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    • 52. 发明授权
    • Carotene analogs of porphyrins, chlorins and bacteriochlorins as
therapeutic and diagnostic agents
    • 卟啉类胡萝卜素类似物,二氢卟酚和细菌毒素作为治疗和诊断剂
    • US6103751A
    • 2000-08-15
    • US102417
    • 1998-06-22
    • Ravindra K. PandeyWilliam R. PotterThomas J. Dougherty
    • Ravindra K. PandeyWilliam R. PotterThomas J. Dougherty
    • A61K49/00C07D487/22C07D519/00A61K31/40
    • A61K49/0036A61K49/0052C07D487/22C07D519/00
    • A carotene conjugate of the formula: ##STR1## where R.sup.1 is hydrogen or methyl; R.sup.2 is: ##STR2## R.sup.3, R.sup.4 and R.sup.5 are independently, hydrogen, methyl or ethyl; R.sup.6 and R.sup.7 are independently --R.sup.13, --OR , --C(R.sup.6)(O), --C(R.sup.16).sub.2 OR.sup.13, --CH.dbd.CHR.sup.13, or --(CH.sub.2)R.sup.14 ; R.sup.8 is --R.sup.13, --OR.sup.13, --C(R.sup.16)(O), --C(R.sup.16).sub.2 OR.sup.13, --CH.dbd.CHR.sup.13, or --(CH.sub.2)R.sup.14 or taken with R.sup.10 is .dbd.O; R.sup.9 is --R.sup.13, --OR.sup.13, --C(R.sup.16)(O), --C(R.sup.16).sub.2 OR.sup.13, --CH.dbd.CHR.sup.13, or --(CH.sub.2)R.sup.14 or taken with R.sup.10 is a chemical bond; R.sup.10 is --R.sup.13, --OR.sup.13, --C(R.sup.16)(O) , --C(R.sup.16).sub.2 OR.sup.13, --CH.dbd.CHR.sup.13, or --(CH.sub.2)R.sup.14 or taken together with R.sup.9 is a chemical bond or taken with R.sup.8 is .dbd.O; R.sup.11 is R.sup.13, or --OR.sup.13 ; R.sup.12 is --C(R.sup.13).sub.2 C(Y)--, --C(O)O(O)C--, --C(NR.sup.13)O(O)C--, or --C(O)N(R.sup.15)--C(O)--; R.sup.13 is, independently at each occurrence, hydrogen or lower alkyl of from 1 through about 10 carbon atoms; R.sup.14 is an amino acid residue, R.sup.15 is --R.sup.13, --R.sup.14, or --C(O)NHR.sup.13 ; R.sup.16 is, independently at each occurrence, hydrogen or lower alkyl of 1 to about 4 carbon atoms and Y is .dbd.O, .dbd.S, or 2H--.
    • 下式的胡萝卜素缀合物:其中R1是氢或甲基; R2是:R3,R4和R5独立地是氢,甲基或乙基; R6和R7独立地是-R13,-OR,-C(R6)(O),-C(R16)2OR13,-CH = CHR13或 - (CH2)R14; R8是-R13,-OR13,-C(R16)(O),-C(R16)2OR13,-CH = CHR13或 - (CH2)R14,或R10为= R9为-R13,-OR13,-C(R16)(O),-C(R16)2OR13,-CH = CHR13或 - (CH2)R14或R10为化学键; R 10为-R 13,-OR 13,-C(R 16)(O),-C(R 16)2 OR 13,-CH = CHR 13或 - (CH 2)R 14或与R 9一起为化学键, O; R11是R13或-OR13; R 12是-C(R 13)2 C(Y) - , - C(O)O(O)C - , - C(NR 13)O(O)C-或-C(O)N(R 15) O) - ; R 13在每次出现时独立地为氢或1至约10个碳原子的低级烷基; R14是氨基酸残基,R15是-R13,-R14或-C(O)NHR13; R 16在每次出现时独立地为氢或1至约4个碳原子的低级烷基,Y为= O,= S或2H-。
    • 58. 发明授权
    • In situ photodynamic therapy
    • 原位光动力疗法
    • US5257970A
    • 1993-11-02
    • US865918
    • 1992-04-09
    • Thomas J. Dougherty
    • Thomas J. Dougherty
    • A61K9/127A61K31/40A61K31/50A61K31/66A61K41/00A61N1/30
    • A61K9/127A61K31/40A61K31/50A61K31/66A61K41/0057A61K41/0071
    • The process of photodynamic therapy (PDT) is conducted by the step of:1) separately encapsulating at least one activation component for said photodynamic therapy process in a liposome;2) injecting a photosensitizer into a human or animal host;3) injecting the liposome encapsulated components systemically into the same human or animal host; and4) heating the site of the tumor to melt the liposome encapsulated components to permit mixing of the activation components.The mixing of the activation components can result in:a) energy transfer to the previously injected photosensitizer;b) emission of light and absorption of said light by the previously injected photosensitizer; andc) direct formation of at least one cytotoxic species that functions against the tumor.The heating of the site of the tumor is accomplished by one of the following methods: laser, ultra sound, radio-frequency or microwave frequency. Photofrin photosensitizer is a preferred photosensitizer.
