SCOPUS 정보 검색 플랫폼

Volumn 18, Issue 6, 2008, Pages 581-602

Recent advances in the discovery of non-peptidic direct renin inhibitors as antihypertensives: New patent applications in years 2000-2008

(2) Yokokawa, Fumiaki a Maibaum, Jürgen b

a NOVARTIS PHARMA K K (Japan)

b NOVARTIS PHARMA AG (Switzerland)

Author keywords

Aliskiren; Antihypertensive; Aspartic protease; Flap region; Piperidine; RAAS; Renin inhibitor; Renin angiotensin aldosterone system

Indexed keywords

2,4 DIAMINO 6 ETHYL 5 (1,2,3,4 TETRAHYDROQUINOLINE 7 YL)PYRIMIDINE; 2,5 PIPERIDINE DERIVATIVE; 3 ALKOXY 4 ARYL PIPERIDINE DERIVATIVE; 3,4 PIPERIDINE DERIVATIVE; 3,4 PYROLLIDINE DERIVATIVE; 3,4,5 PIPERIDINE DERIVATIVE; 3,5 PIPERIDINE DERIVATIVE; ALISKIREN; ANTIHYPERTENSIVE AGENT; BETA SECRETASE INHIBITOR; CAPTOPRIL; CILAZAPRIL; DIPEPTIDYL CARBOXYPEPTIDASE INHIBITOR; HYDROCHLOROTHIAZIDE; LOSARTAN; MORPHOLINE DERIVATIVE; N ACYLPIPERAZINE DERIVATIVE; N MORPHOLINE DERIVATIVE; N PIPERIDINE DERIVATIVE; NITRO DERIVATIVE; PIPERAZINE DERIVATIVE; PIPERIDINE DERIVATIVE; PYRROLIDINE DERIVATIVE; RENIN INHIBITOR; RO 66 1132; RO 66 1168; TETRAHYDROPYRIDINE DERIVATIVE; UNINDEXED DRUG; VALSARTAN; VALSPODAR;

ALBUMINURIA; ANTIHYPERTENSIVE ACTIVITY; ANTIINFLAMMATORY ACTIVITY; BLOOD PRESSURE REGULATION; CLINICAL TRIAL; COMBINATION CHEMOTHERAPY; DRUG ABSORPTION; DRUG BINDING; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG DESIGN; DRUG DISTRIBUTION; DRUG EFFICACY; DRUG ELIMINATION; DRUG HALF LIFE; DRUG MARKETING; DRUG MEGADOSE; DRUG METABOLISM; DRUG POTENCY; DRUG SAFETY; DRUG STRUCTURE; DRUG SYNTHESIS; HEART VENTRICLE HYPERTROPHY; HUMAN; HYPERTENSION; MONOTHERAPY; NONHUMAN; PATENT; PHARMACOPHORE; REVIEW; SINGLE DRUG DOSE; STRUCTURE ACTIVITY RELATION;

EID: 46849092364 PISSN: 13543776 EISSN: None Source Type: Journal
DOI: 10.1517/13543776.18.6.581 Document Type: Review

Times cited : (23)

References (149)

1
- 0038460302
- Chobanian AV, Bakins GL, Black HR, et al. The seventh report of the joint national committee on prevention, detection, evaluation, and treatment of high blood pressure. J Am Med Assoc 2003;289:2560-72
- Chobanian AV, Bakins GL, Black HR, et al. The seventh report of the joint national committee on prevention, detection, evaluation, and treatment of high blood pressure. J Am Med Assoc 2003;289:2560-72

2
- 12344282783
- Global burden of hypertension: Analysis of worldwide data
- Kearney PM, Whelton M, Reynolds K, et al. Global burden of hypertension: analysis of worldwide data. Lancet 2005;365:217-23
- (2005) Lancet , vol.365 , pp. 217-223
- Kearney, P.M.¹ Whelton, M.² Reynolds, K.³

3
- 0036690114
- Drugs targeting the renin-angiotensin-aldosterone system
- Amin Zaman M, Oparil S, Calhoun DA. Drugs targeting the renin-angiotensin-aldosterone system. Nat Rev Drug Discov 2002;1:621-36
- (2002) Nat Rev Drug Discov , vol.1 , pp. 621-636
- Amin Zaman, M.¹ Oparil, S.² Calhoun, D.A.³

4
- 0000586975
- Preparation, purification and amino acid sequence of a polypeptide renin substrate
- Skeggs LT, Kahn JR, Lentz KE, et al. Preparation, purification and amino acid sequence of a polypeptide renin substrate. J Exp Med 1957;106:439-53
- (1957) J Exp Med , vol.106 , pp. 439-453
- Skeggs, L.T.¹ Kahn, J.R.² Lentz, K.E.³

5
- 20544440652
- Renin inhibitors: What are the therapeutic opportunities?
- Fisher NDL, Hollenberg NK. Renin inhibitors: what are the therapeutic opportunities? J Am Soc Nephrol 2005;16:592-9
- (2005) J Am Soc Nephrol , vol.16 , pp. 592-599
- Fisher, N.D.L.¹ Hollenberg, N.K.²

6
- 33644789557
- Renin inhibition with aliskiren: Where are we now, and where are we going?
- Azizi M, Webb R, Nussberger J, Hollenberg NK. Renin inhibition with aliskiren: where are we now, and where are we going? J Hypertens 2006;24:243-56
- (2006) J Hypertens , vol.24 , pp. 243-256
- Azizi, M.¹ Webb, R.² Nussberger, J.³ Hollenberg, N.K.⁴

