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