Bostwick JS, Giancarli M, Allegretto N, Hua J, Harden D, Guay J, Callejo M, Miller MM, Lawrence RM, Banville J, Guy J, Maxwell BD, Priestley ES, Marinier A, Wexler RR, Bouvier M, Gordon DA, Schumacher WA, Yang J.

Sci Transl Med. 2017 Jan 4;9(371). pii: eaaf5294. doi: 10.1126/scitranslmed.aaf5294.

PMID:
28053157
23.

Discovery of Highly Potent Liver X Receptor β Agonists.

Kick EK, Busch BB, Martin R, Stevens WC, Bollu V, Xie Y, Boren BC, Nyman MC, Nanao MH, Nguyen L, Plonowski A, Schulman IG, Yan G, Zhang H, Hou X, Valente MN, Narayanan R, Behnia K, Rodrigues AD, Brock B, Smalley J, Cantor GH, Lupisella J, Sleph P, Grimm D, Ostrowski J, Wexler RR, Kirchgessner T, Mohan R.

ACS Med Chem Lett. 2016 Oct 23;7(12):1207-1212. eCollection 2016 Dec 8.

24.

Discovery of Phenylglycine Lactams as Potent Neutral Factor VIIa Inhibitors.

Wurtz NR, Parkhurst BL, Jiang W, DeLucca I, Zhang X, Ladziata V, Cheney DL, Bozarth JR, Rendina AR, Wei A, Luettgen JM, Wu Y, Wong PC, Seiffert DA, Wexler RR, Priestley ES.

ACS Med Chem Lett. 2016 Sep 17;7(12):1077-1081. eCollection 2016 Dec 8.

25.

Discovery of 5-Phenyl-N-(pyridin-2-ylmethyl)-2-(pyrimidin-5-yl)quinazolin-4-amine as a Potent I Kur Inhibitor.

Finlay HJ, Johnson JA, Lloyd JL, Jiang J, Neels J, Gunaga P, Banerjee A, Dhondi N, Chimalakonda A, Mandlekar S, Conder ML, Sale H, Xing D, Levesque P, Wexler RR.

ACS Med Chem Lett. 2016 Jun 9;7(9):831-4. doi: 10.1021/acsmedchemlett.6b00117. eCollection 2016 Sep 8.

26.

Synthesis and P1' SAR exploration of potent macrocyclic tissue factor-factor VIIa inhibitors.

Ladziata VU, Glunz PW, Zou Y, Zhang X, Jiang W, Jacutin-Porte S, Cheney DL, Wei A, Luettgen JM, Harper TM, Wong PC, Seiffert D, Wexler RR, Priestley ES.

Bioorg Med Chem Lett. 2016 Oct 15;26(20):5051-5057. doi: 10.1016/j.bmcl.2016.08.088. Epub 2016 Aug 28.

PMID:
27612545
27.

Discovery of a Highly Potent, Selective, and Orally Bioavailable Macrocyclic Inhibitor of Blood Coagulation Factor VIIa-Tissue Factor Complex.

Zhang X, Glunz PW, Johnson JA, Jiang W, Jacutin-Porte S, Ladziata V, Zou Y, Phillips MS, Wurtz NR, Parkhurst B, Rendina AR, Harper TM, Cheney DL, Luettgen JM, Wong PC, Seiffert D, Wexler RR, Priestley ES.

J Med Chem. 2016 Aug 11;59(15):7125-37. doi: 10.1021/acs.jmedchem.6b00469. Epub 2016 Aug 2.

PMID:
27455395
28.

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.

Bioorg Med Chem. 2016 May 15;24(10):2257-72. doi: 10.1016/j.bmc.2016.03.062. Epub 2016 Apr 1.

PMID:
27073051
29.

Atropisomer Control in Macrocyclic Factor VIIa Inhibitors.

Glunz PW, Mueller L, Cheney DL, Ladziata V, Zou Y, Wurtz NR, Wei A, Wong PC, Wexler RR, Priestley ES.

J Med Chem. 2016 Apr 28;59(8):4007-18. doi: 10.1021/acs.jmedchem.6b00244. Epub 2016 Apr 8. Erratum in: J Med Chem. 2018 Apr 26;61(8):3752.

PMID:
27015008
30.