    • 光动力学治疗(PDT)的过程是通过以下步骤进行的:1)在脂质体中分别封装所述光动力学治疗过程的至少一种活化成分; 2)将光敏剂注入人或动物宿主; 3)将脂质体包封的组分全身注入相同的人或动物宿主中; 和4)加热肿瘤部位以熔化脂质体包封的组分以允许活化组分的混合。 活化组分的混合可导致:a)能量转移到先前注射的光敏剂; b)通过先前注射的光敏剂发射光和吸收所述光; 和c)直接形成对肿瘤起作用的至少一种细胞毒性物质。 通过以下方法之一实现肿瘤部位的加热:激光,超声,射频或微波频率。 Photofrin光敏剂是优选的光敏剂。
    • 59. 发明授权
    • Bacteriochlorophyll-a derivatives useful in photodynamic therapy
    • 细菌叶绿素a衍生物可用于光动力学治疗
    • US5173504A
    • 1992-12-22
    • US638172
    • 1991-01-03
    • Thomas J. Dougherty
    • Thomas J. Dougherty
    • A61K41/00C07D487/22
    • C07D487/22A61K41/0071
    • Compounds of formula (1) or formula (2): ##STR1## wherein M is a non-paramagnetic metal selected from Mg.sup.+2, Sn.sup.+2, and Zn.sup.+2, or represents 2 H.sup.30 each H.sup.+ bonded to one of the N atoms connected by the solid lines;R.sup.1 is a saturated of unsaturated hydrocarbyl residue of 8-25 C.;each R.sup.2 is independently selected from the group consisting of vinyl, ethyl, acetyl and 1-hydroxyethyl, andX is COOR.sup.3, wherein R.sup.3 is alkyl (1-C);are useful in photodynamic therapy and diagnosis. These compounds photosensitize target biological substrates to irradiation, and treating said substrates with these sensitizers followed by irradiation leads to the impairment or destruction of the biological substrate. When administered systemically, these compounds accumulate in the undesired target biological substrate. The compounds can also be utilized in vitro, for example to destroy infectious cells or viruses in blood intended for transfusion.
    • (1)或式(2)的化合物:其中M是选自Mg + 2,Sn + 2和Zn + 2的非顺磁性金属,或表示2 H30每个H +与通过实线连接的N个原子之一键合; R1是饱和的8-25℃的不饱和烃基残基。 每个R 2独立地选自乙烯基,乙基,乙酰基和1-羟乙基,X是COOR 3,其中R 3是烷基(1-C); 可用于光动力疗法和诊断。 这些化合物对目标生物底物进行光敏照射,用这些敏化剂处理所述底物,然后照射导致生物底物的损伤或破坏。 当全身施用时,这些化合物积聚在不需要的靶生物底物中。 也可以在体外使用这些化合物,例如以破坏用于输血的血液中的感染性细胞或病毒。
    • 60. 发明授权
    • Method and apparatus for sealing a battery terminal post
    • 密封电池端子柱的方法和装置
    • US4775604A
    • 1988-10-04
    • US80154
    • 1987-07-29
    • Thomas J. DoughertyRichard A. HamannMatthias Geibl
    • Thomas J. DoughertyRichard A. HamannMatthias Geibl
    • H01M2/06H01M2/08H01M2/02
    • H01M2/08H01M2/06
    • The interface between the plastic cover of a battery container and the lead or other metal terminal post which extends therethrough is sealed with a rubber bushing which is compressed and extruded along the terminal post during installation and locked tightly in its compressed and extruded state. The bushing preferably has a pair of oppositely angled intersecting frustoconical surfaces on its exterior surface which are adapted to cooperate with mating surfaces surrounding the opening in the cover and on a locking retainer. The assembly provides a flexible seal which will accommodate the inevitable vertical movement of the terminal post as a result of battery element expansion. Most importantly, the assembly provides an extremely effective barrier to the migration of electrolyte along the terminal post to prevent outer terminal corrosion. The rubber bushing is preferably impregnated with silicone oil which, when the bushing is installed, fills the surface voids in the cast terminal post which otherwise provide paths for electrolyte migration. The silicone oil also provides a lubricant for the controlled compression and extrusion of the bushing.
    • 电池容器的塑料盖和延伸穿过其的导线或其他金属端子柱之间的界面用橡胶衬套密封,橡胶衬套在安装期间沿着端子柱压缩和挤出并且紧密地锁定在其压缩和挤压状态。 套管优选地在其外表面上具有一对相对角度的相交的截头圆锥形表面,其适于与围绕盖中的开口的配合表面和锁定保持器协作。 组件提供了柔性密封,其将适应由于电池元件膨胀而导致的端子柱的不可避免的垂直运动。 最重要的是,该组件为电极沿着端子柱的迁移提供了非常有效的屏障,以防止外部端子腐蚀。 橡胶衬套优选地浸渍有硅油,当安装衬套时,填充铸造端子柱中的表面空隙,否则其提供用于电解质迁移的路径。 硅油还提供润滑剂用于受控压缩和挤压衬套。