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    • 15. 发明授权
    • Spin trapping pharmaceutical compositions and methods for use thereof
    • 旋转捕获药物组合物及其使用方法
    • US06403627B1
    • 2002-06-11
    • US09357297
    • 1999-07-20
    • John M. CarneyRobert A. Floyd
    • John M. CarneyRobert A. Floyd
    • A61K31415
    • A61K31/135A61K31/15A61K31/167A61K31/40A61K31/44A61K31/445C07C291/02
    • Spin trapping compositions in general have now been discovered to be effective in treating a variety of disorders, including disorders such as those arising from ischemia, infection, inflammation, exposure to radiation or cytotoxic compounds, not just of the central and peripheral nervous systems but of peripheral organ disease having a wide variety of etiologies. In the preferred embodiment, the compositions for treating tissue damage from ischemia contain PBN, or active derivatives thereof, in a suitable pharmaceutical carrier for intravenous, oral, topical, or nasal/pulmonary administration. Other preferred spin-trapping agents include 5,5-dimethyl pyrroline N-oxide (DMPO), &agr;-(4-pyridyl-1-oxide)-N-tert-butylnitrone (POBN), and (TEMPO) and spin-trapping derivatives thereof. Examples of derivatives of PBN include halogenated derivatives, bifunctional derivatives, conjugates with drugs or targeting molecules, dimers and cyclodextran polymers of PBN. Many different disorders can be treated using these compounds, including diseases or disorders of the central and peripheral nervous systems, and disorders arising from ischemia, infection, inflammation, oxidation from exposure to radiation or cytotoxic compounds, as well as due to naturally occurring processes such as aging.
    • 现在已经发现旋转捕获组合物现在已被发现有效地治疗各种疾病,包括诸如由局部缺血,感染,炎症,暴露于辐射或细胞毒性化合物引起的疾病,不仅仅是中枢和周围神经系统,而是 外周器官疾病具有多种病因。 在优选的实施方案中,用于治疗缺血组织损伤的组合物在用于静脉内,口服,局部或鼻/肺部施用的合适的药物载体中含有PBN或其活性衍生物。 其他优选的自旋捕获剂包括5,5-二甲基吡咯啉N-氧化物(DMPO),α-(4-吡啶基-1-氧化物)-N-叔丁基硝酮(POBN)和(TEMPO)和自旋捕获衍生物 其中。 PBN衍生物的实例包括卤代衍生物,双官能衍生物,与药物或靶向分子的缀合物,二聚体和PBN的环糊精聚合物。 可以使用这些化合物治疗许多不同的病症,包括中枢和周围神经系统的疾病或病症,以及由缺血,感染,炎症,暴露于辐射或细胞毒性化合物的氧化引起的疾病,以及由于天然存在的过程 作为老化。
    • 19. 发明授权
    • Spin trapping pharmaceutical compositions and methods for use thereof
    • 旋转捕获药物组合物及其使用方法
    • US5622994A
    • 1997-04-22
    • US212800
    • 1994-03-15
    • John M. CarneyRobert A. Floyd
    • John M. CarneyRobert A. Floyd
    • A61K31/15A61K31/167A61K31/40A61K31/44A61K31/255
    • A61K31/44A61K31/15A61K31/167A61K31/40
    • Spin trapping compositions in general have now been discovered to be effective in treating a variety of disorders, including disorders such as those arising from ischemia, infection, inflammation, exposure to radiation or cytotoxic compounds, not just of the central and peripheral nervous systems but of peripheral organ disease having a wide variety of etiologies. In the preferred embodiment, the compositions for treating tissue damage from ischemia contain PBN, or active derivatives thereof, in a suitable pharmaceutical carrier for intravenous, oral, topical, or nasal/pulmonary administration. Many different disorders can be treated using these compounds, including diseases or disorders of the central and peripheral nervous systems, and disorders arising from ischemia, infection, inflammation, oxidation from exposure to radiation or cytotoxic compounds, as well as due to naturally occurring processes such as aging.
    • 现在已经发现旋转捕获组合物现在已被发现有效地治疗各种疾病,包括诸如由局部缺血,感染,炎症,暴露于辐射或细胞毒性化合物引起的疾病,不仅仅是中枢和周围神经系统,而是 外周器官疾病具有多种病因。 在优选的实施方案中,用于治疗缺血组织损伤的组合物在用于静脉内,口服,局部或鼻/肺部施用的合适的药物载体中含有PBN或其活性衍生物。 可以使用这些化合物治疗许多不同的病症,包括中枢和周围神经系统的疾病或病症,以及由缺血,感染,炎症,暴露于辐射或细胞毒性化合物的氧化引起的疾病,以及由于天然存在的过程 作为老化。
    • 20. 再颁专利
    • Phenylbutyl nitrone compositions and methods for prevention of gastric
ulceration
    • 苯丁基硝酮组合物和预防胃溃疡的方法
    • USRE35213E
    • 1996-04-16
    • US97998
    • 1993-07-29
    • Robert A. FloydJohn M. Carney
    • Robert A. FloydJohn M. Carney
    • A61K31/135A61K31/15A61K31/40A61K31/44A61K31/415
    • A61K31/44A61K31/135A61K31/15A61K31/40
    • Compositions containing PBN, or active derivatives thereof, in a suitable pharmaceutical carrier for administration to a patient, are disclosed for treating or preventing gastric ulceration caused by ingestion of non-steroidal anti-inflammatories. Based on animal studies, the dosage is in the range of 3 to 300 mg/kg and is administered prior to, simultaneously, or shortly after ingestion of the NSAID compounds(s). In the preferred embodiment, the range is between 10 and 30 mg/kg, depending on the dosage unit required to protect the mucosa. The preferred method of administration is orally, alone or in combination with the non-steroidal anti-inflammatory. It is believed that the PBN is also useful alone for treatment or prevention of ulcers, aspects of diarrhea, gastritis, esophagitis, ileitis, and as an analgesic.
    • 公开了用于治疗或预防摄取非甾体抗炎药引起的胃溃疡的含有PBN或其活性衍生物的组合物在用于给予患者的合适的药物载体中。 基于动物研究,剂量在3至300mg / kg的范围内,并且在摄入NSAID化合物之前,同时或不久之后施用。 在优选的实施方案中,取决于保护粘膜所需的剂量单位,范围在10至30mg / kg之间。 优选的给药方法是口服,单独使用或与非甾体抗炎剂组合。 据信PBN还可用于治疗或预防溃疡,腹泻,胃炎,食管炎,回肠炎和止痛剂的方面。