Day: November 3, 2022

On November 4, 2021, Behenna, Douglas; Deckhut, Charlotte; Rovira, Alexander; Goldberg, Steven; Kummer, David; Keith, John; Woods, Craig; Rhorer, Timothy; Tanis, Virginia; Martin, Connor; Meduna, Steven; McCarver, Stefan; Valdes, Alexander; Loskot, Steven; Xue, Xiaohua published a patent.Safety of 5-Isopropylnicotinic acid The title of the patent was Imidazopyridazines as modulators of IL-17 in the treatment of inflammatory disorders. And the patent contained the following:

The invention relates compounds of formula I, preparation and use in treating or ameliorating an IL-17 mediated syndrome, disorder and/or disease. Compound I, wherein R1 is (un)substituted C1-6 alkyl, (un)substituted C0-2 alkyl-C3-6 cycloalkyl, and (un)substituted 5- and 6-membered heterocyclyl having 1 and 2 nitrogen atoms; R2 is H, C3-5 cycloalkyl and (un)substituted C1-4 alkyl; R3 is (un)substituted C0-1 alkyl-C3-6 cycloalkyl, (un)substituted C3-6 alkyl and (un)substituted C1-2 alkyl-O-C1-3 alkyl; R4 is (un)substituted C3-6 cycloalkyl, (un)substituted Ph and (un)substituted 5- and 6-membered heteroaryl having 1 to 4 heteroatoms selected from N, O and S; R5 is H and halo; and pharmaceutically acceptable salts thereof, are claimed. Compound II was prepared using a multistep procedure (procedure given). Compound II was evaluated for IL-17A modulatory activity resulting in an IC50 of 0.18μM and 0.30μM using Eu-HTRF and NHK assays, resp. Compounds of the invention were evaluated for IL-17A modulatory activity (data given). The experimental process involved the reaction of 5-Isopropylnicotinic acid(cas: 73591-69-2).Safety of 5-Isopropylnicotinic acid

The Article related to imidazopyridazine preparation modulator il 17 inflammatory disorder, Heterocyclic Compounds (More Than One Hetero Atom): Pyridazines, Cinnolines, and Phthalazines and other aspects.Safety of 5-Isopropylnicotinic acid

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On April 2, 2009, Yi, Chae S.; Kwon, Ki-Hyeok; Lee, Do W. published an article.Category: pyridine-derivatives The title of the article was Aqueous Phase C-H Bond Oxidation Reaction of Arylalkanes Catalyzed by a Water-Soluble Cationic Ru(III) Complex [(pymox-Me2)2RuCl2]+BF4-. And the article contained the following:

The cationic complex [(pymox-Me2)RuCl2]+BF4- was found to be a highly effective catalyst for the C-H bond oxidation reaction of arylalkanes in water. For example, the treatment of ethylbenzene (1.0 mmol) with t-BuOOH (3.0 mmol) and 1.0 mol % of the Ru catalyst in water (3 mL) cleanly produced PhCOCH3 at room temperature Both a large kinetic isotope effect (kH/kD = 14) and a relatively large Hammett value (ρ = -1.1) suggest a solvent-caged oxygen rebounding mechanism via a Ru(IV)-oxo intermediate species. The experimental process involved the reaction of 2-(4,5-Dihydro-4,4-dimethyl-2-oxazolyl)pyridine(cas: 109660-12-0).Category: pyridine-derivatives

The Article related to aqueous carbon hydrogen bond oxidation arylalkane cationic ruthenium complex, Physical Organic Chemistry: Oxidation-Reduction, Including Dehydrogenation and Hydrogenolysis and other aspects.Category: pyridine-derivatives

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On February 29, 1984, Xiao, Xu Rui; Wang, Ching Bore; Tien, H. Ti published an article.COA of Formula: C16H22Br2N2 The title of the article was Photoreduction of alkyl viologens by zinc tetraphenylporphyrin in organic solvent-water systems. And the article contained the following:

Light-induced redox reactions between Zn meso-tetraphenylporphyrin (ZnTPP) and alkyl viologens (CnV2+) in organic solvent-surfactant-H2O solutions were studied as functions of the organic-solvent content of the solutions, the surfactant charge, and the alkyl viologen hydrophobicity. The best system was an oil-in-water emulsion containing 5 × 10-5 M ZnTPP and 10-3M C10V2+ stabilized by n-C16H33NMe3+ X- (X = Br, Cl) and 6% DMF, AcNMe2 or DMSO in H2O. The experimental process involved the reaction of 1,1′-Dipropyl-[4,4′-bipyridine]-1,1′-diium bromide(cas: 52243-87-5).COA of Formula: C16H22Br2N2

