Method for delivery of nucleic acids to cells using hypericin polyamine
complexes
    1.
    发明授权
    Method for delivery of nucleic acids to cells using hypericin polyamine complexes 失效
    使用金丝桃碱多胺复合物将核酸递送至细胞的方法

    公开(公告)号:US5824654A

    公开(公告)日:1998-10-20

    申请号:US300725

    申请日:1994-09-02

    摘要: The invention provides improved methods for delivery of nucleic acids to cells, which comprise forming ternary complexes between a hydrophobic, membrane-binding anion such as hypericin; a polycation such as polylysine; and a nucleic acid such as DNA; and contacting cells with the tenary complexes. Also provided are pharmaceutical formulations comprising these ternary complexes and a pharmaceutically acceptable carrier or diluent. The methods and compositions find use in mediating DNA uptake into cells, including gene therapy applications.

    摘要翻译: 本发明提供了将核酸递送至细胞的改进方法,其包括在疏水性的膜结合阴离子例如金丝桃素之间形成三元复合物; 聚阳离子如聚赖氨酸; 和核酸如DNA; 并使细胞与助剂络合物接触。 还提供了包含这些三元配合物和药学上可接受的载体或稀释剂的药物制剂。 该方法和组合物可用于介导DNA吸收进入细胞,包括基因治疗应用。

    Method for preventing or reducing collateral phototoxic damage to neighboring tissues during photodynamic therapy of a target tissue
    4.
    发明授权
    Method for preventing or reducing collateral phototoxic damage to neighboring tissues during photodynamic therapy of a target tissue 有权
    在靶组织的光动力学治疗期间预防或减少邻近组织的附着光毒性损伤的方法

    公开(公告)号:US07122518B2

    公开(公告)日:2006-10-17

    申请号:US10720688

    申请日:2003-11-25

    申请人: Gad Lavie

    发明人: Gad Lavie

    IPC分类号: A61K31/195

    摘要: A method is provided for preventing or reducing the adverse effects of photodynamic therapy such as collateral damage by regulating the localized phototoxicity of an effector photosensitizer molecule. During photodynamic therapy, the activity of the effector photosensitizer molecule in neighboring tissues of the tissue targeted for destruction is quenched by a quenching photosensitizer molecule.

    摘要翻译: 提供了一种通过调节效应物光敏剂分子的局部光毒性来预防或减少光动力学治疗如附带损伤的不利影响的方法。 在光动力学治疗期间,通过猝灭光敏剂分子来猝灭靶向于破坏的组织的相邻组织中效应物光敏剂分子的活性。

    Helianthrone derivatives as anti-cancer agents
    6.
    发明授权
    Helianthrone derivatives as anti-cancer agents 有权
    海龙龙衍生物作为抗癌剂

    公开(公告)号:US06867235B2

    公开(公告)日:2005-03-15

    申请号:US10209427

    申请日:2002-07-30

    摘要: Hypericin, helianthrone and derivatives thereof of general formula (I) wherein the dotted line between positions 11 and 12 represent an optional C11-C12 bond; R is independently selected from the group consisting of hydroxy, C1-C10 alkoxy, NH—C1-C10 alkyl, and NH-hydroxy(C1-C10)alkyl; R′ is independently selected from the group consisting of hydroxy and C1-C10 alkoxy; R″ is independently selected from the group consisting of hydrogen, hydroxy, C1-C10 alkoxy, NH—C1-C10 alkyl, and NH-hydroxy(C1-C10)alkyl; and R1, R2, R3, R4, R5 and R6 are independently selected from the group consisting of hydrogen, hydroxy, chloro, bromo, C1-C10 alkyl, C1-C10 alkoxy, and C1-C10 alkoxycarbonyl, provided that R″ is not hydrogen when there is a C11-C12 bond, are useful as inhibitors of angiogenesis and can be used to prevent formation of metastases and restenosis and for the treatment of angiogenesis-associated ophthalmologic disorders. In addition, the helianthrones of formula (I) can be used for the treatment of tumors in the absence of light irradiation. New compounds include those of formula I which are other than hypericin and known hypericin derivatives and there is either a C11-C12 bond or at least one R″ is other than hydrogen.

