ENEMA PREPARATIONS AND THEIR USE
    102.
    发明申请
    ENEMA PREPARATIONS AND THEIR USE 审中-公开
    ENEMA制剂及其使用

    公开(公告)号:US20110293528A1

    公开(公告)日:2011-12-01

    申请号:US13141919

    申请日:2009-12-23

    摘要: This invention relates to improved methods of photodynamic treatment and diagnosis of cancer and non-cancerous conditions, and in particular to improved enema preparations for use in such methods, said enema preparations comprising a photosensitiser which is 5-aminolevulinic acid (5-ALA) or a precursor or derivative thereof, e.g. a 5-ALA ester. Such preparations may further comprise one or more viscosity enhancing agents, mucoadhesive or mucolytic agents, penetration enhancers or chelating agents. The methods and preparations herein described are particularly suitable for use in photodynamic methods of treating and/or diagnosing cancer and non-cancerous conditions in the colon and/or rectum.

    摘要翻译: 本发明涉及光动力学治疗和诊断癌症和非癌症病症的改进方法,特别是涉及用于这些方法的改善的灌肠剂制剂,所述灌肠制剂包含5-氨基乙酰丙酸(5-ALA)的光敏剂或 其前体或衍生物,例如 一种5-ALA酯。 这样的制剂还可以包含一种或多种粘度增强剂,粘膜粘附或粘液溶解剂,渗透增强剂或螯合剂。 本文所述的方法和制剂特别适用于治疗和/或诊断结肠和/或直肠癌和非癌症病症的光动力学方法。

    Acid addition salts of 5-aminolevulinic acid or its derivatives
    103.
    发明授权
    Acid addition salts of 5-aminolevulinic acid or its derivatives 有权
    5-氨基乙酰丙酸或其衍生物的酸加成盐

    公开(公告)号:US07888526B2

    公开(公告)日:2011-02-15

    申请号:US10594361

    申请日:2005-03-29

    IPC分类号: C07C229/22 A61K31/195

    CPC分类号: A61K41/0061 C07C229/22

    摘要: The present invention provides an acid addition salt of 5-aminolevulinic acid (5-ALA) or of a 5-ALA derivative (e.g. a 5-ALA ester) with an acid which has a pKa of about 5 or less, preferably about 3 or less, with the proviso that the acid is other than hydrochloric acid. Particularly preferred salts are those derived from acids selected from the group comprising sulphonic acid and its derivatives, hydrobromic acid, sulfuric acid, nitric acid and phosphoric acid. The salts in accordance with the invention are particularly suitable for use as photosensitizing agents in diagnosis and photochemotherapy of disorders or abnormalities of external or internal surfaces of the body.

    摘要翻译: 本发明提供5-氨基乙酰丙酸(5-ALA)或5-ALA衍生物(例如5-ALA酯)与酸的加成盐,所述酸的pKa为约5或更小,优选约3或 较少,条件是酸不是盐酸。 特别优选的盐是衍生自选自磺酸及其衍生物,氢溴酸,硫酸,硝酸和磷酸的酸的酸。 根据本发明的盐特别适用于诊断和光化学治疗身体的外表面或内表面的病症或异常的光敏剂。

    PHARMACEUTICAL AND NUTRACEUTICAL PRODUCTS COMPRISING VITAMIN K2
    106.
    发明申请
    PHARMACEUTICAL AND NUTRACEUTICAL PRODUCTS COMPRISING VITAMIN K2 审中-公开
    包含维生素K2的药物和营养产品

    公开(公告)号:US20100048704A1

    公开(公告)日:2010-02-25

    申请号:US12373601

    申请日:2007-07-13

    摘要: A pharmaceutical and nutraceutical product is provided comprising vitamin K2 or a compound within the vitamin K2 class of compounds, optionally and preferably in combination with one or more polyunsaturated fatty acids, either in purified form or as a marine oil (i.e. fish and/or krill oil). Also provided is the use of vitamin K2 or a compound within the vitamin K2 class of compounds, preferably in combination with one or more polyunsaturated fatty acids, either in purified form or as a marine oil, in the treatment or prophylaxis of disorders related to bone, cartilage and the cardiovascular system. Preferred compounds within the vitamin K2 class of compounds are MK-7, MK-8, MK-9 and MK-10, in particular MK-7 or MK-9. The marine oil is preferably krill oil or fish oil.

