Use of substituted amidino compounds in the treatment of chronic obstructive pulmonary disease

    公开(公告)号:US06380259B2

    公开(公告)日:2002-04-30

    申请号:US09732453

    申请日:2000-12-07

    IPC分类号: A61K31165

    CPC分类号: A61K31/166

    摘要: Use in medicaments for the treatment of chronic obstructive pulmonary disease of compounds of formula wherein the C(═NH)—NHR3 group may be in tautomeric or isomeric form, or a pharmaceutically acceptable salt thereof, in which: R1 is amino which is mono- or disubstituted by a substituent selected from an aliphatic hydrocarbon radical, an araliphatic hydrocarbon radical, an aromatic radical, and a cycloaliphatic hydrocarbon radical or is amino which is disubstituted by a divalent aliphatic hydrocarbon radical or a said radical interrupted by oxygen; R2 is hydrogen, halogen, trifluoromethyl, an aliphatic hydrocarbon radical, hydroxy or is hydroxy which is etherified by an aliphatic, araliphatic or aromatic alcohol or by an aliphatic alcohol which is substituted by carboxy, by esterified carboxy or by amidated carboxy or which is esterified by an aliphatic or araliphatic carboxylic acid; R3 is hydrogen or an acyl radical which is derived from an organic carbonic acid, an organic carboxylic acid, a sulfonic acid, or a carbamic acid; X1 and X3, independently or one another, are oxygen (—O—) or sulphur (—S—); and X2 is a divalent aliphatic hydrocarbon radical which may be interrupted by an aromatic radical; wherein the phenyl rings of formula I may be, independently or one another, further substituted by one or more substituents selected from halogen, trifluoromethyl, an aliphatic hydrocarbon radical, hydroxy, and hydroxy which is etherified by an aliphatic alcohol or which is esterified by an aliphatic or araliphatic carboxylic acid; wherein aryl in the above definitions may be, independently of one another, further substituted by one or more substituents selected from halogen, trifluoromethyl, an aliphatic hydrocarbon radical, hydroxy, and hydroxy which is etherified by an aliphatic alcohol or which is esterified by an aliphatic or araliphatic carboxylic acid; wherein a cycloaliphatic hydrocarbon radical may be substituted by an aliphatic radical.

    Quantification of hydroperoxides using prostaglandin H synthase
    3.
    发明授权
    Quantification of hydroperoxides using prostaglandin H synthase 失效
    使用前列腺素H合酶定量氢过氧化物

    公开(公告)号:US4675281A

    公开(公告)日:1987-06-23

    申请号:US629174

    申请日:1984-07-09

    CPC分类号: C12Q1/26

    摘要: A method of assessing certain disease conditions of body tissues and body fluids by the measurement of hydroperoxides therein; includes using the enzyme prostaglandin H synthase and observing the rate of enzyme-catalyzed oxygenation reaction, preferably with equipment such as a polarographic oxygen electrode that monitors the oxygen concentration. The presence of increased amounts of hydroperoxide cause a faster attainment of the optimal rate of enzyme-catalyzed oxygen consumption. This enzymic assay provides high sensitivity and selectivity for hydroperoxides. Cyanide may also be introduced to temper the reaction velocity to facilitate monitoring the enzyme reaction.

    摘要翻译: 通过测量其中的氢过氧化物来评估身体组织和体液的某些疾病状况的方法; 包括使用酶前列腺素H合酶并观察酶催化氧合反应的速率,优选用诸如监测氧浓度的极谱氧电极的设备。 增加量的过氧化氢的存在导致更快地达到酶催化的氧消耗的最佳速率。 该酶测定法为氢过氧化物提供高灵敏度和选择性。 还可以引入氰化物来调节反应速度以便于监测酶的反应。