化合物及びこれを用いた標識生体物質

    公开(公告)号:WO2021215514A1

    公开(公告)日:2021-10-28

    申请号:PCT/JP2021/016361

    申请日:2021-04-22

    Abstract: 下記式(1)の化合物、これを有する標識生体物質。 Z1、Z2は特定の6員環を示す。但し、Z1、Z2の少なくとも一方は、L1もしくはL2が結合する窒素原子に対してオルト位に特定の置換基を有するベンゼン環、又は、上記オルト位に位置する環構成原子が窒素原子である特定の含窒素6員環である。 R1~R4、R11~R13、L1、L2、R21は特定の基を示し、n、α1、α2、mは特定の数を示す。 上記化合物は、-(CH2-CH2-O)m-R21で表される構造を複素環上に少なくとも1つ有し、カルボキシ基又は生体物質に結合可能な置換基を特定の位置に少なくとも1つ有し、Z1、Z2の少なくとも一方が上記特定の含窒素6員環である場合、特定の置換基同士が結合して環を形成していてもよい。

    NEAR-INFRARED (NIR) TRICARBOCYANINE N-TRIAZOLE CHROMOPHORES

    公开(公告)号:WO2020020905A1

    公开(公告)日:2020-01-30

    申请号:PCT/EP2019/069834

    申请日:2019-07-23

    Abstract: The present invention provides a tricarbocyanine N -triazoles family of bright, photostable and cell- permeable NIR chromophores containing neutral triazole groups. In particular, a compound of formula (I), a derivative or a salt thereof is provided. Formula (I) wherein, R1 is absent or selected from the group consisting C1-C6 alkyl, and C1-C9 alkyl substituted with one or more of the following groups: halogen, hydroxyl, aryl, carboxylic acids; C3-C6 cycloalkyl, aryl groups substituted with one or more of the following groups: alkyl, cycloalkyl, naphthalenyl, phenanthrenyl, amino, aminoalkyl, aminocycloalkyl, formyl, trifluoromethyl, carboxyl, halogen, hydroxyl, hydroxyalkyl, alkyloxy, hydroxyaryl, nitro; thiophenyl, pyridinyl, imidazolyl, acetal, benzyl; R2 and R3 are each independently selected from the group consisting of C1-C6 alkyl, and C1-C6 alkyl substituted with one or more of the following groups: carboxylic acids, substituted amides, sulphonate groups, aryl, succinimidyl esters, maleimides, polyethyleneglycol-based substituents; R4, R5, R8 and R9 are each independently absent, C1-C6 alkyl or H; R6 and R10 are each independently H; R7 and R11 are each independently selected from the group consisting of H, Me and sulphonate; or R6-R7 and/or R10-R11 form an aromatic ring and/or R5-R6 and/or R9-R10 form an aromatic ring; R12 is selected from the group consisting of H, C1-C6 alkyl, and C1-C9 alkyl substituted with one or more of the following groups: hydroxyl, aryl, carboxylic esters, carboxylic acids; amine, aminoalkyl, aminocycloalkyl, aminoaryl, tosyl, hydroxyalkyl, hydroxyaryl, thioalkyl, thioaryl; X and Y are each independently selected from the group consisting of C, S, O and N; and Z is either C or N. The invention further relates to processes for the preparation of the compounds, and uses of the compounds in therapeutic, diagnostic, surgery and analytical applications.

    IR DYES FOR FLUORESCENCE IMAGING
    6.
    发明申请
    IR DYES FOR FLUORESCENCE IMAGING 审中-公开
    荧光成像红外线

    公开(公告)号:WO2016085884A1

    公开(公告)日:2016-06-02

    申请号:PCT/US2015/062212

    申请日:2015-11-23

    Applicant: LI-COR, INC.

    Abstract: A method for organ imaging, comprising: administering to a subject a diagnostic effective amount of 2-((E)-2-((E)-3-(2-((E)-3,3-dimethyl-5-sulfonato-1-(4- sulfonatobutyl)indolin-2-ylidene)ethylidene)-2-phenoxycyclohex-1-en-1-yl)vinyl)-3,3- dimethyl-1-(4-sulfonatobutyl)-3H-indol-1-ium-5-sulfonate or 2-((E)-2-((E)-3-(2-((E)-3,3- dimethyl-5-sulfonato-1-(4-sulfonatobutyl)indolin-2-ylidene)ethylidene)-2-(4- sulfonatophenoxy)cyclohex-1-en-1-yl)vinyl)-3,3-dimethyl-1-(4-sulfonatobutyl)-3H-indol-1- ium-5-sulfonate. In one embodiment, the organ includes one or more of kidney, bladder, liver, gall bladder, spleen, intestine, heart, lungs and muscle.