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.

Bioorg Med Chem Lett. 2016 Jan 15;26(2):472-478. doi: 10.1016/j.bmcl.2015.11.089. Epub 2015 Nov 26.

PMID:
26704266
31.

Triphenylethanamine Derivatives as Cholesteryl Ester Transfer Protein Inhibitors: Discovery of N-[(1R)-1-(3-Cyclopropoxy-4-fluorophenyl)-1-[3-fluoro-5-(1,1,2,2-tetrafluoroethoxy)phenyl]-2-phenylethyl]-4-fluoro-3-(trifluoromethyl)benzamide (BMS-795311).

Qiao JX, Wang TC, Adam LP, Chen AY, Taylor DS, Yang RZ, Zhuang S, Sleph PG, Li JP, Li D, Yin X, Chang M, Chen XQ, Shen H, Li J, Smith D, Wu DR, Leith L, Harikrishnan LS, Kamau MG, Miller MM, Bilder D, Rampulla R, Li YX, Xu C, Lawrence RM, Poss MA, Levesque P, Gordon DA, Huang CS, Finlay HJ, Wexler RR, Salvati ME.

J Med Chem. 2015 Nov 25;58(22):9010-26. doi: 10.1021/acs.jmedchem.5b01363. Epub 2015 Nov 17.

PMID:
26524347
32.

In vitro, antithrombotic and bleeding time studies of BMS-654457, a small-molecule, reversible and direct inhibitor of factor XIa.

Wong PC, Quan ML, Watson CA, Crain EJ, Harpel MR, Rendina AR, Luettgen JM, Wexler RR, Schumacher WA, Seiffert DA.

J Thromb Thrombolysis. 2015 Nov;40(4):416-23. doi: 10.1007/s11239-015-1258-7.

PMID:
26249722
33.

Structure-Based Design of Macrocyclic Coagulation Factor VIIa Inhibitors.

Priestley ES, Cheney DL, DeLucca I, Wei A, Luettgen JM, Rendina AR, Wong PC, Wexler RR.

J Med Chem. 2015 Aug 13;58(15):6225-36. doi: 10.1021/acs.jmedchem.5b00788. Epub 2015 Jul 28.

PMID:
26151189
34.

Discovery of a Potent Parenterally Administered Factor XIa Inhibitor with Hydroxyquinolin-2(1H)-one as the P2' Moiety.

Hu Z, Wong PC, Gilligan PJ, Han W, Pabbisetty KB, Bozarth JM, Crain EJ, Harper T, Luettgen JM, Myers JE Jr, Ramamurthy V, Rossi KA, Sheriff S, Watson CA, Wei A, Zheng JJ, Seiffert DA, Wexler RR, Quan ML.

ACS Med Chem Lett. 2015 Apr 8;6(5):590-5. doi: 10.1021/acsmedchemlett.5b00066. eCollection 2015 May 14.

35.

Design and synthesis of potent, selective phenylimidazole-based FVIIa inhibitors.

Glunz PW, Cheng X, Cheney DL, Weigelt CA, Wei A, Luettgen JM, Wong PC, Wexler RR, Priestley ES.

Bioorg Med Chem Lett. 2015;25(10):2169-73. doi: 10.1016/j.bmcl.2015.03.062. Epub 2015 Mar 30.

PMID:
25881820
36.

Discovery of novel P1 groups for coagulation factor VIIa inhibition using fragment-based screening.

Cheney DL, Bozarth JM, Metzler WJ, Morin PE, Mueller L, Newitt JA, Nirschl AH, Rendina AR, Tamura JK, Wei A, Wen X, Wurtz NR, Seiffert DA, Wexler RR, Priestley ES.

J Med Chem. 2015 Mar 26;58(6):2799-808. doi: 10.1021/jm501982k. Epub 2015 Mar 12.

PMID:
25764119
37.

Structure-based design of inhibitors of coagulation factor XIa with novel P1 moieties.

Pinto DJ, Smallheer JM, Corte JR, Austin EJ, Wang C, Fang T, Smith LM 2nd, Rossi KA, Rendina AR, Bozarth JM, Zhang G, Wei A, Ramamurthy V, Sheriff S, Myers JE Jr, Morin PE, Luettgen JM, Seiffert DA, Quan ML, Wexler RR.

