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The 5-HT2CR agonist lorcaserin, clinically approved for the treatment of obesity, causes important side effects mainly related to subtype selectivity. In the search for 5-HT2CR allosteric modulators as safer antiobesity drugs, a chemical library from Vivia Biotech was screened using ExviTech platform. Structural modifications of identified hit VA240 in synthesized analogues 6-41 afforded compound 11 (N-[(1-benzyl-1H-indol-3-yl)methyl]pyridin-3-amine, VA012), which exhibited dose-dependent enhancement of serotonin efficacy, no significant off-target activities, and low binding competition with serotonin or other orthosteric ligands. PAM 11 was very active in feeding inhibition in rodents, an effect that was not related to the activation of 5-HT2AR. A combination of 11 with the SSRI sertraline increased the anorectic effect. Subchronic administration of 11 reduced food intake and body weight gain without causing CNS-related malaise. The behavior of compound 11 identified in this work supports the interest of a serotonin 5-HT2CR PAM as a promising therapeutic approach for obesity.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N154 – PubChem

 

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The invention provides named compounds of formula (I), wherein R4 is a N-substituted quinuclidine (I) pharmaceutical compositions containing them and a process for preparing the pharmaceutical compositions. Their use in therapy for? the treatment of conditions mediated by M3 muscarinic receptors, such as chronic obstructive pulmonary disease is also disclosed.

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The disclosure relates to compounds of formula (I): wherein Ra, Rb, R, and n are as defined in the disclosure, to pharmaceutical compositions comprising said compounds, and to processes for making and methods of using the same.

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Pyridazine – Wikipedia,
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The invention relates to inhibitors of PI5P4K inhibitors useful in the treatment of cancers, neurodegenerative diseases, inflammatory disorders, and metabolic diseases, having the Formula (I); where A1, A2, G, R1, R2, R3, R4, and W are described herein.

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Pyridazine – Wikipedia,
Pyridazine | C4H4N124 – PubChem

 

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The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds to treat disorders associated with GSK-3.

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This study was done to assess the proliferation bacterial and susceptibility resistance antibiotic pattern of (UTIs) pathogens. For identification of mid stream urine samples 40causative microbial agents from 10-50 years clinical sample with clinical symptoms to be UTI were collected and appropriate biochemical tests. These samples were collected from Teaching Laboratories Center in Baghdad. The antimicrobial sensitivity test was carried out by Well Diffusion Assay technique using Muller- Hinton agar. Overall female only the most isolates were Escherichia coli with average rate of 50% followed by Enter obacter spp. (12%). Whereas, Klebsiella, Pseudomonas Aeruginosa and Enter occurs faecalis showed frequency rate of 9% for each. (Family Solanaceae) species Capsicum frutescent L. Usually used most of the spice, (red peppers) is also increased benefits with multiple healths human. In the study, yield extract included constituents phytochemical of (n-hexane, chloroform, ethyl acetate, acetone and methanol) extracts of dried fruit. Antibacterial activity in vitro of extracts was determined by WADA method gram positive bacteria (Staphylococcus Aureus) and gram negative bacteria (Escherichia coli, Pseudomonas Aeruginosa, Klebsiella pneumonia and Enterococcus faecalis). MIC evaluated by two fold serial broth tube dilution method ranged between 0.312 to 5 mg/mL.

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Pyridazine – Wikipedia,
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Insecticidal agents characterized as 1-(benzoyl)-3-(6-oxopyridazinyl)urea are provided. Agricultural compositions and an insecticidal method are disclosed.

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Pyridazine – Wikipedia,
Pyridazine | C4H4N112 – PubChem

 

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Compounds of Formula (IA), IB), IC), and (ID) wherein R1, R2, R3, R4, R5, and R6 are as respectively defined herein for Formula (IA), (IB), (IC), and (ID), or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.

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Pyridazine – Wikipedia,
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A new method of amination of diazines and triazines, using potassium amide, liquid ammonia and potassium permanganate, has been described.

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Pyridazine – Wikipedia,
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Ultrasound-assisted extraction (UAE) of pectic polysaccharide from oriental tobacco leaves was studied by orthogonal matrix method (L9(3)4). Furthermore, the crude polysaccharide was purified and two components (Fr-I and Fr-II) were obtained. FT-IR spectral analysis of the purified EPS revealed prominent characteristic groups. The monosaccharide composition analysis indicated the main composition between Fr-I and Fr-II was different. Furthermore, thermo gravimetric analysis (TGA) indicated the degradation temperature (Td) of the Fr-I (215 C) was higher than those of Fr-II (162 C). Detected by the pyrolysis GC/MS, though the main kinds of pyrolysis products from both Fr-I and Fr-II were similar, the larger amount of heterocycle and aromatic compounds liberated after hydrolysis of Fr-II. Finally, On the basis of the antioxidant activity test in vitro, Fr-II has stronger antioxidant activities than Fr-I. The thermal behavior and antioxidant activity might be attributed to the configuration of the sugar units and chemical compositions.

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Reference:
Pyridazine – Wikipedia,
Pyridazine | C4H4N160 – PubChem