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Electric Literature of 5469-70-5, 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, 5469-70-5, 3-Aminopyridazine, introducing its new discovery.

Disclosed are imidazole compounds, as well as pharmaceutical compositions and methods of use thereof. One embodiment is a compound having the structure Formula (I) and pharmaceutically acceptable salts, prodrugs and N-oxides thereof (and solvates and hydrates thereof), wherein A, Z, X, R1, R2 m, p and a are as described herein. In certain embodiments, a compound disclosed herein inhibits TGF-beta, and can be used to treat disease by blocking TGF-beta signaling.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N43 – PubChem

 

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Synthetic Route of 5469-70-5, 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, 5469-70-5, molcular formula is C4H5N3, introducing its new discovery.

In this work, a series of 2-substituted-thio-N-(4-substituted-thiazol/1H-imidazol-2-yl)acetamide derivatives were developed as beta-secretase (BACE-1) inhibitors. Supported by docking study, a small library of derivatives were designed, synthesized and biologically evaluated in vitro. In addition, the selected compounds were tested with affinity (KD) towards BACE-1, blood brain barrier (BBB) permeability and cytotoxicity. The studies revealed that the most potent analog 41 (IC50 = 4.6 muM) with high predicted BBB permeability and low cellular cytotoxicity, could serve as a good lead structure for further optimization.

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Reference£º
Pyridazine – Wikipedia,
Pyridazine | C4H4N100 – PubChem

 

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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, 5469-70-5, name is 3-Aminopyridazine, introducing its new discovery. Application In Synthesis of 3-Aminopyridazine

CuI-catalyzed amination of arylhalides with guanidines or amidines: A facile synthesis of 1-H-2-substituted benzimidazoles

(Figure Presented) CuI/L5 (N,N?-dimethylethylenediamine) proves to be an efficient catalyst system for the amination of arylhalides with guanidines. The same catalyst system is then successfully applied to the one-step synthesis of 1-H-2-aminobenzimidazoles through tandem aminations of 1,2-dihaloarenes in modest yields. This methodology is also applicable for the preparation of 1-H or 1-substutituted 2-aryl- or 2-alkyl-benzimidazoles.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N70 – PubChem

 

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I hope this article can help some friends in scientific research. I am very proud of our efforts over the past few months and hope to 5469-70-5, help many people in the next few years.Application In Synthesis of 3-Aminopyridazine

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2-Aminoimidazole-based antagonists of the 5-HT6 receptor ? A new concept in aminergic GPCR ligand design

A new strategy in the design of aminergic GPCR ligands is proposed ? the use of aromatic, heterocyclic basic moieties in place of the evergreen piperazine or alicyclic and aliphatic amines. This hypothesis has been tested using a benchmark series of 5-HT6R antagonists obtained by coupling variously substituted 2-aminoimidazole moieties to the well established 1-benzenesulfonyl-1H-indoles, which served as the ligands cores. The crystallographic studies revealed that upon protonation, the 2-aminoimidazole fragment triggers a resonance driven conformational change leading to a form of higher affinity. This molecular switch may be responsible for the observed differences in 5-HT6R activity of the studied chemotypes with different amine-like fragments. Considering the multiple functionalization sites of the embedded guanidine fragment, diverse libraries were constructed, and the relationships between the structure and activity, metabolic stability, and solubility were established. Compounds from the N-(1H-imidazol-2-yl)acylamide chemotype (10a?z) exhibited high affinity for 5-HT6R and very high selectivity over 5-HT1A, 5-HT2A, 5-HT7 and D2 receptors (negligible binding), which was attributed to their very weak basicity. The lead compound in the series 4-methyl-5-[1-(naphthalene-1-sulfonyl)-1H-indol-3-yl]-1H-imidazol-2-amine (9i) was shown to reverse the cognitive impairment caused by the administration of scopolamine in rats indicating procognitive potential.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N76 – PubChem

 

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Synthetic Route of 5469-70-5, A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 5469-70-5, Name is 3-Aminopyridazine, molecular formula is C4H5N3. In a Patent,once mentioned of 5469-70-5

