Allosteric hemoglobin modifiers useful for decreasing oxygen affinity
and preserving oxygen carrying capability of stored blood
    5.
    发明授权
    Allosteric hemoglobin modifiers useful for decreasing oxygen affinity and preserving oxygen carrying capability of stored blood 失效
    变性血红蛋白改性剂可用于降低氧气亲和力并保持储存血液的携氧能力

    公开(公告)号:US5122539A

    公开(公告)日:1992-06-16

    申请号:US702947

    申请日:1991-05-20

    Abstract: Compounds of the general structural formula: ##STR1## wherein X, Y and Z may each be CH.sub.2, NH, or O, R.sub.2-6 are either hydrogen, halogen, or a substituted or unsubstituted C.sub.1, C.sub.2, or C.sub.3 alkyl group and these moieties maybe the same or different, or alkyl moieties of aliphatic or aromatic rings incorporating two of the R.sub.2-6 sites, R.sub.7-8 are hydrogen, methyl, or ethyl groups and these moieties may be the same or different, or alkyl moieties as part of an aliphatic ring connecting R.sub.7 and R.sub.8, and R.sub.9 is a hydrogen, loweralkyl such as methyl, ethyl or propyl, or a salt cation such as sodium, potassium, or ammonium are useful for right-shifting hemoglobin towards a low oxygen affinity state. The compounds are capable of acting on hemoglobin in whole blood. In addition, the compounds can maintain the oxygen affinity in blood during storage and can restore the oxygen affinity of outdated blood.

    Abstract translation: 通式结构式的化合物:其中X,Y和Z各自为CH 2,NH或O,R 2-6为氢,卤素或取代或未取代的C 1,C 2或C 3烷基, 部分可以相同或不同,或者包含两个R2-6位点的脂族或芳环的烷基部分,R7-8是氢,甲基或乙基,这些部分可以相同或不同,或者作为部分的烷基部分 连接R7和R8的脂族环,R9是氢,低级烷基如甲基,乙基或丙基,或盐阳离子如钠,钾或铵可用于将血红蛋白右移至低氧亲和力状态。 该化合物能够作用于全血中的血红蛋白。 此外,化合物可以在储存期间保持血液中的氧亲和力,并且可以恢复过时血液的氧亲和力。

    Aldehydic agents for allosteric modification of hemoglobin
    7.
    发明授权
    Aldehydic agents for allosteric modification of hemoglobin 失效
    用于血红蛋白变构修饰的醛类药物

    公开(公告)号:US5599974A

    公开(公告)日:1997-02-04

    申请号:US308805

    申请日:1994-09-19

    Abstract: Chemical compounds which interact inside the central water cavity of hemoglobin and bridge between the two .alpha. subunits can be used to allosterically modify hemoglobin towards tense and relaxed states. The functional groups employed are aldehydes and carboxylic acids, wherein the aldehydes form covalent bonds (schiff base) with amino acid residues of hemoglobin and the carboxylic acids form ionic bonds with amino acid residues of hemoglobin. Particularly useful compounds within the practice of this invention bond to the n-terminal valine of one .alpha. subunit of hemoglobin, and the lysine 99 and/or arginine 141 of the other .alpha. subunit.

    Abstract translation: 在血红蛋白的中心水腔和两个α亚基之间的桥梁之间相互作用的化学化合物可用于将血红蛋白改变为变态和松弛状态。 所使用的官能团是醛和羧酸,其中醛与血红蛋白的氨基酸残基形成共价键(席夫碱),羧酸与血红蛋白的氨基酸残基形成离子键。 在本发明实践中特别有用的化合物与血红蛋白的一个α亚基的n末端缬氨酸结合,另一个α亚基的赖氨酸99和/或精氨酸141结合。

    Tritium labelled N-mustard type compounds and a process for their
production
    9.
    发明授权
    Tritium labelled N-mustard type compounds and a process for their production 失效
    氚标记的N-芥菜型化合物及其生产方法

    公开(公告)号:US4795627A

    公开(公告)日:1989-01-03

    申请号:US662276

    申请日:1984-10-18

    CPC classification number: A61K51/0442 A61K51/0446 A61K51/0453

    Abstract: The present invention describes novel tritium labelled nitrogen mustard type compounds, and their aziridinium type analog, and a process for the production of same. The compounds are of value in medical research and development and also as active ingredients of pharmaceutical compositions. The compounds can be used to develop analogs of human disease states and can also be used to evaluate the mechanism of neurotransmitter regulation and function, both in vitro and in vivo.

    Abstract translation: 本发明描述了新型氚标记的氮芥类化合物及其吖啶鎓型类似物及其制备方法。 这些化合物在医学研究和开发中是有价值的,也是药物组合物的有效成分。 这些化合物可用于开发人类疾病状态的类似物,也可用于评估体外和体内神经递质调节和功能的机制。

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