Kobayashi, Jun-ichi et al. published their research in Bioorganic & Medicinal Chemistry in 2021 |CAS: 1459793-02-2

The Article related to trpm8 antagonist adverse event, cyp3a4 induction, oab, phenylglycinamide, reactive metabolite, trpm8, trpm8 antagonist, Pharmacology: Drug Interactions and General Pharmacology and other aspects.Recommanded Product: 1459793-02-2

On January 15, 2021, Kobayashi, Jun-ichi; Hirasawa, Hideaki; Fujimori, Yoshikazu; Nakanishi, Osamu; Kamada, Noboru; Ikeda, Tetsuya; Yamamoto, Akitoshi; Kanbe, Hiroki published an article.Recommanded Product: 1459793-02-2 The title of the article was Identification of N-acyl-N-indanyl-α-phenylglycinamides as selective TRPM8 antagonists designed to mitigate the risk of adverse effects. And the article contained the following:

Transient receptor potential melastatin 8 (TRPM8), a temperature-sensitive ion channel responsible for detecting cold, is an attractive mol. target for the treatment of pain and other disorders. We have previously discovered a selective TRPM8 antagonist, KPR-2579, which inhibited bladder afferent hyperactivity induced by acetic acid instillation into the bladder. However, addnl. studies have revealed potential adverse effects with KPR-2579, such as the formation of a reactive metabolite, CYP3A4 induction, and convulsions. In this report, we describe the optimization of α-phenylglycinamide derivatives to mitigate the risk of these adverse effects. The optimal compound 13x exhibited potent inhibition against icilin-induced wet-dog shakes and cold-induced frequent voiding in rats, with a wide safety margin against the potential side effects. The experimental process involved the reaction of (S)-2,3-Dihydrobenzofuran-3-amine hydrochloride(cas: 1459793-02-2).Recommanded Product: 1459793-02-2

The Article related to trpm8 antagonist adverse event, cyp3a4 induction, oab, phenylglycinamide, reactive metabolite, trpm8, trpm8 antagonist, Pharmacology: Drug Interactions and General Pharmacology and other aspects.Recommanded Product: 1459793-02-2

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Rochette, Elise M. et al. published their research in Chemical Communications (Cambridge, United Kingdom) in 2013 |CAS: 1459793-02-2

The Article related to chiral sulfinimide radical stereoselective cyclization, General Organic Chemistry: Synthetic Methods and other aspects.Formula: C8H10ClNO

Rochette, Elise M.; Lewis, William; Dossetter, Al G.; Stockman, Robert A. published an article in 2013, the title of the article was Highly diastereoselective radical cyclisations of chiral sulfinimines.Formula: C8H10ClNO And the article contains the following content:

Chiral amines are formed by the highly diastereoselective intramol. addition of alkyl and aryl radicals onto chiral mesityl sulfinimines. The experimental process involved the reaction of (S)-2,3-Dihydrobenzofuran-3-amine hydrochloride(cas: 1459793-02-2).Formula: C8H10ClNO

The Article related to chiral sulfinimide radical stereoselective cyclization, General Organic Chemistry: Synthetic Methods and other aspects.Formula: C8H10ClNO

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Nakanishi, Teruo et al. published their research in Seikagaku in 1970 |CAS: 29735-85-1

The Article related to benzofurans inhibition deaminases, deaminases inhibition benzofurans, inhibition deaminases benzofurans, amp deaminase inhibition benzofurans, and other aspects.Quality Control of 5-Hydroxybenzofuran-3-carboxylic acid

Nakanishi, Teruo; Saeki, Toru published an article in 1970, the title of the article was Inhibitory action of benzofuran compounds on 5′-AMP deaminase and adenosine deaminase.Quality Control of 5-Hydroxybenzofuran-3-carboxylic acid And the article contains the following content:

The inhibitory action of benzofuran derivatives on 5′-AMP deaminase (I) and adenosine deaminase (II) was investigated by using a number of synthetic compounds Introduction of carboxyl or hydroxyl groups increased the inhibitory action on I, but no pronounced effect of the substituent was observed on II. No common feature in structure seems to exist for the inhibition of these 2 deaminases. The experimental process involved the reaction of 5-Hydroxybenzofuran-3-carboxylic acid(cas: 29735-85-1).Quality Control of 5-Hydroxybenzofuran-3-carboxylic acid

The Article related to benzofurans inhibition deaminases, deaminases inhibition benzofurans, inhibition deaminases benzofurans, amp deaminase inhibition benzofurans, and other aspects.Quality Control of 5-Hydroxybenzofuran-3-carboxylic acid

