METHOD FOR PREPARING MORPHINAN DERIVATIVE HAVING DIARYL ETHER SKELETON USING NOVEL COPPER CATALYST

    公开(公告)号:US20230312570A1

    公开(公告)日:2023-10-05

    申请号:US18023461

    申请日:2021-08-27

    发明人: Masaaki HIROSE

    IPC分类号: C07D471/08 B01J23/72

    CPC分类号: C07D471/08 B01J23/72

    摘要: Provided is a method which is for preparing a morphinan derivative having a diaryl ether skeleton represented by general formula (III) (In the formula, R1 represents a hydrogen atom, etc., R2, R3, and R4 are the same or different and each represent a hydrogen atom, or an arbitrary substituent, etc., R5 represent a hydrogen atom, a hydroxy group, etc., R14 and R15 are the same or different and each represent a hydrogen atom, or an arbitrary substituent, etc.), and in which a phenyl group is introduced into the 4-position phenol of a morphinan derivative through the Ullmann reaction of a system using a monovalent copper compound or a novel catalytic system simultaneously using a monovalent copper compound and zero-valent metallic copper.

    METHOD FOR PRODUCING MORPHINAN DERIVATIVE

    公开(公告)号:US20220267327A1

    公开(公告)日:2022-08-25

    申请号:US17626697

    申请日:2020-07-17

    IPC分类号: C07D471/08

    摘要: Provided is, for example, a method for producing a morphinan derivative represented by General Formula (II), including the step of: allowing metal sodium and ethylenediamine to act on a morphinan derivative represented by General Formula (I) in presence of an auxiliary solvent. wherein R1 represents a hydrogen atom, or a C1-10 alkyl group, a C3-6 cycloalkyl group, a C2-6 alkenyl group, a C6-10 aryl group, or a heteroaryl group optionally having a substituent, R2 represents an amino protecting group, R3 represents a methoxy group, R4 and R5 represent a hydrogen atom or a hydroxy group, R6 and R7 represent a hydrogen atom or an electron-donating group, wherein R6 and R7 are not simultaneously a hydrogen atom, and X represents O or CH2.

    AGENT FOR IMPROVING QUALITY OF SLEEP

    公开(公告)号:US20210369654A1

    公开(公告)日:2021-12-02

    申请号:US17285264

    申请日:2019-10-16

    IPC分类号: A61K31/194 A23L33/10

    摘要: The present invention provides a food composition or pharmaceutical composition which includes, as an active ingredient, at least one substance selected from the group consisting of citric acid and a salt thereof, or sodium bicarbonate. Ingestion or administration of the food composition or pharmaceutical composition leads to an improvement in quality of sleep.

    VOLTAGE-DEPENDENT T-TYPE CALCIUM CHANNEL INHIBITOR

    公开(公告)号:US20210323930A1

    公开(公告)日:2021-10-21

    申请号:US16479674

    申请日:2018-01-22

    摘要: A compound represented by General Formula (I), a tautomer, a stereoisomer, or a pharmaceutically acceptable salt of the compound, or a solvate thereof is used as a voltage-dependent T-type calcium channel inhibitor, in the formula, A represents a benzene ring which may have a substituent or the like; B represents a hetero-fused ring consisting of a 5- or 6-membered heteroaryl ring having one to three same or different heteroatoms selected from an oxygen atom, a sulfur atom, and a nitrogen atom, and a carbon atom, as a ring-constituting atom, and a benzene ring, or the like, and the hetero-fused ring may have a substituent, and is bonded to a cyclopropyl group via a carbon atom constituting these rings; R1 represents a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, or the like; R2 and R3 may be the same as or different from each other, and each represents a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, or the like, or R2 and R3 together form CH2CH2 or the like; R4 represents a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, or the like; m represents 0, 1, or 2; and n represents 0 or 1.

    MEDICAMENT FOR TREATING COUGH
    10.
    发明申请

    公开(公告)号:US20210000840A1

    公开(公告)日:2021-01-07

    申请号:US16979383

    申请日:2019-03-14

    IPC分类号: A61K31/551

    摘要: The present invention pertains to a medicament for preventing or treating cough, including, as an active ingredient, a compound having P2X4 receptor antagonistic action, a tautomer, stereoisomer, or pharmaceutically acceptable salt of the compound, or a hydrate or solvate thereof.