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Items: 1 to 20 of 102

1.

Lead optimization of 5-amino-6-(2,2-dimethyl-5-oxo-4-phenylpiperazin-1-yl)-4-hydroxyhexanamides to reduce a cardiac safety issue: discovery of DS-8108b, an orally active renin inhibitor.

Nakamura Y, Fujimoto T, Ogawa Y, Namiki H, Suzuki S, Asano M, Sugita C, Mochizuki A, Miyazaki S, Tamaki K, Nagai Y, Inoue S, Nagayama T, Kato M, Chiba K, Takasuna K, Nishi T.

Bioorg Med Chem. 2013 Jun 1;21(11):3175-96. doi: 10.1016/j.bmc.2013.03.022. Epub 2013 Mar 26.

PMID:
23598247
2.

Synthesis and optimization of novel (3S,5R)-5-(2,2-dimethyl-5-oxo-4-phenylpiperazin-1-yl)piperidine-3-carboxamides as orally active renin inhibitors.

Mori Y, Ogawa Y, Mochizuki A, Nakamura Y, Fujimoto T, Sugita C, Miyazaki S, Tamaki K, Nagayama T, Nagai Y, Inoue S, Chiba K, Nishi T.

Bioorg Med Chem. 2013 Sep 15;21(18):5907-22. doi: 10.1016/j.bmc.2013.06.057. Epub 2013 Jul 2.

PMID:
23886807
3.

Effects of SC-56525, a potent, orally active renin inhibitor, in salt-depleted and renal hypertensive dogs.

McMahon EG, Yang PC, Babler MA, Bittner SE, Suleymanov OD, Cain-Janicki KJ, Bedell LJ, Hanson GJ, Cook CS.

Hypertension. 1995 Jul;26(1):95-100.

4.

Structure-based drug design: the discovery of novel nonpeptide orally active inhibitors of human renin.

Rahuel J, Rasetti V, Maibaum J, Rüeger H, Göschke R, Cohen NC, Stutz S, Cumin F, Fuhrer W, Wood JM, Grütter MG.

Chem Biol. 2000 Jul;7(7):493-504.

5.

Design and optimization of renin inhibitors: Orally bioavailable alkyl amines.

Tice CM, Xu Z, Yuan J, Simpson RD, Cacatian ST, Flaherty PT, Zhao W, Guo J, Ishchenko A, Singh SB, Wu Z, Scott BB, Bukhtiyarov Y, Berbaum J, Mason J, Panemangalore R, Cappiello MG, Müller D, Harrison RK, McGeehan GM, Dillard LW, Baldwin JJ, Claremon DA.

Bioorg Med Chem Lett. 2009 Jul 1;19(13):3541-5. doi: 10.1016/j.bmcl.2009.04.140. Epub 2009 May 5.

PMID:
19457666
6.

Discovery of DS-8108b, a Novel Orally Bioavailable Renin Inhibitor.

Nakamura Y, Fujimoto T, Ogawa Y, Sugita C, Miyazaki S, Tamaki K, Takahashi M, Matsui Y, Nagayama T, Manabe K, Mizuno M, Masubuchi N, Chiba K, Nishi T.

ACS Med Chem Lett. 2012 Aug 18;3(9):754-8. doi: 10.1021/ml300168e. eCollection 2012 Sep 13.

7.

Design and optimization of a substituted amino propanamide series of renin inhibitors for the treatment of hypertension.

Chen A, Bayly C, Bezençon O, Richard-Bildstein S, Dubé D, Dubé L, Gagné S, Gallant M, Gaudreault M, Grimm E, Houle R, Lacombe P, Laliberté S, Lévesque JF, Liu S, MacDonald D, Mackay B, Martin D, McKay D, Powell D, Remen L, Soisson S, Toulmond S.

Bioorg Med Chem Lett. 2010 Apr 1;20(7):2204-9. doi: 10.1016/j.bmcl.2010.02.036. Epub 2010 Feb 18.

PMID:
20206513
8.

Renin inhibitors for the treatment of hypertension: design and optimization of a novel series of spirocyclic piperidines.

Chen A, Aspiotis R, Campeau LC, Cauchon E, Chefson A, Ducharme Y, Falgueyret JP, Gagné S, Han Y, Houle R, Laliberté S, Larouche G, Lévesque JF, McKay D, Percival D.

Bioorg Med Chem Lett. 2011 Dec 15;21(24):7399-404. doi: 10.1016/j.bmcl.2011.10.013. Epub 2011 Oct 19.

PMID:
22071301
9.

Design and synthesis of a potent and specific renin inhibitor with a prolonged duration of action in vivo.

Thaisrivongs S, Pals DT, Harris DW, Kati WM, Turner SR.

J Med Chem. 1986 Oct;29(10):2088-93.

PMID:
3531518
10.

Effect of an orally active renin inhibitor Cl-992 on blood pressure in normotensive and hypertensive monkeys.

Ryan MJ, Hicks GW, Batley BL, Rapundalo ST, Patt WC, Taylor DG, Keiser JA.

