More research is needed about 3,6-Dichloropyridazine

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A versatile access to pyridazines with tethered imidazolium groups-new precursors for mono- and binucleating NHC/pyridazine hybrid ligands

One or two imidazolium groups have been attached to the 3- and 6-positions of the pyridazine heterocycle, providing valuable precursors for mono- and binucleating NHC/pyridazine hybrid ligands. For N-methyl imidazole with specific backbone substituents an unexpected methyl group transfer is observed, which defines the scope of the synthetic procedure. H-Bonding patterns in the solid state are elucidated by X-ray crystallography for seven chloride or PF6- salts of the new compounds.

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Pyridazine | C4H4N1888 – PubChem

 

Discovery of 3,6-Dichloropyridazine

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Electric Literature of 141-30-0, A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 141-30-0, Name is 3,6-Dichloropyridazine, molecular formula is C4H2Cl2N2. In a Patent£¬once mentioned of 141-30-0

DIAZEPINE AND DIAZOCANE COMPOUNDS AS MC4 AGONISTS

The present invention relates to compounds of formula (I) wherein R1, R2, R3, R4, L and n are as defined in the specification. These compounds are useful as MC4 agonists

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Extracurricular laboratory:new discovery of 3,6-Dichloropyridazine

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OXIME DERIVATIVES

The present invention relates to novel oxime derivatives of the general formula (I), their tautomeric forms, their stereoisomers, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, methods for their preparation, use of these compounds in medicine and the intermediates involved in their preparation.

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Brief introduction of 3,6-Dichloropyridazine

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PYRIDINONES/PYRAZINONES, METHOD OF MAKING, AND METHOD OF USE THEREOF

Pyridone and pyrazinone compounds of Formula (I) including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed

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Top Picks: new discover of 3,6-Dichloropyridazine

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Electric Literature of 141-30-0, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.141-30-0, Name is 3,6-Dichloropyridazine, molecular formula is C4H2Cl2N2. In a Article£¬once mentioned of 141-30-0

Discovery of Small Molecule Splicing Modulators of Survival Motor Neuron-2 (SMN2) for the Treatment of Spinal Muscular Atrophy (SMA)

Spinal muscular atrophy (SMA), a rare neuromuscular disorder, is the leading genetic cause of death in infants and toddlers. SMA is caused by the deletion or a loss of function mutation of the survival motor neuron 1 (SMN1) gene. In humans, a second closely related gene SMN2 exists; however it codes for a less stable SMN protein. In recent years, significant progress has been made toward disease modifying treatments for SMA by modulating SMN2 pre-mRNA splicing. Herein, we describe the discovery of LMI070/branaplam, a small molecule that stabilizes the interaction between the spliceosome and SMN2 pre-mRNA. Branaplam (1) originated from a high-throughput phenotypic screening hit, pyridazine 2, and evolved via multiparameter lead optimization. In a severe mouse SMA model, branaplam treatment increased full-length SMN RNA and protein levels, and extended survival. Currently, branaplam is in clinical studies for SMA.

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New explortion of 3,6-Dichloropyridazine

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Cp*IrIII-Catalyzed [3+2] Annulations of N-Aryl-2-aminopyrimidines with Sulfoxonium Ylides to Access 2-Alkyl Indoles Through C?H Bond Activation

The iridium-catalyzed aromatic C?H alkylation followed by intramolecular annulation reactions between N-aryl-2-aminopyridines and sulfoxonium ylides for the synthesis of 2-alkyl indoles is described. This highly efficient and step-economical cyclization reaction displays excellent functional group compatibility and regioselectivity. Afterwards, the directing group in C?H alkylation can be readily removed to obtain the free N?H indoles. Thus, the sulfoxonium ylide, a carbene precursor, is proved as a useful surrogate of diazo compounds in C?H activation chemistry.

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Top Picks: new discover of 3,6-Dichloropyridazine

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Discovery of substituted 6-pheny-3H-pyridazin-3-one derivatives as novel c-Met kinase inhibitors

We report a series of phenyl substituted pyridazin-3-ones substituted with morpholino-pyrimidines. The SAR of the phenyl was explored and their c-Met kinase and cell-based inhibitory activity toward c-Met driven cell lines were evaluated. Described herein is a potent c-Met inhibitor by structural modification of the parent morpholino-pyridazinone scaffold, with particular focus on the phenyl and pyrimidine substituents.

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Pyridazine – Wikipedia,
Pyridazine | C4H4N1759 – PubChem

 

Discovery of 3,6-Dichloropyridazine

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Electric Literature of 141-30-0, Because a catalyst decreases the height of the energy barrier, its presence increases the reaction rates of both the forward and the reverse reactions by the same amount.141-30-0, Name is 3,6-Dichloropyridazine, molecular formula is C4H2Cl2N2. In a article£¬once mentioned of 141-30-0

Hydrogen bond directed synthesis of pyridazine and naphthyridine containing macrocycles

This work describes a high-yielding, one-step synthesis of pyrizadine and naphthyridine containing macrocycles directed by intramolecular H-bonding. The Royal Society of Chemistry 2005.

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Extended knowledge of 141-30-0

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Synthesis and identification of novel pyridazinylpyrazolone based diazo compounds as inhibitors of human islet amyloid polypeptide aggregation

We have carried out a docking inspired synthesis and screening of a library of diazenyl-derivatives of pyridazinylpyrazolone molecules for their ability to modulate the amyloidogenic self-assembly of human islet amyloid polypeptide (hIAPP). hIAPP is a 37-residue peptide which is involved in glycemic control along with insulin. Its extracellular fibrillar assemblies in pancreatic beta-cells are responsible for type 2 diabetes. A three-step synthetic scheme was used to prepare these novel compounds using 2-(6-chloropyridazin-3-yl)-5-methyl-2,4-dihydro-3H-pyrazol-3-one as a key intermediate that was reacted with various diazo electrophiles to generate a library of compounds with yields ranging from 64 to 85%. The effect of the compounds on hIAPP amyloid fibril formation was evaluated with a thioflavin T (ThT) fluorescence-based kinetic assay. Furthermore, TEM imaging was carried out to corroborate the interactions of the compounds with hIAPP and subsequent hIAPP inhibition at the different level of fibrillization. The CD spectroscopy showed that upon incubation with SSE15314 for 12 h, the percentage of alpha-helices was maintained to a level of hIAPP at 0 h. The current study presents identification and characterization of SSE15314 as the hit, which completely inhibited the fibril formation and can be further optimized into a lead compound.

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Discovery of 141-30-0

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Electronic and Photophysical Properties of ReI(CO)3Br Complexes Modulated by Pyrazolyl-Pyridazine Ligands

The direct reaction of a series of substituted (1H-pyrazol-1-yl)pyridazine (LI: 6-(1H-pyrazolyl)pyridazine; LII: 3-chloro-6-(1H-pyrazole-1-yl)-pyridazine; LIII: 6-(1H-3,5-dimethylpyrazolyl)pyridazine-3-carboxylic acid; LIV: 3,6-bis-N-pyrazolyl-pyridazine; and LV: 3,6-bis-N-3-methylpyrazolyl-pyridazine) with the bromotricarbonyl(tetrahydrofuran)-rhenium(I) dimer leads to the monometallic complexes [(LX)Re(CO)3Br] (I-V), which displays a nonregular octahedral geometry around the ReI center and a fac-isomerism for the carbonyl groups, whereas pyridazine and pyrazolyl rings remain highly coplanar after coordination to rhenium. Cyclic voltammetry shows one irreversible oxidation and one irreversible reduction for each compound as measured in N,N-dimethylformamide. Oxidation ranges from 0.94 V for III to 1.04 V for I and have been attributed to the ReI/ReII couple. In contrast, the reductions are ligand centered, ranging from -1.64 V for II to -1.90 V for III and V. Density functional theory calculations on the vertical one electron oxidized and one electron reduced species, using the gas-phase optimized geometry for the neutral complex confirm this assignment. Compounds I-V show two absorption bands, one around 410 nm (metal-to-ligand charge transfer (MLCT), Redpi ? pi?) and the other at ?300 nm (intraligand, pi ? pi?). Excitation at 400 nm at 77 K leads to unstructured and monoexponential emission with large Stokes shift, whose maxima vary between 570 (III) and 636 (II) nm. The quantum yields for these emissions in solution are intensified strongly going from air to argon equilibrated solution. Singlet oxygen quantum yields change from 0.03 (III) to 0.21 (IV). These data are consistent with emission from 3MLCT. The emission undergoes a bathochromic shift when R1 is a pi-donating group (Cl or N-pyrazolyl) and a hypsochromic shift for a pi-acceptor (COOH). The bimolecular emission quenching rate constant by triethylamine (TEA) for II, IV, and V is 1.09, 0.745, and 0.583 ¡Á 108 M-1 s-1, respectively. Photolysis in dichloromethane-CO2 saturated solution with TEA as a sacrificial electron donor leads in all cases to formic acid generation.

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Pyridazine – Wikipedia,
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