    摘要翻译: 通式(I)的金丝桃素,向日葵及其衍生物,其中位置11和12之间的虚线代表任选的C 11 -C 12键; R独立地选自羟基,C 1 -C 10烷氧基,NH-C 1 -C 10烷基和NH-羟基(C 1 -C 10)烷基; R'独立地选自羟基和C 1 -C 10烷氧基; R“独立地选自氢,羟基,C 1 -C 10烷氧基,NH-C 1 -C 10烷基和NH-羟基(C 1 -C 10)烷基; R 1,R 2,R 3,R 4,R 5和R 6独立地选自氢,羟基,氯,溴,C 1 -C 10烷基,C 1 -C 10烷氧基和C 1 -C 10烷氧基羰基,条件是R“ 当存在C11-C12键时,不是氢,可用作血管发生的抑制剂,可用于预防转移和再狭窄的形成以及用于治疗血管发生相关的眼科疾病。 此外,式(I)的长方体可用于在不存在光照射的情况下治疗肿瘤。 新化合物包括除金丝桃素和已知金丝桃素衍生物之外的式I的那些,并且存在C 11 -C 12键或至少一个R“不是氢。

    Helianthrone derivatives as anti-cancer agents
    7.
    发明申请
    Helianthrone derivatives as anti-cancer agents 审中-公开
    海龙龙衍生物作为抗癌剂

    公开(公告)号:US20050038115A1

    公开(公告)日:2005-02-17

    申请号:US10948212

    申请日:2004-09-24

    摘要: Hypericin and helianthrone derivatives of general formula (I) wherein the dotted line between positions 11 and 12 represent an optional C11-C12 bond; R is independently selected from the group consisting of hydroxy, C1-C10 alkoxy, NH—C1-C10 alkyl, and NH-hydroxy(C1-C10)alkyl; R′ is independently selected from the group consisting of hydroxy and C1-C10 alkoxy; R″ is independently selected from the group consisting of hydrogen, hydroxy, C1-C10 alkoxy, NH—C1-C10 alkyl, and NH-hydroxy(C1-C10)alkyl; and R1, R2, R3, R4, R5 and R6 are independently selected from the group consisting of hydrogen, hydroxy, chloro, bromo, C1-C10 alkyl, C1-C10 alkoxy, and C1-C10 alkoxycarbonyl, provided that R″ is not hydrogen when there is a C11-C12 bond and when there is a C11-C12 bond and both R′ are hydroxy, both R″ groups are not hydroxy. These compounds and pharmaceutical compositions containing them as active agents are useful as inhibitors of angiogenesis and can be used to prevent formation of metastases and restenosis and for the treatment of angiogenesis-associated ophthalmologic disorders. In addition, the helianthrone derivatives of formula (I) can be used for the treatment of tumors in the absence of light irradiation.

    摘要翻译: 通式(I)的金丝桃素和helianthrone衍生物,其中位置11和12之间的虚线表示任选的C 11 -C 12键; R独立地选自羟基,C 1 -C 10烷氧基,NH-C 1 -C 10烷基和NH-羟基(C 1 -C 10)烷基; R'独立地选自羟基和C 1 -C 10烷氧基; R“独立地选自氢,羟基,C 1 -C 10烷氧基,NH-C 1 -C 10烷基和NH-羟基(C 1 -C 10)烷基; R 1,R 2,R 3,R 4,R 5和R 6独立地选自氢,羟基,氯,溴,C 1 -C 10烷基,C 1 -C 10烷氧基和C 1 -C 10烷氧基羰基,条件是R“ 当存在C 11 -C 12键时不是氢,当存在C 11 -C 12键并且两个R'都是羟基时,两个R“不是羟基。 含有它们作为活性剂的这些化合物和药物组合物可用作血管发生的抑制剂,并且可用于预防转移和再狭窄的形成和用于治疗血管生成相关性眼科疾病。 此外,式(I)的龙眼酮衍生物可用于在不存在光照射的情况下治疗肿瘤。

