Drugs comprising porphyrins
    1.
    发明授权
    Drugs comprising porphyrins 失效
    药物包括卟啉

    公开(公告)号:US5028621A

    公开(公告)日:1991-07-02

    申请号:US352774

    申请日:1989-05-16

    摘要: To obtain tumor-selective, photosensitizing drugs useful in the localization of neoplastic tissue and treatment of abnormal neoplastic tissue such as tumors, one of two methods is used. In the first method, a hydrolyzed mixture of the products of reaction of hematoporphyrin with acetic acid and sulfuric acid is cycled through a microporous membrane system to exclude low molecular weight products. In the second method, drugs are synthesized or derived from other pyrrole compounds. The drugs (1) include two covalently bound groups, each with four rings, some of which are pyrroles such as phlorins, porphyrins, chlorins, substituted pyrroles, substituted chlorins or substituted phlorins, each group being arranged in a ring structure, connected covalently to another group and have a triplet energy state above 37.5 kilocalories per mole; (2) are soluble in water, forming an aggregate of over 10,000 molecular weight in water and have an affinity for each other compared to serum protein such that 10 to 100 percent remain self aggregated in serum protein; and (3) are lipophyllic and able to disaggregate and attach to cell plasma, nuclear membrane, mitochondria, lysosomes and tissue. The drug obtained by the first method has an empirical formula of approximately C.sub.68 H.sub.70 N.sub.8 O.sub.11 or C.sub.68 H.sub.66 N.sub.8 O.sub.11 Na.sub.4. Neoplastic tissue retains the drug after it has cleared normal tissues and illumination results in necrosis. Moreover, other photosensitizing materials may be combined with a carrier that enters undesirable tissues and cells of the reticular endothelial system such as macrophages. These photosensitizing materials: (1) must have a triplet energy state above 3.5 kilocalories per mole; (2) cannot be easily oxidized; and (3) not physically quench any required energy state. Preferably, this photosensitizing material should be lipophlic.

    摘要翻译: 为了获得肿瘤选择性的光敏药物,可用于肿瘤组织的定位和治疗异常肿瘤组织如肿瘤,使用两种方法之一。 在第一种方法中,血卟啉与乙酸和硫酸的反应产物的水解混合物循环通过微孔膜系统以排除低分子量产物。 在第二种方法中,合成或衍生自其他吡咯化合物的药物。 药物(1)包括两个共价结合的基团,每个具有四个环,其中一些是吡咯,例如卟啉,卟啉,二氢卟酚,取代的吡咯,取代的二氢卟酚或取代的藜芦烯,每个组排列成环结构,共价连接到 另一组,三重态能量每摩尔高于37.5千卡; (2)可溶于水,与血清蛋白质相比,在水中形成了超过10,000分子量的聚集体,并且与血清蛋白质具有亲和力,使得10%至100%在血清蛋白中保持自我聚集; 和(3)是脂蛋白的并且能够解聚并附着于细胞血浆,核膜,线粒体,溶酶体和组织。 通过第一种方法获得的药物具有约C68H70N8O11或C68H66N8O11Na4的经验式。 肿瘤组织清除正常组织后保留药物,照明会导致坏死。 此外,其它光敏材料可以与进入网状内皮系统的不希望的组织和细胞如巨噬细胞的载体组合。 这些光敏材料:(1)必须具有每千克3.5千卡以上的三线态能量状态; (2)不易氧化; 和(3)不能物理地淬灭任何所需的能量状态。 优选地,该光敏材料应该是脂肪族的。

    Drugs comprising porphyrins
    2.
    发明授权
    Drugs comprising porphyrins 失效
    药物包括卟啉

