Iodo-Hexose Compounds Useful to Treat Cancer
    4.
    发明申请
    Iodo-Hexose Compounds Useful to Treat Cancer 有权
    可用于治疗癌症的碘己糖化合物

    公开(公告)号:US20100152121A1

    公开(公告)日:2010-06-17

    申请号:US12581550

    申请日:2009-10-19

    IPC分类号: A61K31/70 C07H5/02 A61P35/00

    CPC分类号: C07H15/04

    摘要: Methods of treating glioblastoma and pancreatic cancer are provided by the administration of a therapeutically effective amount of a iodo-hexose compound to a subject in need thereof. The subject disclosure includes methods of treating glioblastoma and pancreatic cancer comprising the administration of a therapeutically effective amount of a 2-deoxy-2-iodo-D-hexose compound including 2-deoxy-2-iodo-D-mannose, 2-deoxy-2-iodo-D-glucose, 2-deoxy-2-iodo-D-galactose, and/or 2-deoxy-2-iodo-D-talose to a subject in need thereof.

    摘要翻译: 通过向有需要的受试者施用治疗有效量的碘代己糖化合物来提供治疗胶质母细胞瘤和胰腺癌的方法。 本发明公开内容包括治疗胶质母细胞瘤和胰腺癌的方法,包括施用治疗有效量的2-脱氧-2-碘-D-己糖化合物,包括2-脱氧-2-碘-D-甘露糖,2-脱氧-2- 2-碘-D-葡萄糖,2-脱氧-2-碘-D-半乳糖和/或2-脱氧-2-碘-D-托洛糖。

    Submicron liposome suspensions obtained from preliposome lyophilizates
    5.
    发明授权
    Submicron liposome suspensions obtained from preliposome lyophilizates 失效
    从preliposome冻干液获得的亚微米脂质体悬浮液

    公开(公告)号:US07238366B1

    公开(公告)日:2007-07-03

    申请号:US09122427

    申请日:1998-07-24

    IPC分类号: A61K9/127

    摘要: This invention provides an aqueous/t-butanol solvent-system, facile reconstitute, submicron-reconsitiute preliposome-lyophilaye and method of its preparation and use.In one embodiment this entails a modified method for the preparation of a submicron and stable liposome formulation of the non-cross-resistant anthracycline Annamycin is described. The optimal lipid composition was DMPC:DMPG at a 7:3 molar ratio and the optimal lipid:drug weight ratio 50:1. The selected formulation is a preliposome lyophilized powder that contains the phospholipids, Annamycin, and 1.7 mg Tween 20 per mg of Annamycin. The liposome suspension is obtained on the day of use by adding normal saline at 37° C. (1 ml per mg Annamycin) and hand-shaking for one minute. The presence of Tween 20 is essential in shortening the reconstitution step (from >2 hours to 1 minute), avoiding the early formation of free drug crystals, and reducing the median particle size (from 1.5 μm to 0.15-0.20 μm) without destruction of the liposome vesicles. The chemical stability of the preliposome powder at room temperature was >3 months and the chemical and physical stability of the liposome suspension at room temperature >24 hours. The in vitro cytotoxicity of the formulation was equivalent to that prepared by the standard evaporation method. The results of the study indicate that small amounts of surfactant may be used to enhance the reconstitution step and reduce the liposome size of lyophilized liposome formulations of lipophilic drugs.

    摘要翻译: 本发明提供了一种水性/叔丁醇溶剂系统,易于重构,亚微米 - 重新分离的前脂质体 - 冻干物及其制备和使用的方法。 在一个实施方案中,这涉及用于制备非交联耐蒽环霉素Annamycin的亚微米和稳定的脂质体制剂的修饰方法。 最佳脂质组成为DMPC:DMPG,摩尔比为7:3,最佳脂质:药物重量比为50:1。 选择的制剂是含有磷脂,安环素和每毫克安环霉素1.7mg吐温20的前脂质体冻干粉末。 在使用当天通过在37℃下加入生理盐水(1毫升/毫克安环霉素)获得脂质体悬浮液,并手摇1分钟。 Tween 20的存在对于缩短重构步骤(从2小时至1分钟)是必不可少的,避免早期形成游离药物晶体,并将中值粒度(从1.5μm至0.15-0.20μm)降低,而不破坏 脂质体囊泡。 原脂质体粉末在室温下的化学稳定性> 3个月,脂质体悬浮液在室温> 24小时的化学和物理稳定性。 制剂的体外细胞毒性等同于通过标准蒸发法制备的细胞毒性。 研究结果表明,少量的表面活性剂可用于增强重组步骤,降低亲脂性药物冻干脂质体制剂的脂质体大小。

    14-acyloxy-2'-halo-anthracycline anti-cancer antibiotics
    9.
    发明授权
    14-acyloxy-2'-halo-anthracycline anti-cancer antibiotics 失效
    14-酰氧基-2'-卤 - 蒽环类抗癌抗生素

    公开(公告)号:US4772688A

    公开(公告)日:1988-09-20

    申请号:US42624

    申请日:1987-04-23

    IPC分类号: C07H15/252 C07H15/24

    CPC分类号: C07H15/252

    摘要: Compounds of the formula (I) and pharmaceutical preparations containing the same are disclosed ##STR1## wherein R.sup.1 is --OOCR.sup.3 or --OOC(CH.sub.2).sub.n COOR.sup.4 ; R.sup.2 is hydrogen, hydroxy or methoxy; one of X and X' is a halogen atom selected from the group consisting of fluorine, chlorine, bromine and iodine and the other is hydrogen; one of Y and Y' is hydrogen and the other is selected from the group consisting of hydrogen, hydroxy and acyloxy; one of Z and Z' is hydrogen and the other is selected from the group consisting of hydrogen, hydroxy and acyloxy; R.sup.3 is an alkyl group containing 1 to 8 carbon atoms; R.sup.4 is a hydrogen atom, a metal atom, or an alkyl group containing 1 to 4 carbon atoms; and n is an integer of 0 to 6. These compounds are active in the inhibition of malignant diseases.

    摘要翻译: 公开了式(I)化合物和含有该化合物的药物制剂,其中R 1是-OOCR 3或-OOC(CH 2)n COOR 4; R2是氢,羟基或甲氧基; X和X'之一是选自氟,氯,溴和碘的卤素原子,另一个是氢; Y和Y'之一是氢,另一个选自氢,羟基和酰氧基; Z和Z'之一是氢,另一个选自氢,羟基和酰氧基; R3是含有1至8个碳原子的烷基; R4是氢原子,金属原子或含有1至4个碳原子的烷基; n为0〜6的整数。这些化合物在恶性疾病的抑制中具有活性。