The Article related to photoreduction alkyl viologen zinc tetraphenylporphyrin, reduction photochem alkyl viologen, Physical Organic Chemistry: Oxidation-Reduction, Including Dehydrogenation and Hydrogenolysis and other aspects.COA of Formula: C16H22Br2N2

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Kaczmarek, Lukasz; Nantka-Namirski, Pawel published an article in 1979, the title of the article was Bipyridines. XI. Synthesis of 4,5-diazacarbazole.Category: pyridine-derivatives And the article contains the following content:

3,3′-Dinitro-2,2′-bipyridine (I) was reduced with SnCl2 in concentrated HCl to give 71% 3,3′-diamino-2,2′-bipyridine (II), which was also prepared in 34% yield by heating 2-chloro-3-acetylaminopyridine with Cu in DMF and subsequently deacetylating the product in acidic medium. Hydrogenation of I (Pd/C, 2.5 atm) converted both NO2 groups into NHOH groups in 79% yield; subsequent cyclization in polyphosphoric acid at 300° gave 77% III. II with H2SO4-HNO3 gave 40% IV (R = NO2), with PhNCO, 94% IV (R = CONHPh), with Ac2O, 65% IV (R = Ac, V), with CS2, 25% VI, and with ZnCl2 at 350-400°, 55% VII. V was converted in 70% yield into the N,N’-dioxide by the action of 3-ClC6H4CO3H. in vivo Biol. tests with sarcoma 180 and leukemias were neg. The experimental process involved the reaction of [2,2′-Bipyridine]-3,3′-diamine(cas: 75449-26-2).Category: pyridine-derivatives

The Article related to bipyridinediamine preparation reaction, diazacarbazole, dipyridopyrazine, dipyridodiazepinethione, dipyridopyrrole, neoplasm inhibitor bipyridinediamine derivative, Heterocyclic Compounds (More Than One Hetero Atom): Pyridazines, Cinnolines, and Phthalazines and other aspects.Category: pyridine-derivatives

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On March 20, 1997, Kawano, Eiji; Nagai, Masashi; Inubushi, Atsurou; Shimada, Keiichi; Tobari, Hiroko published a patent.Category: pyridine-derivatives The title of the patent was Nitrogen monoxide synthetase inhibitor comprising 2-aminopyridines as active ingredient. And the patent contained the following:

A nitrogen monoxide synthetase (NOS) inhibitor which contains as the active ingredient 2-aminopyridines or pharmaceutically acceptable salts thereof. It has been found that 2-aminopyridines and pharmaceutically acceptable salts thereof have potent effects of inhibiting nitrogen monoxide synthetase. Namely, a medicinal composition containing 2-aminopyridines and pharmaceutically acceptable salts thereof is useful as a nitrogen monoxide formation inhibitor for treatment of NOS-related diseases e.g. septic shock, rheumatism, allergy, parkinsonism, cardiovascular diseases, obesity, and pain. The experimental process involved the reaction of 3-Methylpyridine-2,6-diamine(cas: 51566-22-4).Category: pyridine-derivatives

The Article related to nitrogen monoxide synthetase inhibitor aminopyridine preparation, Pharmacology: Effects Of Nervous System- and Behavior-Affecting Drugs and Neuromuscular Agents and other aspects.Category: pyridine-derivatives

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Vyas, Bhavesh M.; Singh, Adarsh J.; Dhattiwala, Abdulkadir S.; Mansuri, Sabera M.; Patel, Varsha J. published an article in 2014, the title of the article was Comparative CNS activities of clinically employed antihistamines (H1 antagonist).SDS of cas: 132-20-7 And the article contains the following content:

Aim: H1 Antihistamines are classified into first generation and second generation agents. The main differences between the first and second generations of drugs are their propensity to cause central nervous system (CNS) side effects. Therefore, present study was aimed to analyze the effects of different H1 antihistamines (first and second generation) on CNS using different animal exptl. models. Materials & methods: H1 antihistamines such as pheniramine maleate (3 mg/kg, 6 mg/kg), cetirizine (0.6 mg/kg, 1.2 mg/kg), levocetirizine (0.6mg/kg, 1.2 mg/kg), loratadine (1 mg/kg, 2 mg/kg) and desloratidine (0.6 mg/kg, 1.2 mg/kg) are evaluated and compared for their effects on CNS using exptl. animal model (Pentobarbitone sleeping time, spontaneous motor activity, motor co-ordination) in Swiss albino mice. Results & Discussion: Desloratadine (0.6mg/kg, 1.2 mg/kg) and loratadine (1 mg/kg, 2 mg/kg) did not produce significant (P < 0.05) effect on sleeping time when compared to control. At 120 min time interval after treatment with cetirizine (1.2 mg/kg) and levocetirizine (1.2 mg/kg) was shown reduction in locomotor activity and remaining three drugs such as pheniramine (6 mg/kg), loratadine (2 mg/kg) and desloratadine did produced any effect on locomotor activity. Treatment with higher dose of pheniramine (6 mg/kg) and cetirizine (1.2 mg/kg) was shown significant (P<0.05) motor coordination while other drugs did not induce any motor in-coordination. First generation antihistamines were shown significant effect on CNS activity at low and high dose while only some second generation antihistamines showed significant effect on CNS at high dose. Conclusion: Numerous well-performed, sensitive measures of psychomotor and cognitive performances are needed to study to compare the effect of first generation and second generation antihistamines on CNS to avoid serious impairment of CNS function. The experimental process involved the reaction of N,N-Dimethyl-3-phenyl-3-(pyridin-2-yl)propan-1-amine maleate(cas: 132-20-7).SDS of cas: 132-20-7

