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Items: 1 to 20 of 95

1.

The discovery of SB-435495. A potent, orally active inhibitor of lipoprotein-associated phospholipase A(2) for evaluation in man.

Blackie JA, Bloomer JC, Brown MJ, Cheng HY, Elliott RL, Hammond B, Hickey DM, Ife RJ, Leach CA, Lewis VA, Macphee CH, Milliner KJ, Moores KE, Pinto IL, Smith SA, Stansfield IG, Stanway SJ, Taylor MA, Theobald CJ, Whittaker CM.

Bioorg Med Chem Lett. 2002 Sep 16;12(18):2603-6.

PMID:
12182870
2.

N-1 substituted pyrimidin-4-ones: novel, orally active inhibitors of lipoprotein-associated phospholipase A2.

Boyd HF, Fell SC, Flynn ST, Hickey DM, Ife RJ, Leach CA, Macphee CH, Milliner KJ, Moores KE, Pinto IL, Porter RA, Rawlings DA, Smith SA, Stansfield IG, Tew DG, Theobald CJ, Whittaker CM.

Bioorg Med Chem Lett. 2000 Nov 20;10(22):2557-61.

PMID:
11086729
3.

The identification of clinical candidate SB-480848: a potent inhibitor of lipoprotein-associated phospholipase A2.

Blackie JA, Bloomer JC, Brown MJ, Cheng HY, Hammond B, Hickey DM, Ife RJ, Leach CA, Lewis VA, Macphee CH, Milliner KJ, Moores KE, Pinto IL, Smith SA, Stansfield IG, Stanway SJ, Taylor MA, Theobald CJ.

Bioorg Med Chem Lett. 2003 Mar 24;13(6):1067-70.

PMID:
12643913
4.

The identification of a potent, water soluble inhibitor of lipoprotein-associated phospholipase A2.

Boyd HF, Hammond B, Hickey DM, Ife RJ, Leach CA, Lewis VA, Macphee CH, Milliner KJ, Pinto IL, Smith SA, Stansfield IG, Theobald CJ, Whittaker CM.

Bioorg Med Chem Lett. 2001 Mar 12;11(5):701-4.

PMID:
11266173
5.

Potent, orally active inhibitors of lipoprotein-associated phospholipase A(2): 1-(biphenylmethylamidoalkyl)-pyrimidones.

Boyd HF, Fell SC, Hickey DM, Ife RJ, Leach CA, Macphee CH, Milliner KJ, Pinto IL, Rawlings DA, Smith SA, Stansfield IG, Stanway SJ, Theobald CJ, Whittaker CM.

Bioorg Med Chem Lett. 2002 Jan 7;12(1):51-5.

PMID:
11738571
6.

1-(Arylpiperazinylamidoalkyl)-pyrimidones: orally active inhibitors of lipoprotein-associated phospholipase A(2).

Bloomer JC, Boyd HF, Hickey DM, Ife RJ, Leach CA, Macphee CH, Milliner KJ, Pinto IL, Rawlings DA, Smith SA, Stansfield IG, Stanway SJ, Taylor MA, Theobald CJ, Whittaker CM.

Bioorg Med Chem Lett. 2001 Jul 23;11(14):1925-9.

PMID:
11459662
7.

2-(Alkylthio)pyrimidin-4-ones as novel, reversible inhibitors of lipoprotein-associated phospholipase A2.

Boyd HF, Flynn ST, Hickey DM, Ife RJ, Jones M, Leach CA, Macphee CH, Milliner KJ, Rawlings DA, Slingsby BP, Smith SA, Stansfield IG, Tew DG, Theobald CJ.

Bioorg Med Chem Lett. 2000 Feb 21;10(4):395-8.

PMID:
10714508
8.

SB-480848. GlaxoSmithKline.

Rotella DP.

Curr Opin Investig Drugs. 2004 Mar;5(3):348-51. Review.

PMID:
15083604
9.

Iminopyrimidinones: a novel pharmacophore for the development of orally active renin inhibitors.

McKittrick BA, Caldwell JP, Bara T, Boykow G, Chintala M, Clader J, Czarniecki M, Courneya B, Duffy R, Fleming L, Giessert R, Greenlee WJ, Heap C, Hong L, Huang Y, Iserloh U, Josien H, Khan T, Korfmacher W, Liang X, Mazzola R, Mitra S, Moore K, Orth P, Rajagopalan M, Roy S, Sakwa S, Strickland C, Vaccaro H, Voigt J, Wang H, Wong J, Zhang R, Zych A.

Bioorg Med Chem Lett. 2015 Apr 1;25(7):1592-6. doi: 10.1016/j.bmcl.2015.02.003. Epub 2015 Feb 10.

