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公开(公告)号:US20170233429A1
公开(公告)日:2017-08-17
申请号:US15581834
申请日:2017-04-28
Applicant: FUJIFILM Corporation
Inventor: Hidenobu KUNIYOSHI , Daisuke NAKAGAWA , Takuya MATSUMOTO , Yuji YOSHIMITSU
IPC: C07H19/10
CPC classification number: C07H19/10 , A61K31/7068 , A61P35/00 , A61P35/02
Abstract: Disclosed are a compound and a pharmaceutical composition that exhibit an excellent drug efficacy against a tumor, in particular a tumor which has acquired resistance to gemcitabine. Specifically, provided is a thionucleoside derivative represented by General Formula [1] (in the formula, R1 represents a hydroxyl group which may be protected, a C1-20 alkoxy group which may be substituted, or the like; R2 represents a C1-20 alkoxy group which may be substituted, a C3-8 cycloalkoxy group which may be substituted, or the like; and R3 represents a hydrogen atom or the like); or a salt thereof. Further, provided is a pharmaceutical composition containing such a thionucleoside derivative or a salt thereof.
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公开(公告)号:US20210380633A1
公开(公告)日:2021-12-09
申请号:US17409692
申请日:2021-08-23
Applicant: FUJIFILM CORPORATION
Inventor: Yosuke YAMAMOTO , Kazuhei KANEKO , Motomasa TAKAHASHI , Makoto TAKAHASHI , Mika IMAMURA , Hirotaka SATOU , Hirofumi OMURA , Yuji YOSHIMITSU , Keita TANAKA , Daisuke NAKAGAWA
Abstract: Provided are a method for producing a peptide compound including a step of using an aromatic heterocyclic compound represented by Formula (1) represented by Formula (1); a protective group-forming reagent including the compound; and the compound. In Formula (1), a ring A represents an aromatic heterocyclic ring, YA's each independently represent —OH, —NHR, —SH, or —X0, where X0 represents Cl, Br, or I, RA and RC each independently represent an aliphatic hydrocarbon group or an organic group having an aliphatic hydrocarbon group, RBs' each independently represent a monovalent aliphatic hydrocarbon group, a (1+c)-valent aromatic group, or a (1+c)-valent heteroaromatic group, where, in a case where both a and c is 0, RB is a monovalent aliphatic hydrocarbon group, and the number of carbon atoms in at least one aliphatic hydrocarbon group of RA, RB, or RC is 12 or more.
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公开(公告)号:US20210015802A1
公开(公告)日:2021-01-21
申请号:US17037103
申请日:2020-09-29
Applicant: FUJIFILM Corporation
Inventor: Hirofumi FUKUNAGA , Sachiko SHINJO , Daisuke NAKAGAWA , Shinichiro SEKINE , Takayuki YAMAKAWA
IPC: A61K31/4375 , A61K31/395 , A61K31/555 , C07F5/00 , C07D257/02 , C07D255/02 , C07F1/08 , C07D471/04 , A61K51/00 , C07B59/00 , A61K31/145 , A61K31/223 , A61K31/27 , A61K31/785 , C07D487/00
Abstract: A compound represented by Formula [3] or a salt thereof and a method of making the same, in the formula, L3 represents a group represented by Formula [2c] wherein R3c, R4c, R5c, and R6c are the same as or different from each other and represent a hydrogen atom or a C1-6 alkyl group; p3 represents an integer of 1 to 3; q3 represents an integer of 0 to 3; and r3 represents an integer of 1 to 6; A1 represents any one of the groups represented by Formulae [4] to [9], wherein * represents a binding position; and R7 represents a carboxyl-protecting group; and m represents an integer of 1 to 3.
