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The invention provides a novel inhibitor compound represented by general formula (I), and the compound has good kinase inhibitory activity. The compounds of the present invention are useful in the prevention and/or treatment of diseases mediated by TAM family kinase receptors and/or their ligand abnormal expression. In addition, the compounds of the present invention may also target CSFSFSF1 kinase, useful in preventing and/or treating diseases mediated by TAM family kinase receptors/and CSFSFSF1R kinase receptors and/or their ligand abnormal expression. (by machine translation)

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N1559 – PubChem

 

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The synthesis of a series of push-pull derivatives bearing triphenylamine electron-donating group, cyclopenta[c]thiophen-4,6-dione electron acceptor and various pi-linkers including (hetero)aromatic fragments is reported. All target chromophores with systematically varied pi-linker structure were further investigated by electrochemistry, absorption measurements, and EFISH experiments in conjunction with DFT calculations. Based on electrochemical and photophysical measurements, when a polarizable 2,5-thienylene moiety is embedded into the chromophore pi-backbone the highest intramolecular charge transfer (ICT) is observed. Benzene, pyrimidine, and pyridazine derivatives exhibit lower polarizability and extent of the ICT across these pi-linkers. The elongation of the pi-conjugated system via additional ethenylene linker results in a significant reduction of the HOMO-LUMO gap and an enhancement of the NLO response. Whereas it does not significantly influence electrochemical and linear optical properties, the orientation of the pyrimidine ring seems to be a key parameter on the mubeta value due to significant variation of the dipolar moment (mu) value. In 2a and 2c, pyrimidine is oriented to behave as an acceptor and thus generate dipolar molecule with mu above 5 D, whereas in 2b and 2d ground state dipole moment is significantly reduced. This study seems to indicate a high aromaticity of pyrimidine and pyridazine derivatives, close to the benzene analogues and significantly higher than thiophene analogues.

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An efficient synthesis of a series of 6-chloro-3-substituted-[1,2,4]triazolo[4,3-b]pyridazines is described via intramolecular oxidative cyclization of various 6-chloropyridazin-3-yl hydrazones with iodobenzene diacetate. The structures of the newly synthesized compounds were assigned on the basis of elemental analysis, IR, NMR (1H and 13C) and mass spectral data. All the thirty three compounds 3a-q and 4b-q synthesized in the present study were evaluated for their in vitro cytotoxic activities against two Acute Lymphoblastic Leukemia (ALL) cell lines named, SB-ALL and NALM-6, and a human breast adenocarcinoma cell lines (MCF-7). The results revealed that triazoles 4 exhibit better cytotoxicity than their hydrazone precursors 3. Among triazoles, compounds 4f, 4j and 4q exhibited potent cytotoxic activity against SB-ALL and NALM-6 with IC50 values in the range of ?1.64?5.66 muM and ?1.14?3.7 muM, respectively, compared with doxorubicin (IC50 = 0.167 muM, SB-ALL). Compounds 4f, 4j and 4q were subjected to apoptosis assay after 48 h treatment and these compounds induced apoptosis of NALM-6 cells via caspase 3/7 activation. Results revealed that compound 4q represents potential promising lead.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N1806 – PubChem

 

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A new hexadentate ligand 3,6-bis[(6-methyl-2-pyridyl)(2-pyridyl)methyl]pyridazine (mbdpdz) was prepared by a condensation reaction of 3,6-dichloropyridazine and (6-methyl-2-pyridyl)(2-pyridyl)methyllithium, and the following binuclear copper(II) complexes were obtained: [Cu2(mbdpdz)Cl4] 1, [Cu2(mbdpdz)Br4] 2, [Cu2(mbdpdz)-Cl2(OH)]Cl 3 and [Cu2(mbdpdz)Br2(OH)]Br 4. The crystal and molecular structures of the two isomorphous complexes 3 and 4 are reported. Both complexes crystallize in the monoclinic system, space group C2/c, with eight formula units per unit cell. Complex 3: a = 28.364(3), b = 13.511(1), c = 16.858(1) A, beta = 109.70(1). Complex 4: a = 28.528(5), b = 13.459(2), c = 17.348(3) A, beta = 109.35(1). The copper centres in the binuclear cation in 3 and 4 have a square-pyramidal geometry, with a bridging hydroxide angle of 115.1(3) and 116.2(5) respectively. The Cu…Cu distance was 3.251(2) A in both binuclear complexes. These hydroxo-bridged complexes were obtained by refluxing acetonitrile-water suspensions of 1 and 2, respectively. Variable-temperature magnetic studies on all complexes indicate the existence of antiferromagnetic exchange phenomena. Extended-Hueckel calculations were performed on complexes 3 and 4 in order to identify the electronic origin of the spin coupling of these molecules.

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1,2,4-triazolo[4,3-b]pyridazine derivatives, represented by wherein Z represents cyclobutyl or pyrrolidin-1-yl, are selective ligands for GABA A receptors, in particular having high affinity for the alpha2 and/or alpha3 subunit thereof, are useful in the treatment of anxiety and convulsions.

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Pyridazine – Wikipedia,
Pyridazine | C4H4N1541 – PubChem

 

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The invention relates to isoxazolo-pyridazine compounds, in particular those of formula I as described above and to a pharmaceutically acceptable salts thereof, having affinity and selectivity for the GABA A alpha5 receptor binding site, their manufacture, pharmaceutical compositions containing them and their use as cognitive enhancers or for the treatment of cognitive disorders like Alzheimer”s disease.

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Pyridazine – Wikipedia,
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It is shown by means of the fixed-structure method, UV spectroscopy and dipole-moment method that the product of the reaction of 3,6-dichloropyridazine with hydrazine in solution in methanol and acetonitrile has the 3-chloro-6-hydrazinopyridazine structure.

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A variety of double-armed diaza-crown ethers were first prepared through high pressure SNAr reaction, in which unique aromatic heterocycles were successfully attached as secondary binding sites.Direct introduction of aromatic heterocycles such as pyridazine, oxazole, and thiazole rings upon nitrogen atom of the diaza-18-crown-6 provided remarkably high binding and transport selectivity for Ag+ ion.

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The invention discloses a method for preparing azintamide method, comprises the steps of preparing […] compound solution, then the reaction preparation azintamide, after the azintamide purification, characterized in that in the preparation of […] compound in the solution process, the water and sodium sulfide are mixed and dissolved; dissolved by adding sulfur; addition of 3, 6 – reflect two chlorine clip clop qin of sodium sulfite is added into the system, to prevent oxidation; pour the reaction preparation azintamide in sodium sulfite, prevent oxidation; drip […] alcohol and N, N – diethyl – 2 – chloroacetamide mixed solution, while monitoring the pH value is 8 – 10 within the scope of the; then the azintamide purification. The preparation of the invention azintamide method step is simple, environmental protection, high yield, low cost, and is suitable for mass production. (by machine translation)

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The present invention relates to difluoromethyl-phenyl triazoles of general formula (I) which are modulators of GABAA receptors containing the alpha5 subunit, useful in treating central nervous system diseases and other diseases. In addition, the invention relates to processes for preparing pharmaceutical compositions as well as processes for manufacture the compounds according to the invention.

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Reference:
Pyridazine – Wikipedia,
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