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The present invention relates to compounds of formula I, wherein A, R1 to R7 are defined in the description, and to pharmaceutically acceptable salts thereof. The present invention also relates to the manufacture of such compounds or their pharmaceutically acceptable salts, pharmaceutical compositions containing them and their use as medicaments for the treatment and/or prophylaxis of diseases which can be treated with HDL-cholesterol raising agents, such as dyslipidemia, atherosclerosis and cardiovascular diseases.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N464 – PubChem

 

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NOVEL 2-HETEROARYL-SUBSTITUTED BENZIMIDAZOLE DERIVATIVE

A glucokinase activator is provided; and a remedy and/or a preventive for diabetes, or a remedy and/or a preventive for diabetes such as retinopathy, nephropathy, neurosis, ischemic cardiopathy, arteriosclerosis, and further a remedy and/or a preventive for obesity are provided. A glucokinase activator characterized by containing a 2-heteroaryl-substituted benzimidazole derivative of a general formula (I-0) or its pharmaceutically-acceptable salt: [in the formula, X represents a carbon atom or a nitrogen atom; X1, X2, X3 and X4 each independently represent a carbon atom or a nitrogen atom; the ring A represents a 5- or 6-membered nitrogen-containing aromatic hetero ring of a formula (II): (in the formula, X represents a carbon atom or a nitrogen atom); R1 represents an aryl, etc.; R2 represents a hydroxy, etc.; R3 represents a -C1-6 alkyl, etc.; R4 represents a -C1-6 alkyl, etc.; X5 represents -O-, etc.; a indicates an integer of 1, 2 or 3; q indicates an integer of from 0 to 2; m indicates an integer of from 0 to 2].

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N469 – PubChem

 

The important role of Pyridazine-3-carboxylic acid

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Development of fluorescent probes specific for parallel-stranded G-quadruplexes by a library approach

A 241-membered cyanine-based library was constructed by the combinatorial chemistry strategy. Combined with high-throughput screening, we successfully discovered a novel fluorescent probe (CyC-M716) capable of identifying a subset of parallel G-quadruplexes with propeller loops stretching across three tetrad layers with high sensitivity and selectivity.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N504 – PubChem

 

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Non-Porous Iron(II)-Based Sensor: Crystallographic Insights into a Cycle of Colorful Guest-Induced Topotactic Transformations

Materials capable of sensing volatile guests at room temperature by an easily monitored set of outputs are of great appeal for development as chemical sensors of small volatile organics and toxic gases. Herein the dinuclear iron(II) complex, [FeII2(L)2(CH3CN)4](BF4)4?2 CH3CN (1) [L=4-(4-methylphenyl)-3-(3-pyridazinyl)-5-pyridyl-4H-1,2,4-triazole], is shown to undergo reversible single-crystal-to-single-crystal (SCSC) transformations upon exposure to vapors of different guests: 1 (MeCN)?2 (EtOH)?3 (H2O)?1 (MeCN). Whilst 1 and 2 remain dimetallic, SCSC to 3 involves conversion to a 1D polymeric chain (due to a change in L bridging mode), which, remarkably, can undergo SCSC de-polymerization, reforming dimetallic 1. Additionally, SC-XRD studies of two ordered transient forms, 1TF3 and 2TF3, confirm that guest exchange occurs by diffusion of the new guests into the non-porous lattices as the old guests leave. These reversible SCSC events also induce color and magnetic responses. Indeed dark red 1 is spin crossover active (T1/2? 356 K; T1/2? 369 K), whilst orange 2 and yellow 3 remain high spin.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N495 – PubChem

 

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Reactions of ionised pyridazine, aminopyrazine and aminopyridine and their isomeric alpha-distonic ions

The reactions of ionised pyridazine, aminopyrazine and aminopyridine and the corresponding alpha-distonic ions are examined by a combination of tandem mass spectrometric techniques, including analysis of metastable ion (MI), collision induced dissociation and neutralisation-reionisation mass spectra (NRMS). Further insight into the relative stability and energy barriers towards tautomerism of each ionised heterocycle with its alpha-distonic isomer is obtained by computational methods. In all these systems, both the conventional radical-cation and the alpha-distonic tautomer are stable species which exist in discrete energy wells, with a significant barrier towards their interconversion. Although each alpha-distonic ion is sufficiently stable to survive neutralisation-reionisation, the conventional ionised heterocycle is more stable in each case. The possibility of investigating proton-transport catalysis in the tautomerism of these ionic systems is discussed.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N484 – PubChem

 

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Synthesis and biological activity of pyridopyridazine derivatives: A mini review

