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Irradiation through a Vycor filter of 3,4-diazabicyclo<2.4.0>oct-4-en-2-ones (3) obtained by photoaddition of 3(2H)-pyridazinones (1) and olefin resulted in isomerization to give 2,3-diazatricyclo<3.3.0.02,8>octa-4-ones (4).

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N326 – PubChem

 

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The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of TYK2, and the treatment of TYK2-mediated disorders.

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Pyridazine – Wikipedia,
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In this work, we are interested in studying the effect of the addition of a heterocyclic organic compound derived from pyridazine named ethyl (6-methyl-3-oxopyridazin-2-yl) acetate (GK2) on inhibition of the corrosion of mild steel (C38) in a molar hydrochloric acid solution. This study was performed using the method of weight loss, potentiodynamic polarization and the electrochemical impedance spectroscopy (EIS). Gravimetric measurements indicate that the inhibitor has GK2 efficiency increases with the concentration to reach a maximum value of 83.1% at 10?3 M. In addition, studies revealed that the potentiodynamic polarization act as a mixed inhibitor with predominance at cathodic domain. EIS shows that increasing the concentration of the inhibitor leads to an increase of the charge transfer resistance and reducing the double layer capacitance. Effect of temperature was studied between 308 and 343 K and determination of adsorption and activation parameters is also discussed.

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Reference:
Pyridazine – Wikipedia,
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A number of pyridazinone derivatives bearing an arylpiperazinylalkyl chain were synthesized and tested icv in a model of acute nociception induced by thermal stimuli in mice (tail flick). The most interesting and potent compound in this series was 6a, which showed an ED50=3.5 mug, a value about 3-fold higher with respect to morphine by the same route of administration. When administered per os, 6a was 4-fold more potent than morphine in the same test, suggesting a significant bioavailability. The same compound also showed high potency in the hot plate test. The antinociceptive effect of 6a was completely reversed by pretreatment with yohimbine both in the hot plate test and in the tail flick test. This demonstrated the involvement of the adrenergic system, which was confirmed by in vitro radioligand binding studies.

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Reference:
Pyridazine – Wikipedia,
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The present invention provides an integrase inhibitor. The inventors have have found the following compound of formula (I) possessing an integrase inhibitory activity. (wherein, R C and R D taken together with the neighboring carbon atoms form a ring which may be a condensed ring, Y is hydroxy, mercapto or amino; Z is O, S or NH ; R A is a group shown by (wherein, C ring is N-containing aromatic heterocycle) or the like)

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Pyridazine – Wikipedia,
Pyridazine | C4H4N285 – PubChem

 

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Rainbow trout bone proteins were prepared by heating at 121C for 30 min, followed by filtration, concentration, and lyophilization. Nutritional properties and flavor analyses of hydrolysates digested by five different enzymes were investigated, respectively. Results showed that the crude protein content of rainbow trout bone was 15.90% and had a well-balanced nutritional value. The content of total amino acids was 983.64 mg/g. The amount of free amino acids of hydrolysates digested by alkaline protease, neutral protease, flavourzyme, papain, and trypsin for 3 hr was 207.83, 224.13, 1,001.59, 283.26, and 303.64 mg/g, respectively. During the hydrolysis, the main flavor compounds were identified by GC-MS to be alcohols, aldehydes, ketones, acids, and alkanes. After hydrolysis, the main molecular weight of peptides was focused on the range of 1,000?3,000 Da in all enzymatic hydrolysates. This study provided a theoretical basis to comprehensive utilization of rainbow trout bone in food industry.

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Following a ligand-based drug design approach, a potent mixed formyl peptide receptor 1 (FPR1) and formyl peptide receptor-like 1 (FPRL1) agonist (14a) and a potent and specific FPRL1 agonist (14x) were identified. These compounds belong to a large series of pyridazin-3(2H)-one derivatives substituted with a methyl group at position 6 and a methoxy benzyl at position 4. At position 2, an acetamide side chain is essential for activity. Likewise, the presence of lipophilic and/or electronegative substituents in the position para to the aryl group at the end of the chain plays a critical role for activity. Affinity forFPR1 receptors was evaluated by measuring intracellular calcium flux in HL-60 cells transfected with FPR1, FPRL1, and FPRL2. Agonists were able to activate intracellular calcium mobilization and chemotaxis in human neutrophils. Themost potent chemotactic agent (EC50 =0.6 muM) was the mixed FPR/FPRL1 agonist 14h.

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Pyridazine – Wikipedia,
Pyridazine | C4H4N302 – PubChem

 

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Treatment of the monohydrazones of alpha-dicarbonyl compounds with Meldrum’s acid gives the condensation products (13)-(19) under standard conditions.Reaction of pyruvaldehyde 2-phenylhydrazone or 2-t-butylhydrazone with Meldrum’s acid at 80 deg C gives the corresponding 2-substituted-2,3-dihydro-6-methyl-3-oxo-pyridazine-4-carboxylic acids (29) and (30).Cyclisation of the other N-monosubstituted condensation products (13), (14), (16), (18), and (19) to 3-oxopyridazine-4-carboxylic acids (31)-(35) can be effected under basic conditions.Gas-phase pyrolysis of the N-aryl derivatives (13)-(16) at 550 deg C and 10E-2 Torr gives N-arylpyridazin-3-ones (38)-(41) while the N-t-butyl derivatives (18) and (19) at 750 deg C and 10E-2 Torr give N-unsubstituted pyridazin-3-ones (44) and (45) by additional loss of 2-methylpropene. 2-t-Butylpyridazin-3-ones (42) and (43) can be isolated from the same precursors under milder conditions (500 deg C and 10E-2 Torr).Pyrolysis of the N,N-dimethyl derivative (17) gave only polymeric material.

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Pyridazine – Wikipedia,
Pyridazine | C4H4N318 – PubChem

 

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The present invention relates to Bicyclic Heterocycle Derivatives, compositions comprising a Bicyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of GPR119 in a patient.

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Pyridazine – Wikipedia,
Pyridazine | C4H4N295 – PubChem

 

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Formyl peptide receptors (FPRs) play an essential role in the regulation of endogenous inflammation and immunity. In the present studies, a large series of pyridazin-3(2H)-one derivatives bearing an arylacetamide chain at position 2 was synthesized and tested for FPR agonist activity. The pyridazin-3(2H)-one ring was confirmed to be an appropriate scaffold to support FPR agonist activity, and its modification at the 4 and 6 positions led to the identification of additional active agonists, which induced intracellular Ca2+ flux in HL-60 cells transfected with either FPR1, FPR2, or FPR3. Seven formyl peptide receptor 1 (FPR1)-specific and several mixed FPR1/FPR2 dual agonists were identified with low micromolar EC50 values. Furthermore, these agonists also activated human neutrophils, inducing intracellular Ca2+ flux and chemotaxis. Finally, molecular docking studies indicated that the most potent pyridazin-3(2H)-ones overlapped in their best docking poses with fMLF and WKYMVM peptides in the FPR1 and FPR2 ligand binding sites, respectively. Thus, pyridazinone-based compounds represent potential lead compounds for further development of selective and/or potent FPR agonists.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N310 – PubChem