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n-Type Thiophene Semiconductors

The new fluorocarbon-functionalized and/or heterocycle-modified polythiophenes, in particular, alpha,omega-diperfluorohexylsexithiophene DFH-6T can be straightforwardly prepared in high yield and purity. Introduction of such modifications to a thiophene core affords enhanced thermal stability and volatility, and increased electron affinity versus the unmodified compositions of the prior art. Evaporated films behave as n-type semiconductors, and can be used to fabricate thin film transistors with FET mobilities 0.01 cm2/Vs-some of the highest reported to date for n-type organic semiconductors.

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Pyridazine – Wikipedia,
Pyridazine | C4H4N1543 – PubChem

 

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Synthesis and properties of open-cage fullerene C60 derivatives: Impact of the extended P-pi conjugation

We have developed a method for the synthesis of open-cage fullerene C60 derivatives with extended p-conjugation bearing thienyl groups. By applying this method to an asymmetric diketo derivative, the symmetric form can be obtained without changing the molecular formula. To investigate the structure-property relationship for the asymmetric and symmetric forms, we conducted electrochemical and photophysical measurements. The UV-vis absorption edge was shifted by 210 nm upon changing from the asymmetric to the symmetric form due to the narrower HOMO-LUMO gap, which was also demonstrated by electrochemical analyses. From theoretical calculations, the major contribution of the longest wavelength absorption for the symmetric form is assignable to unusual intramolecular charge transfer transitions whereas p-p* transitions are dominant for the asymmetric form.

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Pyridazine – Wikipedia,
Pyridazine | C4H4N1725 – PubChem

 

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Multiheterocyclic Motifs via Three-Component Reactions of Benzynes, Cyclic Amines, and Protic Nucleophiles

A broadly general, three-component reaction strategy for the construction of compounds containing multiple heterocycles is described. Thermal benzyne formation (by the hexadehydro-Diels-Alder (HDDA) reaction) in the presence of tertiary cyclic amines and a protic nucleophile (HNu) gives, via ring-opening of intermediate ammonium ion/Nu- ion pairs, heterocyclic products. Many reactions are efficient even when the stoichiometric loading of the three reactants approaches unity. Use of HOSO2CF3 as the HNu gives ammonium triflate intermediates, which can then be ring opened by an even wider variety of nucleophiles.

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Pyridazine – Wikipedia,
Pyridazine | C4H4N1879 – PubChem

 

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Compounds with antiulcer and antisecretory activity. II. 3-Heteroaryl-benzimidazolin-2-ones

Some benzimidazolin-2-ones with different hetrocyclic rings at position 3 were synthesized and their antisecretory and antiulcer activity evaluated. The most promising compound, 1-methyl-3-(2-pyrazinyl)-5-chlorobenzimidazolin-2-one 35, because of unfavorable subacute toxicity in dog, was not further developed.

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Pyridazine – Wikipedia,
Pyridazine | C4H4N1619 – PubChem

 

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Discovery of Clinical Candidate 4-[2-(5-Amino-1H-pyrazol-4-yl)-4-chlorophenoxy]-5-chloro-2-fluoro-N-1,3-thiazol-4-ylbenzenesulfonamide (PF-05089771): Design and Optimization of Diaryl Ether Aryl Sulfonamides as Selective Inhibitors of NaV1.7

A series of acidic diaryl ether heterocyclic sulfonamides that are potent and subtype selective NaV1.7 inhibitors is described. Optimization of early lead matter focused on removal of structural alerts, improving metabolic stability and reducing cytochrome P450 inhibition driven drug-drug interaction concerns to deliver the desired balance of preclinical in vitro properties. Concerns over nonmetabolic routes of clearance, variable clearance in preclinical species, and subsequent low confidence human pharmacokinetic predictions led to the decision to conduct a human microdose study to determine clinical pharmacokinetics. The design strategies and results from preclinical PK and clinical human microdose PK data are described leading to the discovery of the first subtype selective NaV1.7 inhibitor clinical candidate PF-05089771 (34) which binds to a site in the voltage sensing domain.

