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    • 91. 发明申请
    • HYDROXYALKYL CYCLODEXTRIN-ANTIFUNGAL POLYENE ANTIBIOTICS COMPLEXES
    • 羟克霉素环糊精 - 抗真菌多聚体抗生素复合物
    • WO1989010739A1
    • 1989-11-16
    • PCT/US1989001912
    • 1989-05-05
    • BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM
    • BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEMANAISSIE, Elias, J.PITHA, JosephBODEY, Gerald, P.
    • A61K09/18
    • B82Y5/00A61K31/7048A61K47/6951
    • The present invention involves a composition of matter comprising amphotericin B and hydroxyalkyl-gamma-cyclodextrin. The hydroxyalkyl-gamma-cyclodextrin is preferably hydroxypropyl-gamma-cyclodextrin, most preferably 2-hydroxypropyl-gamma-cyclodextrin. The cyclodextrin utilized in the practice of the present invention comprises rings of eight glucose units bound in 1-4 glucosidic linkages, each glucose unit having a hydroxyalkyl radical in ether linkage. The hydroxyalkyl radical is bound in ether linkage to carbon-5 of the glucose unit. The composition of matter of the present invention preferably comprises a cyclodextrin ring of eight glucose units bound in 1-4 glucosidic linkages, substantially each glucose unit having a 2-hydroxypropyl radical in ether linkage. The present invention also involves a method for the treatment of an animal with fungal infection. This method comprises administering to the animal a fungicidally effective amount of a composition of matter as described above comprising amphotericin B and hydroxyalkyl-gamma-cyclodextrin. The administration is preferably parenteral, particularly for disseminated fungal infection, but could be internal or topical, depending upon the particular site of fungal infection and desires of the treating physician. The disseminated fungal infection most preferably treated is a yeast infection such as a Candida albicans, Candida tropicalis, Candida parapsiloses or Torulopsis glabrata infection. The fungicidally effective amount useful for treatment of disseminated fungal infection contains between about 0.4 mg amphotericin B per kg body weight and about 4.0 mg amphotericin B per kg body weight.
    • 本发明涉及包含两性霉素B和羟烷基-γ-环糊精的物质组合物。 羟烷基-γ-环糊精优选为羟丙基-γ-环糊精,最优选为2-羟丙基-γ-环糊精。 在本发明的实践中使用的环糊精包含以1-4个糖苷键连接的8个葡萄糖单元的环,每个葡萄糖单元具有醚键中的羟烷基。 羟烷基与醚键连接成葡萄糖单元的碳-5。 本发明的物质组合物优选包含以1-4个糖苷键连接的8个葡萄糖单元的环糊精环,基本上每个葡萄糖单元具有醚键中的2-羟丙基。 本发明还涉及一种用于治疗具有真菌感染的动物的方法。 该方法包括向动物施用杀真菌有效量的包含两性霉素B和羟烷基-γ-环糊精的如上所述的物质组合物。 给药优选为肠胃外,特别是对于播散性真菌感染,但可以是内部或局部,这取决于治疗医师的真菌感染和欲望的特定部位。 最优选处理的播散性真菌感染是酵母感染,例如白色念珠菌,热带假丝酵母,副伤寒假丝酵母或光滑罗非鱼感染。 用于治疗播散性真菌感染的杀真菌有效量含有约0.4mg两性霉素B / kg体重和约4.0mg两性霉素B / kg体重。
    • 93. 发明申请
    • GLYCOSAMINOGLYCAN DERIVATIVES AND THEIR USE AS INHIBITORS OF TUMOR INVASIVENESS OR METASTATIC PROFUSION
    • 谷氨酰胺糖苷衍生物及其作为肿瘤侵袭或分子生物学抑制剂的用途
    • WO1988001280A1
    • 1988-02-25
    • PCT/US1987002035
    • 1987-08-18
    • BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM
    • BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEMNICOLSON, Garth, L.IRIMURA, TatsuroNAKAJIMA, Motowo
    • C08B37/10
    • A61K31/715C08B37/0075
    • Method for impeding the formation of tumor metastasis or tumor invasiveness in a host. Such inhibition comprises administration to the host of a glycosaminoglycan derivative substantially devoid of anticoagulation activity and is an effective inhibitory of heparanase activity. Such a glycosaminoglycan derivative may be provided by purchase or synthesis as directed herein. Parenteral administration to a tumor-bearing host of the glycosaminoglycan derivative results in the exposure of host-borne tumor cells thereto. Such exposure to effective levels of the derivative results in the inhibition of tumor heparanase activity and a lessening of invasiveness and metastatic spread. Heparin, a glycosaminoglycan particularly effective as a heparanase inhibitor and an anti-clotting agent, is a preferred glycosaminoglycan for derivatization. Upon derivatization according to the present invention heparin may be converted into a glycosaminoglycan derivative substantially devoid of anticoagulant activity but yet being an effective inhibitor of heparanase activity. Mere reduction of heparin carboxyl groups results in the production of a glycosaminoglycan derivative inhibitory to heparanase activity but without substantially anticoagulant activity non-anticoagulating, heparanase-inhibiting glycosaminoglycan derivatives may also be prepared from heparin, for example, by: at least partial N-desulfation and then N-acetylation; or N-, O-desulfation followed by N-resulfation.
