Lipoxygenase inhibiting 1-arylalkyl-, 1-arylthio-, and
1-aryloxypyrazole-4,5-diones
    86.
    发明授权
    Lipoxygenase inhibiting 1-arylalkyl-, 1-arylthio-, and 1-aryloxypyrazole-4,5-diones 失效
    抑制脂氧合酶的1-芳基烷基 - ,1-芳硫基 - 和1-芳氧基吡唑-4,5-二酮

    公开(公告)号:US4659732A

    公开(公告)日:1987-04-21

    申请号:US769928

    申请日:1985-08-27

    CPC分类号: C07D231/28

    摘要: Combating diseases of the respiratory tract, inflammations, rheumatism, thromboembolic diseases, ischaemias and infarcts, cardiac arrhythmias and arteriosclerosis with pyrazolediones of the formula ##STR1## wherein R represents an aryl or heteroaryl radical which has 6 to 12 C atoms and optionally contains 1 to 3 identical or different substituents from the group comprising halogen, trifluoromethyl, alkyl, alkenyl, alkoxy, alkylamino, cyano, trifluoromethoxy, nitro, hydroxyl, SO.sub.n -alkyl (n=0 to 2) or SO.sub.n -trifluoromethyl ) n=0 to 2), alkyl, alkenyl and alkoxy each having up to 4 C atoms,R.sup.1 represents hydrogen or a hydrocarbon radical which has 1 to 18 C atoms and optionally contains a hydroxyl, ether, ester or carboxyl group and optionally contains 1 to 3 halogen atoms, and X represents one of the groups --CH.sub.2 --CH.sub.2 --CH.sub.2 --, --O--CH.sub.2 --CH.sub.2 --, --S--CH.sub.2 --CH.sub.2 --, --CH.sub.2 --CH.sub.2 --, --CH.sub.2 -- or ##STR2## the oxygen or sulphur atom being bonded to the radical R.

    摘要翻译: 通过具有下式(IMAGE)的吡唑啉酮来治疗呼吸道疾病,炎症,风湿病,血栓栓塞性疾病,缺血性和梗塞,心律失常和动脉硬化,其中R表示具有6至12个C原子的芳基或杂芳基,并且任选地包含1至 3个与卤素,三氟甲基,烷基,烯基,烷氧基,烷基氨基,氰基,三氟甲氧基,硝基,羟基,SO1-烷基(n = 0〜2)或SO-三氟甲基)相同或不同的取代基,n = 0〜2) 烷基,链烯基和烷氧基各自具有至多4个C原子,R 1表示氢或具有1至18个C原子并且任选地含有羟基,醚,酯或羧基并且任选地含有1至3个卤素原子的烃基, X代表键合的氧或硫原子之一-CH2-CH2-CH2-,-O-CH2-CH2-,-S-CH2-CH2-,-CH2-CH2-,-CH2-或< 到激进的

    Thrombin inhibitory new dihydroxybenzene ether derivatives
    88.
    发明授权
    Thrombin inhibitory new dihydroxybenzene ether derivatives 失效
    凝血酶抑制新二羟基苯醚衍生物

    公开(公告)号:US4590291A

    公开(公告)日:1986-05-20

    申请号:US385355

    申请日:1982-06-07

    摘要: An ether derivative of a dihydroxybenzene of the formula ##STR1## in which R.sup.1 is 1 to 3 identical or different substituents selected from hydrogen, halogen, trifluoromethyl, carboxyl, alkyl, alkoxy, alkylmercapto and carbalkoxy, with in each case 1 to 4 carbon atoms in the alkyl and alkoxy groups, andR.sup.2 and R.sup.3 are different and each is an alkyl or alkenyl chain in which 1 or 2 CH.sub.2 chain members are optionally replaced by O, S, CO or a phenylene group, and/or in which the chain is optionally substituted by 1 to 3 identical or different substituents selected from hydroxyl, halogen, trifluoromethyl, phenyl, carboxyl, alkyl, alkoxy, alkylmercapto, carbalkoxy, and acyl, the phenyl radical in turn optionally being substituted by halogen, trifluoromethyl, carboxyl, alkyl, alkoxy, alkylmercapto or carbaloxy, and the abovementioned alkyl, alkoxy and acyl groups in each case containing 1 to 4 carbon atoms, and in which at least one of the radicals R.sup.2 or R.sup.3 is substituted and/or in at least one of the radicals R.sup.2 or R.sup.3 1 or 2 chain members are replaced by 1 or 2 identical or different radicals selected from O, S, CO and phenylene, is effective in combating cardiac infarcations, angina pectoric, thromboembolic illnesses, in venous and arterial regions and arteriosclerosis.

    摘要翻译: 其中R 1是1至3个相同或不同的选自氢,卤素,三氟甲基,羧基,烷基,烷氧基,烷基巯基和烷氧基的取代基的式“IMAGE”的二羟基苯的醚衍生物,在每种情况下为1至4个碳原子 在烷基和烷氧基中,且R 2和R 3不同,并且各自为烷基或烯基链,其中1或2个CH 2链成员任选被O,S,CO或亚苯基取代,和/或其中链 任选地被1至3个相同或不同的选自羟基,卤素,三氟甲基,苯基,羧基,烷基,烷氧基,烷基巯基,烷氧基和酰基的取代基取代,苯基依次任选被卤素,三氟甲基,羧基,烷基 ,烷氧基,烷基巯基或卡巴氧基,以及上述烷基,烷氧基和酰基,每种情况下含有1至4个碳原子,并且其中至少一个基团R 2或R 3被取代和/或至少一个o 基团R 2或R 3 1或2链成员被选自O,S,CO和亚苯基的1或2个相同或不同的基团取代,有效地对抗静脉和动脉区域的心脏梗塞,心绞痛,血栓栓塞性疾病,以及 动脉硬化。