    公开(公告)号:US4649151A

    公开(公告)日:1987-03-10

    申请号:US609991

    申请日:1984-05-14

    摘要: To obtain tumor-selective, photosensitizing drugs useful in the localization of neoplastic tissue and treatment of abnormal neoplastic tissue such as tumors, one of two methods is used. In the first method, a hydrolyzed mixture of the products of reaction of hematoporphyrin with acetic acid and sulfuric acid is cycled through a microporous membrane system to exclude low molecular weight products. In the second method, drugs are synthesized or derived from other pyrrole compounds. The drugs: (1) include two covalently bound groups, each with four rings, some of which are pyrroles such as phlorins, porphyrins, chlorins, substituted pyrroles, substituted chlorins or substituted phlorins, each group being arranged in a ring structure, connected covalently to another group and have a triplet energy state above 37.5 kilocalories per mole; (2) are soluble in water, forming an aggregate of over 10,000 molecular weight in water and have an affinity for each other compared to serum protein such that 10 to 100 percent remain self aggregated in serum protein; and (3) are lipophyllic and able to disaggregate and attach to cell plasma, nuclear membrane, mitochondria, lysosomes and tissue. The drug obtained by the first method has an empirical formula of approximately C.sub.68 H.sub.70 N.sub.8 O.sub.11 or C.sub.68 H.sub.66 N.sub.8 O.sub.11 Na.sub.4.

    摘要翻译: 为了获得肿瘤选择性的光敏药物,可用于肿瘤组织的定位和治疗异常肿瘤组织如肿瘤,使用两种方法之一。 在第一种方法中,血卟啉与乙酸和硫酸的反应产物的水解混合物循环通过微孔膜系统以排除低分子量产物。 在第二种方法中,合成或衍生自其他吡咯化合物的药物。 药物:(1)包括两个共价结合的基团,每个具有四个环,其中一些是吡咯,例如卟啉,卟啉,二氢卟酚,取代的吡咯,取代的二氢卟酚或取代的藜芦烯,每个组排列成环结构,共价连接 到另一组,并具有高于每摩尔37.5千卡的三线态能量状态; (2)可溶于水,与血清蛋白质相比,在水中形成了超过10,000分子量的聚集体,并且与血清蛋白质具有亲和力,使得10%至100%在血清蛋白中保持自我聚集; 和(3)是脂蛋白的并且能够解聚并附着于细胞血浆,核膜,线粒体,溶酶体和组织。 通过第一种方法获得的药物具有约C68H70N8O11或C68H66N8O11Na4的经验式。

    Methods for treatment of tumors
    3.
    发明授权
    Methods for treatment of tumors 失效
    肿瘤治疗方法

    公开(公告)号:US4932934A

    公开(公告)日:1990-06-12

    申请号:US236603

    申请日:1988-08-24

    摘要: To obtain tumor-selective, photosensitizing drugs useful in the localization of neoplastic tissue and treatment of abnormal neoplastic tissue such as tumors, one of two methods is used. In the first method, a hydrolyzed mixture of the products of reaction of hematoporphyrin with acetic acid and sulfuric acid is cycled through a microporous membrane system to exclude low molecular weight products. In the second method, drugs are synthesized or derived from other pyrrole compounds. The drugs: (1) include two covalently bound groups, each with four rings, some of which are pyrroles such as phlorins, porphyrins, chlorins, substituted pyrroles, substituted chlorins or substituted phlorins, each group being arranged in a ring structure, connected covalently to another group and have a triplet energy state above 37.5 kilocalories per mole; (2) are soluble in water, forming an aggregate of over 10,000 molecular weight in water and have an affinity for each other compared to serum protein such that 10 to 100 percent remain self aggregated in serum protein; and (3) are lipophillic and able to disaggregate and attach to cell plasma, nuclear membrane, mitochondria, lysosomes and tissue. The drug obtained by the first method has an empirical formula of approximately C.sub.68 H.sub.70 N.sub.8 O.sub.11 or C.sub.68 H.sub.66 N.sub.8 O.sub.11 Na.sub.4. Neoplastic tissue retains the drug after it has cleared normal tissues and illumination results in necrosis. Moreover, other photosensitizing materials may be combined with a carrier that enters undesirable tissues and cells of the reticular endothelial system such as macrophages. These photosensitizing materials: (1) must have a triplet energy state above 3.5 kilocalories per mole; (2) cannot be easily oxidized; and (3) not physically quench any required energy state. Preferably, this photosensitizing material should be lipophilic.