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公开(公告)号:US20180008583A1
公开(公告)日:2018-01-11
申请号:US15712815
申请日:2017-09-22
Applicant: FUJIFILM Corporation
Inventor: Hirofumi FUKUNAGA , Sachiko SHINJO , Daisuke NAKAGAWA , Shinichiro SEKINE , Takayuki YAMAKAWA
IPC: A61K31/4375 , A61K31/27 , A61K31/145 , A61K31/223 , C07D487/00 , A61K31/785
Abstract: Provided are a method for efficiently manufacturing a nitrogen-containing compound, which is used for manufacturing a treatment agent for integrin-related diseases, or a salt thereof and a manufacturing intermediate of the compound or a salt thereof.A method for manufacturing a novel nitrogen-containing compound or a salt thereof includes (1) a step of obtaining a compound represented by Formula [10] or a salt thereof through an amidation reaction; and (2) a step of deprotecting the compound represented by Formula [10] or a salt thereof.
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公开(公告)号:US20240317796A1
公开(公告)日:2024-09-26
申请号:US18735130
申请日:2024-06-05
Applicant: FUJIFILM Corporation
Inventor: Daisuke NAKAGAWA , Hiroaki TSUYAMA , Hayato YOSHIDA , Takuma MOGI
IPC: C07K1/06 , C07C43/23 , C07C217/58 , C07C271/16 , C07K1/30
CPC classification number: C07K1/062 , C07C43/23 , C07C217/58 , C07C271/16 , C07K1/066 , C07K1/30
Abstract: An object of the present invention is to provide a method for producing a peptide compound with an excellent yield, a protective group-forming reagent having an excellent yield, and a novel substituted benzyl compound. According to the present invention, there is provided a method for producing a peptide compound, including a step of using a substituted benzyl compound represented by Formula (1).
In Formula (1), Y represents —OH, —NHR, —SH, or —X, R represents a hydrogen atom, an alkyl group, an arylalkyl group, a heteroarylalkyl group, or a 9-fluorenylmethoxycarbonyl group, X represents Cl, Br, or I, m represents 1 or 2, n represents an integer of 1 to 5, RB's each independently represent an aliphatic hydrocarbon group, RA, s each independently represent an aliphatic hydrocarbon group or an organic group having an aliphatic hydrocarbon group, where the number of carbon atoms in at least one aliphatic hydrocarbon group is 12 or more, and a benzene ring in Formula (1) may further have a substituent in addition to RA.-
公开(公告)号:US20140142302A1
公开(公告)日:2014-05-22
申请号:US14166105
申请日:2014-01-28
Applicant: FUJIFILM Corporation
Inventor: Hidetomo FURUYAMA , Hideki KURIHARA , Kentarou FURUYA , Takahiro TERAO , Shinichirou SEKINE , Daisuke NAKAGAWA
IPC: C07D471/04 , C07F7/10 , C07D519/00
CPC classification number: C07D471/04 , A61K31/4375 , C07D519/00 , C07F7/10
Abstract: A 1,5-naphthyridine derivative represented by Formula [1] (in which R1, R2, R3, R4 and R5 represent a hydrogen atom, -L-Z (in which Z represents a non-aromatic heterocyclic group or the like; and L represents a single bond or the like), or the like, R6 represents -L-Z or the like, R7 and R8 represent a hydrogen atom or the like, and Q represents an oxygen atom or the like), or a salt thereof has an excellent inhibitory activity with respect to the PI3K-AKT pathway and the Ras-Raf-MEK-ERK pathway, and is useful for treatments such as prophylactic treatments and therapeutic treatments of diseases in which the PI3K-AKT pathway and the Ras-Raf-MEK-ERK pathway are involved.