7
- 0037769830
- Renin inhibitors as novel treatments for cardiovascular diseases
- Maibaum J, Feldman DL. Renin inhibitors as novel treatments for cardiovascular diseases. Expert Opin Ther Patents 2003;13:589-603
- (2003) Expert Opin Ther Patents , vol.13 , pp. 589-603
- Maibaum, J.¹ Feldman, D.L.²

8
- 33749985149
- Oral renin inhibitors
- Staessen JA, Li Y, Richart T. Oral renin inhibitors. Lancet 2006;368:1449-56
- (2006) Lancet , vol.368 , pp. 1449-1456
- Staessen, J.A.¹ Li, Y.² Richart, T.³

9
- 42949109643
- Aliskiren, the first renin inhibitor for clinical treatment
- Jensen CH, Herold P, Brunner HR. Aliskiren, the first renin inhibitor for clinical treatment. Nat Rev Drug Discov 2008;7(5):399-410
- (2008) Nat Rev Drug Discov , vol.7 , Issue.5 , pp. 399-410
- Jensen, C.H.¹ Herold, P.² Brunner, H.R.³

10
- 34047207774
- Aliskiren for renin inhibitors: A new class of antihypertensives
- Van Tassell BW, Munger MA. Aliskiren for renin inhibitors: a new class of antihypertensives. Ann Pharmacother 2007;41:456-64
- (2007) Ann Pharmacother , vol.41 , pp. 456-464
- Van Tassell, B.W.¹ Munger, M.A.²

11
- 33947182655
- Aliskiren, an oral renin inhibitor, provides dose-dependent efficacy and sustained 24-hour blood pressure control in patients with hypertension
- Oh BH, Mitchell J, Herron J, et al. Aliskiren, an oral renin inhibitor, provides dose-dependent efficacy and sustained 24-hour blood pressure control in patients with hypertension. J Am Coll Cardiol 2007;49:1157-63
- (2007) J Am Coll Cardiol , vol.49 , pp. 1157-1163
- Oh, B.H.¹ Mitchell, J.² Herron, J.³

12
- 34848903955
- Siragy HM, Kar S, Kirkpatrick P. Aliskiren Nat Rev Drug Discov 2007;6:779-80
- (2007) Aliskiren Nat Rev Drug Discov , vol.6 , pp. 779-780
- Siragy, H.M.¹ Kar, S.² Kirkpatrick, P.³

13
- 33845366982
- Renin inhibition with aliskiren provides additive antihypertensive efficacy when used in combination with hydrochlorothiazide
- Villamil A, Chrysant SG, Calhoun D, et al. Renin inhibition with aliskiren provides additive antihypertensive efficacy when used in combination with hydrochlorothiazide. J Hypertens 2007;25:217-26
- (2007) J Hypertens , vol.25 , pp. 217-226
- Villamil, A.¹ Chrysant, S.G.² Calhoun, D.³

14
- 36248931230
- Antihypertensive efficacy of the oral direct renin inhibitor aliskiren as add-on therapy in patients not responding to amlodipine monotherapy
- Drummond W, Munger MA, Essop MR, et al. Antihypertensive efficacy of the oral direct renin inhibitor aliskiren as add-on therapy in patients not responding to amlodipine monotherapy. J Clin Hypertens 2007;9:742-50
- (2007) J Clin Hypertens , vol.9 , pp. 742-750
- Drummond, W.¹ Munger, M.A.² Essop, M.R.³

15
- 34447521458
- Efficacy and safety of combined use of aliskiren and valsartan in patients with hypertension: A randomized, double-blind trial
- Oparil S, Yarows SA, Patel S, et al. Efficacy and safety of combined use of aliskiren and valsartan in patients with hypertension: a randomized, double-blind trial. Lancet 2007;370:221-9
- (2007) Lancet , vol.370 , pp. 221-229
- Oparil, S.¹ Yarows, S.A.² Patel, S.³

16
- 39849089447
- Comparative efficacy and safety of aliskiren, an oral direct renin inhibitor, and ramipril in hypertension: A 6-month, randomized, double-blind trial
- Andersen K, Weinberger MH, Egan B, et al. Comparative efficacy and safety of aliskiren, an oral direct renin inhibitor, and ramipril in hypertension: a 6-month, randomized, double-blind trial. J Hypertens 2008;26:589-99
- (2008) J Hypertens , vol.26 , pp. 589-599
- Andersen, K.¹ Weinberger, M.H.² Egan, B.³

17
- 0021855138
- Stereochemical analysis of peptide bond hydrolysis catalyzed by the aspartic proteinase penicillopepsin
- James MN, Sielecki AR. Stereochemical analysis of peptide bond hydrolysis catalyzed by the aspartic proteinase penicillopepsin. Biochemistry 1985;24:3701-13
- (1985) Biochemistry , vol.24 , pp. 3701-3713
- James, M.N.¹ Sielecki, A.R.²

18
- 0028216054
- Recent developments in renin inhibitors: Part I
- Raddatz P. Recent developments in renin inhibitors: part I. Expert Opin Ther Patents 1994;4:489-504
- (1994) Expert Opin Ther Patents , vol.4 , pp. 489-504
- Raddatz, P.¹

19
- 0028154764
- Recent developments in renin inhibitors: Part II
- Raddatz P. Recent developments in renin inhibitors: part II. Expert Opin Ther Patents 1994;4:1347-59
- (1994) Expert Opin Ther Patents , vol.4 , pp. 1347-1359
- Raddatz, P.¹

