THIONUCLEOSIDE DERIVATIVE OR SALT THEREOF, AND PHARMACEUTICAL COMPOSITION

    公开(公告)号:US20170233429A1

    公开(公告)日:2017-08-17

    申请号:US15581834

    申请日:2017-04-28

    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.

    METHOD FOR PRODUCING PEPTIDE COMPOUND, PROTECTIVE GROUP-FORMING REAGENT, AND SUBSTITUTED BENZYL COMPOUND

    公开(公告)号:US20240317796A1

    公开(公告)日:2024-09-26

    申请号:US18735130

    申请日:2024-06-05

    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.

    1,5-NAPHTHYRIDINE DERIVATIVE OR SALT THEREOF
    6.
    发明申请
    1,5-NAPHTHYRIDINE DERIVATIVE OR SALT THEREOF 有权
    1,5-萘啶衍生物或其盐

    公开(公告)号:US20140142302A1

    公开(公告)日:2014-05-22

    申请号:US14166105

    申请日:2014-01-28

    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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