Bioorg Med Chem Lett. 2015 Apr 1;25(7):1635-42. doi: 10.1016/j.bmcl.2015.01.028. Epub 2015 Feb 4.

PMID:
25728130
38.

Pyridine and pyridinone-based factor XIa inhibitors.

Corte JR, Fang T, Hangeland JJ, Friends TJ, Rendina AR, Luettgen JM, Bozarth JM, Barbera FA, Rossi KA, Wei A, Ramamurthy V, Morin PE, Seiffert DA, Wexler RR, Quan ML.

Bioorg Med Chem Lett. 2015 Feb 15;25(4):925-30. doi: 10.1016/j.bmcl.2014.12.050. Epub 2014 Dec 31.

PMID:
25592713
39.

Phenylimidazoles as potent and selective inhibitors of coagulation factor XIa with in vivo antithrombotic activity.

Hangeland JJ, Friends TJ, Rossi KA, Smallheer JM, Wang C, Sun Z, Corte JR, Fang T, Wong PC, Rendina AR, Barbera FA, Bozarth JM, Luettgen JM, Watson CA, Zhang G, Wei A, Ramamurthy V, Morin PE, Bisacchi GS, Subramaniam S, Arunachalam P, Mathur A, Seiffert DA, Wexler RR, Quan ML.

J Med Chem. 2014 Dec 11;57(23):9915-32. doi: 10.1021/jm5010607. Epub 2014 Dec 2.

PMID:
25405503
40.

4-Benzothiazole-7-hydroxyindolinyl diaryl ureas are potent P2Y1 antagonists with favorable pharmacokinetics: low clearance and small volume of distribution.

Qiao JX, Wang TC, Hiebert S, Hu CH, Schumacher WA, Spronk SA, Clark CG, Han Y, Hua J, Price LA, Shen H, Chacko SA, Everlof G, Bostwick JS, Steinbacher TE, Li YX, Huang CS, Seiffert DA, Rehfuss R, Wexler RR, Lam PY.

ChemMedChem. 2014 Oct;9(10):2327-43. doi: 10.1002/cmdc.201402141. Epub 2014 Jul 2.

PMID:
24989964
41.

Orally bioavailable factor Xa inhibitors containing alpha-substituted gem-dimethyl P4 moieties.

Orwat MJ, Qiao JX, He K, Rendina AR, Luettgen JM, Rossi KA, Xin B, Knabb RM, Wexler RR, Lam PY, Pinto DJ.

Bioorg Med Chem Lett. 2014 Aug 1;24(15):3341-5. doi: 10.1016/j.bmcl.2014.05.101. Epub 2014 Jun 7.

PMID:
24951330
42.

Discovery of 4-aryl-7-hydroxyindoline-based P2Y1 antagonists as novel antiplatelet agents.

Yang W, Wang Y, Lai A, Qiao JX, Wang TC, Hua J, Price LA, Shen H, Chen XQ, Wong P, Crain E, Watson C, Huang CS, Seiffert DA, Rehfuss R, Wexler RR, Lam PY.

J Med Chem. 2014 Jul 24;57(14):6150-64. doi: 10.1021/jm5006226. Epub 2014 Jul 7.

PMID:
24931384
43.

Design and Synthesis of Phenylpyrrolidine Phenylglycinamides As Highly Potent and Selective TF-FVIIa Inhibitors.

Zhang X, Jiang W, Jacutin-Porte S, Glunz PW, Zou Y, Cheng X, Nirschl AH, Wurtz NR, Luettgen JM, Rendina AR, Luo G, Harper TM, Wei A, Anumula R, Cheney DL, Knabb RM, Wong PC, Wexler RR, Priestley ES.

ACS Med Chem Lett. 2013 Dec 26;5(2):188-92. doi: 10.1021/ml400453z. eCollection 2014 Feb 13.

44.

Design, synthesis and evaluation of phenethylaminoheterocycles as K(v)1.5 inhibitors.

Johnson JA, Xu N, Jeon Y, Finlay HJ, Kover A, Conder ML, Sun H, Li D, Levesque P, Hsueh MM, Harper TW, Wexler RR, Lloyd J.