Abstract translation: 由式[1]表示的1,5-萘啶衍生物(其中R 1,R 2,R 3,R 4和R 5表示氢原子,-LZ(其中Z表示非芳香族杂环基等),L表示 单键等)等,R6表示-LZ等,R7和R8表示氢原子等,Q表示氧原子等)或其盐具有优异的抑制性 相对于PI3K-AKT途径和Ras-Raf-MEK-ERK途径的活性,可用于治疗PI3K-AKT途径和Ras-Raf-MEK-ERK的疾病的预防性治疗和治疗性治疗 涉及到途径。
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公开(公告)号:US20240108607A1
公开(公告)日:2024-04-04
申请号:US18112423
申请日:2023-02-21
Applicant: FUJIFILM Corporation
Inventor: Hirofumi FUKUNAGA , Sachiko SHINJO , Daisuke NAKAGAWA , Shinichiro SEKINE , Takayuki YAMAKAWA
IPC: A61K31/4375 , A61K31/145 , A61K31/223 , A61K31/27 , A61K31/395 , A61K31/555 , A61K31/785 , A61K51/00 , C07B59/00 , C07D255/02 , C07D257/02 , C07D471/04 , C07D487/00 , C07F1/08 , C07F5/00
CPC classification number: A61K31/4375 , A61K31/145 , A61K31/223 , A61K31/27 , A61K31/395 , A61K31/555 , A61K31/785 , A61K51/00 , C07B59/00 , C07D255/02 , C07D257/02 , C07D471/04 , C07D487/00 , C07F1/08 , C07F5/00
Abstract: A compound represented by Formula [3] or a salt thereof and a method of making the
in the formula, L3 represents a group represented by Formula [2c]
wherein R3c, R4c, R5c and R6c are the same as or different from each other and represent a hydrogen atom or a C1-6 alkyl group; p3 represents an integer of 1 to 3; q3 represents an integer of 0 to 3; and r3 represents an integer of 1 to 6; A1 represents any one of the groups represented by Formulae [4] to [9],
wherein * represents a binding position; and R7 represents a carboxyl-protecting group; and m represents an integer of 1 to 3.-
公开(公告)号:US20210380634A1
公开(公告)日:2021-12-09
申请号:US17408474
申请日:2021-08-22
Applicant: FUJIFILM CORPORATION
Inventor: Yosuke YAMAMOTO , Kazuhei KANEKO , Motomasa TAKAHASHI , Makoto TAKAHASHI , Mika IMAMURA , Hirotaka SATOU , Hirofumi OMURA , Yuji YOSHIMITSU , Daisuke NAKAGAWA , Keita TANAKA
Abstract: Provided are a method for producing a peptide compound including a step of using a condensed polycyclic aromatic hydrocarbon compound represented by Formula (1); a protective group-forming reagent including the compound; and the compound. In Formula (1), a ring A represents a condensed polycyclic aromatic hydrocarbon ring, YA's each independently represent —CH2OH, —CH2NHR, —CH2SH, or —CH2X0, where R represents a hydrogen atom, an alkyl group, or an aralkyl group, and X0 represents Cl, Br, or I, k represents an integer of 1 to 5, n represents 1 or 2, and RA's each independently represent an aliphatic hydrocarbon group or an organic group having an aliphatic hydrocarbon group.
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公开(公告)号:US20180319834A1
公开(公告)日:2018-11-08
申请号:US16037375
申请日:2018-07-17
Applicant: FUJIFILM Corporation
Inventor: Hidenobu KUNIYOSHI , Daisuke NAKAGAWA , Takuya MATSUMOTO , Yuji YOSHIMITSU
IPC: C07H19/10 , A61P35/02 , A61K31/7068 , A61P35/00
CPC classification number: C07H19/10 , A61K31/7068 , A61P35/00 , A61P35/02
Abstract: Disclosed are a compound and a pharmaceutical composition that exhibit an excellent drug efficacy against a tumor, in particular a tumor which has acquired resistance to gemcitabine. Specifically, provided is a thionucleoside derivative represented by General (in the formula, R1 represents a hydroxyl group which may be protected, a C1-20 alkoxy group which may be substituted, or the like; R2 represents a C1-20 alkoxy group which may be substituted, a C3-8 cycloalkoxy group which may be substituted, or the like; and R3 represents a hydrogen atom or the like); or a salt thereof. Further, provided is a pharmaceutical composition containing such a thionucleoside derivative or a salt thereof.
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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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