Detalhe da pesquisa
1.
MK-8719, a Novel and Selective O-GlcNAcase Inhibitor That Reduces the Formation of Pathological Tau and Ameliorates Neurodegeneration in a Mouse Model of Tauopathy.
J Pharmacol Exp Ther
; 374(2): 252-263, 2020 08.
Artigo
Inglês
| MEDLINE | ID: mdl-32493725
2.
Novel oxazolidinone calcitonin gene-related peptide (CGRP) receptor antagonists for the acute treatment of migraine.
Bioorg Med Chem Lett
; 25(21): 4777-4781, 2015 Nov 01.
Artigo
Inglês
| MEDLINE | ID: mdl-26231160
3.
Methyl-substitution of an iminohydantoin spiropiperidine ß-secretase (BACE-1) inhibitor has a profound effect on its potency.
Bioorg Med Chem Lett
; 25(21): 4812-4819, 2015 Nov 01.
Artigo
Inglês
| MEDLINE | ID: mdl-26195137
4.
(E)-Alkenes as replacements of amide bonds: development of novel and potent acyclic CGRP receptor antagonists.
Bioorg Med Chem Lett
; 24(1): 258-61, 2014 Jan 01.
Artigo
Inglês
| MEDLINE | ID: mdl-24332093
5.
In vivo quantification of calcitonin gene-related peptide receptor occupancy by telcagepant in rhesus monkey and human brain using the positron emission tomography tracer [11C]MK-4232.
J Pharmacol Exp Ther
; 347(2): 478-86, 2013 Nov.
Artigo
Inglês
| MEDLINE | ID: mdl-23975906
6.
MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats.
Bioorg Med Chem Lett
; 22(12): 3941-5, 2012 Jun 15.
Artigo
Inglês
| MEDLINE | ID: mdl-22607672
7.
Orally bioavailable imidazoazepanes as calcitonin gene-related peptide (CGRP) receptor antagonists: discovery of MK-2918.
Bioorg Med Chem Lett
; 21(9): 2683-6, 2011 May 01.
Artigo
Inglês
| MEDLINE | ID: mdl-21251825
8.
Pharmacological properties of MK-3207, a potent and orally active calcitonin gene-related peptide receptor antagonist.
J Pharmacol Exp Ther
; 333(1): 152-60, 2010 Apr.
Artigo
Inglês
| MEDLINE | ID: mdl-20065019
9.
Novel CGRP receptor antagonists from central amide replacements causing a reversal of preferred chirality.
Bioorg Med Chem Lett
; 20(22): 6827-30, 2010 Nov 15.
Artigo
Inglês
| MEDLINE | ID: mdl-20850973
10.
Identification of potent, highly constrained CGRP receptor antagonists.
Bioorg Med Chem Lett
; 20(8): 2572-6, 2010 Apr 15.
Artigo
Inglês
| MEDLINE | ID: mdl-20299218
11.
SAR of tertiary carbinamine derived BACE1 inhibitors: role of aspartate ligand amine pKa in enzyme inhibition.
Bioorg Med Chem Lett
; 20(6): 1885-9, 2010 Mar 15.
Artigo
Inglês
| MEDLINE | ID: mdl-20176482
12.
First demonstration of cerebrospinal fluid and plasma A beta lowering with oral administration of a beta-site amyloid precursor protein-cleaving enzyme 1 inhibitor in nonhuman primates.
J Pharmacol Exp Ther
; 328(1): 131-40, 2009 Jan.
Artigo
Inglês
| MEDLINE | ID: mdl-18854490
13.
Novel CGRP receptor antagonists through a design strategy of target simplification with addition of molecular flexibility.
Bioorg Med Chem Lett
; 19(19): 5787-90, 2009 Oct 01.
Artigo
Inglês
| MEDLINE | ID: mdl-19703767
14.
Discovery of MK-8719, a Potent O-GlcNAcase Inhibitor as a Potential Treatment for Tauopathies.
J Med Chem
; 62(22): 10062-10097, 2019 11 27.
Artigo
Inglês
| MEDLINE | ID: mdl-31487175
15.
Discovery of oxadiazoyl tertiary carbinamine inhibitors of beta-secretase (BACE-1).
J Med Chem
; 49(25): 7270-3, 2006 Dec 14.
Artigo
Inglês
| MEDLINE | ID: mdl-17149856
16.
9-hydroxyazafluorenes and their use in thrombin inhibitors.
J Med Chem
; 48(7): 2282-93, 2005 Apr 07.
Artigo
Inglês
| MEDLINE | ID: mdl-15801822
17.
Synthesis and evaluation of imidazole acetic acid inhibitors of activated thrombin-activatable fibrinolysis inhibitor as novel antithrombotics.
J Med Chem
; 46(25): 5294-7, 2003 Dec 04.
Artigo
Inglês
| MEDLINE | ID: mdl-14640538
18.
Discovery and evaluation of potent P1 aryl heterocycle-based thrombin inhibitors.
J Med Chem
; 47(12): 2995-3008, 2004 Jun 03.
Artigo
Inglês
| MEDLINE | ID: mdl-15163182
19.
[(11)C]MK-4232: The First Positron Emission Tomography Tracer for the Calcitonin Gene-Related Peptide Receptor.
ACS Med Chem Lett
; 4(9): 863-8, 2013 Sep 12.
Artigo
Inglês
| MEDLINE | ID: mdl-24900761
20.
Discovery of MK-3207: A Highly Potent, Orally Bioavailable CGRP Receptor Antagonist.
ACS Med Chem Lett
; 1(1): 24-9, 2010 Apr 08.
Artigo
Inglês
| MEDLINE | ID: mdl-24900170