    摘要翻译: 为了获得肿瘤选择性的光敏药物,可用于肿瘤组织的定位和治疗异常肿瘤组织如肿瘤,使用两种方法之一。 在第一种方法中,血卟啉与乙酸和硫酸的反应产物的水解混合物循环通过微孔膜系统以排除低分子量产物。 在第二种方法中,合成或衍生自其他吡咯化合物的药物。 药物:(1)包括两个共价结合的基团,每个具有四个环,其中一些是吡咯,例如卟啉,卟啉,二氢卟酚,取代的吡咯,取代的二氢卟酚或取代的藜芦烯,每个组排列成环结构,共价连接 到另一组,并具有高于每摩尔37.5千卡的三线态能量状态; (2)可溶于水,与血清蛋白质相比,在水中形成了超过10,000分子量的聚集体,并且与血清蛋白质具有亲和力,使得10%至100%在血清蛋白中保持自我聚集; 和(3)是脂肪性的并且能够分解并附着于细胞血浆,核膜,线粒体,溶酶体和组织。 通过第一种方法获得的药物具有约C68H70N8O11或C68H66N8O11Na4的经验式。 肿瘤组织清除正常组织后保留药物,照明会导致坏死。 此外,其它光敏材料可以与进入网状内皮系统的不希望的组织和细胞如巨噬细胞的载体组合。 这些光敏材料:(1)必须具有每千克3.5千卡以上的三线态能量状态; (2)不易氧化; 和(3)不能物理地淬灭任何所需的能量状态。 优选地,该光敏材料应该是亲脂的。

    Apparatus for treatment of tumors
    4.
    发明授权
    Apparatus for treatment of tumors 失效
    用于治疗肿瘤的装置

    公开(公告)号:US4889129A

    公开(公告)日:1989-12-26

    申请号:US243163

    申请日:1988-09-08

    摘要: To provide to and receive radiation from a photodynamic drug in neoplastic tissue, a laser system transmits radiation through an interface into a radiation delivery system, which is in juxtaposition with neoplastic tissue containing a photodynamic drug. The laser system may be a single argon laser pumping a dye laser, two parallel sets of argon lasers pumping a dye laser, a krypton laser or a xenon laser. In addition to transmitting radiation from the laser to the delivery system, the interface system may: (1) direct a portion of the light back to the laser's power supply to control the intensity of the radiation emitted from the laser; and/or (2) receive light from the light conductors of the delivery system. The interface channels light to radiation sensing devices which are either from a beam splitter indicating the magnitude of the radiation delivered from the laser system to the radiation delivery system or radiation leaking through the light conductor. Luminescent light from the photodynamic drug is selected and provides an indication of drug density and in some embodiments depth of the activity.

    摘要翻译: 为了提供和接受来自肿瘤组织中的光动力药物的辐射,激光系统将辐射通过界面传播到放射递送系统中,辐射递送系统与包含光动力药物的肿瘤组织并置。 激光系统可以是泵浦染料激光器的单个氩激光器,两个并联的氩激光器泵浦染料激光器,氪激光器或氙激光器。 除了将激光发射到传送系统之外,接口系统可以:(1)将一部分光引导回激光器的电源以控制从激光器发射的辐射的强度; 和/或(2)从输送系统的光导体接收光。 接口通道照射到辐射感测装置,辐射传感装置来自分束器,其指示从激光系统传送到辐射传播系统的辐射的大小或通过光导体泄漏的辐射。 选择来自光动力药物的发光,并提供药物密度的指示,并且在一些实施方案中提供活动深度。

    Treatment of tumors using chlorins
    5.
    发明授权
    Treatment of tumors using chlorins 失效
    使用二氢卟酚治疗肿瘤