    Methods and polycyclic aromatic compound containing compositions for
treating T-cell-mediated diseases
    8.
    发明授权
    Methods and polycyclic aromatic compound containing compositions for treating T-cell-mediated diseases 失效
    用于治疗T细胞介导的疾病的方法和含多环芳香族化合物的组合物

    公开(公告)号:US5514714A

    公开(公告)日:1996-05-07

    申请号:US39790

    申请日:1993-03-30

    摘要: T cell-mediated diseases in mammals are treated using compositions comprising a polycyclic aromatic compound, preferably hypericin or pseudohypericin, and related compounds, including isomers, analogs, derivatives, salts, or ion pairs of hypericin or pseudohypericin. The above composition may be administered in combination with an immunosuppressive agent. Pharmaceutical compositions useful for treating a T cell-mediated disease comprise the above polycyclic aromatic compound, alone or in combination with an immunosuppressive agent. The compositions and methods are useful in treating diseases which include multiple sclerosis, myasthenia gravis, scleroderma, polymyositis, graft-versus-host disease, graft rejection, Graves disease, Addison's disease, autoimmune uveoretinitis, autoimmune thyroiditis, pemphigus vulgaris and rheumatoid arthritis. Psoriasis and systemic lups erythematosus. Also provided are methods for diminishing the expression of CD4 Molecules on the surface of a T lymphocyte, and for inducing multidrug resistance in a cell, comprising incubating the cell with an effective concentration of a polycyclic aromatic compound.

    摘要翻译: 哺乳动物中的T细胞介导的疾病使用包含多环芳族化合物,优选金丝桃素或假倍孕素的组合物以及相关化合物,包括金丝桃素或假倍孕素的异构体,类似物,衍生物,盐或离子对来治疗。 上述组合物可以与免疫抑制剂组合施用。 可用于治疗T细胞介导的疾病的药物组合物包含单独的或与免疫抑制剂组合的上述多环芳族化合物。 组合物和方法可用于治疗包括多发性硬化,重症肌无力,硬皮病,多发性肌炎,移植物抗宿主病,移植排斥,格雷夫斯病,艾迪生病,自身免疫性葡萄膜葡萄膜炎,自身免疫性甲状腺炎,寻常型天疱疮和类风湿性关节炎的疾病。 牛皮癣和系统性红斑狼疮。 还提供了减少T淋巴细胞表面上的CD4分子的表达以及用于在细胞中诱导多药耐药性的方法,包括用有效浓度的多环芳族化合物孵育细胞。

    Antiviral agents
    9.
    发明授权
    Antiviral agents 失效
    抗病毒剂

    公开(公告)号:US06576784B1

    公开(公告)日:2003-06-10

    申请号:US08068379

    申请日:1993-05-27

    IPC分类号: C07C6976

    CPC分类号: C07C69/00 C07C2603/00

    摘要: Novel antiviral (including antiretroviral) compounds are mono- or dicarboxylic acid esters of hypericin in which one or both of the methyl groups of hypericin are substituted by carboxylic acid ester groups of the formula COOR3 in which R3 is alkyl, the chain of which is optionally interrupted by one or more oxygen or sulphur atoms. R3 is preferably methyl, ethyl, propyl, butyl, 2-methoxyethyl or 2-(2-methoxyethoxy)ethyl. The compounds may be formulated into pharmaceutical compositions and may be used in any manner which has previously been known for hypericin.

    摘要翻译: 新型抗病毒药(包括抗逆转录酶病毒)化合物是金丝桃素的单酸或二羧酸酯,其中金丝桃碱的一个或两个甲基被式COOR3的羧酸酯基取代,其中R3是烷基,其链可任选地 被一个或多个氧或硫原子中断。 R3优选为甲基,乙基,丙基,丁基,2-甲氧基乙基或2-(2-甲氧基乙氧基)乙基。 化合物可以配制成药物组合物,并且可以以先前已知为金丝桃素的任何方式使用。