The Article related to pheniramine maleate cetirizine antihistamine motor activity coordination, Pharmacology: Effects Of Nervous System- and Behavior-Affecting Drugs and Neuromuscular Agents and other aspects.SDS of cas: 132-20-7

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On December 31, 2011, Balhara, Yatan Pal Singh; Jain, Raka; Dhawan, Anju; Mehta, Manju published an article.Application In Synthesis of N,N-Dimethyl-3-phenyl-3-(pyridin-2-yl)propan-1-amine maleate The title of the article was A comparative study of pheniramine and lorazepam for physiological and cognitive/psychomotor task impairment. And the article contained the following:

Context: Pheniramine is being used harmfully in combination with opiates and benzodiazepines through injecting route. Aims: The present study is an attempt to compare the physiol. and psychomotor/cognitive task performance on pheniramine and lorazepam. Settings and Design: The study used a double blind randomly allotted cross-over design. Materials and Methods: The doses of the drugs used were placebo (normal saline) – 2 mL, Pheniramine maleate – 45.5 mg, Lorazepam – 2 mg. The assessments were made at base line and then at 15 min, 120 min and 240 min. The subjects were assessed for the socio-demog. profile, drug use history, physiol. parameters (pulse rate, BP, respiratory rate), and psychomotor/cognitive tasks. Statistical Anal. Used: Anal. was carried out using SPSS ver 10.0. In between, drug comparisons were done using one-way ANOVA (multiple comparisons). Results: Physiol. and cognitive/psychomotor tasks performance did not show any significant difference between pheniramine, lorazepam and placebo. Conclusions: The findings suggest the pheniramine and lorazepam have comparable impairment on physiol. and cognitive/psychomotor task performance. The experimental process involved the reaction of N,N-Dimethyl-3-phenyl-3-(pyridin-2-yl)propan-1-amine maleate(cas: 132-20-7).Application In Synthesis of N,N-Dimethyl-3-phenyl-3-(pyridin-2-yl)propan-1-amine maleate

The Article related to pheniramine maleate lorazepam cognition psychomotor impairment drug addiction, Pharmacology: Effects Of Nervous System- and Behavior-Affecting Drugs and Neuromuscular Agents and other aspects.Application In Synthesis of N,N-Dimethyl-3-phenyl-3-(pyridin-2-yl)propan-1-amine maleate

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Shravani, Bezawada; Anuradha, H. V.; Shivamurthy, M. C. published an article in 2017, the title of the article was Tramadol induced partial seizure: a rare adverse drug reaction – case report.Synthetic Route of 132-20-7 And the article contains the following content:

Tramadol is a synthetic codeine analog, acts at μ-opioid receptors (MOR) receptor and used to treat moderate pain with its onset of action being 10-15 min to 1 h and duration lasting upto 4-6 h. It inhibits uptake of norepinephrine and serotonin. It commonly causes vomiting, dry mouth sedation, very rarely seizures. Risk of seizure is more when used at high doses, abused for long time, used concomitantly with certain serotonergic or monoaminergic drugs and in patients with history of epilepsy. A 23 yr young unmarried female patient diagnosed as a case of Acute Pancreatitis and Systemic lupus erythematosis complained of severe low back pain and was prescribed one dose of Inj. Tramadol 50mg i.v. She developed jerky movements of the upper portion of her body involving the left arm and shoulder and uprolling of eye balls to one side after 10 min. This single episode lasted for about a minute and subsided thereafter immediately. Patient was conscious during the episode. No further such episodes noticed. No previous history of drug allergy or past and family history of seizures. No history of smoking, alc., drug abuse. No significant drug interactions were noted with inj. tramadol. This case illustrates that tramadol when used at low doses and without any predisposing risk factors as explained has the propensity to cause seizure. This reaction could be an idiosyncratic reaction. It alarms one to be more vigilant and monitor adverse reaction while prescribing various dose ranges of Tramadol. The experimental process involved the reaction of N,N-Dimethyl-3-phenyl-3-(pyridin-2-yl)propan-1-amine maleate(cas: 132-20-7).Synthetic Route of 132-20-7

