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Discovery of BI 135585, an in vivo efficacious oxazinanone-based 11beta hydroxysteroid dehydrogenase type 1 inhibitor

A potent, in vivo efficacious 11beta hydroxysteroid dehydrogenase type 1 (11beta HSD1) inhibitor (11j) has been identified. Compound 11j inhibited 11beta HSD1 activity in human adipocytes with an IC50 of 4.3?nM and in primary human adipose tissue with an IC80 of 53?nM. Oral administration of 11j to cynomolgus monkey inhibited 11beta HSD1 activity in adipose tissue. Compound 11j exhibited >1000¡Á selectivity over other hydroxysteroid dehydrogenases, displays desirable pharmacodynamic properties and entered human clinical trials in 2011.

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Pyridazine – Wikipedia,
Pyridazine | C4H4N772 – PubChem

 

Final Thoughts on Chemistry for 19064-67-6

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DERIVATIVES OF 2H PYRIDAZIN-3-ONES, THEIR PREPARATION AND THEIR USE AS SCD-1 INHIBITORS

The present invention concerns compounds of general formula (I) characterized in that (formula 1) wherein, in particular: -R1 represents one or more groups such as: trifluoromethyl, halogen such as F, Cl, -when n=m=1, W represents CH then Y represents oxygen, -U represents: either – (C=O) CH2NH- and is branched at position 4 of pyridazinone, then R2 represents H, or -(C=O) NH- and U is branched at positions (4), (5) or (6) of pyridazinone, then R2 represents H, – R3 represents a hydrogen or methyl and the addition salts with pharmaceutically acceptable bases and acids and the different isomers, and their mixtures in any proportion for use as SCD-1 enzyme inhibitors for the treatment of obesity, type-2 diabetes and lipid disorders

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Pyridazine – Wikipedia,
Pyridazine | C4H4N723 – PubChem

 

Final Thoughts on Chemistry for 6-Chloro-3-hydroxypyridazine

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In heterogeneous catalysis, the catalyst is in a different phase from the reactants. HPLC of Formula: C4H3ClN2O, At least one of the reactants interacts with the solid surface in a physical process called adsorption in such a way. 19064-67-6, name is 6-Chloro-3-hydroxypyridazine. In an article£¬Which mentioned a new discovery about 19064-67-6

Identification of triazolopyridazinones as potent p38alpha inhibitors

Structure-activity relationship (SAR) investigations of a novel class of triazolopyridazinone p38alpha mitogen activated protein kinase (MAPK) inhibitors are disclosed. From these studies, increased in vitro potency was observed for 2,6-disubstituted phenyl moieties and N-ethyl triazolopyridazinone cores due to key contacts with Leu108, Ala157 and Val38. Further investigation led to the identification of three compounds, 3g, 3j and 3m that are highly potent inhibitors of LPS-induced MAPKAP kinase 2 (MK2) phosphorylation in 50% human whole blood (hWB), and possess desirable in vivo pharmacokinetic and kinase selectivity profiles.

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Pyridazine – Wikipedia,
Pyridazine | C4H4N750 – PubChem

 

New explortion of 6-Chloro-3-hydroxypyridazine

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Pyridinone and Pyridazinone Derivatives

The present invention provides for compounds of formula (I) wherein A1, A2, A3, A4, J, and X3 have any of the values defined therefor in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, diabetes, obesity, cancer, and AIDS. Also provided are pharmaceutical compositions comprising one or more compounds of formula I.

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Pyridazine – Wikipedia,
Pyridazine | C4H4N730 – PubChem

 

Final Thoughts on Chemistry for 19064-67-6

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Synthetic Route of 19064-67-6, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.19064-67-6, Name is 6-Chloro-3-hydroxypyridazine, molecular formula is C4H3ClN2O. In a Article£¬once mentioned of 19064-67-6

Copper-catalyzed aerobic dehydrogenation of C-C to C=C bonds in the synthesis of pyridazinones

A simple and efficient procedure for the synthesis of pyridazin-3(2H)-ones through copper-catalyzed dehydrogenation of a single C-C bond of 4,5-dihydropyridazin-3(2H)-ones to a C=C bond with oxygen as the terminal oxidant is described. Functional groups including hydroxy, carboxylic, bromo, chloro, cyano, nitro and alkoxy were all tolerated under the reaction conditions. Moreover, this methodology was applied to the preparation of a series of structurally similar N-substituted 6-phenylpyridazinone compounds containing fluorine. The dehydrogenation reactions exhibit good yields and selectivity. Copper-catalyzed dehydrogenation of a C-C bond of 4,5-dihydropyridazinones to a C=C bond with oxygen as the terminal oxidant is described. Various functional groups were tolerated under the reaction conditions. The method was also applied to the preparation of a series of N-substituted 6-phenylpyridazinones containing fluoride. The dehydrogenation reactions exhibit good yields and selectivity.

