Method of reducing chemotherapy toxicity using
(methylaminopropylamino)propyl dihydrogen phosphorothioate
    2.
    发明授权
    Method of reducing chemotherapy toxicity using (methylaminopropylamino)propyl dihydrogen phosphorothioate 失效
    (甲基氨基丙基氨基)丙基二硫代磷酸酯降低化疗毒性的方法

    公开(公告)号:US5292497A

    公开(公告)日:1994-03-08

    申请号:US39690

    申请日:1993-03-29

    摘要: A method of decreasing the toxicity of chemical therapeutic agents administered in cancer chemotherapy including adminstration to a patient undergoing chemotherapy. This reduction in toxicity can be accomplished by administering an effective amount of S-3-(3-methylaminopropylamino)propyl dihydrogen phosphorothioate. Methods of inducing mucolytic activity and reducing toxicity of acetominophen overdose are also discussed. Such activities are induced through the administration of S-3-(3-methylaminopropylamino)propyl dihydrogen phosphorothioate.

    摘要翻译: 一种降低化学治疗剂在癌症化学疗法中的毒性的方法,包括给予经历化疗的患者。 这种毒性的降低可以通过施用有效量的S-3-(3-甲基氨基丙基氨基)丙基二硫代磷酸酯来实现。 还讨论了诱导醋酸布洛芬过量的粘液分解活性和降低毒性的方法。 通过施用S-3-(3-甲基氨基丙基氨基)丙基二硫代磷酸酯诱导这些活性。

    Methods of using aminothiols to promote hematopoietic progenitor cell
growth
    3.
    发明授权
    Methods of using aminothiols to promote hematopoietic progenitor cell growth 失效
    使用氨基硫醇促进造血祖细胞生长的方法

    公开(公告)号:US5846958A

    公开(公告)日:1998-12-08

    申请号:US390713

    申请日:1995-02-17

    摘要: The present invention relates to methods of stimulating the growth of hematopoietic progenitor cells. In particular, it relates to the use of thiols and related compounds in stimulating the growth of hematopoietic progenitor cells in vitro and in vivo. Furthermore, the present invention relates to methods of using these compounds for the treatment of marrow failure states and immunodeficient conditions, including but not limited to myelodysplastic syndromes and acquired immunodeficiency syndrome.

    摘要翻译: 本发明涉及刺激造血祖细胞生长的方法。 特别地,它涉及硫醇和相关化合物在体外和体内刺激造血祖细胞生长中的应用。 此外,本发明涉及使用这些化合物治疗骨髓衰竭状态和免疫缺陷病症的方法,包括但不限于骨髓增生异常综合征和获得性免疫缺陷综合征。

    Compositions of N-(phosphonoacetyl)-L-aspartic acid and methods of their
use as broad spectrum antivirals
    5.
    发明授权
    Compositions of N-(phosphonoacetyl)-L-aspartic acid and methods of their use as broad spectrum antivirals 失效
    N-(膦酰基乙酰基)-L-天冬氨酸的组合物及其作为广谱抗病毒药物的方法

    公开(公告)号:US5491135A

    公开(公告)日:1996-02-13

    申请号:US32234

    申请日:1993-03-17

    申请人: Herbert A. Blough

    发明人: Herbert A. Blough

    摘要: Compositions and methods are disclosed which utilize the broad spectrum antiviral activity of PALA. This compound and its pharmaceutically acceptable analogs possess potent activity while displaying minimal toxicity and, therefore, are characterized by a relatively high therapeutic index. Compositions optionally containing other therapeutic agents, such as other antiviral agents, are also disclosed and are found to possess synergistic and/or additive antiviral activity.

    摘要翻译: 公开了利用PALA广谱抗病毒活性的组合物和方法。 该化合物及其药学上可接受的类似物具有有效的活性,同时显示出最小的毒性,因此其特征在于相对较高的治疗指数。 还公开了任选地含有其它治疗剂的组合物,例如其它抗病毒剂,并且被发现具有协同和/或添加的抗病毒活性。

    Thermally stable trimetrexates and processes for producing the same
    8.
    发明授权
    Thermally stable trimetrexates and processes for producing the same 失效
    热稳定性三甲氧戊酸及其制备方法

    公开(公告)号:US6017922A

    公开(公告)日:2000-01-25

    申请号:US80290

    申请日:1998-05-18

    CPC分类号: C07D239/95

    摘要: The present invention provides for thermally stable forms of 2,4-diamino-5-methyl-6-[(3,4,5-trimethoxyanilino)methyl] quinazoline, or trimetrexate. A crystalline 2,4-diamino-5-methyl-6-[(3,4,5-trimethoxyanilino)methyl] quinazoline monohydrate, or trimetrexate monohydrate, belonging to the space group P1(#2) and having a triclinic cell with dimensions of about a=7.699 .ANG., b=9.606 .ANG. and c=13.012 .ANG. is disclosed. A novel Schiff base compound, 2,4-diamino-5-methyl-6-[(3,4,5-trimethoxyphenylimino)-methinyl]quinazoline, is also disclosed. The present invention further provides novel methods of producing stable trimetrexate free base compounds, including crystalline trimetrexate monohydrate. The crystalline monohydrate form provides increased stability over the anhydrous form.

    摘要翻译: 本发明提供2,4-二氨基-5-甲基-6 - [(3,4,5-三甲氧基苯胺基)甲基]喹唑啉或三甲氧甲酸酯的热稳定形式。 属于空间群P + E,ov 1 + EE(#2)的结晶的2,4-二氨基-5-甲基-6 - [(3,4,5-三甲氧基苯胺基)甲基]喹唑啉一水合物或三甲氧甲酸一水合物, 并且具有尺寸为约a = 7.699 ANGSTROM,b = 9.606 ANGSTROM和c = 13.012 ANGSTROM的三斜晶胞。 还公开了一种新型席夫碱化合物,2,4-二氨基-5-甲基-6 - [(3,4,5-三甲氧基苯基亚氨基) - 甲基苯基]喹唑啉。 本发明还提供了生产稳定的三甲氧铵游离碱化合物,包括结晶三甲氧甲酸一水合物的新方法。 结晶一水合物形式比无水形式提供了更高的稳定性。

    Suppression of HIV expression by organic thiophosphate
    9.
    发明授权
    Suppression of HIV expression by organic thiophosphate 失效
    有机硫代磷酸盐抑制HIV表达

    公开(公告)号:US5824664A

    公开(公告)日:1998-10-20

    申请号:US37633

    申请日:1993-03-26

    CPC分类号: A61K31/66 A61K31/70

    摘要: Chronic HIV infection is treated by administering to a subject an organic thiophosphate alone or in combination with another anti-HIV or anti-AIDS drug. The organic thiophosphate is preferably WR 151327, a compound with antioxidant and free radical scavenging activities, or a functional derivative or analogue thereof. WR 151327 suppresses induction of HIV expression in chronically infected cells mediated by cytokines such as TNF.alpha. and GM-CSF. Pharmaceutical compositions comprising at least one organic thiophosphate in combination with one or more anti-HIV or anti-AIDS drugs are also disclosed.

    摘要翻译: 通过向受试者单独或与另一种抗艾滋病毒或抗艾滋病药物组合施用有机硫代磷酸盐来治疗慢性HIV感染。 有机硫代磷酸酯优选为WR 151327,具有抗氧化和自由基清除活性的化合物或其功能衍生物或类似物。 WR 151327抑制由细胞因子如TNFα和GM-CSF介导的慢性感染细胞中的HIV表达的诱导。 还公开了包含至少一种有机硫代磷酸酯与一种或多种抗艾滋病毒或抗艾滋病药物组合的药物组合物。