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Andrews, Mark et al. published their patent in 2021 |CAS: 29735-85-1

The Article related to heteroaryl aryl amidoamide preparation il17 modulator, Heterocyclic Compounds (More Than One Hetero Atom): Other 5-Membered Rings, Two Or More Hetero Atoms and other aspects.Recommanded Product: 29735-85-1

On December 16, 2021, Andrews, Mark; Soerensen, Morten Dahl; Larsen, Mogens; Devaux, Nicolas; Barros Ribeiro da Silva, Vicinius; Perron, Quentin; Liang, Xifu; Seitzberg, Jimmi Gerner published a patent.Recommanded Product: 29735-85-1 The title of the patent was N-Heteroaryl and N-aryl amidoamides as small molecule modulators of IL-17 and their preparation. And the patent contained the following:

The invention relates to a compound according to formula I and pharmaceutically acceptable salts, hydrates, or solvates thereof. The invention further relates to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating diseases, e.g. dermal diseases, with said compounds, and to the use of said compounds in the manufacture of medicaments. Compounds of formula I wherein X, Y, Z and V are independently N, CH and CR4; R1 is (un)substituted C1-4 alkyl, (un)substituted C3-7 cycloalkyl, C1-6 alkoxy, (un)substituted Ph, etc.; R2 is (un)substituted 5- to 6-membered heteroaryl; R3 is CHR5R6, (un)substituted C3-10 cycloalkyl, (un)substituted tetrahydronaphthyl, etc.; R4 is (un)substituted C1-6 alkyl, (un)substituted C1-6 alkoxy, OH, NH2 and halo; R5 and R6 are independently H, (un)substituted Ph, (un)substituted C1-6 alkyl, (un)substituted C3-7 cycloalkyl, etc.; and pharmaceutically acceptable salts, hydrates and solvates thereof, are claimed. Example compound II was prepared by deprotection of N-[(1S)-1-(dicyclopropylmethyl)-2-[[5-[3,5-dimethyl-1-(2-trimethylsilylethoxymethyl)pyrazol-4-yl]-6-fluoro-2-pyridyl]amino]-2-oxo-ethyl]-2-isopropylpyrazole-3-carboxamide. The invention compounds were evaluated for their IL-17 modulatory activity. From the assay, it was determined that compound II exhibited EC50 value of 15 nM. The experimental process involved the reaction of 5-Hydroxybenzofuran-3-carboxylic acid(cas: 29735-85-1).Recommanded Product: 29735-85-1

The Article related to heteroaryl aryl amidoamide preparation il17 modulator, Heterocyclic Compounds (More Than One Hetero Atom): Other 5-Membered Rings, Two Or More Hetero Atoms and other aspects.Recommanded Product: 29735-85-1

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Hirasawa, Hideaki et al. published their patent in 2016 |CAS: 1459793-02-2

The Article related to glycine amide preparation trpm8 inhibitor, nerve hyperexcitability disease treatment glycine amide trpm8 inhibition, Pharmacology: Other (All Agents and Effects Not Otherwise Assignable) and other aspects.Application In Synthesis of (S)-2,3-Dihydrobenzofuran-3-amine hydrochloride

On May 26, 2016, Hirasawa, Hideaki; Kawamura, Naohiro; Kobayashi, Junichi published a patent.Application In Synthesis of (S)-2,3-Dihydrobenzofuran-3-amine hydrochloride The title of the patent was TRPMB inhibitors containing α-substituted glycine amides. And the patent contained the following:

Disclosed is a pharmaceutical composition containing a compound I [A1 = C6-10 aryl (optionally substituted with halo, hydroxy, C1-6 alkyl, etc.), 5-membered heterocyclyl (optionally substituted with halo, hydroxy, C1-6 alkyl, etc.) or 6-membered heterocyclyl (optionally substituted with halo, hydroxy, C1-6 alkyl, etc.); A2 = C6-10 aryl (optionally substituted with halo, hydroxy, C1-6 alkyl, etc.), heterocyclyl (optionally substituted with halo, hydroxy, C1-6 alkyl, etc.) or C3-6 cycloalkyl; X = CH or N; Y = -CR1R2- or oxygen atom; R1, R2 = independently H, halo or C1-6 alkyl; R3, R4 = independently H, halo, C1-6 alkyl, etc., wherein R3 and R4 cannot be H together when X = CH and R1 = R2 = H; n = 1 or 2], or pharmaceutically acceptable salt thereof as an active component. The composition is claimed useful for the treatment of diseases or conditions associated with afferent nerve hyperexcitability or injury, e.g. LUTS (lower urinary tract symptoms). For example, a compound (II) showed potent inhibitory effect on icilin-induced wet-dog shaking in rat. The experimental process involved the reaction of (S)-2,3-Dihydrobenzofuran-3-amine hydrochloride(cas: 1459793-02-2).Application In Synthesis of (S)-2,3-Dihydrobenzofuran-3-amine hydrochloride

