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Items: 1 to 20 of 105

1.

Synthesis and biological evaluation of a 6-aminofuro[3,2-c]pyridin-3(2H)-one series of GPR 119 agonists.

Sakairi M, Kogami M, Torii M, Kuno Y, Ohsawa Y, Makino M, Kataoka D, Okamoto R, Miyazawa T, Inoue M, Takahashi N, Harada S, Watanabe N.

Arzneimittelforschung. 2012 Nov;62(11):537-44. doi: 10.1055/s-0032-1323760.

PMID:
22972470
2.

Discovery and biological evaluation of novel 4-amino-2-phenylpyrimidine derivatives as potent and orally active GPR119 agonists.

Negoro K, Yonetoku Y, Misawa-Mukai H, Hamaguchi W, Maruyama T, Yoshida S, Takeuchi M, Ohta M.

Bioorg Med Chem. 2012 Sep 1;20(17):5235-46. doi: 10.1016/j.bmc.2012.06.049.

PMID:
22836190
3.

Discovery of 6,7-dihydro-5H-pyrrolo[2,3-a]pyrimidines as orally available G protein-coupled receptor 119 agonists.

Katamreddy SR, Carpenter AJ, Ammala CE, Boros EE, Brashear RL, Briscoe CP, Bullard SR, Caldwell RD, Conlee CR, Croom DK, Hart SM, Heyer DO, Johnson PR, Kashatus JA, Minick DJ, Peckham GE, Ross SA, Roller SG, Samano VA, Sauls HR, Tadepalli SM, Thompson JB, Xu Y, Way JM.

J Med Chem. 2012 Dec 27;55(24):10972-94. doi: 10.1021/jm301404a.

PMID:
23214471
4.

GPR119 agonists for the potential treatment of type 2 diabetes and related metabolic disorders.

Shah U, Kowalski TJ.

Vitam Horm. 2010;84:415-48. doi: 10.1016/B978-0-12-381517-0.00016-3. Review.

PMID:
21094910
5.

AS1907417, a novel GPR119 agonist, as an insulinotropic and β-cell preservative agent for the treatment of type 2 diabetes.

Yoshida S, Tanaka H, Oshima H, Yamazaki T, Yonetoku Y, Ohishi T, Matsui T, Shibasaki M.

Biochem Biophys Res Commun. 2010 Oct 1;400(4):745-51. doi: 10.1016/j.bbrc.2010.08.141.

PMID:
20816753
6.

Identification of a novel GPR119 agonist, AS1269574, with in vitro and in vivo glucose-stimulated insulin secretion.

Yoshida S, Ohishi T, Matsui T, Shibasaki M.

Biochem Biophys Res Commun. 2010 Sep 24;400(3):437-41. doi: 10.1016/j.bbrc.2010.08.097.

PMID:
20804735
7.

Novel GPR119 agonist AS1535907 contributes to first-phase insulin secretion in rat perfused pancreas and diabetic db/db mice.

Yoshida S, Ohishi T, Matsui T, Tanaka H, Oshima H, Yonetoku Y, Shibasaki M.

Biochem Biophys Res Commun. 2010 Nov 12;402(2):280-5. doi: 10.1016/j.bbrc.2010.10.015.

PMID:
20937249
8.

Endogenous and synthetic agonists of GPR119 differ in signalling pathways and their effects on insulin secretion in MIN6c4 insulinoma cells.

Ning Y, O'Neill K, Lan H, Pang L, Shan LX, Hawes BE, Hedrick JA.

Br J Pharmacol. 2008 Dec;155(7):1056-65. doi: 10.1038/bjp.2008.337.

9.

High-throughput screening for GPR119 modulators identifies a novel compound with anti-diabetic efficacy in db/db mice.

Zhang M, Feng Y, Wang J, Zhao J, Li T, He M, Yang D, Nosjean O, Boutin J, Renard P, Wang MW.

PLoS One. 2013 May 21;8(5):e63861. doi: 10.1371/journal.pone.0063861.

10.
11.

The therapeutic potential of GPR119 agonists for type 2 diabetes.

Ohishi T, Yoshida S.

Expert Opin Investig Drugs. 2012 Mar;21(3):321-8. doi: 10.1517/13543784.2012.657797. Review.

PMID:
22292451
12.

Synthesis and structure-activity relationship of fused-pyrimidine derivatives as a series of novel GPR119 agonists.

Negoro K, Yonetoku Y, Moritomo A, Hayakawa M, Iikubo K, Yoshida S, Takeuchi M, Ohta M.

Bioorg Med Chem. 2012 Nov 1;20(21):6442-51. doi: 10.1016/j.bmc.2012.08.054.