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Pyridazine – Wikipedia,
Pyridazine | C4H4N759 – PubChem

 

Discovery of 6-Chloro-3-hydroxypyridazine

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The Discovery of LML134, a Histamine H3 Receptor Inverse Agonist for the Clinical Treatment of Excessive Sleep Disorders

Histamine H3 receptor (H3R) inverse agonists that have been in clinical trials for the treatment of excessive sleep disorders, have been plagued with insomnia as a mechanism-based side effect. We focused on the identification of compounds that achieve high receptor occupancy within a short time, followed by rapid disengagement from the receptor, a target profile that could provide therapeutic benefits without the undesired side effect of insomnia. This article describes the optimization work that led to the discovery of 1-(1-methyl-6-oxo-1,6-dihydropyridazin-3-yl)piperidin-4-yl 4-cyclobutylpiperazine-1-carboxylate (18 b, LML134).

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Pyridazine – Wikipedia,
Pyridazine | C4H4N769 – PubChem

 

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FUNGICIDAL OXADIAZOLES

Disclosed are compounds of Formula 1, including all geometric and stereoisomers, tautomers, N-oxides, and salts thereof, wherein R1, L and J are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.

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Pyridazine – Wikipedia,
Pyridazine | C4H4N739 – PubChem

 

Brief introduction of 6-Chloro-3-hydroxypyridazine

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Synthesis and Chemistry of Some Pyridazine Nucleosides Related to Certain 5-Substituted Pyrimidine Nucleosides

Condensation of 3,4-dichloro-6-<(trimethylsilyl)oxy>pyridazine (3) with 1-O-acetyl-2,3,5-tri-O-benzoyl-beta-D-ribofuranose (4), by the stannic chloride catalyzed procedure, has furnished 3,4-dichloro-1-(2,3,5-tri-O-benzoyl-beta-D-ribofuranosyl)pyridazin-6-one (5).Nucleophilic displacement of the chloro groups and removal of the benzoyl blocking groups from 5 has furnished 3-chloro-4-methoxy-, 3,4-dimethoxy-, 4-amino-3-chloro-, 3-chloro-4-methylamino-, 3-chloro-4-hydroxy-, and 4-hydroxy-3-methoxy-1-beta-D-ribofuranosylpyridazin-6-one.An unusual reaction of 5 with dimethylamine is reported.Condensation of 4,5-dichloro-3-nitro-6-<(trimethylsilyl)oxy>pyridazine with 4 yielded 4,5-dichloro-3-nitro-1-(2,3,5-tri-O-benzoyl-beta-D-ribofuranosyl)pyridazin-6-one (24).Nucleophilic displacement of the aromatic nitro group from 24 is discussed.Condensation of 3 with 3,5-di-O-p-toluoyl 2-deoxy-D-erythro-pentofuranosyl chloride (28) afforded an alpha,beta mixture of 2-deoxy nucleosides.The syntheses of certain 3-substituted pyridazine 2′-deoxy nucleosides are reported.

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A new application about 6-Chloro-3-hydroxypyridazine

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Pyrazolopyridine-4-Yl Pyridazinone Derivatives and Addition Salts Thereof, and Pde Inhibitors Comprising the Same Derivatives or Salts as Active Ingredient

Novel pyrazolopyridine-4-yl pyridazinone derivatives serve as phosphodiesterase inhibitors and are useful compounds for use in pharmaceutical products. Specifically, the compounds of the present invention are pyrazolopyridine-4-yl pyridazinone derivatives represented by the following general formula (1): (Example: 6-(2-ethyl-7-methoxy-pyrazolo[1,5-a]pyridine-4-yl)-5-methyl-4, 5-dihydro-3(2H)-pyridazinone).

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Pyridazine – Wikipedia,
Pyridazine | C4H4N744 – PubChem

 

Top Picks: new discover of 19064-67-6

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 19064-67-6 is helpful to your research. Reference of 19064-67-6

Reference of 19064-67-6, 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, 19064-67-6, molcular formula is C4H3ClN2O, introducing its new discovery.

1H, 13C, and 15N NMR spectra of some pyridazine derivatives

1H, 13C, and 15N NMR chemical shifts for pyridazines 4-22 were measured using 1D and 2D NMR spectroscopic methods including 1H-1H gDQCOSY,1H-13C gHMQC,1H-13C gHMBC,and1H-15N CIGAR-HMBC experiments. (0 2010 John Wiley & Sons, Ltd.

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Pyridazine – Wikipedia,
Pyridazine | C4H4N753 – PubChem