The Article related to glycine amide preparation trpm8 inhibitor, nerve hyperexcitability disease treatment glycine amide trpm8 inhibition, Pharmacology: Other (All Agents and Effects Not Otherwise Assignable) and other aspects.Application In Synthesis of (S)-2,3-Dihydrobenzofuran-3-amine hydrochloride

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Cheng, Jie Fei et al. published their patent in 2005 |CAS: 29735-85-1

The Article related to heterocyclic compound preparation malonyl coa decarboxylase inhibitor, cardiovascular disease prophylaxis management treatment heterocyclic compound, diabetes prophylaxis management treatment heterocyclic compound, cancer prophylaxis management treatment heterocyclic compound, obesity prophylaxis management treatment heterocyclic compound and other aspects.Product Details of 29735-85-1

On February 3, 2005, Cheng, Jie Fei; Nguyen, Bao Ngoc; Liu, Xuewei; Lopaschuk, Gary D.; Dyck, Jason R. published a patent.Product Details of 29735-85-1 The title of the patent was Preparation of heterocyclic compounds useful as malonyl-CoA decarboxylase inhibitors. And the patent contained the following:

The present invention provides methods for the use of compounds I [X1, X2, X3 = O, N, NH, NR5, S, C; R1, R2 = H, halogen, substituted C1-6-alkyl, substituted C1-6-alkenyl, substituted C1-6-alkynyl, alkoxy, (un)substituted Ph, aryl, (un)substituted heteroaryl, NHCONR5R6, COR5, CONR5R6, S(O)nR5, SO2NR5R6; R3, R4 = H, Br, Cl, F, I, OH, OMe, CO2H, CO2R5, CONR5R6, S(O)nR5, SO2NR5R6, substituted C1-6-alkyl, C1-6-alkoxy, (un)substituted Ph, aryl, heteroaryl; R5, R6 = H, (un)substituted C1-6-alkyl, (un)substituted Ph, aryl, heteroaryl], its enantiomers, diastereomers, tautomers, or physiol. acceptable salts or prodrugs, pharmaceutical compositions containing the same, and methods for the prophylaxis, management and treatment of metabolic diseases and diseases modulated by MCD inhibition. Thus, benzofuran I [X1 = CC(:O)NHC6H3(OMe)2-3,4, X2 = CH, X3 = O, R3 = 4-Br, R4 = 6-Br] was prepared from 5-methoxybenzofuran-2-carboxylic acid via regioselective bromination at C(3), decarboxylation, debromination-carboxylation at C(3), O-demethylation, regioselective dibromination and amidation with 3,4-dimethoxyaniline. The compounds disclosed in this invention are useful for the prophylaxis, management and treatment of diseases involving in malonyl-CoA regulated glucose/fatty acid metabolism pathway. The inhibitory activity of I vs. malonyl-CoA decarboxylase was determined [Ki = 31.6 – 4750.2 μM]. In particular, these compounds and pharmaceutical composition containing the same are indicated in the prophylaxis, management and treatment of cardiovascular diseases, diabetes, cancer and obesity. The experimental process involved the reaction of 5-Hydroxybenzofuran-3-carboxylic acid(cas: 29735-85-1).Product Details of 29735-85-1

The Article related to heterocyclic compound preparation malonyl coa decarboxylase inhibitor, cardiovascular disease prophylaxis management treatment heterocyclic compound, diabetes prophylaxis management treatment heterocyclic compound, cancer prophylaxis management treatment heterocyclic compound, obesity prophylaxis management treatment heterocyclic compound and other aspects.Product Details of 29735-85-1

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Hirasawa, Hideaki et al. published their patent in 2014 |CAS: 1459793-02-2

The Article related to glycine amide preparation trpm8 inhibitor, nerve hyperexcitability disease treatment glycine amide trpm8 inhibition, Benzene, Its Derivatives, and Condensed Benzenoid Compounds: Benzocyclopropenes, Benzocyclobutenes, and Indenes and other aspects.Product Details of 1459793-02-2

On November 13, 2014, Hirasawa, Hideaki; Kawamura, Naohiro; Kobayashi, Junichi published a patent.Product Details of 1459793-02-2 The title of the patent was Preparation of α-substituted glycine amides as TRPM8 inhibitors. And the patent contained the following:

Title compounds I [A1 = C6-10 aryl (optionally substituted with halo, hydroxy, C1-6 alkyl, etc.), 5-membered heterocyclyl (optionally substituted with halo, hydroxy, C1-6 alkyl, etc.) or 6-membered heterocyclyl (optionally substituted with halo, hydroxy, C1-6 alkyl, etc.); A2 = C6-10 aryl (optionally substituted with halo, hydroxy, C1-6 alkyl, etc.), heterocyclyl (optionally substituted with halo, hydroxy, C1-6 alkyl, etc.) or C3-6 cycloalkyl; X = CH or N; Y = -CR1R2- or oxygen atom; R1, R2 = independently H, halo or C1-6 alkyl; R3, R4 = independently H, halo, C1-6 alkyl, etc.; n = 1 or 2; or pharmacol. acceptable salts thereof] were prepared For example, to a solution of (R)-4,6-difluoroindan-1-ylamine (0.1 g) in methanol (1 mL) was added benzaldehyde (0.063 g), the resulting mixture was stirred at 60° for 1 h, treated with nicotinic acid (0.073 g) and 4-phenylcyclohexen-1-ylisocyanide (0.108 g) [room temperature → 60° (overnight)], cooled to room temperature, concentrated in vacuo, and treated with THF (3 mL), water (12 μL) and HCl (4 mol/L in dioxane, 440 μL) at room temperature for 1.5 h to give, after work-up, compound II (0.076 g). The invention compounds showed potent inhibitory effect on icilin-induced wet-dog shaking in rat. Compounds I are claimed useful for the treatment of diseases or conditions associated with afferent nerve hyperexcitability or injury. The experimental process involved the reaction of (S)-2,3-Dihydrobenzofuran-3-amine hydrochloride(cas: 1459793-02-2).Product Details of 1459793-02-2

The Article related to glycine amide preparation trpm8 inhibitor, nerve hyperexcitability disease treatment glycine amide trpm8 inhibition, Benzene, Its Derivatives, and Condensed Benzenoid Compounds: Benzocyclopropenes, Benzocyclobutenes, and Indenes and other aspects.Product Details of 1459793-02-2

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Lena, Gersande’s team published research in Journal of Medicinal Chemistry in 2008 | CAS: 53860-74-5

6-Methoxybenzofuran-2-carbaldehyde(cas: 53860-74-5) belongs to benzofurans.SDS of cas: 53860-74-5Benzofurans containing one furan ring that have been implicated as psychoactive recreational drugs include 6-(2-aminopropyl)benzofuran (6-APB), 5-(2-aminopropyl)benzofuran (5-APB), 5-(2-ethylaminopropyl)benzofuran (5-EAPB), and 5-methylaminopropylbenzofuran (5-MAPB).

Lena, Gersande; Trapani, Joseph A.; Sutton, Vivien R.; Ciccone, Annette; Browne, Kylie A.; Smyth, Mark J.; Denny, William A.; Spicer, Julie A. published their research in Journal of Medicinal Chemistry on December 11 ,2008. The article was titled 《Dihydrofuro[3,4-c]pyridinones as Inhibitors of the Cytolytic Effects of the Pore-Forming Glycoprotein Perforin》.SDS of cas: 53860-74-5 The article contains the following contents:

Dihydrofuro[3,4-c]pyridinones are the first class of small mols. reported to inhibit the cytolytic effects of the lymphocyte toxin perforin. A lead structure was identified from a high throughput screen, and a series of analogs I (X = O, S; Y = O, NH; R = Ph, 4-FC6H4, 2-furyl, 5-methyl-2-thienyl, 3-thienyl, 2-benzofuryl, 3-benzothienyl, 3-indolyl, etc.) were designed and prepared to explore structure-activity relationships around the core bicyclic ring and pendant aryl(heteroaryl) ring. This resulted in the identification of a submicromolar inhibitor of the perforin-induced lysis of Jurkat T-lymphoma cells. After reading the article, we found that the author used 6-Methoxybenzofuran-2-carbaldehyde(cas: 53860-74-5SDS of cas: 53860-74-5)

6-Methoxybenzofuran-2-carbaldehyde(cas: 53860-74-5) belongs to benzofurans.SDS of cas: 53860-74-5Benzofurans containing one furan ring that have been implicated as psychoactive recreational drugs include 6-(2-aminopropyl)benzofuran (6-APB), 5-(2-aminopropyl)benzofuran (5-APB), 5-(2-ethylaminopropyl)benzofuran (5-EAPB), and 5-methylaminopropylbenzofuran (5-MAPB).

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Hirota, Takashi’s team published research in Journal of Heterocyclic Chemistry in 1986 | CAS: 53860-74-5

6-Methoxybenzofuran-2-carbaldehyde(cas: 53860-74-5) belongs to benzofurans.Application of 53860-74-5Benzofurans containing one furan ring that have been implicated as psychoactive recreational drugs include 6-(2-aminopropyl)benzofuran (6-APB), 5-(2-aminopropyl)benzofuran (5-APB), 5-(2-ethylaminopropyl)benzofuran (5-EAPB), and 5-methylaminopropylbenzofuran (5-MAPB).

Hirota, Takashi; Fujita, Hiroko; Sasaki, Kenji; Namba, Tetsuto published their research in Journal of Heterocyclic Chemistry on December 31 ,1986. The article was titled 《A novel synthesis of benzofuran and related compounds. III. The Vilsmeier reaction of phenoxyacetaldehyde diethyl acetals》.Application of 53860-74-5 The article contains the following contents:

2-Benzofurancarboxaldehydes, e.g., I (R = H, OMe; R1 = OMe, OEt, NEt2) were prepared in 15-58% yields by the Vilsmeier reaction 3,5-RR1C6H3OCH2CH(OEt)2 (II). A rare geminidiol III was isolated in one case. II were prepared in 65-91% yields by treating 3,5-RR1C6H3ONa with BrCH2CH(OEt)2. In the experiment, the researchers used 6-Methoxybenzofuran-2-carbaldehyde(cas: 53860-74-5Application of 53860-74-5)

6-Methoxybenzofuran-2-carbaldehyde(cas: 53860-74-5) belongs to benzofurans.Application of 53860-74-5Benzofurans containing one furan ring that have been implicated as psychoactive recreational drugs include 6-(2-aminopropyl)benzofuran (6-APB), 5-(2-aminopropyl)benzofuran (5-APB), 5-(2-ethylaminopropyl)benzofuran (5-EAPB), and 5-methylaminopropylbenzofuran (5-MAPB).

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem

Fatome, Marc’s team published research in European Journal of Medicinal Chemistry in 1977 | CAS: 53860-74-5

6-Methoxybenzofuran-2-carbaldehyde(cas: 53860-74-5) belongs to benzofurans.Safety of 6-Methoxybenzofuran-2-carbaldehydeBenzofurans containing one furan ring that have been implicated as psychoactive recreational drugs include 6-(2-aminopropyl)benzofuran (6-APB), 5-(2-aminopropyl)benzofuran (5-APB), 5-(2-ethylaminopropyl)benzofuran (5-EAPB), and 5-methylaminopropylbenzofuran (5-MAPB).

In 1977,European Journal of Medicinal Chemistry included an article by Fatome, Marc; Andrieu, Louis; Laval, Jean Denis; Clavel, Jean Marc; Blanco, Luis; Guillaumel, Jean; Rene, Loic; Royer, Rene. Safety of 6-Methoxybenzofuran-2-carbaldehyde. The article was titled 《Comparison of radioprotective activities of similar substituted derivatives of benzofurane and 2H-chromene》. The information in the text is summarized as follows:

The radioprotective activities of I(R1, R2, R3, R4 = H, OMe; Z = MeCO, CHO, CN, CO2Et) were less than those of II (same substituents as I). In the experiment, the researchers used many compounds, for example, 6-Methoxybenzofuran-2-carbaldehyde(cas: 53860-74-5Safety of 6-Methoxybenzofuran-2-carbaldehyde)

6-Methoxybenzofuran-2-carbaldehyde(cas: 53860-74-5) belongs to benzofurans.Safety of 6-Methoxybenzofuran-2-carbaldehydeBenzofurans containing one furan ring that have been implicated as psychoactive recreational drugs include 6-(2-aminopropyl)benzofuran (6-APB), 5-(2-aminopropyl)benzofuran (5-APB), 5-(2-ethylaminopropyl)benzofuran (5-EAPB), and 5-methylaminopropylbenzofuran (5-MAPB).

Referemce:
Benzofuran – Wikipedia,
Benzofuran | C8H6O – PubChem