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NEW AZAQUINOLINE DERIVATIVES

The present invention covers azaquinoline compounds of general formula (I), with A being (A1) or (A2), and in which T, R1, R2, R3, R4, R5, R6, and Q are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment, control and/or prevention of diseases, in particular of helminth infections, as a sole agent or in combination with other active ingredients.

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Pyridazine – Wikipedia,
Pyridazine | C4H4N2448 – PubChem

 

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Antirhinoviral heteroamine-substituted pyridazines

Novel pyridazinamines having antirhinoviral activity, compositions containing these compounds as active ingredient, and a method of inhibiting combating or preventing the growth of viruses in warm-blooded animals suffering from diseases caused by these viruses.

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PYRIDAZINONE DERIVATIVES AS PHOSHOINOSITIDE 3-KINASES INHIBITORS

Compounds of formula (I) described herein inhibit phosphoinositide 3-kinases (PI3K) and useful for the treatment of disorders associated with PI3K enzymes.

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Pyridazine – Wikipedia,
Pyridazine | C4H4N3119 – PubChem

 

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Discovery of 1,2,3-triazole-based fibroblast growth factor receptor modulators

To avoid production of a phospholipidosis-inducing metabolite, we replaced the amide structure of SUN13837 (1) with a 1,2,3-triazole. The resulting 1,2,3-triazole analog of 1 (compound 2) displayed greater neuroprotective activity than 1. Structural modification of 2 yielded compound 10, which showed improved neuroprotective activity and negligible mechanism-based inactivation against CYP3A4. In addition, installation of a methyl group at the 5-position of 1,2,3-triazole of 10 significantly boosted the neuroprotective activity. These 1,2,3-triazole derivatives displayed reduced phospholipidosis risk, sufficient systemic exposure, and high central nervous system penetration, and therefore may be potentially useful agents for the treatment of neurodegenerative diseases.

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Pyridazine – Wikipedia,
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Studies on a series of milnacipran analogs containing a heteroaromatic group as potent norepinephrine and serotonin transporter inhibitors

A series of milnacipran analogs containing a heteroaromatic group were synthesized and studied as monoamine transporter inhibitors. Many compounds exhibited higher potency than milnacipran at NET and NET/SERT with no significant change in lipophilicity. For example, compound R-26f was about 10-fold more potent than milnacipran with IC50 values of 8.7 and 26 nM at NET and SERT, respectively.

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Pyridazine – Wikipedia,
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The important role of 6-Chloropyridazine-3-carboxylic acid

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Palladium-catalyzed C-2 selective arylation of quinolines

An efficient method for the Pd-catalyzed regioselective C-2 arylation of quinolines is presented. Reactions of various substituted quinolines and unactivated arenes have been conducted under mild conditions. The result shows good product yields of 2-arylquinolines, which are highly useful building blocks for the synthesis of bioactive alkaloid natural products and drug molecules.

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Synthesis of novel fused azecine ring systems through application of the tert-amino effect

Novel fused azecine ring systems were synthesized via the microwave-assisted thermal isomerization of terphenyl or biphenyl-pyridazine compounds possessing a vinyl and a tert-amino group, through application of a new extension of the tert-amino effect. Substrates for the ring closure were prepared from ortho-dihalobenzene or pyridazinone by consecutive Suzuki couplings with ortho-sec-amino- and formylphenylboronic acids, followed by Knoevenagel condensation of the aldehydes obtained.

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PYRIDAZINONE DERIVATIVE AND PDE INHIBITOR CONTAINING THE SAME AS ACTIVE INGREDIENT

It is to provide a novel pyridazinone derivative represented by the following general formula (1), which is useful as a pharmaceutical and has a phosphodiesterase inhibitory action: wherein R1 represents H or C1-6 alkyl, each of R2 and R3 represents H, X, C1-6 alkoxy, Z represents O or S, and A represents AA or BB, wherein AA represents: and BB represents: wherein R4 represents H or C1-6 alkyl, and each of R5 and R6 represents C1-6 alkyl.

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Pyridazine | C4H4N1400 – PubChem

 

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METHODS FOR TREATING HCV

This invention relates to combinations of therapeutic molecules useful for treating hepatitis C virus infection. The present invention relates to methods, uses, dosing regimens, and compositions.

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New pyridazine-bridged NHC/pyrazole ligands and their sequential silver(I) coordination

A family of new pyridazine-bridged NHC/pyrazole ligand precursors HL 1-5 were prepared and fully characterized including analysis by XRD {HL1 = 3-[3-(2,6-diisopropylphenyl)-3H-imidazolium-1-yl]-6-(3- pyridin-2-yl-pyrazol-1-yl)-pyridazine, HL2 = 3-[3-(2,4,6- trimethylphenyl)-3H-imidazolium-1-yl]-6-(3-pyridin-2-yl-pyrazol-1-yl) -pyridazine, HL3 = 3-[3-(2,4,6-trimethylphenyl)-3H-imidazolium-1-yl]- 6-(3,5-dimethylpyrazol-1-yl)-pyridazine, HL4 = 3-(3-tert-butyl-3H- imidazolium-1-yl)-6-(3,5-dimethylpyrazol-1-yl)-pyridazine, HL5 = 3-[3-(2,4,6-trimethylphenyl)-3H-imidazolium-1-yl]-6-(3-methyl-5-phenylpyrazol-1- yl)-pyridazine, X = PF6- or BF4-}. Reaction of the ligand precursors with Ag2O yielded various silver(I) complexes whose structures have been elucidated crystallographically. In complexes [(L3)2Ag](PF6) (4) and[(L 4)2Ag](PF6) (4?) the single silver(I) ion is coordinated in a linear fashion by the NHC moieties of the two ligand strands. An NMR titration with AgBF4 reveals that 4 can bind two more silver(I) ions. The complex [(L5)2Ag2](PF 6)2 (5?) features an additional silver(I) centre bound to the two pyrazole rings, whereas in [(L3)2Ag 2](BF4)2 (6) ligand reshuffling has occurred to give antiparallel ligand strands with {CNHCNpyrazole} coordination of each metal ion. Secondary interactions with the pyridazine N-atom are observed in some cases. An additional third silver(I) ion can be accommodated between the central pyridazine bridges, as shown in [(L 3)2Ag3](PF6)2(BF 4) (7). The sequence of binding events and the identity of the species in solution have been investigated by NMR spectroscopy and ESI mass spectrometry. A family of new pyridazine-bridged ditopic ligands has been prepared, which provide both an organometallic NHC and a classic N-donor compartment. Two opposing strands of these ligands sequentially bind up to three silver(I) ions. Complexation starts at the NHC subunit and involves some ligand reshuffling to form a trisilver arrangement, which has been elucidated by NMR spectroscopy and X-ray crystallography. Copyright

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