20
- 0030576323
- Bioactive hydroxyethylene dipeptide isosteres with hydrophobic (P3-P1)-moieties. A novel strategy towards small non-peptide renin inhibitors
- Rasetti V, Cohen NC, Rüeger H, et al. Bioactive hydroxyethylene dipeptide isosteres with hydrophobic (P3-P1)-moieties. A novel strategy towards small non-peptide renin inhibitors. Bioorg Med Chem Lett 1996;6:1589-94
- (1996) Bioorg Med Chem Lett , vol.6 , pp. 1589-1594
- Rasetti, V.¹ Cohen, N.C.² Rüeger, H.³

21
- 0141608479
- Design and synthesis of novel 2,7-dialkyl substituted 5(S)-amino-4(S)-hydroxy-8-phenyl-octanecarboxamides as in vitro potent peptidomimetic inhibitors of human renin
- Göschke R, Cohen NC, Wood JM, et al. Design and synthesis of novel 2,7-dialkyl substituted 5(S)-amino-4(S)-hydroxy-8-phenyl-octanecarboxamides as in vitro potent peptidomimetic inhibitors of human renin. Bioorg Med Chem Lett 1997;7:2735-40
- (1997) Bioorg Med Chem Lett , vol.7 , pp. 2735-2740
- Göschke, R.¹ Cohen, N.C.² Wood, J.M.³

22
- 0033941893
- Structure-based drug design: The discovery of novel nonpeptide orally active inhibitors of human renin
- Rahuel J, Rasetti V, Maibaum J, et al. Structure-based drug design: the discovery of novel nonpeptide orally active inhibitors of human renin. Chem Biol 2000;7:493-504
- (2000) Chem Biol , vol.7 , pp. 493-504
- Rahuel, J.¹ Rasetti, V.² Maibaum, J.³

23
- 0042661157
- Structure-based design of aliskiren, a novel orally effective renin inhibitor
- Wood JM, Maibaum J, Rahuel J, et al. Structure-based design of aliskiren, a novel orally effective renin inhibitor. Biochem Biophys Res Commun 2003;308:698-705
- (2003) Biochem Biophys Res Commun , vol.308 , pp. 698-705
- Wood, J.M.¹ Maibaum, J.² Rahuel, J.³

24
- 34848888592
- 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, et al. 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. J Med Chem 2007;50:4818-31
- (2007) J Med Chem , vol.50 , pp. 4818-4831
- Göschke, R.¹ Stutz, S.² Rasetti, V.³

25
- 34848869297
- 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, et al. 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. J Med Chem 2007;50:4832-44
- (2007) J Med Chem , vol.50 , pp. 4832-4844
- Maibaum, J.¹ Stutz, S.² Göschke, R.³

26
- 14044271546
- Aliskiren, a novel, orally effective renin inhibitor, lowers blood pressure in marmosets and spontaneously hypertensive rats
- Wood JM, Schnell CR, Cumin F, et al. Aliskiren, a novel, orally effective renin inhibitor, lowers blood pressure in marmosets and spontaneously hypertensive rats. J. Hypertens 2005;23:417-26
- (2005) J. Hypertens , vol.23 , pp. 417-426
- Wood, J.M.¹ Schnell, C.R.² Cumin, F.³

27
- 0026753520
- Species specificity of renin kinetics in transgenic rats harboring the human renin and angiotensinogen genes
- Ganten D, Wagner J, Zen K, et al. Species specificity of renin kinetics in transgenic rats harboring the human renin and angiotensinogen genes. Proc Natl Acad Sci 1992;89:7806-10
- (1992) Proc Natl Acad Sci , vol.89 , pp. 7806-7810
- Ganten, D.¹ Wagner, J.² Zen, K.³

28
- 33644798157
- The renin inhibitor aliskiren is a potent and long-acting antihypertensive in double transgenic rats expressing human renin and angiotensinogen genes
- Rigel DF, Fu F, Li S, et al. The renin inhibitor aliskiren is a potent and long-acting antihypertensive in double transgenic rats expressing human renin and angiotensinogen genes. J Am Coll Cardiol 2004;43:483A
- (2004) J Am Coll Cardiol , vol.43
- Rigel, D.F.¹ Fu, F.² Li, S.³

29
- 25444454353
- Aliskiren, a human renin inhibitor, ameliorates cardiac and renal damage in double-transgenic rats
- Pilz B, Shagdarsuren E, Wellner M, et al. Aliskiren, a human renin inhibitor, ameliorates cardiac and renal damage in double-transgenic rats. Hypertension 2005;46:569-76
- (2005) Hypertension , vol.46 , pp. 569-576
- Pilz, B.¹ Shagdarsuren, E.² Wellner, M.³

30
- 0031823522
- A new model of diabetic nephropathy with progressive renal impairment in the transgenic (mRen-2)27 rat (TGR)
- Kelly DJ, Wilkinson-Berka JL, Allen TJ, et al. A new model of diabetic nephropathy with progressive renal impairment in the transgenic (mRen-2)27 rat (TGR). Kidney Int 1998;54:343-52
- (1998) Kidney Int , vol.54 , pp. 343-352
- Kelly, D.J.¹ Wilkinson-Berka, J.L.² Allen, T.J.³

