Detalhe da pesquisa
1.
Pharmacology of a Potent and Novel Inhibitor of the NOD-Like Receptor Pyrin Domain-Containing Protein 3 (NLRP3) Inflammasome that Attenuates Development of Nonalcoholic Steatohepatitis and Liver Fibrosis.
J Pharmacol Exp Ther
; 386(2): 242-258, 2023 08.
Artigo
em Inglês
| MEDLINE | ID: mdl-37308266
2.
Selective Inhibition of Autotaxin Is Efficacious in Mouse Models of Liver Fibrosis.
J Pharmacol Exp Ther
; 360(1): 1-13, 2017 Jan.
Artigo
em Inglês
| MEDLINE | ID: mdl-27754931
3.
Structural Basis for Inhibition of Human Autotaxin by Four Potent Compounds with Distinct Modes of Binding.
Mol Pharmacol
; 88(6): 982-92, 2015 Dec.
Artigo
em Inglês
| MEDLINE | ID: mdl-26371182
4.
Pharmacodynamics, pharmacokinetics and safety of GSK2190915, a novel oral anti-inflammatory 5-lipoxygenase-activating protein inhibitor.
Br J Clin Pharmacol
; 75(3): 779-90, 2013 Mar.
Artigo
em Inglês
| MEDLINE | ID: mdl-22803688
5.
JT002, a small molecule inhibitor of the NLRP3 inflammasome for the treatment of autoinflammatory disorders.
Sci Rep
; 13(1): 13524, 2023 08 19.
Artigo
em Inglês
| MEDLINE | ID: mdl-37598239
6.
Overcoming Preclinical Safety Obstacles to Discover (S)-N-((1,2,3,5,6,7-Hexahydro-s-indacen-4-yl)carbamoyl)-6-(methylamino)-6,7-dihydro-5H-pyrazolo[5,1-b][1,3]oxazine-3-sulfonamide (GDC-2394): A Potent and Selective NLRP3 Inhibitor.
J Med Chem
; 65(21): 14721-14739, 2022 11 10.
Artigo
em Inglês
| MEDLINE | ID: mdl-36279149
7.
Pharmacology of AM211, a potent and selective prostaglandin D2 receptor type 2 antagonist that is active in animal models of allergic inflammation.
J Pharmacol Exp Ther
; 338(1): 290-301, 2011 Jul.
Artigo
em Inglês
| MEDLINE | ID: mdl-21487069
8.
Discovery and optimization of a biphenylacetic acid series of prostaglandin D2 receptor DP2 antagonists with efficacy in a murine model of allergic rhinitis.
Bioorg Med Chem Lett
; 21(21): 6608-12, 2011 Nov 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-21958540
9.
Sodium [2'-[(cyclopropanecarbonyl-ethyl-amino)-methyl]-4'-(6-ethoxy-pyridin-3-yl)-6-methoxy-biphenyl-3-yl]-acetate (AM432): a potent, selective prostaglandin D2 receptor antagonist.
Bioorg Med Chem Lett
; 21(3): 1036-40, 2011 Feb 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-21211969
10.
Pharmacological blockade of the DP2 receptor inhibits cigarette smoke-induced inflammation, mucus cell metaplasia, and epithelial hyperplasia in the mouse lung.
J Pharmacol Exp Ther
; 332(3): 764-75, 2010 Mar.
Artigo
em Inglês
| MEDLINE | ID: mdl-19996299
11.
5-Lipoxygenase-activating protein inhibitors. Part 3: 3-{3-tert-Butylsulfanyl-1-[4-(5-methoxy-pyrimidin-2-yl)-benzyl]-5-(5-methyl-pyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethyl-propionic acid (AM643)-A potent FLAP inhibitor suitable for topical administration.
Bioorg Med Chem Lett
; 20(15): 4598-601, 2010 Aug 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-20566292
12.
5-Lipoxygenase-activating protein inhibitors. Part 2: 3-{5-((S)-1-Acetyl-2,3-dihydro-1H-indol-2-ylmethoxy)-3-tert-butylsulfanyl-1-[4-(5-methoxy-pyrimidin-2-yl)-benzyl]-1H-indol-2-yl}-2,2-dimethyl-propionic acid (AM679)--a potent FLAP inhibitor.
Bioorg Med Chem Lett
; 20(1): 213-7, 2010 Jan 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-19914828
13.
Pharmacological characterization of 3-[3-tert-butylsulfanyl-1-[4-(6-methoxy-pyridin-3-yl)-benzyl]-5-(pyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethyl-propionic acid (AM103), a novel selective 5-lipoxygenase-activating protein inhibitor that reduces acute and chronic inflammation.
J Pharmacol Exp Ther
; 331(3): 1042-50, 2009 Dec.
Artigo
em Inglês
| MEDLINE | ID: mdl-19749079
14.
Novel tricyclic antagonists of the prostaglandin D2 receptor DP2 with efficacy in a murine model of allergic rhinitis.
Bioorg Med Chem Lett
; 19(16): 4647-51, 2009 Aug 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-19608418
15.
Author Correction: JT002, a small molecule inhibitor of the NLRP3 inflammasome for the treatment of autoinflammatory disorders.
Sci Rep
; 13(1): 20081, 2023 Nov 16.
Artigo
em Inglês
| MEDLINE | ID: mdl-37973811
16.
Identification of 4-(Aminomethyl)-6-(trifluoromethyl)-2-(phenoxy)pyridine Derivatives as Potent, Selective, and Orally Efficacious Inhibitors of the Copper-Dependent Amine Oxidase, Lysyl Oxidase-Like 2 (LOXL2).
J Med Chem
; 60(10): 4403-4423, 2017 05 25.
Artigo
em Inglês
| MEDLINE | ID: mdl-28471663
17.
5-Lipoxygenase-activating protein (FLAP) inhibitors. Part 4: development of 3-[3-tert-butylsulfanyl-1-[4-(6-ethoxypyridin-3-yl)benzyl]-5-(5-methylpyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethylpropionic acid (AM803), a potent, oral, once daily FLAP inhibitor.
J Med Chem
; 54(23): 8013-29, 2011 Dec 08.
Artigo
em Inglês
| MEDLINE | ID: mdl-22059882
18.
Pharmacology of AM803, a novel selective five-lipoxygenase-activating protein (FLAP) inhibitor in rodent models of acute inflammation.
Eur J Pharmacol
; 640(1-3): 211-8, 2010 Aug 25.
Artigo
em Inglês
| MEDLINE | ID: mdl-20519143
19.
5-lipoxygenase-activating protein inhibitors: development of 3-[3-tert-butylsulfanyl-1-[4-(6-methoxy-pyridin-3-yl)-benzyl]-5-(pyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethyl-propionic acid (AM103).
J Med Chem
; 52(19): 5803-15, 2009 Oct 08.
Artigo
em Inglês
| MEDLINE | ID: mdl-19739647
20.
Expedited SAR study of high-affinity ligands to the alpha(2)delta subunit of voltage-gated calcium channels: Generation of a focused library using a solution-phase Sn2Ar coupling methodology.
Bioorg Med Chem Lett
; 16(3): 746-9, 2006 Feb.
Artigo
em Inglês
| MEDLINE | ID: mdl-16321528