This review presents most of the literature data about synthesis and biological activity of pyridopyridazine derivatives. There are six structural isomers of the bicyclic ring system containing pyridine moiety condensed with pyridazine nucleus. Pyridopyridazine derivatives show antitumor, antibacterial, analgesic and diuretics activities. The derivatives have been identified as the selective phosphodiesterase 5 and phosphodiesterase 4 inhibitors. Pyridopyridazines are novel class of GABA-A receptor benzodiazepine binding site ligands. Some of pyrido[3,2-c]pyridazine derivatives possess molluscicidal activity and can be used as biodegradable agrochemicals. The broad spectrum of biological activity of pyridopyridazine derivatives is the main reason for the preparation of new compounds containing this scaffold.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N503 – PubChem

 

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2164-61-6, Name is Pyridazine-3-carboxylic acid, belongs to pyridazine compound, is a common compound. Recommanded Product: 2164-61-6In an article, once mentioned the new application about 2164-61-6.

1,2,4-Triazolyl octahydropyrrolo[2,3-b]pyrroles: A new series of potent and selective dopamine D3 receptor antagonists

A novel series of 1,2,4-triazolyl octahydropyrrolo[2,3-b]pyrroles showing high affinity and selectivity at the DA D3 receptor is reported here. Compounds endowed with high selectivity over the hERG channel were identified and their pharmacokinetic properties thoroughly analyzed. A few derivatives with appropriate developability characteristics were selected for further studies and progression along the screening cascade. In particular, derivative 60a, (DA D3 pKi = 8.4, DA D2 pKi = 6.0 and hERG fpKi = 5.2) showed a balanced profile and further refinements are in progress around this molecule.

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Reference£º
Pyridazine – Wikipedia,
Pyridazine | C4H4N491 – PubChem

 

Properties and Exciting Facts About Pyridazine-3-carboxylic acid

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Purification and Some Properties of Nicotinate Phosphoribosyltransferase from Hog Liver

Purification of nicotinate phosphoribosyltransferase (NPRTase, EC 2.4.2.11) from hog liver and some of its properties were investigated.Purified enzyme was found to be homogeneous by the criterion of polyacrylamide gel disc electrophoresis and to have a molecular weight of about 120,000.The subunit molecular weight was found to be 64,000, using SDS polyacrylamide gel disc electrophoresis.The optimum pH and isoelectric point of the enzyme were 7.3-7.4 and 4.8, respectively.Mn(2+), Co(2+), and Mg(2+) were effective in meeting the NPRTase requirement for a divalent cation.ATP had a stimulative effect on the enzyme activity in the presence of Mg(2+), on the other hand, in the presence of Mn(2+), ATP had an inhibitory effect on the enzyme activity.Of the purine nucleotides examined, only ATP stimulated NPRTase activity, and GTP did not.On the contrary, all other nucleotides inhibited the activity.Nicotinate mononucleotide, which is a reaction product, inhibited NPRTase activity.Among the nicotinic acid analogues tested, only pyrazine-2-carboxylic acid inhibited the activity.Nicotinamide, quinolinic acid, adenine, and hypoxanthine were not phosphoribosylated by NPRTase.Incubation of NPRTase with SH-modifying reagents caused loss of NPRTase activity.

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Reference£º
Pyridazine – Wikipedia,
Pyridazine | C4H4N482 – PubChem

 

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Synthetic Route of 2164-61-6, Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In some cases, the catalyzed mechanism may include additional steps.In a article, 2164-61-6, molcular formula is C5H4N2O2, introducing its new discovery.

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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Reference£º
Pyridazine – Wikipedia,
Pyridazine | C4H4N496 – PubChem

 

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Design, synthesis and antibacterial properties of pyrimido[4,5-b]indol-8-amine inhibitors of DNA gyrase

According to the World Health Organization (WHO), approximately 1.7 million deaths per year are caused by tuberculosis infections. Furthermore, it has been predicted that, by 2050, antibacterial resistance will be the cause of approximately 10 million deaths annually if the issue is not tackled. As a result, novel approaches to treating broad-spectrum bacterial infections are of vital importance. During the course of our wider efforts to discover unique methods of targeting multidrug-resistant (MDR) pathogens, we identified a novel series of amide-linked pyrimido[4,5-b]indol-8-amine inhibitors of bacterial type II topoisomerases. Compounds from the series were highly potent against gram-positive bacteria and mycobacteria, with excellent potency being retained against a panel of relevant Mycobacterium tuberculosis drug-resistant clinical isolates.

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Reference£º
Pyridazine – Wikipedia,
Pyridazine | C4H4N489 – PubChem