31
- 33644788906
- Aliskiren, a human renin inhibitor, reverses angiotensin II-induced renal and cardiac damage in dTGR in a regression study design [abstract]
- Pilz B, Shagdasurren E, Wellner M, et al. Aliskiren, a human renin inhibitor, reverses angiotensin II-induced renal and cardiac damage in dTGR in a regression study design [abstract]. Hypertension 2004;44:526-7
- (2004) Hypertension , vol.44 , pp. 526-527
- Pilz, B.¹ Shagdasurren, E.² Wellner, M.³

32
- 0033577692
- Substituted piperidines-highly potent renin inhibitors due to induced fit adaptation of the active site
- Vieira E, Binggeli A, Breu V, et al. Substituted piperidines-highly potent renin inhibitors due to induced fit adaptation of the active site. Bioorg Med Chem Lett 1999;9:1397-402
- (1999) Bioorg Med Chem Lett , vol.9 , pp. 1397-1402
- Vieira, E.¹ Binggeli, A.² Breu, V.³

33
- 0003694381
- Piperidine-renin inhibitors compounds with improved physicochemical properties
- Güller R, Binggeli A, Breu V, et al. Piperidine-renin inhibitors compounds with improved physicochemical properties. Bioorg Med Chem Lett 1999;9:1403-8
- (1999) Bioorg Med Chem Lett , vol.9 , pp. 1403-1408
- Güller, R.¹ Binggeli, A.² Breu, V.³

34
- 0033102135
- Renin inhibition by substituted piperidines: A novel paradigm for the inhibition of monomeric aspartic proteinases
- Oefner C, Binggeli A, Breu V, et al. Renin inhibition by substituted piperidines: a novel paradigm for the inhibition of monomeric aspartic proteinases. Chem Biol 1999;6:127-31
- (1999) Chem Biol , vol.6 , pp. 127-131
- Oefner, C.¹ Binggeli, A.² Breu, V.³

35
- 0035273245
- Piperidine renio inhibitors: From lead to drug candidates
- Märki HP, Binggeli A, Bittner B, et al. Piperidine renio inhibitors: from lead to drug candidates. Il Farmaco 2001;56:21-7
- (2001) Il Farmaco , vol.56 , pp. 21-27
- Märki, H.P.¹ Binggeli, A.² Bittner, B.³

36
- 0037203973
- Designing non-peptide peptidomimetics in the 21st century: Inhibitors targeting conformational ensembles
- Bursavich MG, Rich DH. Designing non-peptide peptidomimetics in the 21st century: inhibitors targeting conformational ensembles. J Med Chem 2002;45:541-58
- (2002) J Med Chem , vol.45 , pp. 541-558
- Bursavich, M.G.¹ Rich, D.H.²

37
- 0036354363
- Preformulation approaches to improve the oral bioavailability of two novel piperidine renin inhibitors in dog
- Bittner B, Chou R, Schleimer M, et al. Preformulation approaches to improve the oral bioavailability of two novel piperidine renin inhibitors in dog. Arzneimittelforschung 2002;52:593-9
- (2002) Arzneimittelforschung , vol.52 , pp. 593-599
- Bittner, B.¹ Chou, R.² Schleimer, M.³

38
- 34548392290
- Ensemble-docking approach on BACE-1: Pharmacophore perception and guidelines for drug design
- Limongelli V, Marinelli L, Cosconati S, et al. Ensemble-docking approach on BACE-1: pharmacophore perception and guidelines for drug design. ChemMed Chem 2007;2:667-78
- (2007) ChemMed Chem , vol.2 , pp. 667-678
- Limongelli, V.¹ Marinelli, L.² Cosconati, S.³

39
- 33846340818
- Renin inhibitors. In: Wood A, editor
- Elsevier, Inc, 41:155-67
- Tice CM. Renin inhibitors. In: Wood A, editor, Annual reports in Med Chem. Elsevier, Inc.; 2006;41:155-67
- (2006) Annual reports in Med Chem
- Tice, C.M.¹

40
- 45149121968
- Cardiovascular agents: Renin inhibitors and factor Xa inhibitors
- Kasani A, Subedi R, Stier M, et al. Cardiovascular agents: renin inhibitors and factor Xa inhibitors. Heterocycles 2007;73:47-85
- (2007) Heterocycles , vol.73 , pp. 47-85
- Kasani, A.¹ Subedi, R.² Stier, M.³

41
- 46849112535
- Ltd. WO03093267;
- Actelion Pharm. Ltd. WO03093267; 2003
- (2003)
- Pharm, A.¹

42
- 46849104595
- Ltd. WO04096804;
- Actelion Pharm. Ltd. WO04096804; 2004
- (2004)
- Pharm, A.¹

43
- 46849113574
- Ltd. WO04096116;
- Actelion Pharm. Ltd. WO04096116; 2004
- (2004)
- Pharm, A.¹

44
- 46849096584
- Ltd. WO04096366;
- Actelion Pharm. Ltd. WO04096366; 2004
- (2004)
- Pharm, A.¹

45
- 46849116963
- Ltd. WO04096799;
- Actelion Pharm. Ltd. WO04096799; 2004
- (2004)
- Pharm, A.¹

46
- 46849110898
- Ltd. WO04096803;
- Actelion Pharm. Ltd. WO04096803; 2004
- (2004)
- Pharm, A.¹

47
- 46849121077
- Ltd. WO05040173;
- Actelion Pharm. Ltd. WO05040173; 2005
- (2005)
- Pharm, A.¹

48
- 46849121499
- Ltd. WO05040165;
- Actelion Pharm. Ltd. WO05040165; 2005
- (2005)
- Pharm, A.¹

