Category: imidazoles-derivatives

On November 5, 2020, Rosen, Yael; Dangoor, David; Fisher, Richard published a patent.HPLC of Formula: 65896-14-2 The title of the patent was Methods of treating pruritus by topically administering an α-2 adrenoreceptor agonist. And the patent contained the following:

The present disclosure related to methods of treating pruritus in a subject by topically administering an α-2 adrenoreceptor agonist to a subject. The experimental process involved the reaction of N-(2-Bromo-6-fluorophenyl)-4,5-dihydro-1H-imidazol-2-amine hydrochloride(cas: 65896-14-2).HPLC of Formula: 65896-14-2

The Article related to pruritus treatment topical alpha2 adrenoreceptor agonist, Pharmacology: Other (All Agents and Effects Not Otherwise Assignable) and other aspects.HPLC of Formula: 65896-14-2

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

On August 31, 2015, Liu, Xiao-ping; Xu, Hui-lan; Sun, Rui; Li, Xue; Hu, Bao-hua; Hu, Chun published an article.Synthetic Route of 73590-85-9 The title of the article was Synthesis and characterization of two impurities in esomeprazole, an antiulcerative drug. And the article contained the following:

Impurity control is a key factor for drug quality. Study for impurities is helpful to optimize the production process and improve the quality of drugs. Synthesis and characterization of two of impurities in esomeprazole, which used for treatment of acid-related diseases was described in this paper. The two impurities are known as 2-[(3,5-dimethyl-4-methoxy-2-pyridinyl)methylsulfinyl]-1H-benzimidazole (impurity 1) and (R)-5-methoxy-2-[(4-methoxy-3,5-dimethylpyridin-2-yl)methylsulfinyl]-1H-benzimidazole (esomeprazole impurity F), whose structures are characterized with MS, IR, 1H-NMR and elemental analyses, and the purities of the two impurities are above 99% by HPLC anal. The two target compounds can be used as the reference substance of the impurities of esomeprazole. The experimental process involved the reaction of 5-Methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridyl)methyl]thio]benzimidazole(cas: 73590-85-9).Synthetic Route of 73590-85-9

The Article related to antiulcerative drug esomeprazole impurity acid disease, Pharmacology: Other (All Agents and Effects Not Otherwise Assignable) and other aspects.Synthetic Route of 73590-85-9

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

On January 25, 2021, Forrest, Michael D. published a patent.Related Products of 50743-01-6 The title of the patent was Therapeutic modifiers of the reverse mode of ATP synthase for treating diseases. And the patent contained the following:

Compounds that slow the ATP-hydrolyzing mode of ATP synthase are useful for treating various diseases and disorders including cancer, particularly cancers that utilize the Warburg effect. The experimental process involved the reaction of 5-Bromo-1H-imidazole-4-carbaldehyde(cas: 50743-01-6).Related Products of 50743-01-6

The Article related to atp synthase reverse mode modifier disease treatment, Pharmacology: Other (All Agents and Effects Not Otherwise Assignable) and other aspects.Related Products of 50743-01-6

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

On January 15, 2013, Si, Yuhui; Sun, Gangchun; Li, Zhicheng; Li, Yaping published an article.HPLC of Formula: 73590-85-9 The title of the article was Synthesis and resolution of omeprazole. And the article contained the following:

Omeprazole was synthesized and resolved by chiral resolution agent to obtain the S-isomer (Esomeprazole). The resolving conditions were as follows: S-(-)-1, 1′-Binaphthyl-2, 2′-diol, racemic omeprazole and alkali (molar ratio 1:1.6:1.8) reacted in ethanol and water (3.7:1 in v:v) at room temperature for 12 h. The magnesium salt of Esomeprazole was obtained in a high yield (89%) and excellent enantioselectivity (97.95% ee). The experimental process involved the reaction of 5-Methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridyl)methyl]thio]benzimidazole(cas: 73590-85-9).HPLC of Formula: 73590-85-9

The Article related to esomeprazole omeprazole synthesis chiral resolution, Pharmacology: Other (All Agents and Effects Not Otherwise Assignable) and other aspects.HPLC of Formula: 73590-85-9

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

On June 24, 2021, Machacek, Michelle; Altman, Michael D.; Huang, Chunhui; Reutershan, Michael H.; Sloman, David L.; Siliphaivanh, Phieng; Schneider, Sebastian E.; Yeung, Charles S.; Witter, David J.; Gibeau, Craig R.; Ye, Yingchun published a patent.Safety of 6-(Trifluoromethyl)-5,6,7,8-tetrahydroimidazo[1,2-a]pyridine-2-carboxylic acid The title of the patent was Protein-arginine N-methyltransferase PRMT5 inhibitors for therapy. And the patent contained the following:

The present invention provides compounds and pharmaceutically acceptable salts, esters, and prodrugs thereof, which are PRMT5 inhibitors. These compounds can treat cancer, sickle cell, and hereditary persistence of fetal Hb mutations. The experimental process involved the reaction of 6-(Trifluoromethyl)-5,6,7,8-tetrahydroimidazo[1,2-a]pyridine-2-carboxylic acid(cas: 1774893-22-9).Safety of 6-(Trifluoromethyl)-5,6,7,8-tetrahydroimidazo[1,2-a]pyridine-2-carboxylic acid

The Article related to methyltransferase prmt5 inhibitor pharmaceutical, Pharmacology: Other (All Agents and Effects Not Otherwise Assignable) and other aspects.Safety of 6-(Trifluoromethyl)-5,6,7,8-tetrahydroimidazo[1,2-a]pyridine-2-carboxylic acid

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

On April 1, 2020, Hilton-Proctor, J. P.; Ilyichova, O.; Zheng, Z.; Jennings, I. G.; Johnstone, R. W.; Shortt, J.; Mountford, S. J.; Scanlon, M. J.; Thompson, P. E. published an article.Formula: C6H11N3 The title of the article was Substituted 1-methyl-4-phenylpyrrolidin-2-ones – Fragment-based design of N-methylpyrrolidone-derived bromodomain inhibitors. And the article contained the following:

The synthesis of a 4-Ph substituted analog – 1-methyl-4-phenylpyrrolidin-2-one – and the use of aryl substitution reactions as a divergent route for derivatives I (R = H, Br, Ph, 2-phenylethyl, etc.; R1 = 2-Br, 4-Ph, morpholine-4-sulfonyl, etc.) were described. Ultimately, this has led to structurally complex, chiral compounds (R/S)-II (R2 = H, Me; R3 = H, 3,4-dimethoxyphenyl; R4 = H, N,N-diethylsulfamoyl) with progressively improved affinity as inhibitors of bromodomain-containing protein 4. The experimental process involved the reaction of N-(3-Aminopropyl)-imidazole(cas: 5036-48-6).Formula: C6H11N3

The Article related to methyl phenylpyrrolidinone preparation bromodomain inhibitor, brd4, bromodomain, epigenetics, fragment-based drug design, k-ac, Heterocyclic Compounds (One Hetero Atom): Pyrroles and Pyrrolizines and other aspects.Formula: C6H11N3

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

On February 10, 2010, Kent, Perry; Nguyen, Truong published a patent.Related Products of 5709-67-1 The title of the patent was High temperature thermal cutoff device. And the patent contained the following:

The present disclosure provides high temperature thermal cutoff devices having a high-temperature thermal pellet with a transition temperature of greater than or equal to ∼240° and comprising at least one organic compound The pellet is disposed in a housing, which is sealed with a high-temperature seal that provides substantial sealing up to at least the transition temperature The high-temperature TCO also has a current interruption assembly, which establishes elec. continuity in a 1st operating condition corresponding to an operating temperature of less than said transition temperature and discontinues elec. continuity when the operating temperature exceeds the transition temperature Methods of making such high-temperature thermal cut off devices are also provided. The experimental process involved the reaction of 2-Nitro-1H-benzo[d]imidazole(cas: 5709-67-1).Related Products of 5709-67-1

The Article related to thermal cutoff device high temperature organic compound, tco, Electric Phenomena: Conductors, Semiconductors, Resistors, Contacts and other aspects.Related Products of 5709-67-1

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

On September 30, 2009, Leece, Elizabeth A.; Girard, Nicolas M.; Maddern, Kieren published an article.Application In Synthesis of N-(2-Bromo-6-fluorophenyl)-4,5-dihydro-1H-imidazol-2-amine hydrochloride The title of the article was Alfaxalone in cyclodextrin for induction and maintenance of anesthesia in ponies undergoing field castration. And the article contained the following:

To evaluate the induction and maintenance of anesthesia using alfaxalone following pre-anesthetic medication with romifidine and butorphanol in ponies undergoing castration in the field. Prospective clin. study. Seventeen male ponies weighing 169 ± 29 kg. The ponies were sedated with romifidine and butorphanol i.v. Induction time was recorded following administration of alfaxalone 1 mg/kg-1 and diazepam 0.02 mg/kg-1 i.v. If movement during surgery occurred, alfaxalone 0.2 mg/kg-1 was administered i.v. The quality of anesthetic induction, and recovery were scored on a subjective scale of 1 (good) to 5 (poor). The number of attempts to attain sternal recumbency and standing, quality of recovery and times from induction to end of surgery, first head lift, sternal recumbency and standing were recorded. Induction quality was good [median score (range) 1 (1-3)] with a mean ±SD time of 29 ± 6 s taken to achieve lateral recumbency. Ten ponies required incremental doses of alfaxalone during surgery. Mean times to the end of surgery, first head lift, sternal recumbency and standing were 26 ± 9 min, 31 ± 9 min, 33 ± 9 min and 34 ± 9 min resp. The number of attempts to attain sternal recumbency was 1(1-1) and to attain standing was 1(1-2). Quality of recovery was good, with a recovery score of 1(1-2). Alfaxalone provided smooth induction and recovery characteristics and was considered suitable for maintenance of anesthesia for castration in ponies. The experimental process involved the reaction of N-(2-Bromo-6-fluorophenyl)-4,5-dihydro-1H-imidazol-2-amine hydrochloride(cas: 65896-14-2).Application In Synthesis of N-(2-Bromo-6-fluorophenyl)-4,5-dihydro-1H-imidazol-2-amine hydrochloride

The Article related to alfaxan cyclodextrin anesthesia horse anesthetic, Mammalian Hormones: Corticosteroid, Gonadal, and Placental Hormones and other aspects.Application In Synthesis of N-(2-Bromo-6-fluorophenyl)-4,5-dihydro-1H-imidazol-2-amine hydrochloride

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

On May 31, 1982, Rastogi, Rashmi; Sharma, Satyavan published an article.Computed Properties of 5709-67-1 The title of the article was Synthesis of 2-substituted benzofurans as potential anthelmintics. And the article contained the following:

Thirteen title compounds, e.g. I (R = 2-O2NC6H4, 2-H2NC6H4, 2-benzimidazolyl) and II (X = NH, S), were prepared starting from 2-benzofurancarbonyl chloride. The title compounds were tested as anthelmintics, bactericides, and fungicides and found to be inactive. The experimental process involved the reaction of 2-Nitro-1H-benzo[d]imidazole(cas: 5709-67-1).Computed Properties of 5709-67-1

The Article related to benzofuran substituted preparation anthelmintic, bactericide substituted benzofuran, fungicide substituted benzofuran, benzimidazolylbenzofuran, benzothiazolylbenzofuran, Heterocyclic Compounds (One Hetero Atom): Areno- and Diarenofurans and other aspects.Computed Properties of 5709-67-1

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

On August 31, 2022, Xu, Xinqi; Zhang, Yajiao; Wang, Shaoyu; Xu, Lian; Su, Bingmei; Wang, Lichao; Lin, Juan published an article.SDS of cas: 73590-85-9 The title of the article was Nonpolarity paving in substrate tunnel of a Limnobacter sp. Phenylacetone monooxygenase for efficient single whole-cell synthesis of esomeprazole. And the article contained the following:

Baeyer-Villiger monooxygenase (BVMO) mediated sulfoxidation is a sustainable approach for the synthesis of esomeprazole. In this work, a novel phenylacetone monooxygenase from Limnobacter sp. (LnPAMO) was found to have trace activity for synthesis of enantiopure esomeprazole. Through engineering in the substrate tunnel using a mutagenesis strategy called “nonpolarity paving” and some modifications in cofactor binding domains, a mutant harboring 15 mutations (LnPAMO Mu15) was obtained with 6.6 x 103-fold higher activity to convert omeprazole sulfide into esomeprazole. The activities of the mutant for synthesis of (S)-Me Ph sulfoxide and (S)-pantoprazole also increased much, indicating the versatility of the mutant for sulfoxide synthesis. Importantly, no over-oxidation byproduct omeprazole sulfone was detected in the sulfoxidation products by both mass spectrometry and HPLC anal. Then NADP-dependent Burkholderia stabili formate dehydrogenase was ligated behind Mu15 along with a ribosome binding site sequence in pET-28a for co-expression. By single whole-cell of recombinant Escherichia coli BL21 coexpressing Mu15 and formate dehydrogenase, omeprazole sulfide was efficiently converted into esomeprazole without production of sulfone (16 g/L substrate, enantiomeric excess > 99.9% (S) and > 99% conversion) and the space-time-yield reached 1.67 g product/L/h. The experimental process involved the reaction of 5-Methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridyl)methyl]thio]benzimidazole(cas: 73590-85-9).SDS of cas: 73590-85-9

The Article related to esomeprazole limnobacter phenylacetone monooxygenase whole cell synthesis, esomeprazole, phenylacetone monooxygenase, single-cell sulfoxidation, substrate tunnel, Fermentation and Bioindustrial Chemistry: Fermentation Engineering and other aspects.SDS of cas: 73590-85-9

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem