Category: 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.; 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

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

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