49
- 46849112916
- Ltd. WO05054243;
- Actelion Pharm. Ltd. WO05054243; 2005
- (2005)
- Pharm, A.¹

50
- 46849093734
- Ltd. WO05054244;
- Actelion pharm. Ltd. WO05054244; 2005
- (2005)
- Actelion pharm¹

51
- 46849097904
- Actelion Pharm. Ltd. WO06021401; 2006
- Actelion Pharm. Ltd. WO06021401; 2006

52
- 46849086845
- Actelion Pharm. Ltd. WO06021402; 2006
- Actelion Pharm. Ltd. WO06021402; 2006

53
- 46849100759
- Actelion Pharm. Ltd. WO06021403; 2006
- Actelion Pharm. Ltd. WO06021403; 2006

54
- 46849117641
- Actelion Pharm. Ltd. WO06021399; 2006
- Actelion Pharm. Ltd. WO06021399; 2006

55
- 46849105981
- Ltd. WO06058546;
- Actelion Pharm. Ltd. WO06058546; 2006
- (2006)
- Pharm, A.¹

56
- 46849119918
- Ltd. WO06061791;
- Actelion Pharm. Ltd. WO06061791; 2006
- (2006)
- Pharm, A.¹

57
- 46849113955
- Ltd. WO06063610;
- Actelion Pharm. Ltd. WO06063610; 2006
- (2006)
- Pharm, A.¹

58
- 46849085685
- Ltd. WO06064484;
- Actelion Pharm. Ltd. WO06064484; 2006
- (2006)
- Pharm, A.¹

59
- 46849083618
- Ltd. WO06079981;
- Actelion Pharm. Ltd. WO06079981; 2006
- (2006)
- Pharm, A.¹

60
- 46849107616
- Ltd. WO06092268;
- Actelion Pharm. Ltd. WO06092268; 2006
- (2006)
- Pharm, A.¹

61
- 46849098312
- Actelion Pharm. Ltd. WO06131884; 2006
- Actelion Pharm. Ltd. WO06131884; 2006

62
- 46849099909
- Ltd. WO04002957;
- Actelion Pharm. Ltd. WO04002957; 2004
- (2004)
- Pharm, A.¹

63
- 46849121075
- Ltd. WO05040120;
- Actelion Pharm. Ltd. WO05040120; 2005
- (2005)
- Pharm, A.¹

64
- 46849083181
- Novartis AG. WO06074924; 2006
- Novartis AG. WO06074924; 2006

65
- 46849087084
- Ltd. WO07049224;
- Actelion Pharm. Ltd. WO07049224; 2007
- (2007)
- Pharm, A.¹

66
- 46849084669
- Novartis AG. WO05051911; 2005
- Novartis AG. WO05051911; 2005

67
- 46849085686
- Novartis AG. WO06069788; 2006
- Novartis AG. WO06069788; 2006

68
- 46849114207
- Novartis AG. WO06094763; 2006
- Novartis AG. WO06094763; 2006

69
- 46849110054
- Novartis AG. WO06125621; 2006
- Novartis AG. WO06125621; 2006

70
- 46849107227
- Ltd. WO07088514;
- Actelion Pharm. Ltd. WO07088514; 2007
- (2007)
- Pharm, A.¹

71
- 46849123032
- Ltd. WO06129237;
- Actelion Pharm. Ltd. WO06129237; 2006
- (2006)
- Pharm, A.¹

72
- 46849098892
- Actelion Pharm. Ltd. WO07102127; 2007
- Actelion Pharm. Ltd. WO07102127; 2007

73
- 46849117422
- Werner-Lambert Co. WO04089903;
- Werner-Lambert Co. WO04089903; 2004
- (2004)

74
- 9644295730
- The discovery and preparation of disubstituted novel amino-aryl-piperidine-based renin inhibitors
- CODY WL, Holsworth DD, Powell NA, et al. The discovery and preparation of disubstituted novel amino-aryl-piperidine-based renin inhibitors. Bioorg Med Chem 2005; 13: 59-68
- (2005) Bioorg Med Chem , vol.13 , pp. 59-68
- CODY, W.L.¹ Holsworth, D.D.² Powell, N.A.³

75
- 46849111294
- Speedel Experimenta AG. WO05061457; 2005
- Speedel Experimenta AG. WO05061457; 2005

76
- 46849115471
- Speedel Experimenta AG. WO06005741; 2006
- Speedel Experimenta AG. WO06005741; 2006

77
- 46849113573
- Speedel Experimenta AG. WO06103275; 2006
- Speedel Experimenta AG. WO06103275; 2006

78
- 46849106399
- Speedel Experimenta AG. WO06103273; 2006
- Speedel Experimenta AG. WO06103273; 2006

79
- 46849100761
- Speedel Experimenta AG. WO07082907; 2007
- Speedel Experimenta AG. WO07082907; 2007

80
- 46849118698
- Speedel Experimenta AG. WO06103277; 2006
- Speedel Experimenta AG. WO06103277; 2006

81
- 46849094419
- Successful outcome of Aliskiren, the first-in-class renin inhibitor, vs. Irbesartan, in a 650 patient hypertension study, recently completed by Novartis. Available from: http://www.speedelpharma.com/section/7/ subsections/4?form_link=1094654092
- Successful outcome of Aliskiren, the first-in-class renin inhibitor, vs. Irbesartan, in a 650 patient hypertension study, recently completed by Novartis. Available from: http://www.speedelpharma.com/section/7/ subsections/4?form_link=1094654092