2-AMINO-7,8-DIHYDRO-6H-PYRIDO[4,3-D] PYRIMIDIN-5-ONES

Disclosed are 2-amino-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one compounds, their stereoisomers, tautomers, pharmaceutically acceptable salts, and prodrugs thereof; compositions that include a pharmaceutically acceptable carrier and one or more of the 2-amino-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one compounds, either alone or in combination with at least one additional therapeutic agent. Disclosed also are methods of using the 2-amino-7,8-dihydro-6H-pyrido[4,3-d]pyrimidin-5-one compounds, either alone or in combination with at least one additional therapeutic agent, in the prophylaxis or treatment of cellular proliferative, viral, autoimmune, cardiovascular, and central nevous system diseases.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N32 – PubChem

 

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1-Pyridylmethyl-3-acyl guanidines

1-Acyl-3-pyridyl guanidine and 1-acyl-3-pyridylalkyl guanidine compounds, methods for the treatment of blood pressure disorders, including hypertension, in humans and other mammals.

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Pyridazine – Wikipedia,
Pyridazine | C4H4N45 – PubChem

 

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Construction of sulfur-containing moieties in the total synthesis of natural products

Covering: January 2013 to September 2018 Sulfur-containing natural products are a large class of significant functional molecules. Many of these compounds exhibit potent biological activities and pharmacological properties; in fact, some of them have been developed into important drugs. The total synthesis of sulfur-containing natural products is a subject that has long attracted significant attention from synthetic organic chemists; to achieve this goal, various methods have been developed over the past years. This review surveys total syntheses of sulfur-containing natural products that introduce sulfur atoms using different sulfurization agents to construct related sulfur-containing moieties.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N99 – PubChem

 

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6-Methyl-5-azacytidine – Synthesis, conformational properties and biological activity. A comparison of molecular conformation with 5- azacytidine

The title compound was prepared by the isocyanate procedure and the trimethylsilyl method. The measurement of 1H NMR spectrum of 6-methyl-5- azacytidine (1) revealed a preference of gamma(t) (46%) rotamer around C(5′)- C(4′) bond, a predominance of N conformation of the ribose ring (K(eq) 0.33) and a preference of syn conformation around the C-N glycosyl bond. An analogous measurement of 5-azacytidine has shown a preference of gamma+ (60%) rotamer around the C(5′)-C(4′) bond, a predominance of N conformation of the fibose ring (K(eq) 0.41) and a preference of anti conformation around the C- N glycosyl bond 6-Methyl-5-azacytidine (1) inhibits the growth of bacteria E coli to the extent of 85% at 4000 muM concentration and the growth of LoVo/L, a human colon carcinoma cell line, to the extent of 30% at 100 muM concentration but did not inhibit L1210 cells at ? 100 muM concentration 6- Methyl-5-azacytidine (1) exhibited no in vitro antiviral activity at ? 1 muM concentration.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N75 – PubChem

 

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Synthesis and biological evaluation of 4(5)-(6-alkylpyridin-2-yl)imidazoles as transforming growth factor-beta type 1 receptor kinase inhibitors

A series of 4(5)-(6-alkylpyridin-2-yl)imidazoles 13a-p, 17a, and 17b have been synthesized and evaluated for ALK5 inhibitory activity in an enzyme assay and in cell-based luciferase reporter assays. The quinoxalinyl analogue 13e inhibited ALK5 phosphorylation with an IC50 of 0.012 muM and showed more than 90% inhibition at 0.05 muM in a luciferase reporter assay using HaCaT cells transiently transfected with p3TP-luc reporter construct. The binding mode of 13e generated by flexible docking studies shows that 13e fits well into the active site cavity of ALK5 by forming several tight interactions.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N79 – PubChem

 

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IMIDAZOLYL INHIBITORS OF 15-LIPOXYGENASE

The present invention provides imidazolyl inhibitors of 15-LO, pharmaceutical compositions containing such inhibitors and methods for treating diseases related to the 15-LO cascade using such compounds and compositions

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N14 – PubChem