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Pyridazine – Wikipedia,
Pyridazine | C4H4N1914 – PubChem

 

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Novel C-aryl glucoside SGLT2 inhibitors as potential antidiabetic agents: Pyridazinylmethylphenyl glucoside congeners

Novel C-aryl glucoside SGLT2 inhibitors containing pyridazine motif were designed and synthesized for biological evaluation. Among the compounds tested, pyridazine containing methylthio moiety 22l or thiadiazole ring 22ah showed the best in vitro inhibitory activities in this series (IC50 = 13.4, 11.4 nM, respectively) against SGLT2 to date. Subsequently, compound 22l exhibited reasonable urinary glucose excretion and glucosuria in normal SD rats, thereby demonstrating that this pyridazine series possesses both in vitro SGLT2 inhibition and in vivo efficacy, albeit to a lower degree.

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Pyridazine – Wikipedia,
Pyridazine | C4H4N1771 – PubChem

 

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Preparation of new octopus shaped homoleptic and heteroleptic ruthenium(II)-bisdiazine complexes

The preparation of RuL3 (1), RuL2L'(2) and Ru(pod)(3) complexes containing polyethylene glycol chains is described. The complexes are further functionalized by 4-oxyanisyl or by hydrophilic hydroxyl groups. These new complexes may interact in supramolecular assemblies with suitable acceptors such as mono- and bisviologens to form biomimetic models for photosynthesis.

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Pyridazine – Wikipedia,
Pyridazine | C4H4N1777 – PubChem

 

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LIGANDS FOR CARDIAC BETA1 ADRENORECEPTOR FOR IMAGING CONGESTIVE HEART FAILURE

Novel beta1 adrenoreceptor ligands that find use as imaging agents within nuclear medicine applications (e.g., PET imaging and SPECT imaging) are provided. Methods of imaging, including methods of imaging congestive heart failure, are also provided. The novel compounds may exhibit high affinity and selectivity, minimal metabolism, minimalnon-specific binding and have a favorable log P value (< 0). In some instances, beta 1-AR selective ligands are conjugated to an imaging moiety in such a way that it does not impact the antagonist affinity and their use. In other instances, the conjugation may be directly to the antagonist at several sites that will not impact affinity. In further instances, the conjugation may be by means of a linking group, which can be used to alter the pharmacokinetics and clearance of the complex The proportionality constant is the rate constant for the particular unimolecular reaction. the reaction rate is directly proportional to the concentration of the reactant. I hope my blog about 141-30-0 is helpful to your research. Synthetic Route of 141-30-0

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Pyridazine – Wikipedia,
Pyridazine | C4H4N1496 – PubChem

 

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Metal-organic coordination architectures of bis(N-imidazolyl) pyridazine: Syntheses, structures, emission and photocatalytic properties

In efforts to explore the effects of metal ions, counter anions on the structures and properties of metal-organic complexes, seven new complexes [ZnL4(OH)2] (1), {[ZnL(AcO)2](CH3CH2OH)}? (2), {[ZnL(H2O)4](SO4)}? (3), [CdL4(OH)2] (4), {[CdL(AcO)2](CH3CH2OH)}? (5), {[CdL(H2O)4](SiF6)}? (6) and {[Cu2L2(SO4)2(H2O)2](H2O)}? (7) [L = 3,6-bis(N-imidazolyl) pyridazine] were synthesized and structurally characterized by elemental analyses, IR spectroscopy and single-crystal X-ray diffraction. Complexes 1 and 4 have similar mononuclear structures. Complexes 2, 3 and 6 have 1-D chain structures, while 5 reveals 2-D neutral infinite sheet structure. One 1-D chain and one 2-D sheet form complicated structure of complex 7. The ligands L adopt didentate bridging mode to coordinate to the metal ions in complexes 2, 3, and 5-7. Obviously, the structural differences among them are attributable to the differences of metal ions, counter anions and coordination modes of ligand. The fluorescent property of complexes 1-6 have been investigated and discussed. In addition, complexes 1-5 exhibit photocatalytic activity and selectivity for dye degradation under UV light.

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Pyridazine – Wikipedia,
Pyridazine | C4H4N1943 – PubChem

 

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PYRIDAZINONES AS GPR119 AGONISTS

The present invention relates to pyridazinone derivatives of general formula (I), wherein the groups A, G and R1 are as defined in the application, the tautomers thereof, stereoisomers thereof, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.

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Pyridazine – Wikipedia,
Pyridazine | C4H4N1326 – PubChem