PEPTIDE
    1.
    发明公开
    PEPTIDE 审中-公开

    公开(公告)号:US20240287131A1

    公开(公告)日:2024-08-29

    申请号:US18605993

    申请日:2024-03-15

    IPC分类号: C07K5/06

    CPC分类号: C07K5/06191

    摘要: The present invention provides a peptide having a fluoroalkyl group in the side chain. The present invention provides a peptide in which 2 or more amino acids are peptide-bonded in which at least one side chain of an amino acid residue constituting the peptide is represented by the following General Formula (1) [in the formula, Z1 is a divalent, trivalent, or tetravalent linking group other than an alkylene group; Rf is a C1-30 alkyl group substituted with at least two fluorine atoms, —SF5, or —SF4—CR101R102—CR103R104Cl (R101, R102, R103, and R104 are each independently a hydrogen atom, a fluorine atom, or a chlorine atom, and two or more of R101, R102, R103, and R104 are fluorine atoms); n3 is 1, 2, or 3, and the black circle indicates a bonding site].

    ACYCLIC THREONINOL NUCLEIC ACID
    2.
    发明公开

    公开(公告)号:US20240009224A1

    公开(公告)日:2024-01-11

    申请号:US18459548

    申请日:2023-09-01

    摘要: The present invention provides a nucleic acid having excellent cell membrane permeability.
    The present invention relates to: a nucleic acid having a structure represented by the following general formula (A1) or (A2) [in the formula, R0 is an alkyl group having 1 to 30 carbon atoms that is substituted with one or more fluorine atoms, a group having 1 to 5 etheric oxygen atoms between carbon atoms of an alkyl group having 2 to 30 carbon atoms that is substituted with one or more fluorine atoms, an alkyl group having 10 to 30 carbon atoms that is not substituted with a fluorine atom, or a group having 1 to 5 etheric oxygen atoms between carbon atoms of an alkyl group having 10 to 30 carbon atoms that is not substituted with a fluorine atom; n11 and n12 each independently represent an integer of 1 or more; B is a nucleobase; and a filled circle indicates a bond]; a cell membrane permeabilizing agent containing the nucleic acid as an active ingredient; and a nucleic acid drug containing the nucleic acid as an active ingredient.

    METHOD FOR PRODUCING PENTAFLUOROSULFANYL GROUP-CONTAINING ARYL COMPOUND

    公开(公告)号:US20230406820A1

    公开(公告)日:2023-12-21

    申请号:US18458239

    申请日:2023-08-30

    摘要: The present invention provides a production method capable of efficiently synthesizing an SF5 group-containing compound, or the like. The present invention is a method for synthesizing an SF5 group-containing compound represented by the general formula (1) from a thioaryl compound represented by the general formula (2) [A1 is an aryl group or a heteroaryl group; G1 is —SH, —SCN, SF3, —S—S—R1, —S—CO—R2, —SR3, —SF2—R4, —S—Si—(R5)3, —S—PO—(R6)2, (N-phthalimidyl)thio group, or a thianthrenium group (R1 is an aryl group or a heteroaryl group; R2 and R5 are an aryl group, a heteroaryl group, an alkyl group, or an alkenyl group; R3 and R4 are an alkyl group or an alkenyl group, R6 is an aryloxy group, a heteroaryloxy group, an alkyloxy group, or an alkenyloxy group)].


    [Chemical Formula 1]



    A1—G1  (2)



    A1—SF5  (1)

    METHOD FOR PRODUCING TETRAFLUOROSULFANYL GROUP-CONTAINING ARYL COMPOUND

    公开(公告)号:US20240228435A1

    公开(公告)日:2024-07-11

    申请号:US18605910

    申请日:2024-03-15

    IPC分类号: C07C381/00

    CPC分类号: C07C381/00

    摘要: The present invention is a method for producing a tetrafluorosulfanyl group-containing aryl compound, in which a thioaryl compound represented by General Formula (2) is subjected to a reaction by adding to an olefin compound represented by General Formula (3) in the presence of a radical initiator to synthesize a tetrafluorosulfanyl group-containing aryl compound represented by General Formula (1) [in the formula, A1 is an aryl group which may have a substituent, or a heteroaryl group which may have a substituent; and R1, R2, R3, and R4 are each independently a hydrogen atom, a fluorine atom, or a chlorine atom, and two or more of R1, R2, R3, and R4 are a fluorine atom].

    PEPTIDE AND METHOD FOR MANUFACTURING SAME

    公开(公告)号:US20220119440A1

    公开(公告)日:2022-04-21

    申请号:US17566249

    申请日:2021-12-30

    IPC分类号: C07K1/06 C07K1/10 C07K5/08

    摘要: A peptide having a fluoroalkyl group as its side chain and a method for producing, which comprises condensing a compound represented by the formula (6-2) or (6-4), where means that an asymmetric carbon atom has an absolute configuration of S or R, Rf is a C1-30 alkyl group which is substituted with at least two fluorine atoms, and which may further be substituted with a halogen atom other than a fluorine atom (when the C1-30 alkyl group is a C2-30 alkyl group, it may have 1 to 5 etheric oxygen atoms between carbon atoms), and R2 is a protecting group for the amino group, with a fluorinated amino acid having its carboxy group protected, an amino acid having its carboxy group protected, a fluorinated peptide having its C-terminal protected, or a peptide having its C-terminal protected.

    METHOD FOR PRODUCING ARYL THIOL ESTER COMPOUND

    公开(公告)号:US20230406819A1

    公开(公告)日:2023-12-21

    申请号:US18240613

    申请日:2023-08-31

    摘要: The present invention provides a production method capable of synthesizing an aryl thiol ester compound under mild conditions rapidly at a high yield. The present invention provides a method for producing an aryl thiol ester compound including producing an aryl thiol ester compound represented by the following general formula (1) from a diazonium compound represented by the following general formula (2) and a thioate compound represented by the following general formula (3) by a Sandmeyer-type coupling reaction using a catalyst, [wherein A1 and A2 are each independently an optionally substituted aryl group or an optionally substituted heteroaryl group; X1 is a monovalent anion; and M1 is a monovalent cation].

    METHOD FOR PRODUCING POLYCARBONATE
    9.
    发明公开

    公开(公告)号:US20240117113A1

    公开(公告)日:2024-04-11

    申请号:US18510812

    申请日:2023-11-16

    IPC分类号: C08G64/04

    CPC分类号: C08G64/04

    摘要: A method for producing a polycarbonate, including reacting a dihydroxy component with a fluorine-containing carbonate component in a presence of a condensation catalyst to obtain a prepolymer, and heating the prepolymer at a temperature lower than a melting temperature of the prepolymer and subjecting the prepolymer to a solid state polymerization while discharging a by-produced fluorine-containing alcohol outside a system,