COMPOUND OR SALT THEREOF AND LIPID PARTICLES

    公开(公告)号:US20210085604A1

    公开(公告)日:2021-03-25

    申请号:US17112239

    申请日:2020-12-04

    Abstract: An object of the present invention is to provide a compound or a salt thereof constituting lipid particles that can achieve a high nucleic acid encapsulation rate and excellent delivery of nucleic acids, and to provide lipid particles that can achieve a high nucleic acid encapsulation rate and excellent delivery of nucleic acids. According to an aspect of the present invention, a compound represented by Formula (1) or a salt thereof is provided. In the formula, X represents —NR1— or —O—, R represents a hydrogen atom, a hydrocarbon group, or the like, R2 and R3 each independently represent a hydrogen atom, a hydrocarbon group, or the like, R4, R5, R6, R7, R8, R9, R10, R11, and R12 each independently represent a hydrogen atom or an alkyl group, groups in any one or more pairs among R4 and R5, R10 and R5, R5 and R12, R4 and R6, R5 and R6, R6 and R7, R6 and R10, R12 and R7, and R7 and R8 may be linked to each other to form a 4- to 7-membered ring which may contain an O atom, a, b, c, and d are each independently represent an integer of 0 to 3, a+b is equal to or greater than 1, and c+d is equal to or greater than 1.

    COMPOUND OR SALT THEREOF AND LIPID PARTICLES

    公开(公告)号:US20240315970A1

    公开(公告)日:2024-09-26

    申请号:US18443959

    申请日:2024-02-16

    CPC classification number: A61K9/1272 A61K9/1278 C07C219/06 C12N15/88

    Abstract: An object of the present invention is to provide a compound or a salt thereof constituting lipid particles that can achieve a high nucleic acid encapsulation rate and excellent delivery of nucleic acids, and to provide lipid particles that can achieve a high nucleic acid encapsulation rate and excellent delivery of nucleic acids. According to an aspect of the present invention, a compound represented by Formula (1) or a salt thereof is provided.




    In the formula, X represents —NR1— or —O—, R1 represents a hydrogen atom, a hydrocarbon group, or the like, R2 and R3 each independently represent a hydrogen atom, a hydrocarbon group, or the like, R4, R5, R6, R7, R8, R9, R10, R11, and R12 each independently represent a hydrogen atom or an alkyl group,



    groups in any one or more pairs among R4 and R5, R10 and R5, R5 and R12, R4 and R6, R5 and R6, R6 and R7, R6 and R10, R12 and R7, and R7 and R8 may be linked to each other to form a 4- to 7-membered ring which may contain an O atom, a, b, c, and d are each independently represent an integer of 0 to 3, a+b is equal to or greater than 1, and c+d is equal to or greater than 1.

    METHOD FOR PRODUCING N-(HETERO)ARYL (METH)ACRYLAMIDE COMPOUND

    公开(公告)号:US20240051916A1

    公开(公告)日:2024-02-15

    申请号:US18488978

    申请日:2023-10-17

    CPC classification number: C07C231/02

    Abstract: Provided is a method for producing an N-(hetero)aryl (meth)acrylamide compound, including reacting a compound represented by General Formula (1) with a compound represented by General Formula (2) at a temperature higher than 120° C. to carry out amidation and to obtain a compound represented by General Formula (3).




    R1 represents a hydrogen atom or an aliphatic group, R2 and R4 represent a hydrogen atom, a chain-like aliphatic group, an aliphatic hydrocarbon ring group, an aryl group, or a heterocyclic group, Ar represents an aromatic ring, R3 represents an electron withdrawing group, m represents an integer of 1 or more, and n represents an integer of 0 or more. R4 is not an α-hydroxybenzyl group.

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