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公开(公告)号:US20220273817A1
公开(公告)日:2022-09-01
申请号:US17743584
申请日:2022-05-13
Applicant: FUJIFILM Corporation
Inventor: Takahiro SEKIGUCHI , Taisuke ENDO , Shun KANEUMI , Masaki NORO , Shintaro TANABE , Masahiko YAMAMOTO
Abstract: An object of the present invention is to provide a lipid composition capable of achieving excellent nucleic acid delivery for a wide variety of nucleic acids. According to the present invention, there is provided a lipid composition containing a first lipid which is a lipid represented by Formula (1) or a salt thereof, sterols, and nucleic acid, in which a ratio of the number of moles of the first lipid in the lipid composition to the number of moles of sterols in the lipid composition is 0.300 or more and less than 1.299. 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 1 or more, and c+d is 1 or more.
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公开(公告)号:US20220096381A1
公开(公告)日:2022-03-31
申请号:US17457793
申请日:2021-12-06
Applicant: FUJIFILM Corporation
Inventor: Taisuke ENDO , Shun KANEUMI , Masaki NORO , Shintaro TANABE , Masahiko YAMAMOTO
Abstract: An object of the present invention is to provide a lipid composition making it possible to achieve excellent delivery of nucleic acids. According to the present invention, there is provided a lipid composition containing a lipid represented by Formula (1) or a salt thereof, a nonionic lipid, a lipid having a nonionic hydrophilic polymer structure, and a nucleic acid, in which the lipid composition contains or does not contain a zwitterionic lipid, and in a case where (A) represents a molar ratio in percentage of the lipid represented by Formula (1) or a salt thereof to total lipids constituting the lipid composition and (B) represents a molar ratio in percentage of the zwitterionic lipid to total lipids constituting the lipid composition, (A) and (B) satisfy 40
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公开(公告)号:US20210085604A1
公开(公告)日:2021-03-25
申请号:US17112239
申请日:2020-12-04
Applicant: FUJIFILM Corporation
Inventor: Shintaro TANABE , Masahiko YAMAMOTO , Kimihiko SATO , Motomasa TAKAHASHI , Kazuhiro TSUNA , Yasutaka TASAKI , Taisuki ENDO , Issei DOI , Hirofumi FUKUNAGA
IPC: A61K9/127 , C12N15/88 , C07C219/06
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.
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公开(公告)号:US20250011361A1
公开(公告)日:2025-01-09
申请号:US18885092
申请日:2024-09-13
Applicant: FUJIFILM Corporation
Inventor: Shintaro TANABE , Tatsuya Nitabaru , Masashi Yoshimura , Keiko Makita , Hirofumi Fukunaga
Abstract: An object of the present invention is to provide a sterol compound capable of realizing an excellent nucleic acid delivery efficiency in a case of being used in a lipid composition, and to provide a lipid composition containing the sterol compound, which is allowed to realize an excellent nucleic acid delivery efficiency. According to the present invention, a compound represented by Formula (1) is provided. In the formula, R201 represents a cyclic hydrocarbon group which may be substituted with one or more substituents, where the substituent is a hydrocarbon group having 1 to 18 carbon atoms.
R102 represents (i) a hydrogen atom, (ii) a hydrocarbon group having 1 to 4 carbon atoms, which may be substituted with one or more substituents selected from OH, SH, COOH, NR106R107, N(R108)C(O)R109, or CF3, (iii) C(O)R103, or (iv) C(O)NR104R105.
The definition of each of the other symbols is as described in the present specification.-
公开(公告)号:US20240315970A1
公开(公告)日:2024-09-26
申请号:US18443959
申请日:2024-02-16
Applicant: FUJIFILM Corporation
Inventor: Shintaro TANABE , Masahiko YAMAMOTO , Kimihiko SATO , Motomasa TAKAHASHI , Kazuhiro TSUNA , Yasutaka TASAKI , Taisuke ENDO , Issei DOI , Hirofumi FUKUNAGA
IPC: A61K9/127 , C07C219/06 , C12N15/88
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.-
公开(公告)号:US20240124389A1
公开(公告)日:2024-04-18
申请号:US18495200
申请日:2023-10-26
Applicant: FUJIFILM Corporation
Inventor: Shintaro TANABE , Tatsuya NITABARU , Mashiko YAMAMOTO , Hirofumi FUKUNAGA , Naoto NAKAMURA , Noriyuki KASAGI , Taisuke ENDO , Keiko SUZUKI
IPC: C07C229/26 , A61K9/127 , C07C229/28
CPC classification number: C07C229/26 , A61K9/127 , C07C229/28
Abstract: An object of 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 and pharmaceutical composition using the compound or a salt thereof, which 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, each symbol has a meaning defined in the present specification.-
公开(公告)号:US20150322063A1
公开(公告)日:2015-11-12
申请号:US14795568
申请日:2015-07-09
Applicant: FUJIFILM Corporation
Inventor: Hidetomo FURUYAMA , Hideki KURIHARA , Takahiro TERAO , Daisuke NAKAGAWA , Shintaro TANABE , Takayuki KATO , Masahiko YAMAMOTO , Shinichiro SEKINE , Tomoyuki MASHIKO , Shinsuke INUKI , Satoshi UEDA
IPC: C07D471/04 , C07D519/00
CPC classification number: C07D471/04 , C07D519/00
Abstract: A compound represented by Formula [1] (in the formula, Z1 represents N, CH, or the like; X1 represents NH or the like; R1 represents a heteroaryl group or the like; each of R2, R3, and R4 represents a hydrogen atom, a halogen atom, an alkoxy group, or the like; and R5 represents a heteroaryl group or the like) or salt thereof.
Abstract translation: 由式[1]表示的化合物(式中,Z1表示N,CH等,X1表示NH等,R 1表示杂芳基等,R 2,R 3,R 4表示氢 原子,卤原子,烷氧基等; R5表示杂芳基等)或其盐。
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