메뉴 건너뛰기




Volumn 7, Issue 10, 2016, Pages 933-938

Discovery of TAK-272: A Novel, Potent, and Orally Active Renin Inhibitor

Author keywords

benzimidazole; dTg rat; hypertension; Renin inhibitor; SBDD; TAK 272

Indexed keywords

1 (4 METHOXYBUTYL) N (2 METHYLPROPYL) N [ 5 (MORPHOLIN 4 YL)CARBONYLPIPERIDIN 3 YL] 1H BENZIMIDAZOLE 2 CARBOXAMIDE HYDROCHLORIDE; ALISKIREN; BENZIMIDAZOLE DERIVATIVE; RENIN INHIBITOR; UNCLASSIFIED DRUG;

EID: 84991517842     PISSN: None     EISSN: 19485875     Source Type: Journal    
DOI: 10.1021/acsmedchemlett.6b00251     Document Type: Article
Times cited : (19)

References (23)
  • 1
    • 0019513437 scopus 로고
    • Maintenance of blood pressure by the renin-angiotensin system in normal man
    • MacGregor, G. A.; Markandu, N. D.; Roulston, J. E.; Jones, J. C.; Morton, J. J. Maintenance of blood pressure by the renin-angiotensin system in normal man Nature 1981, 291, 329-331 10.1038/291329a0
    • (1981) Nature , vol.291 , pp. 329-331
    • MacGregor, G.A.1    Markandu, N.D.2    Roulston, J.E.3    Jones, J.C.4    Morton, J.J.5
  • 2
    • 0036690114 scopus 로고    scopus 로고
    • Drugs Targeting the Renin-Angiotensin-Aldosterone System
    • Zaman, M. A.; Oparil, S.; Calhoun, D. A. Drugs Targeting the Renin-Angiotensin-Aldosterone System Nat. Rev. Drug Discovery 2002, 1, 621-636 10.1038/nrd873
    • (2002) Nat. Rev. Drug Discovery , vol.1 , pp. 621-636
    • Zaman, M.A.1    Oparil, S.2    Calhoun, D.A.3
  • 3
    • 84895070950 scopus 로고    scopus 로고
    • The effect of RAAS blockade on the progression of diabetic nephropathy
    • Roscioni, S. S.; Lambers Heerspink, H. J.; de Zeeuw, D. The effect of RAAS blockade on the progression of diabetic nephropathy Nat. Rev. Nephrol. 2014, 10, 77-87 10.1038/nrneph.2013.251
    • (2014) Nat. Rev. Nephrol. , vol.10 , pp. 77-87
    • Roscioni, S.S.1    Lambers Heerspink, H.J.2    De Zeeuw, D.3
  • 5
    • 77955415650 scopus 로고    scopus 로고
    • Application of direct renin inhibition to chronic kidney diseases
    • Mende, C. W. Application of direct renin inhibition to chronic kidney diseases Cardiovasc. Drugs Ther. 2010, 24, 139-149 10.1007/s10557-010-6232-1
    • (2010) Cardiovasc. Drugs Ther. , vol.24 , pp. 139-149
    • Mende, C.W.1
  • 7
    • 78149259520 scopus 로고    scopus 로고
    • Direct renin inhibitors as a new therapy for hypertension
    • Webb, R. L.; Schiering, N.; Sedrani, R.; Maibaum, J. Direct renin inhibitors as a new therapy for hypertension J. Med. Chem. 2010, 53, 7490-7520 10.1021/jm901885s
    • (2010) J. Med. Chem. , vol.53 , pp. 7490-7520
    • Webb, R.L.1    Schiering, N.2    Sedrani, R.3    Maibaum, J.4
  • 8
    • 46849092364 scopus 로고    scopus 로고
    • Recent advances in the discovery of non-peptidic direct renin inhibitors as antihypertensives
    • Yokokawa, F.; Maibaum, J. Recent advances in the discovery of non-peptidic direct renin inhibitors as antihypertensives Expert Opin. Ther. Pat. 2008, 18, 581-602 10.1517/13543776.18.6.581
    • (2008) Expert Opin. Ther. Pat. , vol.18 , pp. 581-602
    • Yokokawa, F.1    Maibaum, J.2
  • 9
    • 84877951910 scopus 로고    scopus 로고
    • Recent progress on the discovery of non-peptidic direct renin inhibitors for the clinical management of hypertension
    • Yokokawa, F. Recent progress on the discovery of non-peptidic direct renin inhibitors for the clinical management of hypertension Expert Opin. Drug Discovery 2013, 8, 673-690 10.1517/17460441.2013.791279
