Heterocyclic Building Blocks-Pyridazine

Application 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

A series of novel imidazo[1,2-b]pyridazin-3-yl acetamide derivatives (9a-9j) were synthesized from a 3,6-dichloropyridazine. We have developed a simple strategy for the synthesis of functionally diverse imidazole, and pyridiazine derivatives were reported via a series of steps. The work involves bicyclic imidazo-pyridazine ring formation, halogenation, cynation, hydrolysis, peptide coupling, and Buchwald reaction. The structure of the synthesized compounds was confirmed by IR, 1H NMR, 13C NMR,19F NMR, mass spectra, and elemental analysis, and purity is checked by HPLC. All synthesized compounds were screened for anticancer activity against A-549 and Du-145 cancer cell lines by MTT assay. The preliminary bioassay suggests that most of the compounds show anti-proliferation with different degrees; doxorubicin was used as positive control. The synthesized compound shows IC50 values in the range of 1.74muM to 16.17muM in both cell lines. The compounds 9e, 9g, and 9h were active compared with doxorubicin in both the cell lines. The compounds having cyclopentyl ring are active compared with higher and lower carbon analogues.

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Reference：
Pyridazine – Wikipedia,
Pyridazine | C4H4N1638 – PubChem

Application of 5469-70-5, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.5469-70-5, Name is 3-Aminopyridazine, molecular formula is C4H5N3. In a Article，once mentioned of 5469-70-5

In this work, we demonstrate the existence of linear relationships between gas-phase equilibrium bond lengths of the guanidine skeleton of 2-(arylamino)imidazolines and their aqueous pKa value. For a training set of 22 compounds, in the most stable conformation of their lowest energy tautomeric form, three bonds were found to exhibit r2 and q2 values >0.95 and root-mean-squared-error of estimation values ?0.25 when regressed individually against pKa. The equations describing these one-bond-length linear relationships, in addition to a multiple linear regression model using all three bond lengths, were then used to predict the experimental pKa values of an external test set of further 27 derivatives. The optimal protocol we derive here shows an overall mean absolute error (MAE) of 0.20 and standard deviation of errors of 0.18 for the test set. Predictions for a second test set of diphenyl-based bis(2-iminoimidazolidines) yielded an MAE of 0.27 and a standard deviation of 0.10. The predictive power of the optimal model is further demonstrated by its ability to correct erroneously reported experimental values. Finally, a previously established guanidine model is recalibrated at a new level of theory, and predictions are made for novel phenylguanidine derivatives, showing an MAE of just 0.29. The protocols established and tested here pass both of Roy’s modern and stringent MAE-based criteria for a “good” quantitative structure-activity relationship/quantitative structure-property relationship model predictivity. Notably, the ab initio bond length high correlation subset protocol developed in this work demonstrates lower MAE values than the Marvin program by ChemAxon for all test sets.

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Reference：
Pyridazine – Wikipedia,
Pyridazine | C4H4N68 – PubChem

Related Products of 20375-65-9, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.20375-65-9, Name is 3-Phenyl-6-chloropyridazine, molecular formula is C10H7ClN2. In a Article，once mentioned of 20375-65-9

A series of amino acid ester prodrugs of the dual VEGFR-2/FGFR-1 kinase inhibitor 1 (BMS-540215) was prepared in an effort to improve the aqueous solubility and oral bioavailability of the parent compound. These prodrugs were evaluated for their ability to liberate parent drug 1 in in vitro and in vivo systems. The L-alanine prodrug 8 (also known as brivanib alaninate/BMS-582664) was selected as a development candidate and is presently in phase II clinical trials.

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Pyridazine – Wikipedia,
Pyridazine | C4H4N2603 – PubChem

Synthetic Route of 15456-86-7, Chemistry is the experimental science by definition. We want to make observations to prove hypothesis. For this purpose, we perform experiments in the lab. 15456-86-7, Name is 4-Bromo-1,2-dihydropyridazine-3,6-dione,introducing its new discovery.

Regioselective desymmetrization of 4-substituted pyridazin-3,6-diones using sterically hindered 2,4,6-triisopropylphenyl-sulfonylchloride allowed efficient sequential palladium cross-coupling reactions.

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Pyridazine – Wikipedia,
Pyridazine | C4H4N2805 – PubChem

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 Patent，once mentioned of 141-30-0

The present invention discloses novel isoquinoline carboxamide derivatives which are HIV protease inhibitors or prodrugs thereof, a process for their manufacture, pharmaceutical compositions and the use of such compounds in medicine. In particular, the compounds are hydroxyethylamine tripeptide mimetics which act as inhibitors of the HIV aspartyl protease, an essential enzyme in the replicative life cycle of HIV. Consequently, the compounds of this invention may be advantageously used in the treatment of HIV infection, either alone or in combination with other inhibitors of HIV viral replication or with pharmacoenhancers such as cytochrome P450 inhibitors.

