NOVEL CHLORIN E6-FOLIC ACID CONJUGATE, PREPARATION METHOD THEREOF, AND A PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF CANCER COMPRISING THE SAME
    54.
    发明申请
    NOVEL CHLORIN E6-FOLIC ACID CONJUGATE, PREPARATION METHOD THEREOF, AND A PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF CANCER COMPRISING THE SAME 有权
    新氯酸E6-羧酸共聚物,其制备方法和用于治疗包含其的癌症的药物组合物

    公开(公告)号:US20120059018A1

    公开(公告)日:2012-03-08

    申请号:US12594186

    申请日:2009-04-29

    摘要: The present invention relates to a novel chlorin e6-folic acid conjugate, a preparation method thereof, and a pharmaceutical composition for the treatment of cancer comprising the same, and more particularly, to a novel compound prepared by linking chlorin e6 to folic acid, which effectively produces singlet oxygen in various media and has much better tumor selectivity than the known porphyrin-based photosensitizers, thereby being used effectively in photodynamic therapy for malignant tumors, a preparation method thereof, and a pharmaceutical composition for photodynamic treatment of solid tumors comprising the compound.

    摘要翻译: 本发明涉及一种新的二氢卟吩e6-叶酸结合物,其制备方法和用于治疗癌症的药物组合物,特别涉及通过将二氢卟酚e6连接到叶酸而制备的新型化合物,其中 有效地在各种培养基中产生单线态氧,并且具有比已知的基于卟啉的光敏剂更好的肿瘤选择性,从而有效地用于恶性肿瘤的光动力学治疗,其制备方法和用于光动力治疗实体瘤的药物组合物,其包含化合物 。

    PHARMACEUTICAL COMPOSITION FOR TREATING CANCER COMPRISING CHLORIN E6-FOLIC ACID CONJUGATE COMPOUND AND CHITOSAN
    55.
    发明申请
    PHARMACEUTICAL COMPOSITION FOR TREATING CANCER COMPRISING CHLORIN E6-FOLIC ACID CONJUGATE COMPOUND AND CHITOSAN 审中-公开
    用于治疗包含氯林E6-乳酸联合化合物和壳多糖的癌症的药物组合物

    公开(公告)号:US20120035180A1

    公开(公告)日:2012-02-09

    申请号:US12594180

    申请日:2009-04-29

    IPC分类号: A61K31/519 A61P35/00

    摘要: The present invention relates to a pharmaceutical composition for the treatment of cancer comprising a chlorin e6-folic acid conjugate compound and chitosan, and more particularly, to a pharmaceutical composition for photodynamic therapy of solid tumors comprising the novel chlorin e6-folic acid conjugate compound or a pharmaceutically acceptable salt thereof and chitosan, in which the novel compound is prepared by linking chlorin e6 to folic acid, and effectively produces singlet oxygen in various media and has much better tumor selectivity than the known porphyrin-based photosensitizers, thereby being used effectively in photodynamic treatment for malignant tumors.

    摘要翻译: 本发明涉及用于治疗癌症的药物组合物,其包含二氢卟吩e6-叶酸结合化合物和壳聚糖,更具体地,涉及一种用于实体瘤的光动力疗法的药物组合物,其包含新的二氢卟吩e6-叶酸结合物或 其药学上可接受的盐和壳聚糖,其中通过将二氢卟酚e6连接到叶酸来制备新化合物,并且在各种培养基中有效产生单线态氧并且具有比已知的基于卟啉的光敏剂更好的肿瘤选择性,从而有效地用于 恶性肿瘤的光动力治疗。

    METHOD FOR TREATING PORT WINE STAINS
    56.
    发明申请
    METHOD FOR TREATING PORT WINE STAINS 审中-公开
    处理港口葡萄酒的方法

    公开(公告)号:US20120029045A1

    公开(公告)日:2012-02-02

    申请号:US12848755

    申请日:2010-08-02

    IPC分类号: A61K31/409 A61P17/00

    CPC分类号: A61K41/0071

    摘要: A method of using photodynamic therapy to perform selective targeted therapy of biological tissue. The method includes intravenously injecting a porphyrin-based photosensitizing drug followed by irradiating the tissue with light while the drug is being injected. The duration of the irradiation and other parameters are controlled so that the selected biological tissue is treated and non-selected tissue is not damaged. By controlling the flow rate of the injection and other parameters, so that irradiation of the effected tissue overlaps with injection of drug, the target tissue is effectively treated without damage to non-target tissue.