82
- 46849117421
- Werner-Lambert Co. WO04089915;
- Werner-Lambert Co. WO04089915; 2004
- (2004)

83
- 20044391231
- Discovery of novel non-peptidic ketopiperazine-based renin inhibitors
- Holsworth DD, Powell NA, Downing DM, et al. Discovery of novel non-peptidic ketopiperazine-based renin inhibitors. Bioorg Med Chem 2005;13:2657-64
- (2005) Bioorg Med Chem , vol.13 , pp. 2657-2664
- Holsworth, D.D.¹ Powell, N.A.² Downing, D.M.³

84
- 33644967829
- Ketopiperazine-based renin inhibitors: Optimization of the "C" ring
- Holsworth DD, Cai C, Cheng X-M, et al. Ketopiperazine-based renin inhibitors: Optimization of the "C" ring. Bioorg Med Chem Lett 2006;16:2500-4
- (2006) Bioorg Med Chem Lett , vol.16 , pp. 2500-2504
- Holsworth, D.D.¹ Cai, C.² Cheng, X.-M.³

85
- 25144441809
- Benzyl ether structure-activity relationships in a series of ketopiperazine-based renin inhibitors
- Powell NA, Clay EH, Holsworth DD, et al. Benzyl ether structure-activity relationships in a series of ketopiperazine-based renin inhibitors. Bioorg Med Chem Lett 2005;15:4713-6
- (2005) Bioorg Med Chem Lett , vol.15 , pp. 4713-4716
- Powell, N.A.¹ Clay, E.H.² Holsworth, D.D.³

86
- 17144388295
- Equipotent activity in both enantiomers of a series of ketopiperazine-based renin inhibitors
- Powell NA, Clay EH, Holsworth DD, et al. Equipotent activity in both enantiomers of a series of ketopiperazine-based renin inhibitors. Bioorg Med Chem Lett 2005;15:2371-4
- (2005) Bioorg Med Chem Lett , vol.15 , pp. 2371-2374
- Powell, N.A.¹ Clay, E.H.² Holsworth, D.D.³

87
- 46849121904
- Speedel Experimenta AG. WO05037803; 2005
- Speedel Experimenta AG. WO05037803; 2005

88
- 46849096391
- Novartis AG. WO06128659; 2006
- Novartis AG. WO06128659; 2006

89
- 46849112332
- Ltd. WO07034445;
- Actelion Pharm. Ltd. WO07034445; 2007
- (2007)
- Pharm, A.¹

90
- 46849095536
- Takeda Pharm. Co. WO07094513; 2007
- Takeda Pharm. Co. WO07094513; 2007

91
- 46849090831
- Takeda Pharm. Co. WO07117961; 2007
- Takeda Pharm. Co. WO07117961; 2007

92
- 46849087469
- Novartis AG. WO06117183; 2006
- Novartis AG. WO06117183; 2006

93
- 46849116116
- Novartis AG. WO07006534; 2007
- Novartis AG. WO07006534; 2007

94
- 46849091061
- Novartis AG. WO07077005; 2007
- Novartis AG. WO07077005; 2007

95
- 46849110707
- Speedel Experimenta AG. WO07141318; 2007
- Speedel Experimenta AG. WO07141318; 2007

96
- 46849114409
- Novartis AG. WO06069788; 2006
- Novartis AG. WO06069788; 2006

97
- 46849110488
- Novartis AG. WO06100036; 2006
- Novartis AG. WO06100036; 2006

98
- 46849120885
- Novartis AG. WO07144129; 2007
- Novartis AG. WO07144129; 2007

99
- 46849112331
- Novartis AG. WO07144128; 2007
- Novartis AG. WO07144128; 2007

100
- 46849121707
- Ltd. WO07034406;
- Actelion Pharm. Ltd. WO07034406; 2007
- (2007)
- Pharm, A.¹

101
- 46849122776
- Merck Frosst Canada Ltd. WO07009250;
- Merck Frosst Canada Ltd. WO07009250; 2007
- (2007)

102
- 46849087654
- Ltd. WO07099509;
- Actelion Pharm. Ltd. WO07099509; 2007
- (2007)
- Pharm, A.¹

103
- 46849084866
- Inc. WO06042150;
- Vitae Pharm., Inc. WO06042150; 2006
- (2006)
- Pharm, V.¹

104
- 46849107617
- Inc. WO07117560;
- Vitae Pharm., Inc. WO07117560; 2007
- (2007)
- Pharm, V.¹

105
- 46849102468
- Inc. WO07117559;
- Vitae Pharm., Inc. WO07117559; 2007
- (2007)
- Pharm, V.¹

106
- 46849089817
- Inc. WO07117557;
- Vitae Pharm., Inc. WO07117557; 2007
- (2007)
- Pharm, V.¹

107
- 46849109230
- Inc. WO07070201;
- Vitae Pharm. Inc. WO07070201; 2007
- (2007)
- Pharm, V.¹

108
- 46849083399
- Inc. WO08036247;
- Vitae pharm., Inc. WO08036247; 2008
- (2008)
- Vitae pharm¹

109
- 46849109839
- Inc. WO08036216;
- Vitae Pharm., Inc. WO08036216; 2008
- (2008)
- Pharm, V.¹