The Article related to partial seizure acute pancreatitis systemic lupus erythematosis tramadol delivery, Pharmacology: Effects Of Nervous System- and Behavior-Affecting Drugs and Neuromuscular Agents and other aspects.Synthetic Route of 132-20-7

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On July 31, 2013, Beraki, Simret; Litrus, Lily; Soriano, Liza; Monbureau, Marie; To, Lillian K.; Braithwaite, Steven P.; Nikolich, Karoly; Urfer, Roman; Oksenberg, Donna; Shamloo, Mehrdad published an article.COA of Formula: C20H24N2O4 The title of the article was A pharmacological screening approach for discovery of neuroprotective compounds in ischemic stroke. And the article contained the following:

With the availability and ease of small mol. production and design continuing to improve, robust, high-throughput methods for screening are increasingly necessary to find pharmacol. relevant compounds amongst the masses of potential candidates. Here, we demonstrate that a primary oxygen glucose deprivation assay in primary cortical neurons followed by secondary assays (i.e. post-treatment protocol in organotypic hippocampal slice cultures and cortical neurons) can be used as a robust screen to identify neuroprotective compounds with potential therapeutic efficacy. In our screen about 50% of the compounds in a library of pharmacol. active compounds displayed some degree of neuroprotective activity if tested in a pre-treatment toxicity assay but just a few of these compounds, including Carbenoxolone, remained active when tested in a post-treatment protocol. When further examined, Carbenoxolone also led to a significant reduction in infarction size and neuronal damage in the ischemic penumbra when administered six hours post middle cerebral artery occlusion in rats. Pharmacol. testing of Carbenoxolone-related compounds, acting by inhibition of 11-β-hydroxysteroid dehydrogenase-1 (11β-HSD1), gave rise to similarly potent in vivo neuroprotection. This indicates that the increase of intracellular glucocorticoid levels mediated by 11β-HSD1 may be involved in the mechanism that exacerbates ischemic neuronal cell death and inhibiting this enzyme could have potential therapeutic value for neuroprotective therapies in ischemic stroke and other neurodegenerative disorders associated with neuronal injury. The experimental process involved the reaction of N,N-Dimethyl-3-phenyl-3-(pyridin-2-yl)propan-1-amine maleate(cas: 132-20-7).COA of Formula: C20H24N2O4

The Article related to ischemic stroke drug discovery screening neuroprotectant carbenoxolone brain injury, beta hydroxysteroid dehydrogenase, Pharmacology: Effects Of Nervous System- and Behavior-Affecting Drugs and Neuromuscular Agents and other aspects.COA of Formula: C20H24N2O4

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

On December 15, 2018, Moustani, Chrysavgi; Anagnostopoulou, Eleni; Krommyda, Kalliopi; Panopoulou, Christina; Koukoulakis, Konstantinos G.; Bakeas, Evangelos B.; Papadogianakis, Georgios published an article.Product Details of 636-73-7 The title of the article was Novel aqueous-phase hydrogenation reaction of the key biorefinery platform chemical levulinic acid into γ-valerolactone employing highly active, selective and stable water-soluble ruthenium catalysts modified with nitrogen-containing ligands. And the article contained the following:

High catalytic activities (TO = 000 -1) have been achieved by novel water-soluble ruthenium catalysts modified with nitrogen-containing ligands such as the bathophenanthrolinedisulfonic acid disodium salt (BPhDS) in the hydrogenation reaction of the renewable polar platform chem. levulinic acid (LA) which possesses a central relevance in the development of biorefineries of the future in a sustainable way to produce with essentially quant. selectivity of 99.9 mol% γ-valerolactone (GVL) in aqueous media. The apparent activation energy of the Ru/BPhDS catalyst was calculated and amounts a relative low value of 53.3 J/mol when one considers that in the LA hydrogenation reaction this catalyst reduces a less reactive keto group into alc. functionality. A recycling experiment of the Ru/BPhDS catalyst by extraction after addition of di-Et ether has shown that the catalyst is stable without loss of activity and selectivity in a consecutive run. The experimental process involved the reaction of Pyridine-3-sulfonic acid(cas: 636-73-7).Product Details of 636-73-7

The Article related to hydrogenation m levulinate gamma valerolactone catalyst, Industrial Organic Chemicals, Leather, Fats, and Waxes: Manufacture Of Industrial Organic Chemicals and other aspects.Product Details of 636-73-7

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem