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1.
Small-molecule factor B inhibitor for the treatment of complement-mediated diseases.
Proc Natl Acad Sci U S A
; 116(16): 7926-7931, 2019 04 16.
Artículo
en Inglés
| MEDLINE | ID: mdl-30926668
2.
Small-molecule factor D inhibitors targeting the alternative complement pathway.
Nat Chem Biol
; 12(12): 1105-1110, 2016 Dec.
Artículo
en Inglés
| MEDLINE | ID: mdl-27775713
3.
trans-(3S,4S)-Disubstituted pyrrolidines as inhibitors of the human aspartyl protease renin. Part I: prime site exploration using an amino linker.
Bioorg Med Chem Lett
; 25(8): 1782-1786, 2015 Apr 15.
Artículo
en Inglés
| MEDLINE | ID: mdl-25782742
4.
trans-3,4-Disubstituted pyrrolidines as inhibitors of the human aspartyl protease renin. Part II: prime site exploration using an oxygen linker.
Bioorg Med Chem Lett
; 25(8): 1787-1791, 2015 Apr 15.
Artículo
en Inglés
| MEDLINE | ID: mdl-25754490
5.
Discovery of 4-((2S,4S)-4-Ethoxy-1-((5-methoxy-7-methyl-1H-indol-4-yl)methyl)piperidin-2-yl)benzoic Acid (LNP023), a Factor B Inhibitor Specifically Designed To Be Applicable to Treating a Diverse Array of Complement Mediated Diseases.
J Med Chem
; 63(11): 5697-5722, 2020 06 11.
Artículo
en Inglés
| MEDLINE | ID: mdl-32073845
6.
The P1N-isopropyl motif bearing hydroxyethylene dipeptide isostere analogues of aliskiren are in vitro potent inhibitors of the human aspartyl protease renin.
Bioorg Med Chem Lett
; 19(16): 4863-7, 2009 Aug 15.
Artículo
en Inglés
| MEDLINE | ID: mdl-19615901
7.
Discovery and Design of First Benzylamine-Based Ligands Binding to an Unlocked Conformation of the Complement Factor D.
ACS Med Chem Lett
; 9(5): 490-495, 2018 May 10.
Artículo
en Inglés
| MEDLINE | ID: mdl-29795765
8.
Crystal structure of human BACE2 in complex with a hydroxyethylamine transition-state inhibitor.
J Mol Biol
; 355(2): 249-61, 2006 Jan 13.
Artículo
en Inglés
| MEDLINE | ID: mdl-16305800
9.
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
; 50(20): 4818-31, 2007 Oct 04.
Artículo
en Inglés
| MEDLINE | ID: mdl-17824679
10.
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
; 50(20): 4832-44, 2007 Oct 04.
Artículo
en Inglés
| MEDLINE | ID: mdl-17824680
11.
Structure-Based Library Design and Fragment Screening for the Identification of Reversible Complement Factor D Protease Inhibitors.
J Med Chem
; 60(5): 1946-1958, 2017 03 09.
Artículo
en Inglés
| MEDLINE | ID: mdl-28157311
12.
Discovery of Highly Potent and Selective Small-Molecule Reversible Factor D Inhibitors Demonstrating Alternative Complement Pathway Inhibition in Vivo.
J Med Chem
; 60(13): 5717-5735, 2017 07 13.
Artículo
en Inglés
| MEDLINE | ID: mdl-28621538
13.
Structure-based design of substituted piperidines as a new class of highly efficacious oral direct Renin inhibitors.
ACS Med Chem Lett
; 5(7): 787-92, 2014 Jul 10.
Artículo
en Inglés
| MEDLINE | ID: mdl-25050166
14.
The discovery of novel potent trans-3,4-disubstituted pyrrolidine inhibitors of the human aspartic protease renin from in silico three-dimensional (3D) pharmacophore searches.
J Med Chem
; 56(6): 2207-17, 2013 Mar 28.
Artículo
en Inglés
| MEDLINE | ID: mdl-23425156
15.
A novel class of oral direct renin inhibitors: highly potent 3,5-disubstituted piperidines bearing a tricyclic p3-p1 pharmacophore.
J Med Chem
; 56(6): 2196-206, 2013 Mar 28.
Artículo
en Inglés
| MEDLINE | ID: mdl-23360239
16.
Direct renin inhibitors as a new therapy for hypertension.
J Med Chem
; 53(21): 7490-520, 2010 Nov 11.
Artículo
en Inglés
| MEDLINE | ID: mdl-20731374
17.
Structure-based design of aliskiren, a novel orally effective renin inhibitor.
Biochem Biophys Res Commun
; 308(4): 698-705, 2003 Sep 05.
Artículo
en Inglés
| MEDLINE | ID: mdl-12927775
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