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    • 1. 发明授权
    • Methods for regulation of active TNF-.alpha.
    • 调节活性TNF-α的方法
    • US5861382A
    • 1999-01-19
    • US436330
    • 1995-06-29
    • Irun R. CohenOfer LiderLiora CahalonOded ShoseyovRaanan Margalit
    • Irun R. CohenOfer LiderLiora CahalonOded ShoseyovRaanan Margalit
    • A61K31/70C07H11/00A01N43/16C07K14/525C08B37/10
    • A61K31/7024A61K31/70A61K31/7016C07H11/00Y10S514/822Y10S514/825Y10S514/826Y10S514/885Y10S514/886Y10S530/868
    • Substances comprising disaccharides and substances comprising carboxylated and/or sulfated oligosaccharides in substantially purified form, and methods of using same, are disclosed for the regulation of cytokine activity in a host. For instance, the secretion of active Tumor Necrosis Factor Alpha (TNF-.alpha.) can be either inhibited or augmented selectively by administration to the host of an effective amount of a substance of the invention. Thus, the present invention also relates to pharmaceutical compositions and their use for the prevention and/or treatment of pathological processes involving the induction of active cytokine secretion, such as TNF-.alpha.. The invention also relates to the initiation of a desirable immune system-related response by the host to the presence of activators, including pathogens. The substances and pharmaceutical compositions of the present invention may be administered daily, at very low effective doses, typically below 0.1 mg/kg human, or at intervals of tip to about 5-8 days, preferably once a week.
    • PCT No.PCT / US93 / 10868 Sec。 371日期:1995年6月29日 102(e)日期1995年6月29日PCT 1993年11月9日PCT公布。 公开号WO94 / 11006 日期1994年5月26日包含二糖的物质和包含基本纯化形式的羧化和/或硫酸化寡糖的物质及其使用方法被公开用于调节宿主中的细胞因子活性。 例如,活性肿瘤坏死因子α(TNF-α)的分泌可以通过给予宿主有效量的本发明的物质而被选择性地抑制或增强。 因此,本发明还涉及药物组合物及其用于预防和/或治疗涉及诱导活性细胞因子分泌的病理过程如TNF-α的用途。 本发明还涉及由宿主引起包括病原体在内的活化剂的存在引起所需的免疫系统相关应答。 本发明的物质和药物组合物可以以非常低的有效剂量(通常低于0.1mg / kg的人),或以尖端间隔至约5-8天,优选每周一次施用。
    • 2. 发明授权
    • Compositions for the regulation of cytokine activity
    • 用于调节细胞因子活性的组合物
    • US07332480B2
    • 2008-02-19
    • US10831288
    • 2004-04-26
    • Irun R. CohenOfer LiderLiora CahalonOded ShoseyovRaanan Margalit
    • Irun R. CohenOfer LiderLiora CahalonOded ShoseyovRaanan Margalit
    • A61K31/7016A61K31/727C08B37/10
    • A61K31/7024A61K31/70A61K31/7016A61K31/727C07H11/00
    • Substances comprising carboxylated and/or sulfated oligosaccharides in substantially purified form, including compositions containing same and methods of using same, are disclosed for the regulation of cytokine activity in a host. For instance, the secretion of Tumor Necrosis Factor Alpha (TNF-α) can be either inhibited or augmented selectively by administration to the host of effective amounts of substances or their compositions comprising specific oligosaccharides in substantially purified form. Thus, the present invention also relates to pharmaceutical compositions and their use for the prevention and/or treatment of pathological processes involving the induction of active cytokine secretion, such as TNF-α. The invention also relates to the initiation of a desirable immune system-related response by the host to the presence of activators, including pathogens. The substances and pharmaceutical compositions of the present invention may be daily, at very low effective doses, typically below 0.1 mg/kg human, or at intervals of up to about 5-8 days, preferably once a week.
    • 包括基本上纯化形式的羧化和/或硫酸化寡糖的物质,包括含有它们的组合物和使用它们的方法被公开用于调节宿主中的细胞因子活性。 例如,肿瘤坏死因子α(TNF-α)的分泌可以通过向宿主施用有效量的物质或其包含基本纯化形式的特异性寡糖的组合物来选择性地被抑制或增强。 因此,本发明还涉及药物组合物及其用于预防和/或治疗涉及诱导活性细胞因子分泌的病理过程如TNF-α的用途。 本发明还涉及由宿主引起包括病原体在内的活化剂的存在引起所需的免疫系统相关应答。 本发明的物质和药物组合物可以是非常低的有效剂量,通常低于0.1mg / kg人,或间隔至多约5-8天,优选每周一次。
    • 5. 发明授权
    • Anti-cancer therapeutic compounds
    • 抗癌治疗化合物
    • US07285536B2
    • 2007-10-23
    • US10002145
    • 2001-12-05
    • Liora CahalonIrun R. CohenOfer LiderRaanan Margalit
    • Liora CahalonIrun R. CohenOfer LiderRaanan Margalit
    • A61K31/70
    • C07H5/06A61K31/7012A61K31/7016A61K31/702A61K31/7024A61K31/727A61K31/737
    • A treatment for cancer, and in particular, of therapeutic compounds which block the ability of cytokines and chemokines to promote metastasis of malignant cells. The therapeutic compound comprises a carboxylated and/or sulfated oligosaccharide, preferably in a substantially purified form, which is a heparin or heparan-sulfate derived saccharide compound. In one embodiment of the present invention, the carbohydrate or oligosaccharide has a molecular weight of no more than about 3000 daltons, preferably lying in the range of about 400 to about 2000 daltons, most preferably between about 400 and about 1100 daltons. Generally, substances of the present invention inhibit tumor cell migration, as determined by biological assays, and comprise molecules of various sugar units of which the basic unit of activity is associated with a disaccharide. However, larger oligosaccharide chains of up to about 10 sugar units, containing the basic disaccharide unit of activity can also function to inhibit such activity.
    • 癌症治疗,特别是阻断细胞因子和趋化因子促进恶性细胞转移的能力的治疗化合物。 治疗化合物包含羧化和/或硫酸化的寡糖,优选基本上纯化的形式,其是肝素或硫酸乙酰肝素衍生的糖类化合物。 在本发明的一个实施方案中,碳水化合物或寡糖的分子量不超过约3000道尔顿,优选在约400至约2000道尔顿范围内,最优选约400至约1100道尔顿。 通常,本发明的物质通过生物测定法测定,抑制肿瘤细胞迁移,并且包含其基本活性单位与二糖相关的各种糖单元的分子。 然而,含有活性的碱性二糖单位的高达约10个糖单元的较大的寡糖链也可以起到抑制这种活性的作用。