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公开(公告)号:US20240287131A1
公开(公告)日:2024-08-29
申请号:US18605993
申请日:2024-03-15
申请人: AGC Inc. , The University of Tokyo
发明人: Kimiaki KASHIWAGI , Takashi OKAZOE , Kohsuke AIKAWA , Shinsuke SANDO , Jumpei MORIMOTO , Koji KADOTA , Ai KOHATA
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].
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公开(公告)号:US20240009224A1
公开(公告)日:2024-01-11
申请号:US18459548
申请日:2023-09-01
申请人: The University of Tokyo , AGC Inc.
发明人: Takashi OKAZOE , Kohsuke AIKAWA , Honoka WATANABE , Akimitsu OKAMOTO , Kunihiko MORIHIRO , Taiichi KAGEYAMA
IPC分类号: A61K31/7125 , C07F9/09 , A61K31/712 , A61K48/00
CPC分类号: A61K31/7125 , C07F9/09 , A61K31/712 , A61K48/0066
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.-
公开(公告)号:US20230406820A1
公开(公告)日:2023-12-21
申请号:US18458239
申请日:2023-08-30
申请人: AGC Inc. , The University of Tokyo
发明人: Takashi OKAZOE , Tim GATZENMEIER , Kyoko NOZAKI
IPC分类号: C07C327/16 , C07C319/20 , C07D213/71
CPC分类号: C07C327/16 , C07C319/20 , C07D213/71
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)-
公开(公告)号:US20230016405A1
公开(公告)日:2023-01-19
申请号:US17891336
申请日:2022-08-19
申请人: THE UNIVERSITY OF TOKYO , AGC INC.
发明人: Kyoko NOZAKI , Midori AKIYAMA , Kenta MORI , Takashi OKAZOE , Yuichiro ISHIBASHI , Ko INADA
IPC分类号: C07C41/22 , B01J31/22 , C07C319/20 , C07D209/86 , C07C17/263
摘要: A production method of producing a fluorine-containing olefin by allowing a first olefin represented by the following Formula (1) and a second olefin to react with each other in the presence of a ruthenium compound represented by the following Formula (X) is provided.
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公开(公告)号:US20240228435A1
公开(公告)日:2024-07-11
申请号:US18605910
申请日:2024-03-15
申请人: AGC Inc. , The University of Tokyo
发明人: Takashi OKAZOE , Kohsuke AIKAWA , Kyoko NOZAKI , Eisuke YASUO
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].
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公开(公告)号:US20220119440A1
公开(公告)日:2022-04-21
申请号:US17566249
申请日:2021-12-30
申请人: AGC Inc. , THE UNIVERSITY OF TOKYO
发明人: Takashi OKAZOE , Yuichiro ISHIBASHI , Shinsuke SANDO , Jumpei MORIMOTO , Kohsuke AIKAWA , Toshiki MIKAMI , Takahiro ONO
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.
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公开(公告)号:US20230406819A1
公开(公告)日:2023-12-21
申请号:US18240613
申请日:2023-08-31
申请人: AGC Inc. , The University of Tokyo
发明人: Takashi OKAZOE , Tim GATZENMEIER , Kyoko NOZAKI
IPC分类号: C07C327/16 , B01J23/72 , B01J31/02
CPC分类号: C07C327/16 , B01J23/72 , B01J31/0244
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].
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公开(公告)号:US20220235091A1
公开(公告)日:2022-07-28
申请号:US17699044
申请日:2022-03-18
申请人: AGC Inc. , THE UNIVERSITY OF TOKYO
发明人: Takashi OKAZOE , Yuichiro ISHIBASHI , Akimitsu OKAMOTO , Kunihiko MORIHIRO , Kohsuke AIKAWA , Honoka WATANABE
IPC分类号: C07H21/04
摘要: To provide a nucleic acid excellent in cell membrane permeability and a method for its production.
A nucleic acid containing a C2-10 perfluoroalkyl group having from 1 to 5 ether-bonding oxygen atoms between carbon atoms; said nucleic acid wherein said perfluoroalkyl group is directly or indirectly bonded to the 5′- or 3′-end of the nucleic acid, or said perfluoroalkyl group is indirectly introduced between two nucleotides; or a nucleic acid medicine comprising, as an active ingredient, a nucleic acid containing a C2-10 perfluoroalkyl group, which may have from 1 to 5 ether-bonding oxygen atoms between carbon atoms.-
公开(公告)号:US20240117113A1
公开(公告)日:2024-04-11
申请号:US18510812
申请日:2023-11-16
发明人: Takashi OKAZOE , Masahito SUZUKI
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,
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公开(公告)号:US20220002234A1
公开(公告)日:2022-01-06
申请号:US17292582
申请日:2019-11-14
发明人: Akihiko TSUDA , Takashi OKAZOE
IPC分类号: C07C263/10 , B01J19/00 , B01J19/12 , C08G18/76
摘要: The objective of the present invention is to provide a method for producing an isocyanate compound safely and efficiently. The method for producing an isocyanate compound according to the present invention is characterized in comprising the steps of irradiating a high energy light to a halogenated methane at a temperature of 15° C. or lower in the presence of oxygen, and further adding a primary amine compound to be reacted without irradiating a high energy light.
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