Acid addition salts of 5-aminolevulinic acid or its derivatives
    12.
    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:US08692014B2

    公开(公告)日:2014-04-08

    申请号:US12916326

    申请日:2010-10-29

    IPC分类号: C07C229/00 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。

    HYPEROSMOTIC PREPARATIONS COMPRISING 5-AMINOLEVULINIC ACID OR DERIVATIVE AS PHOTOSENSITIZING AGENT
    13.
    发明申请
    HYPEROSMOTIC PREPARATIONS COMPRISING 5-AMINOLEVULINIC ACID OR DERIVATIVE AS PHOTOSENSITIZING AGENT 审中-公开
    包含5-氨基酸或衍生物作为光敏剂的高效制剂

    公开(公告)号:US20130211215A1

    公开(公告)日:2013-08-15

    申请号:US13806578

    申请日:2011-06-23

    IPC分类号: A61K41/00 A61B5/00

    摘要: Provided herein are improved methods of photodynamic treatment and diagnosis of cancer and non-cancerous conditions in the gastrointestinal tract, e.g. in the colon, and in particular hyperosmotic enema preparations for use in such methods. The enema preparations comprise a photosensitizer which is 5-aminolevulinic acid (5-ALA) or a precursor or derivative thereof, e.g. a 5-ALA ester, in combination with at least one hyperosmotic agent. The methods and preparations herein described are particularly suitable for use in photodynamic methods of treating and/or diagnosing colorectal cancer.

    摘要翻译: 本文提供了光动力学治疗和诊断胃肠道中的癌症和非癌性病症的改进方法,例如。 在结肠中,特别是用于这些方法的高渗灌肠剂。 灌肠制剂包含5-氨基乙酰丙酸(5-ALA)或其前体或衍生物的光敏剂,例如5-氨基乙酰丙酸。 5-ALA酯,与至少一种高渗剂组合。 本文描述的方法和制剂特别适用于治疗和/或诊断结肠直肠癌的光动力学方法。

    ACID ADDITION SALTS OF 5-AMINOLEVULINIC ACID OR ITS DERIVATIVES
    14.
    发明申请
    ACID ADDITION SALTS OF 5-AMINOLEVULINIC ACID OR ITS DERIVATIVES 有权
    5-氨基酸或其衍生物的酸添加量

    公开(公告)号:US20110125012A1

    公开(公告)日:2011-05-26

    申请号:US12916326

    申请日:2010-10-29

    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。

    USE OF AMINOLEVULINIC ACID AND DERIVATIVES THEREOF
    16.
    发明申请
    USE OF AMINOLEVULINIC ACID AND DERIVATIVES THEREOF 有权
    氨基酸及其衍生物的使用

    公开(公告)号:US20100137439A1

    公开(公告)日:2010-06-03

    申请号:US12523048

    申请日:2008-01-11

    IPC分类号: A61K31/195 A61P35/00

    摘要: The invention provides the use of a photosensitiser which is 5-aminolevulinic acid (5-ALA) or a derivative (e.g. an ester) of 5-ALA, or a pharmaceutically acceptable salt thereof, in the manufacture of a composition for use in methods of photodynamic therapy (PDT) on an animal, wherein said PDT comprises: (a) administering to said animal a composition comprising said photosensitiser; and (b) photoactivating said photosensitiser, and wherein side-effects (e.g. pain and/or erythema) of said PDT are prevented or reduced by use of one or more of (i)-(iv): (i) said composition comprises said photosensitiser in a concentration of less than 10% wt (e.g. 0.5 to 8% wt), (ii) said composition is administered for less than 2 hours (e.g. 30 minutes to 90 minutes) prior to said photoactivation, (iii) said photoactivation is carried out with a light source having a fluence rate of less than 50 mW/cm2 (e.g. 5 to 40 mW/cm2), (iv) said photoactivation is carried out with sunlight. Preferably, side-effects of PDT are prevented or reduced by using (iii) or (iv) in combination with (i) and/or (ii).