    公开(公告)号:US5225433A

    公开(公告)日:1993-07-06

    申请号:US724749

    申请日:1991-07-02

    摘要: To obtain tumor-selective, photosensitizing drugs useful in the localization of neoplastic tissue and treatment of abnormal neoplastic tissue such as tumors, one of two methods is used. In the first method, a hydrolyzed mixture of the products of reaction of hematoporphyrin with acetic acid and sulfuric acid is cycled through a microporous membrane system to exclude low molecular weight products. In the second method, drugs are synthesized or derived from other pyrrole compounds. The drugs: (1) include two covalently bound groups, each with four rings, some of which are pyrroles such as phlorins, porphyrins, chlorins, substituted pyrroles, substituted chlorins or substituted phlorins, each group being arranged in a ring structure, connected covalently to another group and have a triplet energy state above 37.5 kilocalories per mole; (2) are soluble in water, forming an aggregate of over 10,000 molecular weight in water and have an affinity for each other compared to serum protein such that 10 to 100 per cent remain self aggregated in serum protein; and (3) are lipophyllic and able to disaggregate and attach to cell plasma, nuclear membrane, mitochondria, lysosomes and tissue. The drug obtained by the first method has an empirical formula of approximately C.sub.68 H.sub.70 N.sub.8 O.sub.11 or C.sub.68 H.sub.66 N.sub.8 O.sub.11 Na.sub.4. Neoplastic tissue retains the drug after it has cleared normal tissues and illumination results in necrosis. Moreover, other photosensitizing materials may be combined with a carrier that enters undesirable tissues and cells of the reticular endothelial system such as macrophages. These photosensitizing materials: (1) must have a triplet energy state above 3.5 kilocalories per mole; (2) cannot be easily oxidized; and (3) not physically quench any required energy state. Preferably, this photosensitizing material should be liRIGHTS IN THE U.S. GOVERNMENTThis invention was made with federal support under research grants CA 30840-01 and CA 16717 and contract No. 1-CM-97311, awarded by the National Career Institute, U.S. Department of Health and Human Services. The Government has certain rights to this invention.

    摘要翻译: 为了获得肿瘤选择性的光敏药物,可用于肿瘤组织的定位和治疗异常肿瘤组织如肿瘤,使用两种方法之一。 在第一种方法中,血卟啉与乙酸和硫酸的反应产物的水解混合物循环通过微孔膜系统以排除低分子量产物。 在第二种方法中,合成或衍生自其他吡咯化合物的药物。 药物:(1)包括两个共价结合的基团,每个具有四个环,其中一些是吡咯,例如卟啉,卟啉,二氢卟酚,取代的吡咯,取代的二氢卟酚或取代的藜芦烯,每个组排列成环结构,共价连接 到另一组,并具有高于每摩尔37.5千卡的三线态能量状态; (2)可溶于水,在水中形成超过10,000分子量的聚集体,并且与血清蛋白质相互之间具有亲和力,使得10%至100%在血清蛋白中保持自我聚集; 和(3)是脂蛋白的并且能够解聚并附着于细胞血浆,核膜,线粒体,溶酶体和组织。 通过第一种方法获得的药物具有约C68H70N8O11或C68H66N8O11Na4的经验式。 肿瘤组织清除正常组织后保留药物,照明会导致坏死。 此外,其它光敏材料可以与进入网状内皮系统的不希望的组织和细胞如巨噬细胞的载体组合。 这些光敏材料:(1)必须具有每千克3.5千卡以上的三线态能量状态; (2)不易氧化; 和(3)不能物理地淬灭任何所需的能量状态。 优选地,该光敏材料应该是脂肪族的。

    Method to destroy or impair target cells
    6.
    发明授权
    Method to destroy or impair target cells 失效
    破坏或阻碍目标细胞的方法

    公开(公告)号:US5145863A

    公开(公告)日:1992-09-08

    申请号:US624410

    申请日:1990-12-04

    摘要: To obtain tumor-selective, photosensitizing drugs useful in the localization of neoplastic tissue and treatment of abnormal neoplastic tissue such as tumors, one of two methods is used. In the first method, a hydrolyzed mixture of the products of reaction of hematoporphyrin with acetic acid and sulfuric acid is cycled through a microporous membrane system to exclude low molecular weight products. In the second method, drugs are synthesized or derived from other pyrrole compounds. The drugs: (1) include two covalently bound groups, each with four rings, some of which are pyrroles such as phlorins, porphyrins, chlorins, substituted pyrroles, substituted chlorins or substituted phlorins, each group being arranged in a ring structure, connected covalently to another group and have a triplet energy state above 37.5 kilocalories per mole; (2) are soluble in water, forming an aggregate of over 10,000 molecular weight in water and have an affinity for each other compared to serum protein such that 10 to 100 percent remain self aggregated in serum protein; and (3) are lipophyllic and able to disaggregate and attach to cell plasma, nuclear membrane, mitochondria, lysosomes and tissue. The drug obtained by the first method has an empirical formula of approximately C.sub.68 H.sub.70 N.sub.8 O.sub.11 or C.sub.68 H.sub.66 N.sub.8 O.sub.11 Na.sub.4. Neoplastic tissue retains the drug after it has cleared normal tissues and illumination results in necrosis. Moreover, other photosensitizing materials may be combined with a carrier that enters undesirable tissues and cells of the reticular endothelial system such as macrophages. These photosensitizing materials: (1) must have a triplet energy state above 3.5 kilocalories per mole; (2) cannot be easily oxidized; and (3) not physically quench any required energy state. Preferably, this photosensitizing material should be lipophlic.