J Pharmacol Exp Ther. 1994 Jan;268(1):372-9.

PMID:
8301578
11.

Structural modification of the P2' position of 2,7-dialkyl-substituted 5(S)-amino-4(S)-hydroxy-8-phenyl-octanecarboxamides: the discovery of aliskiren, a potent nonpeptide human renin inhibitor active after once daily dosing in marmosets.

Maibaum J, Stutz S, Göschke R, Rigollier P, Yamaguchi Y, Cumin F, Rahuel J, Baum HP, Cohen NC, Schnell CR, Fuhrer W, Gruetter MG, Schilling W, Wood JM.

J Med Chem. 2007 Oct 4;50(20):4832-44. Epub 2007 Sep 8.

PMID:
17824680
12.

An orally active renin inhibitor: cyclohexylnorstatine-containing dipeptide (KRI-1314).

Miyazaki M, Etoh Y, Iizuka K, Toda N.

J Hypertens Suppl. 1989 Apr;7(2):S25-7.

PMID:
2666609
13.

The P1N-isopropyl motif bearing hydroxyethylene dipeptide isostere analogues of aliskiren are in vitro potent inhibitors of the human aspartyl protease renin.

Yamaguchi Y, Menear K, Cohen NC, Mah R, Cumin F, Schnell C, Wood JM, Maibaum J.

Bioorg Med Chem Lett. 2009 Aug 15;19(16):4863-7. doi: 10.1016/j.bmcl.2009.05.128. Epub 2009 Jun 26.

PMID:
19615901
14.

The discovery and synthesis of potent zwitterionic inhibitors of renin.

Aspiotis R, Chen A, Cauchon E, Dubé D, Falgueyret JP, Gagné S, Gallant M, Grimm EL, Houle R, Juteau H, Lacombe P, Laliberté S, Lévesque JF, MacDonald D, McKay D, Percival MD, Roy P, Soisson SM, Wu T.

Bioorg Med Chem Lett. 2011 Apr 15;21(8):2430-6. doi: 10.1016/j.bmcl.2011.02.067. Epub 2011 Feb 18.

PMID:
21429746
15.

Discovery of a peptide-based renin inhibitor with oral bioavailability and efficacy.

Kleinert HD, Rosenberg SH, Baker WR, Stein HH, Klinghofer V, Barlow J, Spina K, Polakowski J, Kovar P, Cohen J, et al.

Science. 1992 Sep 25;257(5078):1940-3.

PMID:
1411510
16.

Pharmacokinetics and pharmacodynamics of CI-992 following intravenous and oral administration to cynomolgus monkeys.

Cook JA, Burger PJ, Michniewicz BM, Nordblom GD, Hicks GW, Kaplan C, Ryan MJ.

Biopharm Drug Dispos. 1998 Apr;19(3):185-91.

PMID:
9570002
17.

Renin inhibitors for the treatment of hypertension: design and optimization of a novel series of tertiary alcohol-bearing piperidines.

Chen A, Cauchon E, Chefson A, Dolman S, Ducharme Y, Dubé D, Falgueyret JP, Fournier PA, Gagné S, Gallant M, Grimm E, Han Y, Houle R, Huang JQ, Hughes G, Jûteau H, Lacombe P, Lauzon S, Lévesque JF, Liu S, Macdonald D, Mackay B, McKay D, Percival MD, St-Jacques R, Toulmond S.

Bioorg Med Chem Lett. 2011 Jul 1;21(13):3976-81. doi: 10.1016/j.bmcl.2011.05.014. Epub 2011 May 14.

PMID:
21641209
18.

3,4-Diarylpiperidines as potent renin inhibitors.

Lacombe P, Arbour M, Aspiotis R, Cauchon E, Chen A, Dubé D, Falgueyret JP, Fournier PA, Gallant M, Grimm E, Han Y, Juteau H, Liu S, Mellon C, Ramtohul Y, Simard D, St-Jacques R, Tsui GC.

Bioorg Med Chem Lett. 2012 Mar 1;22(5):1953-7. doi: 10.1016/j.bmcl.2012.01.044. Epub 2012 Jan 26.

PMID:
22325946
19.

Novel 2,7-dialkyl-substituted 5(S)-amino-4(S)-hydroxy-8-phenyl-octanecarboxamide transition state peptidomimetics are potent and orally active inhibitors of human renin.

Göschke R, Stutz S, Rasetti V, Cohen NC, Rahuel J, Rigollier P, Baum HP, Forgiarini P, Schnell CR, Wagner T, Gruetter MG, Fuhrer W, Schilling W, Cumin F, Wood JM, Maibaum J.

J Med Chem. 2007 Oct 4;50(20):4818-31. Epub 2007 Sep 8.

PMID:
17824679
20.

Benzyl ether structure-activity relationships in a series of ketopiperazine-based renin inhibitors.

Powell NA, Clay EH, Holsworth DD, Bryant JW, Ryan MJ, Jalaie M, Edmunds JJ.

Bioorg Med Chem Lett. 2005 Nov 1;15(21):4713-6.

PMID:
16143527
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