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1.
Preclinical Efficacy and Anti-Inflammatory Mechanisms of Action of the Bruton Tyrosine Kinase Inhibitor Rilzabrutinib for Immune-Mediated Disease.
J Immunol;
206(7): 1454-1468, 2021 04 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-33674445
2.
Co-inhibition of immunoproteasome subunits LMP2 and LMP7 is required to block autoimmunity.
EMBO Rep;
19(12)2018 12.
Artículo
en Inglés
| MEDLINE | ID: mdl-30279279
3.
Prolonged and tunable residence time using reversible covalent kinase inhibitors.
Nat Chem Biol;
11(7): 525-31, 2015 Jul.
Artículo
en Inglés
| MEDLINE | ID: mdl-26006010
4.
Mitigation of reactive metabolite formation for a series of 3-amino-2-pyridone inhibitors of Bruton's tyrosine kinase (BTK).
Bioorg Med Chem Lett;
27(3): 632-635, 2017 02 01.
Artículo
en Inglés
| MEDLINE | ID: mdl-28025004
5.
A Small Molecule Inhibitor of ITK and RLK Impairs Th1 Differentiation and Prevents Colitis Disease Progression.
J Immunol;
195(10): 4822-31, 2015 Nov 15.
Artículo
en Inglés
| MEDLINE | ID: mdl-26466958
6.
Targeting interleukin-2-inducible T-cell kinase (ITK) and resting lymphocyte kinase (RLK) using a novel covalent inhibitor PRN694.
J Biol Chem;
290(10): 5960-78, 2015 Mar 06.
Artículo
en Inglés
| MEDLINE | ID: mdl-25593320
7.
Finding the perfect spot for fluorine: improving potency up to 40-fold during a rational fluorine scan of a Bruton's Tyrosine Kinase (BTK) inhibitor scaffold.
Bioorg Med Chem Lett;
25(2): 367-71, 2015 Jan 15.
Artículo
en Inglés
| MEDLINE | ID: mdl-25466710
8.
RN486, a selective Bruton's tyrosine kinase inhibitor, abrogates immune hypersensitivity responses and arthritis in rodents.
J Pharmacol Exp Ther;
341(1): 90-103, 2012 Apr.
Artículo
en Inglés
| MEDLINE | ID: mdl-22228807
9.
Phase 1 clinical trial evaluating safety, exposure and pharmacodynamics of BTK inhibitor tolebrutinib (PRN2246, SAR442168).
Clin Transl Sci;
15(2): 442-450, 2022 02.
Artículo
en Inglés
| MEDLINE | ID: mdl-34724345
10.
Discovery of Reversible Covalent Bruton's Tyrosine Kinase Inhibitors PRN473 and PRN1008 (Rilzabrutinib).
J Med Chem;
65(7): 5300-5316, 2022 04 14.
Artículo
en Inglés
| MEDLINE | ID: mdl-35302767
11.
Discovery of the Irreversible Covalent FGFR Inhibitor 8-(3-(4-Acryloylpiperazin-1-yl)propyl)-6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-(methylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (PRN1371) for the Treatment of Solid Tumors.
J Med Chem;
60(15): 6516-6527, 2017 08 10.
Artículo
en Inglés
| MEDLINE | ID: mdl-28665128
12.
The Irreversible Covalent Fibroblast Growth Factor Receptor Inhibitor PRN1371 Exhibits Sustained Inhibition of FGFR after Drug Clearance.
Mol Cancer Ther;
16(12): 2668-2676, 2017 Dec.
Artículo
en Inglés
| MEDLINE | ID: mdl-28978721
13.
Structure-based drug design of RN486, a potent and selective Bruton's tyrosine kinase (BTK) inhibitor, for the treatment of rheumatoid arthritis.
J Med Chem;
58(1): 512-6, 2015 Jan 08.
Artículo
en Inglés
| MEDLINE | ID: mdl-24712864
14.
Pyrrolopyrazines as selective spleen tyrosine kinase inhibitors.
J Med Chem;
56(4): 1677-92, 2013 Feb 28.
Artículo
en Inglés
| MEDLINE | ID: mdl-23350847
15.
Bruton's tyrosine kinase inhibitors: approaches to potent and selective inhibition, preclinical and clinical evaluation for inflammatory diseases and B cell malignancies.
J Med Chem;
55(10): 4539-50, 2012 May 24.
Artículo
en Inglés
| MEDLINE | ID: mdl-22394077
16.
The preparation and utility of bis(sulfinyl)imidoamidine ligands for the copper-catalyzed Diels-Alder reaction.
J Org Chem;
68(1): 3-10, 2003 Jan 10.
Artículo
en Inglés
| MEDLINE | ID: mdl-12515453
17.
N-tert-butanesulfinyl imines: versatile intermediates for the asymmetric synthesis of amines.
Acc Chem Res;
35(11): 984-95, 2002 Nov.
Artículo
en Inglés
| MEDLINE | ID: mdl-12437323
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