    摘要翻译: 一种使用光动力疗法进行生物组织选择性靶向治疗的方法。 该方法包括静脉注射基于卟啉的光敏药物,然后在注射药物时用光照射组织。 控制照射的持续时间和其他参数,使得所选择的生物组织被处理并且未选择的组织不被损坏。 通过控制注射的流量和其它参数,使得受影响的组织的照射与药物的注射重叠,目标组织被有效地处理而不损害非靶组织。

    MULTIMODALITY AGENTS FOR TUMOR IMAGING AND THERAPY
    58.
    发明申请
    MULTIMODALITY AGENTS FOR TUMOR IMAGING AND THERAPY 审中-公开
    用于肿瘤成像和治疗的多功能剂

    公开(公告)号:US20110223102A1

    公开(公告)日:2011-09-15

    申请号:US12677381

    申请日:2008-09-11

    摘要: A compound that is a conjugate of an antagonist to an integrin expressed by a tumor cell and at least one of a tumor avid tetrapyrollic photosensitizer, a fluorescent dye, and a radioisotope labeled moiety wherein the radioisotope is 11C, 18F, 64Cu, 124I, 99Tc, 111In or GdIII and its method of use for diagnosing, imaging and/or treating hyperproliferative tissue such as tumors. Preferably the photosensitizer is a tumor avid tetrapyrollic photosensitizer, e.g. a porphyrin, chlorin or bacteriochlorin, e.g. pheophorbides and pyropheophorbides. Such conjugates have extreme tumor avidity and can be used to inhibit or completely destroy the tumor by light absoption. The integrin is usually αvβ3, α5β1, αvβ5, α4β1, or α2β1. Preferably, the antagonist is an RGD peptide or another antagonist that may be synthetic such as a 4-{2-(3,4,5,6-tetra-hydropyrimidin-2-ylamino)ethyloxy}-benzoyl]amino-2-(S)-amino-ethyl-sulfonylamino group. Such compounds provide tumor avidity and imaging ability thus permitting selective and clear tumor imaging.

    摘要翻译: 作为拮抗剂与由肿瘤细胞表达的整联蛋白结合的化合物,以及至少一种肿瘤病毒四级光敏剂,荧光染料和放射性同位素标记部分,其中放射性同位素为11C,18F,64Cu,124I,99Tc ,111In或GdIII及其用于诊断,成像和/或治疗过度增生组织如肿瘤的方法。 优选地,光敏剂是肿瘤急性四分光敏光敏剂,例如。 卟啉,二氢卟酚或细菌二氢卟酚。 脱镁叶绿素和焦偏镁偏磷酸盐。 这种缀合物具有极端的肿瘤亲合力,可用于通过光吸收抑制或完全破坏肿瘤。 整合素通常为αv&bgr; 3,α5和bgr; 1,αv&bgr; 5,α4和bgr; 1或α2和bgr; 1。 优选地,拮抗剂是可以是合成的RGD肽或另一种拮抗剂,例如4- {2-(3,4,5,6-四 - 嘧啶-2-基氨基)乙氧基} - 苯甲酰基]氨基-2-( S) - 氨基 - 乙基 - 磺酰基氨基。 这样的化合物提供了肿瘤亲合力和成像能力,从而允许选择性和清晰的肿瘤成像。

    Shiga toxin B-subunit as a vector for tumor diagnosis and drug delivery to GB3 expressing tumors
    59.
    发明授权
    Shiga toxin B-subunit as a vector for tumor diagnosis and drug delivery to GB3 expressing tumors 有权
    志贺毒素B亚基作为肿瘤诊断和药物递送到GB3表达肿瘤的载体

    公开(公告)号:US07981400B2

    公开(公告)日:2011-07-19

    申请号:US12723361

    申请日:2010-03-12

    IPC分类号: A61K49/00 C07K14/00

    摘要: The invention relates to new compounds for cancer therapy or diagnosis and more specifically to the use of a non-toxic B subunit of Shiga toxin mutant as a vector for diagnostic products or drugs in over-expressing Gb3 receptor cells, such compounds having the following formula: STxB-Z(n)-Cys-Y(m)-T wherein STxB is the Shiga Toxin B subunit or a functional equivalent thereof, Z(n) wherein n is 0 or 1 and when n is 1, Z is an amino-acid residue devoid of sulfhydryl group, or is a polypeptide, Cys is the amino-acid residue for Cysteine, T is a molecule linked by a covalent bound to the S part of Cys, selected in a group comprising: agents for in vivo diagnosis, cytotoxic agents, prodrugs, or enzymes for the conversion of a prodrug to a drug, Y(m) wherein m is 0 or 1 and when m is 1, Y is a linker between T and Cys, said linker being either cleavable or not cleavable for the release of T after the internalization of the hybrid compound into said cells.

    摘要翻译: 本发明涉及用于癌症治疗或诊断的新化合物,更具体地涉及使用志贺毒素突变体的无毒性B亚基作为过表达Gb3受体细胞的诊断产物或药物的载体,具有下式 :STxB-Z(n)-Cys-Y(m)-T其中STxB是滋贺毒素B亚基或其功能等同物,Z(n)其中n为0或1,当n为1时,Z为氨基 - 没有巯基的酸性残基,或是多肽,Cys是半胱氨酸的氨基酸残基,T是通过共价结合到Cys的S部分的分子连接的分子,所述组分选自:用于体内诊断的试剂 ,前药或前药转化为药物的Y(m),其中m为0或1,当m为1时,Y为T和Cys之间的接头,所述接头可切割或不切割 在将杂化化合物内化至所述细胞后,可以切割T释放T。