    • 阻止宿主中肿瘤转移或肿瘤浸润形成的方法。 这种抑制包括向宿主施用基本上没有抗凝活性的糖胺聚糖衍生物,并且是对肝素酶活性的有效抑制。 这样的糖胺聚糖衍生物可以通过如本文所述的购买或合成来提供。 对葡萄糖胺聚糖衍生物的肿瘤宿主的肠胃外给药导致宿主携带的肿瘤细胞暴露于其中。 这种暴露于有效水平的衍生物导致抑制肿瘤乙酰肝素酶活性和降低侵袭性和转移性扩散。 肝素,作为乙酰肝素酶抑制剂和抗凝血剂特别有效的糖胺聚糖是用于衍生化的优选的糖胺聚糖。 根据本发明的衍生化,肝素可以转化为基本上没有抗凝血活性但仍然是乙酰肝素酶活性的有效抑制剂的糖胺聚糖衍生物。 肝素羧基的简单还原导致抑制乙酰肝素酶活性但不具有非抗凝血活性的糖胺聚糖衍生物的产生,也可由肝素制备乙酰肝素酶抑制糖胺聚糖衍生物,例如:至少部分N-脱硫 然后进行N-乙酰化; 或N-,O-脱硫,随后进行N-硫酸化。
    • 97. 发明申请
    • AN ELECTRONIC AUTOROUTING NAVIGATION SYSTEM FOR VISUALLY IMPAIRED PERSONS
    • 用于视觉受损人员的电子自动导航系统
    • WO1998008108A1
    • 1998-02-26
    • PCT/US1997014525
    • 1997-08-19
    • BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEMHANCOCK, Michael, B.
    • BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM
    • G01S03/02
    • G01C21/20G01S1/70
    • The present invention is an autorouting navigation system (100) for directing one or more visually impaired persons to a physical location. The present invention includes a portable autonavigation unit (100) that includes an input device (106) for selecting a target location corresponding to a physical location of a plurality of location beacons, a receiver (101) configured to receive signals from location beacons, a memory (103) storing information correlating the locations of the location beacons, and an output device (104) for communicating with the user. A microcontroller (105) or microprocessor under program control processes the signals received from the location beacons, analyzes those signals and correlation data, and determines a routing path from the user's present position to the target location. The microcontroller (105) may also provide an indication, such as an audible sound, to the user of whether or not the user is following the routing path to the target location.
    • 本发明是一种用于将一个或多个视障人员引导到物理位置的自动布线导航系统(100)。 本发明包括便携式自动导航单元(100),其包括用于选择对应于多个位置信标的物理位置的目标位置的输入设备(106),被配置为从位置信标接收信号的接收机(101) 存储器(103)存储与位置信标的位置相关的信息,以及用于与用户通信的输出设备(104)。 在程序控制下的微控制器(105)或微处理器处理从位置信标接收到的信号,分析这些信号和相关数据,并且确定从用户的当前位置到目标位置的路由路径。 微控制器(105)还可以向用户提供关于用户是否遵循到目标位置的路由路径的指示,例如可听见的声音。