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Items: 1 to 20 of 89

1.

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.

PMID:
24767843
2.

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.

PMID:
24931384
3.

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.

PMID:
24164581
4.

New azole antagonists with high affinity for the P2Y(1) receptor.

Ruel R, L'Heureux A, Thibeault C, Daris JP, Martel A, Price LA, Wu Q, Hua J, Wexler RR, Rehfuss R, Lam PY.

Bioorg Med Chem Lett. 2013 Jun 15;23(12):3519-22. doi: 10.1016/j.bmcl.2013.04.041.

PMID:
23668989
5.

2-Aminothiazole based P2Y(1) antagonists as novel antiplatelet agents.

Pi Z, Sutton J, Lloyd J, Hua J, Price L, Wu Q, Chang M, Zheng J, Rehfuss R, Huang CS, Wexler RR, Lam PY.

Bioorg Med Chem Lett. 2013 Jul 15;23(14):4206-9. doi: 10.1016/j.bmcl.2013.05.025.

PMID:
23743287
6.

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.

PMID:
24269480
7.

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.

PMID:
24513044
8.

Discovery of diarylurea P2Y(1) antagonists with improved aqueous solubility.

Wang TC, Qiao JX, Clark CG, Jua J, Price LA, Wu Q, Chang M, Zheng J, Huang CS, Everlof G, Schumacher WA, Wong PC, Seiffert DA, Stewart AB, Bostwick JS, Crain EJ, Watson CA, Rehfuss R, Wexler RR, Lam PY.

Bioorg Med Chem Lett. 2013 Jun 1;23(11):3239-43. doi: 10.1016/j.bmcl.2013.03.125.

PMID:
23602442
9.

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.

PMID:
24989964
10.

Modified diadenosine tetraphosphates with dual specificity for P2Y1 and P2Y12 are potent antagonists of ADP-induced platelet activation.

Chang H, Yanachkov IB, Dix EJ, Li YF, Barnard MR, Wright GE, Michelson AD, Frelinger AL 3rd.

J Thromb Haemost. 2012 Dec;10(12):2573-80. doi: 10.1111/jth.12035.

11.

Identification of contractile P2Y1, P2Y6, and P2Y12 receptors in rat intrapulmonary artery using selective ligands.

Mitchell C, Syed NI, Tengah A, Gurney AM, Kennedy C.

J Pharmacol Exp Ther. 2012 Dec;343(3):755-62. doi: 10.1124/jpet.112.198051.

12.

Benzofuran-substituted urea derivatives as novel P2Y(1) receptor antagonists.

Thalji RK, Aiyar N, Davenport EA, Erhardt JA, Kallal LA, Morrow DM, Senadhi S, Burns-Kurtis CL, Marino JP Jr.

Bioorg Med Chem Lett. 2010 Jul 15;20(14):4104-7. doi: 10.1016/j.bmcl.2010.05.072.

PMID:
20542694
13.

Nucleoside triphosphates inhibit ADP, collagen, and epinephrine-induced platelet aggregation: role of P2Y₁ and P2Y₁₂ receptors.

Aslam M, Sedding D, Koshty A, Santoso S, Schulz R, Hamm C, Gündüz D.

Thromb Res. 2013 Nov;132(5):548-57. doi: 10.1016/j.thromres.2013.08.021.

PMID:
24071464
14.

Discovery of 2-(phenoxypyridine)-3-phenylureas as small molecule P2Y1 antagonists.

Chao H, Turdi H, Herpin TF, Roberge JY, Liu Y, Schnur DM, Poss MA, Rehfuss R, Hua J, Wu Q, Price LA, Abell LM, Schumacher WA, Bostwick JS, Steinbacher TE, Stewart AB, Ogletree ML, Huang CS, Chang M, Cacace AM, Arcuri MJ, Celani D, Wexler RR, Lawrence RM.

J Med Chem. 2013 Feb 28;56(4):1704-14. doi: 10.1021/jm301708u.

PMID:
23368907
15.

Discovery of acylurea isosteres of 2-acylaminothiadiazole in the azaxanthene series of glucocorticoid receptor agonists.

Gong H, Yang M, Xiao Z, Doweyko AM, Cunningham M, Wang J, Habte S, Holloway D, Burke C, Shuster D, Gao L, Carman J, Somerville JE, Nadler SG, Salter-Cid L, Barrish JC, Weinstein DS.

Bioorg Med Chem Lett. 2014 Aug 1;24(15):3268-73. doi: 10.1016/j.bmcl.2014.06.010.

PMID:
24980053
16.

Thiazole and thiadiazole analogues as a novel class of adenosine receptor antagonists.

van Muijlwijk-Koezen JE, Timmerman H, Vollinga RC, Frijtag von Drabbe Künzel J, de Groote M, Visser S, IJzerman AP.

J Med Chem. 2001 Mar 1;44(5):749-62.

PMID:
11262085
17.

Virtual screening leads to the discovery of novel non-nucleotide P2Y₁ receptor antagonists.

Costanzi S, Santhosh Kumar T, Balasubramanian R, Kendall Harden T, Jacobson KA.

Bioorg Med Chem. 2012 Sep 1;20(17):5254-61. doi: 10.1016/j.bmc.2012.06.044.

18.

Discovery of a series of potent arylthiadiazole H(3) antagonists.

Xiao D, Palani A, Sofolarides M, Huang Y, Aslanian R, Vaccaro H, Hong L, McKittrick B, West RE Jr, Williams SM, Wu RL, Hwa J, Sondey C, Lachowicz J.

Bioorg Med Chem Lett. 2011 Jan 15;21(2):861-4. doi: 10.1016/j.bmcl.2010.11.065.

PMID:
21186123
19.

Effect of P2Y1 and P2Y12 genetic polymorphisms on the ADP-induced platelet aggregation in a Korean population.

Kim KA, Song WG, Lee HM, Joo HJ, Park JY.

Thromb Res. 2013 Aug;132(2):221-6. doi: 10.1016/j.thromres.2013.06.020.

PMID:
23849096
20.

Synthesis, structure-property relationships and pharmacokinetic evaluation of ethyl 6-aminonicotinate sulfonylureas as antagonists of the P2Y₁₂ receptor.

Bach P, Boström J, Brickmann K, van Giezen JJ, Groneberg RD, Harvey DM, O'Sullivan M, Zetterberg F.

Eur J Med Chem. 2013 Jul;65:360-75. doi: 10.1016/j.ejmech.2013.04.007.

PMID:
23747805
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