Category: 624734-19-6

Crowley, Brendan M. published the artcileNovel oxazolidinone calcitonin gene-related peptide (CGRP) receptor antagonists for the acute treatment of migraine, Related Products of tetrahydropyran, the publication is Bioorganic & Medicinal Chemistry Letters (2015), 25(21), 4777-4781, database is CAplus and MEDLINE.

In the authors’ efforts to develop CGRP receptor antagonists as backups to MK-3207, the authors employed a scaffold hopping approach to identify a series of novel oxazolidinone-based compounds The development of a structurally diverse, potent ((I), cAMP + HS IC₅₀ = 0.67 nM), and selective compound (hERG IC₅₀ = 19 μM) with favorable rodent pharmacokinetics (F = 100%, t_1/2 = 7 h) is described. Key to this development was identification of a 3-substituted spirotetrahydropyran ring that afforded a substantial gain in potency (10 to 35-fold).

Bioorganic & Medicinal Chemistry Letters published new progress about 624734-19-6. 624734-19-6 belongs to tetrahydropyran, auxiliary class Tetrahydropyran,Fluoride,Ketone, name is 3-Fluorodihydro-2H-pyran-4(3H)-one, and the molecular formula is C5H7FO2, Related Products of tetrahydropyran.

Referemce:
https://en.wikipedia.org/wiki/Tetrahydropyran,
Tetrahydropyran – an overview | ScienceDirect Topics

Ramurthy, Savithri published the artcileDesign and Discovery of N-(3-(2-(2-Hydroxyethoxy)-6-morpholinopyridin-4-yl)-4-methylphenyl)-2-(trifluoromethyl)isonicotinamide, a Selective, Efficacious, and Well-Tolerated RAF Inhibitor Targeting RAS Mutant Cancers: The Path to the Clinic, SDS of cas: 624734-19-6, the publication is Journal of Medicinal Chemistry (2020), 63(5), 2013-2027, database is CAplus and MEDLINE.

Direct pharmacol. inhibition of RAS has remained elusive, and efforts to target CRAF have been challenging due to the complex nature of RAF signaling, downstream of activated RAS, and the poor overall kinase selectivity of putative RAF inhibitors. Herein, we describe 15, a selective B/C RAF inhibitor, which was developed by focusing on drug-like properties and selectivity. Our previous tool compound, 3, was potent, selective, efficacious, and well tolerated in preclin. models, but the high human intrinsic clearance precluded further development and prompted further investigation of close analogs. A structure-based approach led to a pyridine series with an alc. side chain that could interact with the DFG loop and significantly improved cell potency. Further mitigation of human intrinsic clearance and time-dependent inhibition led to the discovery of 15. Due to its excellent properties, it was progressed through toxicol. studies and is being tested in phase 1 clin. trials.

Journal of Medicinal Chemistry published new progress about 624734-19-6. 624734-19-6 belongs to tetrahydropyran, auxiliary class Tetrahydropyran,Fluoride,Ketone, name is 3-Fluorodihydro-2H-pyran-4(3H)-one, and the molecular formula is C5H7FO2, SDS of cas: 624734-19-6.

Referemce:
https://en.wikipedia.org/wiki/Tetrahydropyran,
Tetrahydropyran – an overview | ScienceDirect Topics

Martins, Francisco A. published the artcileConformational impact of structural modifications in 2-fluorocyclohexanone, Related Products of tetrahydropyran, the publication is Beilstein Journal of Organic Chemistry (2017), 1781-1787, database is CAplus and MEDLINE.

2-Haloketones are building blocks that combine phys., chem. and biol. features of materials and bioactive compounds, while organic fluorine plays a fundamental role in the design of performance organic mols. Since these features are dependent on the three-dimensional chem. structure of a mol., simple structural modifications can affect its conformational stability and, consequently, the corresponding physicochem./biol. property of interest. In this work, structural changes in 2-fluorocyclohexanone were theor. studied with the aim at finding intramol. interactions that induce the conformational equilibrium towards the axial or equatorial conformer. The interactions evaluated were hydrogen bonding, hyperconjugation, electrostatic and steric effects. While the gauche effect, originated from hyperconjugative interactions, does not appear to cause some preferences for the axial conformation of organofluorine heterocycles, more classical effects indeed rule the conformational equilibrium of the compounds Spectroscopic parameters (NMR chem. shifts and coupling constants), which can be useful to determine the stereochem. and the interactions operating in the series of 2-fluorocyclohexanone derivatives, were also calculated

Beilstein Journal of Organic Chemistry published new progress about 624734-19-6. 624734-19-6 belongs to tetrahydropyran, auxiliary class Tetrahydropyran,Fluoride,Ketone, name is 3-Fluorodihydro-2H-pyran-4(3H)-one, and the molecular formula is C5H7FO2, Related Products of tetrahydropyran.

Referemce:
https://en.wikipedia.org/wiki/Tetrahydropyran,
Tetrahydropyran – an overview | ScienceDirect Topics