Detalhe da pesquisa
1.
Structure-activity relationship (SAR) studies on substituted N-(pyridin-3-yl)-2-amino-isonicotinamides as highly potent and selective glycogen synthase kinase-3 (GSK-3) inhibitors.
Bioorg Med Chem Lett
; 81: 129143, 2023 02 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-36669575
2.
Structure-activity relationship study of central pyridine-derived TYK2 JH2 inhibitors: Optimization of the PK profile through C4' and C6 variations.
Bioorg Med Chem Lett
; 91: 129373, 2023 07 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-37315697
3.
Discovery of pyrrolo[2,1-f][1,2,4]triazine-based inhibitors of adaptor protein 2-associated kinase 1 for the treatment of pain.
Med Chem Res
; : 1-7, 2023 Jun 03.
Artigo
em Inglês
| MEDLINE | ID: mdl-37362320
4.
Calcitonin gene-related peptide (CGRP) receptor antagonists: Heterocyclic modification of a novel azepinone lead.
Bioorg Med Chem Lett
; 43: 128077, 2021 07 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-33932522
5.
Azepino-indazoles as calcitonin gene-related peptide (CGRP) receptor antagonists.
Bioorg Med Chem Lett
; 31: 127624, 2021 01 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-33096162
6.
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
7.
The discovery of VU0652957 (VU2957, Valiglurax): SAR and DMPK challenges en route to an mGlu4 PAM development candidate.
Bioorg Med Chem Lett
; 29(2): 342-346, 2019 01 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-30503632
8.
Discovery and characterization of N-(1,3-dialkyl-1H-indazol-6-yl)-1H-pyrazolo[4,3-b]pyridin-3-amine scaffold as mGlu4 positive allosteric modulators that mitigate CYP1A2 induction liability.
Bioorg Med Chem Lett
; 28(15): 2641-2646, 2018 08 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-29958762
9.
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
10.
Asymmetric Synthesis of the Major Metabolite of a Calcitonin Gene-Related Peptide Receptor Antagonist and Mechanism of Epoxide Hydrogenolysis.
J Org Chem
; 82(7): 3710-3720, 2017 04 07.
Artigo
em Inglês
| MEDLINE | ID: mdl-28306261
11.
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
12.
Design and synthesis of a novel series of (1'S,2R,4'S)-3H-4'-azaspiro[benzo[4,5]imidazo[2,1-b]oxazole-2,2'-bicyclo[2.2.2]octanes] with high affinity for the α7 neuronal nicotinic receptor.
Bioorg Med Chem Lett
; 27(22): 5002-5005, 2017 11 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-29050783
13.
Development of spiroguanidine-derived α7 neuronal nicotinic receptor partial agonists.
Bioorg Med Chem Lett
; 27(3): 578-581, 2017 02 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-27993517
14.
Design and synthesis of a novel series of 4-heteroarylamino-1'-azaspiro[oxazole-5,3'-bicyclo[2.2.2]octanes as α7 nicotinic receptor agonists 2. Development of 4-heteroaryl SAR.
Bioorg Med Chem Lett
; 27(5): 1261-1266, 2017 03 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-28169167
15.
Triazolopyridine ethers as potent, orally active mGlu2 positive allosteric modulators for treating schizophrenia.
Bioorg Med Chem
; 25(2): 496-513, 2017 01 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-27914948
16.
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
17.
Evidence for Classical Cholinergic Toxicity Associated with Selective Activation of M1 Muscarinic Receptors.
J Pharmacol Exp Ther
; 356(2): 293-304, 2016 Feb.
Artigo
em Inglês
| MEDLINE | ID: mdl-26582730
18.
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
19.
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
20.
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