110
- 0020541678
- Novel renin inhibitors containing the amino acid statine
- Boger J, Lohr NS, Ulm EH, et al. Novel renin inhibitors containing the amino acid statine. Nature 1983;303:81-4
- (1983) Nature , vol.303 , pp. 81-84
- Boger, J.¹ Lohr, N.S.² Ulm, E.H.³

111
- 33750132225
- Acylguanidines as small-molecule β-secretase inhibitors
- Cole DC, Manas ES, Stock JR, et al. Acylguanidines as small-molecule β-secretase inhibitors. J Med Chem. 2006;49:6158-61
- (2006) J Med Chem , vol.49 , pp. 6158-6161
- Cole, D.C.¹ Manas, E.S.² Stock, J.R.³

112
- 33947612966
- Application of fragment screening by X-ray crystallography to β-sceretase
- Murray CW, Callaghan O, Chessari G, et al. Application of fragment screening by X-ray crystallography to β-sceretase. J Med Chem 2007;50:1116-23
- (2007) J Med Chem , vol.50 , pp. 1116-1123
- Murray, C.W.¹ Callaghan, O.² Chessari, G.³

113
- 33947636525
- Application of fragment screening by X-ray crystallography to the discovery of aminopyridines as inhibitors of β-secretase
- Congreve M, Aharony D, Albert J, et al. Application of fragment screening by X-ray crystallography to the discovery of aminopyridines as inhibitors of β-secretase. J Med Chem. 2007;50:1124-32
- (2007) J Med Chem , vol.50 , pp. 1124-1132
- Congreve, M.¹ Aharony, D.² Albert, J.³

114
- 38749095202
- Acylguanidine inhibitors of β-secretase: Optimization of the pyrrole ring substituents extending into the S1 and S3 substrate binding pockets
- Cole DC, Stock JR, Chopra R, et al. Acylguanidine inhibitors of β-secretase: optimization of the pyrrole ring substituents extending into the S1 and S3 substrate binding pockets. Bioorg Med Chem Lett. 2008;18:1063-6
- (2008) Bioorg Med Chem Lett , vol.18 , pp. 1063-1066
- Cole, D.C.¹ Stock, J.R.² Chopra, R.³

115
- 46849117958
- Schering Corp.; Pharmacopeia Drug Discovery, Inc. WO05058311; 2005
- Schering Corp.; Pharmacopeia Drug Discovery, Inc. WO05058311; 2005

116
- 46849086675
- Schering Corp.; Pharmacopeia Drug Discovery, Inc. WO06065277; 2006
- Schering Corp.; Pharmacopeia Drug Discovery, Inc. WO06065277; 2006

117
- 46849105156
- Schering Corp.; Pharmacopeia Drug Discovery, Inc. WO06138265; 2006
- Schering Corp.; Pharmacopeia Drug Discovery, Inc. WO06138265; 2006

118
- 46849103508
- Schering Corp. WO06138266; 2006
- Schering Corp. WO06138266; 2006

119
- 46849094616
- Sanofi-Aventis. WO07144769; 2007
- Sanofi-Aventis. WO07144769; 2007

120
- 34250218617
- Discovery of 6-ethyl-2,4-diaminopyrimidine-based small molecule renin inhibitors
- Holsworth DD, Jalaie M, Belliotti T, et al. Discovery of 6-ethyl-2,4-diaminopyrimidine-based small molecule renin inhibitors. Bioorg Med Chem Lett 2007;17:3575-80
- (2007) Bioorg Med Chem Lett , vol.17 , pp. 3575-3580
- Holsworth, D.D.¹ Jalaie, M.² Belliotti, T.³

121
- 34447293062
- Rational design of 6-(2,4-diaminopyrimidinyl)-1,4-benzoxazin-3-ones as small molecule renin inhibitors
- Powell NA, Ciske FL, Cai C, et al. Rational design of 6-(2,4-diaminopyrimidinyl)-1,4-benzoxazin-3-ones as small molecule renin inhibitors. Bioorg Med Chem 2007;15:5912-49
- (2007) Bioorg Med Chem , vol.15 , pp. 5912-5949
- Powell, N.A.¹ Ciske, F.L.² Cai, C.³

122
- 33845430710
- Binding thermodynamics of substituted diaminopyrimidine renin inhibitors
- Sarver RW, Peevers J, Cody WL, et al. Binding thermodynamics of substituted diaminopyrimidine renin inhibitors. Anal Biochem 2007;360:30-40
- (2007) Anal Biochem , vol.360 , pp. 30-40
- Sarver, R.W.¹ Peevers, J.² Cody, W.L.³

123
- 46849103974
- March 14 Issue
- Merrill J. Pfizer Shrugs at Novartis' Tekturna Launch. The Pink Sheet Daily 2007; March 14 Issue
- (2007) Shrugs at Novartis' Tekturna Launch. The Pink Sheet Daily
- Pfizer, M.J.¹

124
- 46849113341
- Novartis AG. WO05051895; 2005
- Novartis AG. WO05051895; 2005

125
- 46849120884
- Speedel Experimenta AG. WO06095020; 2006
- Speedel Experimenta AG. WO06095020; 2006

126
- 46849088271
- Speedel Experimenta AG. WO07031557; 2007
- Speedel Experimenta AG. WO07031557; 2007

127
- 46849089612
- Speedel Experimenta AG. WO05070877; 2005
- Speedel Experimenta AG. WO05070877; 2005

128
- 46849103077
- Speedel Experimenta AG. WO07031558; 2007
- Speedel Experimenta AG. WO07031558; 2007

