EPOXY AZEPANE DERIVATIVE

• Main Authors: HAYASHIDA KOHEI, YAMAMOTO KOHEI, NAMIKI MAYU, SAITO DAISUKE, WATANABE YOSHIKAZU, MOGI YUZO
• Format: Patent
• Language: English; Japanese
• Published: 01.02.2023
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

To provide a morphinan derivative having an opioidκ receptor agonist action.SOLUTION: Disclosed are an azepane derivative represented by formula (I) and a pharmaceutically accepted salt thereof (in the formula, R1, R2, R3, R4 and R5 are H, C1-6 alkyl and the like, respectively; R6 is H, C1-6 alkoxy; R7, R8, R9, R10, R11 are H, C1-6 alkyl and the like, respectively; A and B are methylene, carbonyl and the like respectively, different from each other; X is N or N-oxide; Y is methylene, carbonyl or thiocarbonyl; Z is NR15, O and the like; R15 is H, C1-6 alkyl and the like; m is integer of 0 to 1; and n is integer of 0 to 3).SELECTED DRAWING: None 【課題】オピオイドκ受容体アゴニスト作用を有するモルヒナン誘導体の提供。【解決手段】式（Ｉ）で表されるアゼパン誘導体及びその薬学的に許容される塩。JPEG2023015414000142.jpg4994（Ｒ１はＨ、Ｃ１－６アルキル基等、Ｒ２及びＲ３はＨ、Ｃ１－６アルキル基等、Ｒ４及びＲ５はＨ、Ｃ１－６アルキル基等、Ｒ６はＨ、Ｃ１－６アルコキシ基等、Ｒ７及びＲ８はＨ、Ｃ１－６アルキル基等、Ｒ９及びＲ１０はＨ、Ｃ１－６アルキル基等、Ｒ１１はＨ、Ｃ１－６アルキル基等、Ａ及びＢは異なってメチレン基、カルボニル基等、ＸはＮ又はＮ－オキシド、Ｙはメチレン基、カルボニル基又はチオカルボニル基、ＺはＮＲ１５、Ｏ等、Ｒ１５はＨ、Ｃ１－６アルキル基等、ｍは０～１の整数、ｎは０～３の整数。）【選択図】なし