    摘要翻译: 为了获得肿瘤选择性的光敏药物,可用于肿瘤组织的定位和治疗异常肿瘤组织如肿瘤,使用两种方法之一。 在第一种方法中,血卟啉与乙酸和硫酸的反应产物的水解混合物循环通过微孔膜系统以排除低分子量产物。 在第二种方法中,合成或衍生自其他吡咯化合物的药物。 药物:(1)包括两个共价结合的基团,每个具有四个环,其中一些是吡咯,例如卟啉,卟啉,二氢卟酚,取代的吡咯,取代的二氢卟酚或取代的藜芦烯,每个组排列成环结构,共价连接 到另一组,并具有高于每摩尔37.5千卡的三线态能量状态; (2)可溶于水,与血清蛋白质相比,在水中形成了超过10,000分子量的聚集体,并且与血清蛋白质具有亲和力,使得10%至100%在血清蛋白中保持自我聚集; 和(3)是脂蛋白的并且能够解聚并附着于细胞血浆,核膜,线粒体,溶酶体和组织。 通过第一种方法获得的药物具有约C68H70N8O11或C68H66N8O11Na4的经验式。 肿瘤组织清除正常组织后保留药物,照明会导致坏死。 此外,其它光敏材料可以与进入网状内皮系统的不希望的组织和细胞如巨噬细胞的载体组合。 这些光敏材料:(1)必须具有每千克3.5千卡以上的三线态能量状态; (2)不易氧化; 和(3)不能物理地淬灭任何所需的能量状态。 优选地,该光敏材料应该是脂肪族的。

    Hematoporphyrin derivatives and process of preparing
    8.
    发明授权
    Hematoporphyrin derivatives and process of preparing 失效
    血卟啉衍生物及其制备方法

    公开(公告)号:US4866168A

    公开(公告)日:1989-09-12

    申请号:US889829

    申请日:1986-07-24

    摘要: To obtain tumor-selective, photosensitizing drugs useful in the localization of neoplastic tissue and treatment of abnormal neoplastic tissue such as tumors, one of two methods is used. In the first method, a hydrolyzed mixture of the products of reaction of hematoporphyrin with acetic acid and sulfuric acid is cycled through a microporous membrane system to exclude low molecular weight products. In the second method, drugs are synthesized or derived from other pyrrole compounds. The drugs: (1) include two covalently bound groups, each with four rings, some of which are pyrroles such as phlorins, porphyrins, chlorins, substituted pyrroles, substituted chlorins or substituted phlorins, each group being arranged in a ring structure, connected covalently to another group and have a triplet energy state above 37.5 kilocalories per mole; (2) are soluble in water, forming an aggregate of over 10,000 molecular weight in water and have an affinity for each other compared to serum protein such that 10 to 100 percent remain self aggregated in serum protein; and (3) are lipophyllic and able to disaggregate and attach to cell plasma, nuclear membrane, mitochondria, lysosomes and tissue. The drug obtained by the first method has an empirical formula of approximately C.sub.68 H.sub.70 N.sub.8 O.sub.11 or C.sub.68 H.sub.66 N.sub.8 O.sub.11 Na.sub.4. Neoplastic tissue retains the drug after it has cleared normal tissues and illumination results in necrosis. Moreover, other photosensitizing materials may be combined with a carrier that enters undesirable tissues and cells of the reticular endothelial system such as macrophages. These photosensitizing materials: (1) must have a triplet energy state above 3.5 kilocalories per mole; (2) cannot be easily oxidized; and (3) not physically quench any required energy state. Preferably, this photosensitizing material should be lipophlic.

