Detalhe da pesquisa
1.
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
2.
Optimization of physicochemical properties of pyrrolidine GPR40 AgoPAMs results in a differentiated profile with improved pharmacokinetics and reduced off-target activities.
Bioorg Med Chem
; 85: 117273, 2023 05 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-37030194
3.
Scalable Asymmetric Synthesis of the All Cis Triamino Cyclohexane Core of BMS-813160.
J Org Chem
; 87(4): 1996-2011, 2022 02 18.
Artigo
em Inglês
| MEDLINE | ID: mdl-34355895
4.
Identification of 6-hydroxy-5-phenyl sulfonylpyrimidin-4(1H)-one APJ receptor agonists.
Bioorg Med Chem Lett
; 50: 128325, 2021 10 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-34403724
5.
Annulation reaction enables the identification of an exocyclic amide tricyclic chemotype as retinoic acid Receptor-Related orphan receptor gamma (RORγ/RORc) inverse agonists.
Bioorg Med Chem Lett
; 30(19): 127466, 2020 10 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-32763309
6.
Discovery of (3S,4S)-3-methyl-3-(4-fluorophenyl)-4-(4-(1,1,1,3,3,3-hexafluoro-2-hydroxyprop-2-yl)phenyl)pyrrolidines as novel RORγt inverse agonists.
Bioorg Med Chem Lett
; 30(17): 127392, 2020 09 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-32738966
7.
Discovery and synthesis of tetrahydropyrimidinedione-4-carboxamides as endothelial lipase inhibitors.
Bioorg Med Chem Lett
; 28(23-24): 3721-3725, 2018 12 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-30348490
8.
Identification of bicyclic hexafluoroisopropyl alcohol sulfonamides as retinoic acid receptor-related orphan receptor gamma (RORγ/RORc) inverse agonists. Employing structure-based drug design to improve pregnane X receptor (PXR) selectivity.
Bioorg Med Chem Lett
; 28(2): 85-93, 2018 01 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-29233651
9.
Discovery and synthesis of cyclohexenyl derivatives as modulators of CC chemokine receptor 2 activity.
Bioorg Med Chem Lett
; 26(2): 662-666, 2016 Jan 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-26631321
10.
[2.2.1]-Bicyclic sultams as potent androgen receptor antagonists.
Bioorg Med Chem Lett
; 26(23): 5707-5711, 2016 12 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-27836399
11.
Role of Self-Association and Supersaturation in Oral Absorption of a Poorly Soluble Weakly Basic Drug.
Pharm Res
; 32(8): 2579-94, 2015 Aug.
Artigo
em Inglês
| MEDLINE | ID: mdl-25724158
12.
Synthesis and evaluation of carbamoylmethylene linked prodrugs of BMS-582949, a clinical p38α inhibitor.
Bioorg Med Chem Lett
; 23(10): 3028-33, 2013 May 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-23578688
13.
Discovery of Heteroaryl Urea Isosteres for Formyl Peptide Receptor 2 Agonists.
ACS Med Chem Lett
; 13(6): 943-948, 2022 Jun 09.
Artigo
em Inglês
| MEDLINE | ID: mdl-35707160
14.
Discovery of Milvexian, a High-Affinity, Orally Bioavailable Inhibitor of Factor XIa in Clinical Studies for Antithrombotic Therapy.
J Med Chem
; 65(3): 1770-1785, 2022 02 10.
Artigo
em Inglês
| MEDLINE | ID: mdl-34494428
15.
Novel tricyclic inhibitors of IKK2: discovery and SAR leading to the identification of 2-methoxy-N-((6-(1-methyl-4-(methylamino)-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-7-yl)pyridin-2-yl)methyl)acetamide (BMS-066).
Bioorg Med Chem Lett
; 21(23): 7006-12, 2011 Dec 01.
Artigo
em Inglês
| MEDLINE | ID: mdl-22018461
16.
Discovery of a Hydroxypyridinone APJ Receptor Agonist as a Clinical Candidate.
J Med Chem
; 64(6): 3086-3099, 2021 03 25.
Artigo
em Inglês
| MEDLINE | ID: mdl-33689340
17.
Driving Potency with Rotationally Stable Atropisomers: Discovery of Pyridopyrimidinedione-Carbazole Inhibitors of BTK.
ACS Med Chem Lett
; 11(11): 2195-2203, 2020 Nov 12.
Artigo
em Inglês
| MEDLINE | ID: mdl-33214829
18.
One-Step Diastereoselective Pyrrolidine Synthesis Using a Sulfinamide Annulating Reagent.
Org Lett
; 21(22): 9198-9202, 2019 11 15.
Artigo
em Inglês
| MEDLINE | ID: mdl-31647672
19.
Biphenyl Acid Derivatives as APJ Receptor Agonists.
J Med Chem
; 62(22): 10456-10465, 2019 11 27.
Artigo
em Inglês
| MEDLINE | ID: mdl-31724863
20.
Discovery of a JAK1/3 Inhibitor and Use of a Prodrug To Demonstrate Efficacy in a Model of Rheumatoid Arthritis.
ACS Med Chem Lett
; 10(3): 306-311, 2019 Mar 14.
Artigo
em Inglês
| MEDLINE | ID: mdl-30891131