PMID:
23010456
13.

Discovery of the first potent and orally efficacious agonist of the orphan G-protein coupled receptor 119.

Semple G, Fioravanti B, Pereira G, Calderon I, Uy J, Choi K, Xiong Y, Ren A, Morgan M, Dave V, Thomsen W, Unett DJ, Xing C, Bossie S, Carroll C, Chu ZL, Grottick AJ, Hauser EK, Leonard J, Jones RM.

J Med Chem. 2008 Sep 11;51(17):5172-5. doi: 10.1021/jm8006867.

PMID:
18698756
14.

5-Hydroxy-eicosapentaenoic acid is an endogenous GPR119 agonist and enhances glucose-dependent insulin secretion.

Kogure R, Toyama K, Hiyamuta S, Kojima I, Takeda S.

Biochem Biophys Res Commun. 2011 Dec 9;416(1-2):58-63. doi: 10.1016/j.bbrc.2011.10.141.

PMID:
22079287
15.

Discovery of 5-chloro-4-((1-(5-chloropyrimidin-2-yl)piperidin-4-yl)oxy)-1-(2-fluoro-4-(methylsulfonyl)phenyl)pyridin-2(1H)-one (BMS-903452), an antidiabetic clinical candidate targeting GPR119.

Wacker DA, Wang Y, Broekema M, Rossi K, O'Connor S, Hong Z, Wu G, Malmstrom SE, Hung CP, LaMarre L, Chimalakonda A, Zhang L, Xin L, Cai H, Chu C, Boehm S, Zalaznick J, Ponticiello R, Sereda L, Han SP, Zebo R, Zinker B, Luk CE, Wong R, Everlof G, Li YX, Wu CK, Lee M, Griffen S, Miller KJ, Krupinski J, Robl JA.

J Med Chem. 2014 Sep 25;57(18):7499-508. doi: 10.1021/jm501175v.

PMID:
25208139
16.

Discovery of structurally novel, potent and orally efficacious GPR119 agonists.

Alper P, Azimioara M, Cow C, Mutnick D, Nikulin V, Michellys PY, Wang Z, Reding E, Paliotti M, Li J, Bao D, Zoll J, Kim Y, Zimmerman M, Groessel T, Tuntland T, Joseph SB, McNamara P, Seidel HM, Epple R.

Bioorg Med Chem Lett. 2014 May 15;24(10):2383-7. doi: 10.1016/j.bmcl.2014.03.023.

PMID:
24751443
17.

Discovery of trifluoromethyl(pyrimidin-2-yl)azetidine-2-carboxamides as potent, orally bioavailable TGR5 (GPBAR1) agonists: structure-activity relationships, lead optimization, and chronic in vivo efficacy.

Phillips DP, Gao W, Yang Y, Zhang G, Lerario IK, Lau TL, Jiang J, Wang X, Nguyen DG, Bhat BG, Trotter C, Sullivan H, Welzel G, Landry J, Chen Y, Joseph SB, Li C, Gordon WP, Richmond W, Johnson K, Bretz A, Bursulaya B, Pan S, McNamara P, Seidel HM.

J Med Chem. 2014 Apr 24;57(8):3263-82. doi: 10.1021/jm401731q.

PMID:
24666203
18.

GPR119 is required for physiological regulation of glucagon-like peptide-1 secretion but not for metabolic homeostasis.

Lan H, Vassileva G, Corona A, Liu L, Baker H, Golovko A, Abbondanzo SJ, Hu W, Yang S, Ning Y, Del Vecchio RA, Poulet F, Laverty M, Gustafson EL, Hedrick JA, Kowalski TJ.

J Endocrinol. 2009 May;201(2):219-30. doi: 10.1677/JOE-08-0453.

19.

Stimulating beta cell replication and improving islet graft function by GPR119 agonists.

Gao J, Tian L, Weng G, Bhagroo NV, Sorenson RL, O'Brien TD, Luo J, Guo Z.

Transpl Int. 2011 Nov;24(11):1124-34. doi: 10.1111/j.1432-2277.2011.01332.x.

20.

Design, synthesis, and biological activity of potent and orally available G protein-coupled receptor 40 agonists.

Sasaki S, Kitamura S, Negoro N, Suzuki M, Tsujihata Y, Suzuki N, Santou T, Kanzaki N, Harada M, Tanaka Y, Kobayashi M, Tada N, Funami M, Tanaka T, Yamamoto Y, Fukatsu K, Yasuma T, Momose Y.

J Med Chem. 2011 Mar 10;54(5):1365-78. doi: 10.1021/jm101405t.

PMID:
21319751
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