Bioorg Med Chem Lett. 2014 Jul 15;24(14):3018-22. doi: 10.1016/j.bmcl.2014.05.035. Epub 2014 May 20.

PMID:
24881565
45.

2-Amino-1,3,4-thiadiazoles in the 7-hydroxy-N-neopentyl spiropiperidine indolinyl series as potent P2Y1 receptor antagonists.

Hu CH, Qiao JX, Han Y, Wang TC, Hua J, Price LA, Wu Q, Shen H, Huang CS, Rehfuss R, Wexler RR, Lam PY.

Bioorg Med Chem Lett. 2014 Jun 1;24(11):2481-5. doi: 10.1016/j.bmcl.2014.04.011. Epub 2014 Apr 13.

PMID:
24767843
46.

Identification of 1-{2-[4-chloro-1'-(2,2-dimethylpropyl)-7-hydroxy-1,2-dihydrospiro[indole-3,4'-piperidine]-1-yl]phenyl}-3-{5-chloro-[1,3]thiazolo[5,4-b]pyridin-2-yl}urea, a potent, efficacious and orally bioavailable P2Y(1) antagonist as an antiplatelet agent.

Jeon YT, Yang W, Qiao JX, Li L, Ruel R, Thibeault C, Hiebert S, Wang TC, Wang Y, Liu Y, Clark CG, Wong HS, Zhu J, Wu DR, Sun D, Chen BC, Mathur A, Chacko SA, Malley M, Chen XQ, Shen H, Huang CS, Schumacher WA, Bostwick JS, Stewart AB, Price LA, Hua J, Li D, Levesque PC, Seiffert DA, Rehfuss R, Wexler RR, Lam PY.

Bioorg Med Chem Lett. 2014 Mar 1;24(5):1294-8. doi: 10.1016/j.bmcl.2014.01.066. Epub 2014 Jan 31.

PMID:
24513044
47.

Diphenylpyridylethanamine (DPPE)-based aminoheterocycles as cholesteryl ester transfer protein inhibitors.

Wang Y, Yang W, Finlay HJ, Harikrishnan LS, Jiang J, Kamau MG, Van Kirk K, Nirschl DS, Taylor DS, Chen AY, Yin X, Sleph PG, Yang RZ, Huang CS, Adam LP, Lawrence RM, Wexler RR, Salvati ME.

Bioorg Med Chem Lett. 2014 Feb 1;24(3):860-4. doi: 10.1016/j.bmcl.2013.12.088. Epub 2014 Jan 6.

PMID:
24424134
48.

Tetrahydroquinoline derivatives as potent and selective factor XIa inhibitors.

Quan ML, Wong PC, Wang C, Woerner F, Smallheer JM, Barbera FA, Bozarth JM, Brown RL, Harpel MR, Luettgen JM, Morin PE, Peterson T, Ramamurthy V, Rendina AR, Rossi KA, Watson CA, Wei A, Zhang G, Seiffert D, Wexler RR.

J Med Chem. 2014 Feb 13;57(3):955-69. doi: 10.1021/jm401670x. Epub 2014 Jan 17.

PMID:
24405333
49.

Potent P2Y1 urea antagonists bearing various cyclic amine scaffolds.

Ruel R, L'Heureux A, Thibeault C, Lapointe P, Martel A, Qiao JX, Hua J, Price LA, Wu Q, Chang M, Zheng J, Huang CS, Wexler RR, Rehfuss R, Lam PY.

Bioorg Med Chem Lett. 2013 Dec 15;23(24):6825-8. doi: 10.1016/j.bmcl.2013.10.009. Epub 2013 Oct 11.

PMID:
24269480
50.

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 JX, Wang TC, Ruel R, Thibeault C, L'Heureux A, Schumacher WA, Spronk SA, Hiebert S, Bouthillier G, Lloyd J, Pi Z, Schnur DM, Abell LM, Hua J, Price LA, Liu E, Wu Q, Steinbacher TE, Bostwick JS, Chang M, Zheng J, Gao Q, Ma B, McDonnell PA, Huang CS, Rehfuss R, Wexler RR, Lam PY.

J Med Chem. 2013 Nov 27;56(22):9275-95. doi: 10.1021/jm4013906. Epub 2013 Nov 12.

PMID:
24164581

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