    Abstract translation: 一种器官成像方法,其特征在于,包括:向患者施用诊断有效量的2 - ((E)-2 - ((E)-3-(2 - ((E)-3,3-二甲基-5-磺酸 -1-(4-磺酰基丁基)二氢吲哚-2-亚基)亚乙基)-2-苯氧基环己-1-烯-1-基)乙烯基)-3,3-二甲基-1-(4-磺酰基丁基) 1 - ( - ) - ((E)-2 - ((E)-3-(2 - (((E))-3,3-二甲基-5-磺酸酯基 - (4-磺酰基丁基) 亚乙基)亚乙基)-2-(4-磺酰苯氧基)环己-1-烯-1-基)乙烯基)-3,3-二甲基-1-(4-磺酰基丁基)-3H-吲哚-1-基 - -5-磺酸酯。 在一个实施方案中,器官包括肾,膀胱,肝,胆囊,脾,肠,心脏,肺和肌肉中的一种或多种。

    THIOL/DISULFIDE INDOLE-DERIVED, STYRYL DYE, DYE COMPOSITION COMPRISING SAID DYE, PROCESS FOR LIGHTENING KERATIN MATERIALS USING THIS DYE
    9.
    发明申请
    THIOL/DISULFIDE INDOLE-DERIVED, STYRYL DYE, DYE COMPOSITION COMPRISING SAID DYE, PROCESS FOR LIGHTENING KERATIN MATERIALS USING THIS DYE 审中-公开
    THIOL / DISULFIDE INDOLE-DERIVED,STYRYL DYE,包含合适的染色剂的染色组合物,使用本染色体的KERATIN材料的加工方法

    公开(公告)号:WO2009037325A2

    公开(公告)日:2009-03-26

    申请号:PCT/EP2008/062479

    申请日:2008-09-18

    Abstract: The invention relates to the dyeing of keratin materials using thiol and disulfide, indole-derived, styryl fluorescent dyes. The invention relates to a dye composition comprising thiol and disulfide, indole-derived, styryl fluorescent dyes and to a dyeing process with a lightening effect on keratin materials, in particular keratin fibers, especially human keratin fibers such as the hair, using said composition. It similarly relates to novel thiol and disulfide, indole-derived, styryl fluorescent dyes and to the uses thereof in lightening keratin materials. This composition makes it possible to obtain a lightening effect which is particularly resistant and visible on dark keratin fibers.

    Abstract translation: 本发明涉及使用硫醇和二硫键,吲哚衍生的苯乙烯基荧光染料染色角蛋白材料。 本发明涉及包含硫醇和二硫键,吲哚衍生的苯乙烯基荧光染料的染料组合物,以及使用所述组合物对角蛋白材料,特别是角蛋白纤维,特别是人角蛋白纤维如头发的减轻作用的染色方法。 它同样涉及新型硫醇和二硫键,吲哚衍生的苯乙烯基荧光染料及其在减轻角蛋白材料中的用途。 该组合物使得可以获得在黑色角蛋白纤维上特别耐受和可见的减轻效果。

    RECEPTOR-AVID EXOGENOUS OPTICAL CONTRAST AND THERAPEUTIC AGENTS
    10.
    发明申请
    RECEPTOR-AVID EXOGENOUS OPTICAL CONTRAST AND THERAPEUTIC AGENTS 审中-公开
    受体 - 异常光学对比和治疗药物

    公开(公告)号:WO2005089813A3

    公开(公告)日:2006-08-17

    申请号:PCT/US2005007429

    申请日:2005-03-09

    Abstract: Cyanine dyes, as well as bioconjugates thereof, useful for diagnostic imaging and therapy are disclosed. The conjugates include several cyanine dyes with a variety of bis- and tetrakis (carboxylic acid) homologues. Dyes of the invention may be conjugated to bioactive peptides, carbohydrates, hormones, drugs, or other bioactive agents. The small size of the compounds allows more favorable delivery to tumor cells as compared to larger molecular weight imaging agents. The various dyes are useful over the range of 350 to 1,300 nm; the exact range being dependent upon the particular dye. The use of a biocompatible organic solvent such as dimethylsulfoxide helps to maintain the fluorescence of the compounds. The inventive compounds are useful for diagnostic imaging and therapy, in endoscopic applications for the detection of tumors and other abnormalities, for localized therapy, for photoacoustic tumor imaging, detection and therapy, and for sonofluorescence tumor imaging, detection and therapy.

    Abstract translation: 公开了可用于诊断成像和治疗的花青染料及其生物缀合物。 缀合物包括几种具有多种双和四(羧酸)同系物的花青染料。 本发明的染料可以与生物活性肽,碳水化合物,激素,药物或其他生物活性剂缀合。 与较大的分子量成像剂相比,化合物的小尺寸允许更有利于肿瘤细胞的传递。 各种染料在350至1300nm的范围内是有用的; 精确的范围取决于特定的染料。 使用生物相容性有机溶剂如二甲基亚砜有助于维持化合物的荧光。 本发明的化合物可用于诊断成像和治疗,用于检测肿瘤和其他异常的内窥镜应用,局部治疗,光声肿瘤成像,检测和治疗以及用于声发射肿瘤成像,检测和治疗。

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