Detalhe da pesquisa
1.
Phase 1 clinical trial of losmapimod in facioscapulohumeral dystrophy: Safety, tolerability, pharmacokinetics, and target engagement.
Br J Clin Pharmacol
; 87(12): 4658-4669, 2021 12.
Artigo
em Inglês
| MEDLINE | ID: mdl-33931884
2.
p38α Regulates Expression of DUX4 in a Model of Facioscapulohumeral Muscular Dystrophy.
J Pharmacol Exp Ther
; 374(3): 489-498, 2020 09.
Artigo
em Inglês
| MEDLINE | ID: mdl-32576599
3.
Synthesis of functionalized derivatives of the gamma-secretase modulator BMS-932481 and identification of its major metabolite.
Bioorg Med Chem Lett
; 30(22): 127530, 2020 11 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-32890687
4.
Discovery of new indole-based acylsulfonamide Nav1.7 inhibitors.
Bioorg Med Chem Lett
; 29(4): 659-663, 2019 02 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-30638874
5.
Discovery of morpholine-based aryl sulfonamides as Nav1.7 inhibitors.
Bioorg Med Chem Lett
; 28(5): 958-962, 2018 03 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-29439904
6.
Preclinical Characterization of (R)-3-((3S,4S)-3-fluoro-4-(4-hydroxyphenyl)piperidin-1-yl)-1-(4-methylbenzyl)pyrrolidin-2-one (BMS-986169), a Novel, Intravenous, Glutamate N-Methyl-d-Aspartate 2B Receptor Negative Allosteric Modulator with Potential in Major Depressive Disorder.
J Pharmacol Exp Ther
; 363(3): 377-393, 2017 12.
Artigo
em Inglês
| MEDLINE | ID: mdl-28954811
7.
Discovery of non-zwitterionic aryl sulfonamides as Nav1.7 inhibitors with efficacy in preclinical behavioral models and translational measures of nociceptive neuron activation.
Bioorg Med Chem
; 25(20): 5490-5505, 2017 10 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-28818462
8.
Centrally Delivered BACE1 Inhibitor Activates Microglia, and Reverses Amyloid Pathology and Cognitive Deficit in Aged Tg2576 Mice.
J Neurosci
; 35(17): 6931-6, 2015 Apr 29.
Artigo
em Inglês
| MEDLINE | ID: mdl-25926467
9.
The γ-Secretase Modulator, BMS-932481, Modulates Aß Peptides in the Plasma and Cerebrospinal Fluid of Healthy Volunteers.
J Pharmacol Exp Ther
; 358(1): 138-50, 2016 Jul.
Artigo
em Inglês
| MEDLINE | ID: mdl-27189973
10.
Robust Translation of γ-Secretase Modulator Pharmacology across Preclinical Species and Human Subjects.
J Pharmacol Exp Ther
; 358(1): 125-37, 2016 07.
Artigo
em Inglês
| MEDLINE | ID: mdl-27189974
11.
Expedient Synthesis of Furo[2,3-d][1,3]thiazinamines and Pyrano[2,3-d][1,3]thiazinamines from Enones and Thiourea.
J Org Chem
; 81(8): 3386-90, 2016 Apr 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-27002691
12.
Synthesis of pyrimido[4,5-c]azepine- and pyrimido[4,5-c]oxepine-based γ-secretase modulators.
Bioorg Med Chem Lett
; 26(6): 1554-1557, 2016 Mar 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-26898338
13.
Design and optimization of tricyclic gamma-secretase modulators.
Bioorg Med Chem Lett
; 26(5): 1498-502, 2016 Mar 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-26848108
14.
Discovery of furo[2,3-d][1,3]thiazinamines as beta amyloid cleaving enzyme-1 (BACE1) inhibitors.
Bioorg Med Chem Lett
; 26(23): 5729-5731, 2016 12 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-27816517
15.
Macrocyclic prolinyl acyl guanidines as inhibitors of ß-secretase (BACE).
Bioorg Med Chem Lett
; 25(22): 5040-7, 2015 Nov 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-26497283
16.
Monosubstituted γ-lactam and conformationally constrained 1,3-diaminopropan-2-ol transition-state isostere inhibitors of ß-secretase (BACE).
Bioorg Med Chem Lett
; 21(22): 6916-24, 2011 Nov 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-21782431
17.
Synthesis and SAR of indole-and 7-azaindole-1,3-dicarboxamide hydroxyethylamine inhibitors of BACE-1.
Bioorg Med Chem Lett
; 21(1): 537-41, 2011 Jan 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-21078556
18.
Synthesis and in vivo evaluation of cyclic diaminopropane BACE-1 inhibitors.
Bioorg Med Chem Lett
; 21(22): 6909-15, 2011 Nov 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-21974952
19.
Synthesis and SAR of hydroxyethylamine based phenylcarboxyamides as inhibitors of BACE.
Bioorg Med Chem Lett
; 19(10): 2654-60, 2009 May 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-19375914
20.
Discovery of Indole- and Indazole-acylsulfonamides as Potent and Selective NaV1.7 Inhibitors for the Treatment of Pain.
J Med Chem
; 62(2): 831-856, 2019 01 24.
Artigo
em Inglês
| MEDLINE | ID: mdl-30576602