    • (2013) Expert Opin. Drug Discovery , vol.8 , pp. 673-690
    • Yokokawa, F.1
  • 10
    • 34848869297 scopus 로고    scopus 로고
    • 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, H.-P.; Cohen, N.-C.; Schnell, C. R.; Fuhrer, W.; Gruetter, M. G.; Schilling, W.; Wood, J. M. 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, 4832-4844 10.1021/jm070316i
    • (2007) J. Med. Chem. , vol.50 , pp. 4832-4844
    • Maibaum, J.1    Stutz, S.2    Göschke, R.3    Rigollier, P.4    Yamaguchi, Y.5    Cumin, F.6    Rahuel, J.7    Baum, H.-P.8    Cohen, N.-C.9    Schnell, C.R.10    Fuhrer, W.11    Gruetter, M.G.12    Schilling, W.13    Wood, J.M.14
  • 15
    • 0031024171 scopus 로고    scopus 로고
    • Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings
    • Lipinski, C. A.; Lombardo, F.; Dominy, B. W.; Feeney, P. J. Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings Adv. Drug Delivery Rev. 1997, 23, 3-25 10.1016/S0169-409X(96)00423-1
    • (1997) Adv. Drug Delivery Rev. , vol.23 , pp. 3-25
    • Lipinski, C.A.1    Lombardo, F.2    Dominy, B.W.3    Feeney, P.J.4
  • 16
    • 0037030653 scopus 로고    scopus 로고
    • Molecular properties that influence the oral bioavailability of drug candidates
    • Veber, D. F.; Johnson, S. R.; Cheng, H.-Y.; Smith, B. R.; Ward, K. W.; Kopple, K. D. Molecular properties that influence the oral bioavailability of drug candidates J. Med. Chem. 2002, 45, 2615-2623 10.1021/jm020017n
    • (2002) J. Med. Chem. , vol.45 , pp. 2615-2623
    • Veber, D.F.1    Johnson, S.R.2    Cheng, H.-Y.3    Smith, B.R.4    Ward, K.W.5    Kopple, K.D.6
  • 18
    • 18944393300 scopus 로고    scopus 로고
    • Bioactivation of 4-ipomeanol by CYP4B1: Adduct characterization and evidence for an enedial intermediate
    • Baer, B. R.; Rettie, A. E.; Henne, K. R. Bioactivation of 4-ipomeanol by CYP4B1: adduct characterization and evidence for an enedial intermediate Chem. Res. Toxicol. 2005, 18, 855-864 10.1021/tx0496993
    • (2005) Chem. Res. Toxicol. , vol.18 , pp. 855-864
    • Baer, B.R.1    Rettie, A.E.2    Henne, K.R.3
  • 20
    • 71049126548 scopus 로고    scopus 로고
    • Escape from Flatland: Increasing Saturation as an Approach to Improving Clinical Success
    • Lovering, F.; Bikker, J.; Humbelt, C. Escape from Flatland: Increasing Saturation as an Approach to Improving Clinical Success J. Med. Chem. 2009, 52, 6752-6756 10.1021/jm901241e
    • (2009) J. Med. Chem. , vol.52 , pp. 6752-6756
    • Lovering, F.1    Bikker, J.2    Humbelt, C.3
  • 21
    • 34447109128 scopus 로고    scopus 로고
    • The role of molecular size in ligand efficiency
    • Reynolds, C. H.; Bembenek, S. D.; Tounge, B. A. The role of molecular size in ligand efficiency Bioorg. Med. Chem. Lett. 2007, 17, 4258-4261 10.1016/j.bmcl.2007.05.038
    • (2007) Bioorg. Med. Chem. Lett. , vol.17 , pp. 4258-4261
    • Reynolds, C.H.1    Bembenek, S.D.2    Tounge, B.A.3
  • 22
    • 35748934487 scopus 로고    scopus 로고
    • The Influence of Drug-like Concepts on Decision-Making in Medicinal Chemistry
    • Leeson, P. D.; Springthorpe, B. The Influence of Drug-like Concepts on Decision-Making in Medicinal Chemistry Nat. Rev. Drug Discovery 2007, 6, 881-890 10.1038/nrd2445
    • (2007) Nat. Rev. Drug Discovery , vol.6 , pp. 881-890
    • Leeson, P.D.1    Springthorpe, B.2


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.