129
- 46849118654
- Speedel Experimenta AG. WO07085651; 2007
- Speedel Experimenta AG. WO07085651; 2007

130
- 46849109622
- Inc. WO06003489;
- Vitae Pharm., Inc. WO06003489; 2006
- (2006)
- Pharm, V.¹

131
- 46849089093
- Inc. WO07120523;
- Vitae Pharm., Inc. WO07120523; 2007
- (2007)
- Pharm, V.¹

132
- 46849091259
- Daiichi Sankyo Company, Ltd. WO07148775;
- Daiichi Sankyo Company, Ltd. WO07148775; 2007
- (2007)

133
- 46849092298
- Daiichi Sankyo Company, Ltd. WO07148774;
- Daiichi Sankyo Company, Ltd. WO07148774; 2007
- (2007)

134
- 46849100339
- Inc. WO07123718;
- Vitae Pharm., Inc. WO07123718; 2007
- (2007)
- Pharm, V.¹

135
- 0347951125
- Dihydropyridine neuropeptide YY1 receptor antagonists 2: Bioisosteric urea replacements
- Poindexter GS, Bruce MA, Guy Breitenbucher, et al. Dihydropyridine neuropeptide YY1 receptor antagonists 2: bioisosteric urea replacements. Bioorg Med Chem 2004;12:507-21
- (2004) Bioorg Med Chem , vol.12 , pp. 507-521
- Poindexter, G.S.¹ Bruce, M.A.² Breitenbucher, G.³

136
- 28044468751
- Aliskiren, a novel oral renin inhibitor, has no interaction with cytochrome P450 isoenzyme in vitro
- Vaidyanathan S, Jin Y, Schiller H, et al. Aliskiren, a novel oral renin inhibitor, has no interaction with cytochrome P450 isoenzyme in vitro. Basic Res Pharmacol Toxicol 2005;97(Suppl 1):239
- (2005) Basic Res Pharmacol Toxicol , vol.97 , Issue.SUPPL. 1 , pp. 239
- Vaidyanathan, S.¹ Jin, Y.² Schiller, H.³

137
- 46849115902
- Novartis AG. WO06013094; 2006
- Novartis AG. WO06013094; 2006

138
- 46849101671
- Novartis AG. WO05051895; 2005
- Novartis AG. WO05051895; 2005

139
- 46849112112
- Novartis AG. WO05054177; 2005
- Novartis AG. WO05054177; 2005

140
- 46849087086
- Nicox S A. WO07045551; 2007
- Nicox S A. WO07045551; 2007

141
- 46849115021
- Nicox S A. WO07104652; 2007
- Nicox S A. WO07104652; 2007

142
- 46849099336
- Speedel Experimenta AG. WO08017685; 2008
- Speedel Experimenta AG. WO08017685; 2008

143
- 39749181550
- Generation of a set of simple, interpretable ADMET rules of thumb
- Gleeson MP: Generation of a set of simple, interpretable ADMET rules of thumb. J Med Chem 2008;51:817-34
- (2008) J Med Chem , vol.51 , pp. 817-834
- Gleeson, M.P.¹

144
- 46849092297
- 29 November 2006. Available from
- Next generation of renin inhibitors - Dr. JC Jensen - Speedel R&D Day. 29 November 2006. Available from: http://www.speedel.com/assets/ 9%20Chris%20Jensen%20Next%20Generation%20Renin%20Inhibitors%20 R&D%20Day%2029%20Nov%202006.pdf
- Next generation of renin inhibitors - Dr. JC Jensen - Speedel R&D Day

145
- 46849117643
- Speedel announces start of SPP635 Phase IIA trial in diabetic patients. Available from: http://www.speedel.com/speedelnew/section/7/subsections/ 0?pr_url=http://cws.huginonline.com/S/135077/PR/200712/1174499.xml
- Speedel announces start of SPP635 Phase IIA trial in diabetic patients. Available from: http://www.speedel.com/speedelnew/section/7/subsections/ 0?pr_url=http://cws.huginonline.com/S/135077/PR/200712/1174499.xml

146
- 46849114410
- Speedel Company Fact Sheet. Available from
- Speedel Company Fact Sheet. Available from: http://www.speedel.com/ assets/speedel_corp_factsheetnew.pdf

147
- 46849123033
- Actelion/Merck & Co, Inc, million. Available from
- Actelion/Merck & Co., Inc. Renin alliance achieves fourth milestone - Dosing in Phase II initiated - Actelion receives USD 10 million. Available from: http://www.actelion.com/uninet/www/www_main_p.nsf/ Content/me+05+Dec+2007
- Renin alliance achieves fourth milestone - Dosing in Phase II initiated - Actelion receives USD , vol.10

148
- 56349170842
- Available from
- Vitae Pharmaceuticals: Product Focus. Available from: http://www.vitaepharma.com/pipeline/index.php#Hyper
- Vitae Pharmaceuticals: Product Focus

149
- 46849108837
- Press release issued Monday 20 June 2005-GlaxoSmith Kline and Vitae Pharmaceuticals Establish Strategic Alliance to Develop and Commercialise Novel Hypertension Treatment. Available from: http://www.vitaepharma.com/news/NewsRelease2005Jun20.pdf
- Press release issued Monday 20 June 2005-GlaxoSmith Kline and Vitae Pharmaceuticals Establish Strategic Alliance to Develop and Commercialise Novel Hypertension Treatment. Available from: http://www.vitaepharma.com/news/NewsRelease2005Jun20.pdf

* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.