    摘要翻译: 本发明提供了5-氨基乙酰丙酸(5-ALA)或5-ALA衍生物(例如酯)或其药学上可接受的盐的光敏剂在制备用于 光动力疗法(PDT),其中所述PDT包括:(a)向所述动物施用包含所述光敏剂的组合物; 和(b)光活化所述光敏剂,并且其中通过使用(i) - (iv)中的一种或多种来防止或减少所述PDT的副作用(例如疼痛和/或红斑):(i)所述组合物包含 浓度小于10%wt(例如0.5至8%wt)的光敏剂,(ii)所述组合物在所述光活化前施用少于2小时(例如30分钟至90分钟),(iii)所述光活化是 用光通量小于50mW / cm2(例如5〜40mW / cm2)的光源进行,(iv)所述的光活化是在太阳光下进行的。 优选地,通过使用(iii)或(iv)与(i)和/或(ii)组合来防止或减少PDT的副作用。

    SOLID COMPOSITIONS COMPRISING 5-AMINOLEVULINIC ACID
    17.
    发明申请
    SOLID COMPOSITIONS COMPRISING 5-AMINOLEVULINIC ACID 审中-公开
    包含5-氨基酸的固体组合物

    公开(公告)号:US20120134921A1

    公开(公告)日:2012-05-31

    申请号:US13377692

    申请日:2010-06-11

    IPC分类号: A61K51/04 A61K49/00

    摘要: This invention relates to solid compositions and solid pharmaceutical products for use in methods of photodynamic diagnosis of cancer, pre-cancerous and non-cancerous conditions in the lower part of the gastrointestinal system. The solid pharmaceutical compositions and pharmaceutical products comprise an active ingredient which is 5-aminolevulinic acid (5-ALA) or a precursor or derivative of 5-ALA or pharmaceutically acceptable salts thereof. The invention relates further to methods of photodynamic diagnosis of cancer, pre-cancerous and non-cancerous conditions of the lower gastrointestinal tract, wherein the solid pharmaceutical compositions and pharmaceutical products are used.

    摘要翻译: 本发明涉及用于癌症的光动力学诊断方法,胃肠系统下部癌前和非癌症病症的固体组合物和固体药物产品。 固体药物组合物和药物产品包含5-氨基乙酰丙酸(5-ALA)或5-ALA的前体或衍生物的活性成分或其药学上可接受的盐。 本发明还涉及癌症的光动力学诊断方法,下胃肠道的癌前和非癌症状况,其中使用固体药物组合物和药物产品。

    Separation processes
    19.
    发明申请
    Separation processes 审中-公开
    分离过程

    公开(公告)号:US20070036722A1

    公开(公告)日:2007-02-15

    申请号:US11498651

    申请日:2006-08-03

    CPC分类号: G01N33/5306 G01N33/5432

    摘要: Separation of target material from a liquid sample is achieved by coupling the target to targetable encapsulated gas microbubbles, allowing the microbubbles and coupled target to float to the surface of the sample to form a floating microbubble/target layer, and separating this layer from the sample. In a positive separation process the microbubbles are then removed from the target, e.g. by bursting. In a negative separation process target-free sample material is recovered following separation of the floating layer. The method may also be used diagnostically to detect the presence of a disease marker in a sample. Novel separation apparatus is also described.

    摘要翻译: 目标材料与液体样品的分离是通过将目标物与可靶向包封的气体微泡耦合来实现的,允许微泡和偶联的目标物漂浮到样品表面以形成浮动微泡/目标层,并将该层与样品分离 。 在正分离过程中,然后从目标物中除去微泡。 通过爆裂。 在负分离过程中,在浮选层分离后回收无目标样品材料。 该方法也可以在诊断上用于检测样品中疾病标志物的存在。 还描述了新颖的分离装置。

    Method for the identification of a receptor
    20.
    发明授权
    Method for the identification of a receptor 失效
    识别受体的方法

    公开(公告)号:US06806045B2

    公开(公告)日:2004-10-19

    申请号:US10052299

    申请日:2002-01-18

    IPC分类号: C12Q170

    摘要: A method for the identification and characterization of a receptor in target tissue for which a selected vector has affinity, wherein a transfected cell line expressing the receptor is added to a suspension of encapsulated microbubbles to which the selected vector is coupled and allowing the microbubbles and cells coupled thereto to float to the surface of the suspension. Upon isolating the microbubble-bound cells at the surface, these may be cultured to study the receptor, or cells may be lysed, amplifying the receptor-encoding cDNA and sequencing the cDNA.

    摘要翻译: 用于鉴定和表征所选载体具有亲和力的靶组织中的受体的方法,其中将表达受体的转染细胞系加入到所选载体偶联的包封的微泡的悬浮液中,并允许微泡和细胞 联接到其上以漂浮到悬架的表面。 在分离表面的微泡结合细胞时,可以培养这些细胞以研究受体,或者可以裂解细胞,扩增受体编码的cDNA并测序cDNA。