PMID:
25728416
10.

Identification of NVP-TNKS656: the use of structure-efficiency relationships to generate a highly potent, selective, and orally active tankyrase inhibitor.

Shultz MD, Cheung AK, Kirby CA, Firestone B, Fan J, Chen CH, Chen Z, Chin DN, Dipietro L, Fazal A, Feng Y, Fortin PD, Gould T, Lagu B, Lei H, Lenoir F, Majumdar D, Ochala E, Palermo MG, Pham L, Pu M, Smith T, Stams T, Tomlinson RC, Touré BB, Visser M, Wang RM, Waters NJ, Shao W.

J Med Chem. 2013 Aug 22;56(16):6495-511. doi: 10.1021/jm400807n. Epub 2013 Aug 13.

PMID:
23844574
12.

Lipoprotein-associated PLA2 inhibition--a novel, non-lipid lowering strategy for atherosclerosis therapy.

Leach CA, Hickey DM, Ife RJ, Macphee CH, Smith SA, Tew DG.

Farmaco. 2001 Jan-Feb;56(1-2):45-50.

PMID:
11347966
13.

Design and synthesis of new orally active inhibitors of human neutrophil elastase.

Ohmoto K, Okuma M, Yamamoto T, Kijima H, Sekioka T, Kitagawa K, Yamamoto S, Tanaka K, Kawabata K, Sakata A, Imawaka H, Nakai H, Toda M.

Bioorg Med Chem. 2001 May;9(5):1307-23.

PMID:
11377188
14.
15.

SB-253514 and analogues; novel inhibitors of lipoprotein-associated phospholipase A2 produced by Pseudomonas fluorescens DSM 11579. I. Fermentation of producing strain, isolation and biological activity.

Thirkettle J, Alvarez E, Boyd H, Brown M, Diez E, Hueso J, Elson S, Fulston M, Gershater C, Morata ML, Perez P, Ready S, Sanchez-Puelles JM, Sheridan R, Stefanska A, Warr S.

J Antibiot (Tokyo). 2000 Jul;53(7):664-9.

16.

HTS followed by NMR based counterscreening. Discovery and optimization of pyrimidones as reversible and competitive inhibitors of xanthine oxidase.

Evenäs J, Edfeldt F, Lepistö M, Svitacheva N, Synnergren A, Lundquist B, Gränse M, Rönnholm A, Varga M, Wright J, Wei M, Yue S, Wang J, Li C, Li X, Chen G, Liao Y, Lv G, Tjörnebo A, Narjes F.

Bioorg Med Chem Lett. 2014 Mar 1;24(5):1315-21. doi: 10.1016/j.bmcl.2014.01.050. Epub 2014 Jan 28.

PMID:
24508129
17.

Design and synthesis of new orally active nonpeptidic inhibitors of human neutrophil elastase.

Ohmoto K, Yamamoto T, Horiuchi T, Imanishi H, Odagaki Y, Kawabata K, Sekioka T, Hirota Y, Matsuoka S, Nakai H, Toda M, Cheronis JC, Spruce LW, Gyorkos A, Wieczorek M.

J Med Chem. 2000 Dec 28;43(26):4927-9. No abstract available.

PMID:
11150162
18.

Lipoprotein-associated phospholipase A2, platelet-activating factor acetylhydrolase, generates two bioactive products during the oxidation of low-density lipoprotein: use of a novel inhibitor.

MacPhee CH, Moores KE, Boyd HF, Dhanak D, Ife RJ, Leach CA, Leake DS, Milliner KJ, Patterson RA, Suckling KE, Tew DG, Hickey DM.

Biochem J. 1999 Mar 1;338 ( Pt 2):479-87.

19.

P3 SAR exploration of biphenyl carbamate based Legumain inhibitors.

Higgins C, Bouazzaoui S, Gaddale K, D'Costa Z, Templeman A, O'Rourke M, Young A, Scott C, Harrison T, Mullan P, Williams R.

Bioorg Med Chem Lett. 2014 Jun 1;24(11):2521-4. doi: 10.1016/j.bmcl.2014.04.002. Epub 2014 Apr 12.

PMID:
24775305
20.

Potent and orally active angiotensin II receptor antagonists with equal affinity for human AT1 and AT2 subtypes.

Chang LL, Ashton WT, Flanagan KL, Chen TB, O'Malley SS, Zingaro GJ, Kivlighn SD, Siegl PK, Lotti VJ, Chang RS, et al.

J Med Chem. 1995 Sep 15;38(19):3741-58.

PMID:
7562905

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