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Reference：
Pyridazine – Wikipedia,
Pyridazine | C4H4N1375 – PubChem

Reference of 5469-70-5, 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.5469-70-5, Name is 3-Aminopyridazine, molecular formula is C4H5N3. In a article，once mentioned of 5469-70-5

A class of novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-?B activity including obesity, diabetes, inflammatory and immune diseases, and have the structure of formula (I) or (II): [INSERT CHEMICAL STRUCTURE HERE] including all stereoisomers thereof, tautomers thereof, or a prodrug thereof, or a pharmaceutically acceptable salt thereof, where Q is selected from N, O, and S; Y is aryl or heteroaryl; Z is H, C2-6alkyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, halo, or alkoxy; and A, B, R, Ra, Rb, Rc and Rd are defined herein. Also provided are pharmaceutical compositions and methods of treating obesity, diabetes and inflammatory or immune associated diseases comprising said compounds.

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Pyridazine – Wikipedia,
Pyridazine | C4H4N51 – PubChem

One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, Recommanded Product: 1120-95-2, such as the rate of change in the concentration of reactants or products with time.In a article, mentioned the application of 1120-95-2, Name is 3-Chloropyridazine, molecular formula is C4H3ClN2

The present invention relates to azaspiro derivatives of the formula (I) or a pharmaceutically acceptable salt thereof or a prodrug thereof, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders which are mediated via the TRPM8 receptor.

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Pyridazine – Wikipedia,
Pyridazine | C4H4N402 – PubChem

One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, name: 3-Phenyl-6-chloropyridazine, such as the rate of change in the concentration of reactants or products with time.In a article, mentioned the application of 20375-65-9, Name is 3-Phenyl-6-chloropyridazine, molecular formula is C10H7ClN2

A series of novel P1/P1′-substituted cyclic urea-based HIV-1 protease inhibitors was prepared. Three different synthetic schemes were used to assemble these compounds. The first approach uses amino acid-based starting materials and was originally used to prepare DMP 323. The other two approaches use L-tartaric acid or L-mannitol as the starting material. The required four contiguous R,S,S,R centers of the cyclic urea scaffold are introduced using substrate control methodology. Each approach has specific advantages based on the desired P1/P1′ substituent. Designing analogs based on the enzyme’s natural substrates provided compounds with reduced activity. Attempts at exploiting hydrogen bond sites in the S1/S1′ pocket, suggested by molecular modeling studies, were not fruitful. Several analogs had better binding affinity compared to our initial leads. Modulating the compound’s physical properties led to a 10-fold improvement in translation resulting in better overall antiviral activity.

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Pyridazine – Wikipedia,
Pyridazine | C4H4N2715 – PubChem

Electric Literature of 35857-89-7, Chemistry is the science of change. But why do chemical reactions take place? Why do chemicals react with each other? The answer is in thermodynamics and kinetics.In a document type is Patent, and a compound is mentioned, 35857-89-7, 6-Chloropyridazine-3-carbonitrile, introducing its new discovery.

Compounds of the formula: STR1 where 2 THE R’s are the same or different and are H or CH3, and one of them can be C2 -C9 alkyl or phenyl; R1 is hydrogen, C1 -C4 alkyl, C3 -C6 cycloalkyl, C2l -C4 alkoxycarbonyl, or substituted C1 -C4 alkyl where the substituent is C3 -C6 cycloalkyl or phenyl; and Z is H, Cl or CH3 ; and their pharmaceutically suitable salts. The compounds are useful as sedatives; some of them also exhibit antidepressant activity.

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Reference：
Pyridazine – Wikipedia,
Pyridazine | C4H4N878 – PubChem

In homogeneous catalysis, the catalyst is in the same phase as the reactant. The number of collisions between reactants and catalyst is at a maximum.In a patent, 141-30-0, name is 3,6-Dichloropyridazine, introducing its new discovery. name: 3,6-Dichloropyridazine

A series of 3,8-diazabicyclo[3.2.1]octanes substituted either at the 3 position compounds 1) or at the 8 position (compounds 2) by a chlorinated heteroaryl ring were synthesized, as potential analogues of the potent natural analgesic epibatidine. When tested in the hot plate assay, the majority of the compounds showed significant effects, the most interesting being the 3-(6-chloro-3-pyridazinyl)-3,8-diazabicyclo[3.2.1]octane (la). At a subcutaneous dose of 1 mg/kg, 1a induced a significant increase in the pain threshold, its action lasting for about 45 min. 1a also demonstrated good protection at a dose of 5 mg/kg in the mouse abdominal constriction test, while at 20 mg/kg it completely prevented the constrictions in the animals. Administration of naloxone (1 mg/kg ip) did not antagonize its antinociception while mecamylamine (2 mg/kg ip) did, thus suggesting the involvement of the nicotinic system in its action. Binding studies confirmed high affinity for the alphabeta2 nAChR subtype (K(i) = 4.1±0.21 nM). nAChR functional activity studies on three different cell lines showed that 1a was devoid of any activity at the neuromuscular junction. Finally, due to the analogy in their pharmacological profile with that of epibatidine, compounds were compared from a structural and conformational point of view through theoretical calculations and high-field 1H NMR spectroscopy. Results indicate that all of them present one conformation similar to that of epibatidine.

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Reference：
Pyridazine – Wikipedia,
Pyridazine | C4H4N1609 – PubChem