    摘要翻译: 为了获得肿瘤选择性的光敏药物,可用于肿瘤组织的定位和治疗异常肿瘤组织如肿瘤,使用两种方法之一。 在第一种方法中,血卟啉与乙酸和硫酸的反应产物的水解混合物循环通过微孔膜系统以排除低分子量产物。 在第二种方法中,合成或衍生自其他吡咯化合物的药物。 药物:(1)包括两个共价结合的基团,每个具有四个环,其中一些是吡咯,例如卟啉,卟啉,二氢卟酚,取代的吡咯,取代的二氢卟酚或取代的藜芦烯,每个组排列成环结构,共价连接 到另一组,并具有高于每摩尔37.5千卡的三线态能量状态; (2)可溶于水,与血清蛋白质相比,在水中形成了超过10,000分子量的聚集体,并且与血清蛋白质具有亲和力,使得10%至100%在血清蛋白中保持自我聚集; 和(3)是脂蛋白的并且能够解聚并附着于细胞血浆,核膜,线粒体,溶酶体和组织。 通过第一种方法获得的药物具有约C68H70N8O11或C68H66N8O11Na4的经验式。 肿瘤组织清除正常组织后保留药物,照明会导致坏死。 此外,其它光敏材料可以与进入网状内皮系统的不希望的组织和细胞如巨噬细胞的载体组合。 这些光敏材料:(1)必须具有每千克3.5千卡以上的三线态能量状态; (2)不易氧化; 和(3)不能物理地淬灭任何所需的能量状态。 优选地,该光敏材料应该是脂肪族的。

    Fiber optic positioner
    9.
    发明授权
    Fiber optic positioner 失效
    光纤定位器

    公开(公告)号:US5671317A

    公开(公告)日:1997-09-23

    申请号:US680936

    申请日:1996-07-16

    摘要: Method and apparatus for stabilizing a fiber optic relative to the skin surface of a patient so that radiation from the fiber optic strikes a defined surface area on the skin independently of patient movement. The apparatus comprises a polypod support having a fiber optic supporting platform and at least three legs to form a tripod. Each of the legs has two ends, a first of which is secured to the fiber optic supporting platform and the second of which is securely attached to the skin of the patient, either directly or by means of a foot attached to the second end. The method of the present invention comprises attaching a polypod, as above described, to the skin of a patient and irradiating a defined surface area by means of an end of a fiber optic held by the polypod support.

    摘要翻译: 用于使光纤相对于患者皮肤表面稳定的方法和装置,使得来自光纤的辐射独立于患者运动而撞击皮肤上限定的表面区域。 该装置包括具有光纤支撑平台和至少三条腿以形成三脚架的息肉支架。 每个腿部具有两个端部,第一个端部固定到光纤支撑平台上,其中第二个端部直接地或通过连接到第二端部的脚牢固地附接到患者的皮肤。 本发明的方法包括如上所述将息肉附着到患者​​的皮肤上,并通过由息肉支撑体保持的光纤的一端照射限定的表面区域。

    Fiber optic positioner
    10.
    发明授权
    Fiber optic positioner 失效
    光纤定位器

    公开(公告)号:US06868221B1

    公开(公告)日:2005-03-15

    申请号:US10434420

    申请日:2003-05-08

    IPC分类号: A61B19/00 A61N5/06 G02B6/46

    CPC分类号: A61B90/11 A61B90/50 A61N5/062

    摘要: The present invention relates to an apparatus which includes a polypod support which includes a fiber optic supporting platform. The fiber optic supporting platform includes an opening. The apparatus further includes at least three legs forming a tripod, each of the legs having two ends, a first end being secured to the fiber optic supporting platform and the second end being adapted for attachment to the skin of the patient, a first tube having an outer diameter, a second tube having an outer diameter and an inner diameter, where the inner diameter of the second tube surrounds the outer diameter of the first tube and where the outer diameter of the second tube is slidably mounted within the opening of the fiber optic surrounding platform and a fiber optic.

    摘要翻译: 本发明涉及一种装置,其包括一个包含光纤支撑平台的息肉支架。 光纤支撑平台包括开口。 所述装置还包括形成三脚架的至少三个腿部,所述腿部中的每一个具有两个端部,第一端部固定到所述光纤支撑平台,并且所述第二端部适于附接到所述患者的皮肤,所述第一管具有 外径,第二管具有外径和内径,第二管的内径围绕第一管的外径,第二管的外径可滑动地安装在纤维的开口内 光学周边平台和光纤。