    摘要翻译: 提供药物和营养产品,其包含维生素K2或维生素K2类化合物中的化合物,任选且优选与一种或多种纯化形式的多不饱和脂肪酸或海洋油(即鱼和/或磷虾)组合 油)。 还提供了在维生素K2类化合物中使用维生素K2或化合物,优选与纯化形式的一种或多种多不饱和脂肪酸或海洋油组合用于治疗或预防与骨相关的疾病 ,软骨和心血管系统。 维生素K2类化合物中优选的化合物是MK-7,MK-8,MK-9和MK-10,特别是MK-7或MK-9。 海洋油最好是磷虾油或鱼油。

    Compounds
    109.
    发明申请
    Compounds 审中-公开
    化合物

    公开(公告)号:US20080103110A1

    公开(公告)日:2008-05-01

    申请号:US11662896

    申请日:2005-09-15

    CPC分类号: A61K47/555 A61K47/542

    摘要: The invention provides a water-soluble prodrug compound comprising a therapeutically effective moiety coupled via a metabolically cleavable bond to a protein binding moiety, wherein said therapeutically effective moiety has an anticancer, antiinflammatory, antiinfective or antipain effect, said protein binding moiety binds non-covalently to blood proteins, and the protein binding of said compound is at least 100% higher than that of the therapeutically effective moiety itself, with the exclusion of (i) the monoester of gemcitabine with azelaic acid, (ii) the monoester of dideoxycytidine with 1,12-dodecanedicarboxylic acid, (iii) 2-amino-1,9-dihydro-9(2′-(1-(10-acetyl-decanoyloxy)ethoxymethyl))-guanine, (iv) 5′-cytarabine monoester with 1,4-phenylene diacetic acid, (v) the monoester of metronidazole with 1,4-butanedicarboxylic acid, and (vi) the monoester of metronidazole with 1,6-phenylene diacetic acid; and pre-prodrugs metabolizable thereto.

    摘要翻译: 本发明提供了一种水溶性前药化合物,其包含通过可代谢切割键与蛋白质结合部分相连的治疗有效部分,其中所述治疗有效部分具有抗癌,抗炎,抗感染或抗胰蛋白酶作用,所述蛋白质结合部分非共价结合 并且所述化合物的蛋白质结合比治疗有效部分本身的蛋白质结合至少高100%,排除(i)吉西他滨与壬二酸的单酯,(ii)双脱氧胞苷的单酯与1 ,12-十二烷二羧酸,(iii)2-氨基-1,9-二氢-9(2' - (1-(10-乙酰基 - 癸酰氧基)乙氧基甲基)) - 鸟嘌呤,(iv)5'-阿糖胞苷单酯与1 ,4-亚苯基二乙酸,(v)甲硝唑与1,4-丁烷二羧酸的单酯,和(vi)甲硝唑与1,6-亚苯基二乙酸的单酯; 和其可代谢的前药前药。

    Optical Imaging Contrast Agents
    110.
    发明申请
    Optical Imaging Contrast Agents 审中-公开
    光学成像对比剂

    公开(公告)号:US20080019907A1

    公开(公告)日:2008-01-24

    申请号:US10582680

    申请日:2004-12-17

    IPC分类号: A61K49/00

    摘要: The invention provides contrast agents for optical imaging of vulnerable atherosclerotic plaque in patients. The contrast agents may be used in diagnosis of vulnerable atherosclerotic plaque, for follow up of progress in disease development, for follow up of treatment of vulnerable atherosclerotic plaque and for surgical guidance. Further, the invention provides methods for optical imaging of vulnerable atherosclerotic plaque in patients.

    摘要翻译: 本发明提供用于患者中易受损的动脉粥样硬化斑块的光学成像的造影剂。 对比剂可用于诊断易感动脉粥样硬化斑块,用于跟踪疾病发展进展情况,跟踪治疗脆弱动脉粥样硬化斑块和手术指导。 此外,本发明提供了患者中易受损的动脉粥样硬化斑块的光学成像的方法。