Detalles de la búsqueda
1.
Efficient synthesis of tert-butyl 3-cyano-3-cyclopropyl-2-oxopyrrolidine-4-carboxylates: Highly functionalized 2-pyrrolidinone enabling access to novel macrocyclic Tyk2 inhibitors.
Bioorg Med Chem Lett
; 30(5): 126963, 2020 03 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-31980341
2.
Identification of novel quinazolinedione derivatives as RORγt inverse agonist.
Bioorg Med Chem
; 26(3): 721-736, 2018 02 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-29342416
3.
Discovery of orally efficacious RORγt inverse agonists, part 1: Identification of novel phenylglycinamides as lead scaffolds.
Bioorg Med Chem
; 26(2): 483-500, 2018 01 15.
Artículo
en Inglés
| MEDLINE | ID: mdl-29262987
4.
Assessment of the Target Engagement and D-Serine Biomarker Profiles of the D-Amino Acid Oxidase Inhibitors Sodium Benzoate and PGM030756.
Neurochem Res
; 42(11): 3279-3288, 2017 Nov.
Artículo
en Inglés
| MEDLINE | ID: mdl-28780732
5.
Structure-based optimization of 1H-imidazole-2-carboxamides as Axl kinase inhibitors utilizing a Mer mutant surrogate.
Bioorg Med Chem Lett
; 27(4): 1099-1104, 2017 02 15.
Artículo
en Inglés
| MEDLINE | ID: mdl-28082036
6.
Identification of a new class of potent Cdc7 inhibitors designed by putative pharmacophore model: Synthesis and biological evaluation of 2,3-dihydrothieno[3,2-d]pyrimidin-4(1H)-ones.
Bioorg Med Chem
; 25(7): 2133-2147, 2017 04 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-28284870
7.
Discovery of a Novel Series of Pyrazolo[1,5-a]pyrimidine-Based Phosphodiesterase 2A Inhibitors Structurally Different from N-((1S)-1-(3-Fluoro-4-(trifluoromethoxy)phenyl)-2-methoxyethyl)-7-methoxy-2-oxo-2,3-dihydropyrido[2,3-b]pyrazine-4(1H)-carboxamide (TAK-915), for the Treatment of Cognitive Disorders.
Chem Pharm Bull (Tokyo)
; 65(11): 1058-1077, 2017.
Artículo
en Inglés
| MEDLINE | ID: mdl-29093293
8.
Discovery of TAK-659 an orally available investigational inhibitor of Spleen Tyrosine Kinase (SYK).
Bioorg Med Chem Lett
; 26(24): 5947-5950, 2016 12 15.
Artículo
en Inglés
| MEDLINE | ID: mdl-27839918
9.
Fatigue crack propagation and fracture toughness of cortical bone are radiation dose-dependent.
J Orthop Res
; 41(4): 823-833, 2023 04.
Artículo
en Inglés
| MEDLINE | ID: mdl-35949192
10.
Discovery of a Novel, Highly Potent, and Selective Thieno[3,2-d]pyrimidinone-Based Cdc7 Inhibitor with a Quinuclidine Moiety (TAK-931) as an Orally Active Investigational Antitumor Agent.
J Med Chem
; 63(3): 1084-1104, 2020 02 13.
Artículo
en Inglés
| MEDLINE | ID: mdl-31895562
11.
Lead optimization and structure-based design of potent and bioavailable deoxycytidine kinase inhibitors.
Bioorg Med Chem Lett
; 19(23): 6784-7, 2009 Dec 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-19836232
12.
Design and Synthesis of Conformationally Constrained RORγt Inverse Agonists.
ChemMedChem
; 14(22): 1917-1932, 2019 11 20.
Artículo
en Inglés
| MEDLINE | ID: mdl-31659845
13.
Design, Synthesis, and Biological Evaluation of Retinoic Acid-Related Orphan Receptor γt (RORγt) Agonist Structure-Based Functionality Switching Approach from In House RORγt Inverse Agonist to RORγt Agonist.
J Med Chem
; 62(3): 1167-1179, 2019 02 14.
Artículo
en Inglés
| MEDLINE | ID: mdl-30652849
14.
Identification of Novel, Potent, and Orally Available GCN2 Inhibitors with Type I Half Binding Mode.
ACS Med Chem Lett
; 10(10): 1498-1503, 2019 Oct 10.
Artículo
en Inglés
| MEDLINE | ID: mdl-31620240
15.
Discovery of [ cis-3-({(5 R)-5-[(7-Fluoro-1,1-dimethyl-2,3-dihydro-1 H-inden-5-yl)carbamoyl]-2-methoxy-7,8-dihydro-1,6-naphthyridin-6(5 H)-yl}carbonyl)cyclobutyl]acetic Acid (TAK-828F) as a Potent, Selective, and Orally Available Novel Retinoic Acid Receptor-Related Orphan Receptor γt Inverse Agonist.
J Med Chem
; 61(7): 2973-2988, 2018 04 12.
Artículo
en Inglés
| MEDLINE | ID: mdl-29510038
16.
Discovery of Clinical Candidate N-((1S)-1-(3-Fluoro-4-(trifluoromethoxy)phenyl)-2-methoxyethyl)-7-methoxy-2-oxo-2,3-dihydropyrido[2,3-b]pyrazine-4(1H)-carboxamide (TAK-915): A Highly Potent, Selective, and Brain-Penetrating Phosphodiesterase 2A Inhibitor for the Treatment of Cognitive Disorders.
J Med Chem
; 60(18): 7677-7702, 2017 09 28.
Artículo
en Inglés
| MEDLINE | ID: mdl-28796496
17.
Design, Synthesis, and Evaluation of the Highly Selective and Potent G-Protein-Coupled Receptor Kinase 2 (GRK2) Inhibitor for the Potential Treatment of Heart Failure.
J Med Chem
; 60(16): 6942-6990, 2017 08 24.
Artículo
en Inglés
| MEDLINE | ID: mdl-28699740
18.
Protein crystallization for structure-based drug design.
Methods Mol Biol
; 841: 67-91, 2012.
Artículo
en Inglés
| MEDLINE | ID: mdl-22222449
19.
Mechanism of Inhibition of Novel Tryptophan Hydroxylase Inhibitors Revealed by Co-crystal Structures and Kinetic Analysis.
Curr Chem Genomics
; 4: 19-26, 2010 Apr 14.
Artículo
en Inglés
| MEDLINE | ID: mdl-20556201
20.
Structural basis for the inhibition of Aurora A kinase by a novel class of high affinity disubstituted pyrimidine inhibitors.
Bioorg Med Chem Lett
; 17(3): 688-91, 2007 Feb 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-17157005
Resultados
1 -
20
de 20
1
Próxima >
>>