Detalhe da pesquisa
1.
Synthesis and evaluation of prodrugs of corticotropin-releasing factor-1 (CRF1) receptor antagonist BMS-665053 leading to improved oral bioavailability.
Bioorg Med Chem Lett
; 27(6): 1360-1363, 2017 03 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-28223020
2.
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
3.
Inhibition of AAK1 Kinase as a Novel Therapeutic Approach to Treat Neuropathic Pain.
J Pharmacol Exp Ther
; 358(3): 371-86, 2016 09.
Artigo
em Inglês
| MEDLINE | ID: mdl-27411717
4.
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
5.
Synthesis and evaluation of carbamate and aryl ether substituted pyrazinones as corticotropin releasing factor-1 (CRF1) receptor antagonists.
Bioorg Med Chem Lett
; 26(9): 2184-7, 2016 May 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-27020524
6.
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
7.
[18F](R)-5-chloro-1-(1-cyclopropyl-2-methoxyethyl)-3-(4-(2-fluoroethoxy)-2,5-dimethyl phenylamino)pyrazin-2(1H)-one: introduction of N3-phenylpyrazinones as potential CRF-R1 PET imaging agents.
Bioorg Med Chem Lett
; 22(21): 6651-5, 2012 Nov 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-23010264
8.
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
9.
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
10.
Preclinical pharmacokinetics and pharmacodynamics of apixaban, a potent and selective factor Xa inhibitor.
Eur J Drug Metab Pharmacokinet
; 36(3): 129-39, 2011 Sep.
Artigo
em Inglês
| MEDLINE | ID: mdl-21461793
11.
Evaluation of cynomolgus monkey pregnane X receptor, primary hepatocyte, and in vivo pharmacokinetic changes in predicting human CYP3A4 induction.
Drug Metab Dispos
; 38(1): 16-24, 2010 Jan.
Artigo
em Inglês
| MEDLINE | ID: mdl-19833845
12.
Identification and Preclinical Evaluation of the Bicyclic Pyrimidine γ-Secretase Modulator BMS-932481.
ACS Med Chem Lett
; 10(3): 312-317, 2019 Mar 14.
Artigo
em Inglês
| MEDLINE | ID: mdl-30891132
13.
P-glycoprotein efflux and other factors limit brain amyloid beta reduction by beta-site amyloid precursor protein-cleaving enzyme 1 inhibitors in mice.
J Pharmacol Exp Ther
; 326(2): 502-13, 2008 Aug.
Artigo
em Inglês
| MEDLINE | ID: mdl-18499745
14.
Development and validation of a preclinical food effect model.
J Pharm Sci
; 96(2): 459-72, 2007 Feb.
Artigo
em Inglês
| MEDLINE | ID: mdl-17075867
15.
Identification and Preclinical Pharmacology of the γ-Secretase Modulator BMS-869780.
Int J Alzheimers Dis
; 2014: 431858, 2014.
Artigo
em Inglês
| MEDLINE | ID: mdl-25097793
16.
Utility of high-resolution accurate MS to eliminate interferences in the bioanalysis of ribavirin and its phosphate metabolites.
Bioanalysis
; 4(15): 1895-905, 2012 Aug.
Artigo
em Inglês
| MEDLINE | ID: mdl-22943620
17.
A strategy to minimize reactive metabolite formation: discovery of (S)-4-(1-cyclopropyl-2-methoxyethyl)-6-[6-(difluoromethoxy)-2,5-dimethylpyridin-3-ylamino]-5-oxo-4,5-dihydropyrazine-2-carbonitrile as a potent, orally bioavailable corticotropin-releasing factor-1 receptor antagonist.
J Med Chem
; 52(23): 7653-68, 2009 Dec 10.
Artigo
em Inglês
| MEDLINE | ID: mdl-19954247
18.
In vitro intrinsic clearance-based optimization of N3-phenylpyrazinones as corticotropin-releasing factor-1 (CRF1) receptor antagonists.
J Med Chem
; 52(14): 4161-72, 2009 Jul 23.
Artigo
em Inglês
| MEDLINE | ID: mdl-19552436
19.
Synthesis, structure-activity relationships, and in vivo evaluation of N3-phenylpyrazinones as novel corticotropin-releasing factor-1 (CRF1) receptor antagonists.
J Med Chem
; 52(14): 4173-91, 2009 Jul 23.
Artigo
em Inglês
| MEDLINE | ID: mdl-19552437
20.
N-in-1 dosing pharmacokinetics in drug discovery: experience, theoretical and practical considerations.
J Pharm Sci
; 97(7): 2568-80, 2008 Jul.
Artigo
em Inglês
| MEDLINE | ID: mdl-17914718