Olinecarboxylic acid derivatives
    2.
    发明授权
    Olinecarboxylic acid derivatives 失效
    奥林酸衍生物

    公开(公告)号:US4659734A

    公开(公告)日:1987-04-21

    申请号:US523329

    申请日:1983-08-15

    CPC分类号: C07D513/04

    摘要: A compound of the formula ##STR1## R.sub.1 is hydrogen, alkali metal, alkaline earth metal, lower alkyl, pivaloyloxymethyl or phthalidyl;R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are the same or different and are hydrogen, halogen, lower alkoxy or ##STR2## wherein R.sub.6 and R.sub.7 are lower alkyl or R.sub.6 and R.sub.7 together with the nitrogen atom to which they are attached form a five- to seven-membered unsubstituted or substituted heterocyclic ring containing said nitrogen atom as the sole hetero atom or containing nitrogen, sulfur or oxygen as additional hetereo atoms;A is a saturated or unsaturated hydrocarbon chain of one to five carbon atoms, unsubstituted or substituted by lower alkyl; lower alkoxy; lower alkylthio; hydroxy; halogen; lower alkyl substituted by halogen, amino, loweralkoxycarbonyl, carboxy, lower-alkoxy, loweralkylthio, loweracyloxy or hydroxy; loweralkylamino; carboxy; nitro; cyano; carbonyl; imino; or by substituted or unsubstituted phenyl, phenylthio, phenylamino or phenoxy; andR.sub.2 and R.sub.3 or R.sub.3 and R.sub.4 or R.sub.4 and R.sub.5 together may be alkylenedioxy of 1 to 5 carbon atoms which form a ring with the carbon atoms to which they are attached; or a pharmaceutically acceptable salt thereof.

    摘要翻译: 式(1)的化合物R1是氢,碱金属,碱土金属,低级烷基,新戊酰氧基甲基或苯酞; R 2,R 3,R 4和R 5相同或不同,为氢,卤素,低级烷氧基或者其中R 6和R 7为低级烷基或R 6和R 7与它们所连接的氮原子一起形成5- 含有所述氮原子作为唯一杂原子或含有氮,硫或氧作为额外的反应原子的七元未取代或取代的杂环; A是1至5个碳原子的饱和或不饱和烃链,未被取代或被低级烷基取代; 低级烷氧基 低级烷硫基; 羟基; 卤素; 被卤素,氨基,低级烷氧基羰基,羧基,低级烷氧基,低级烷硫基,低级酰氧基或羟基取代的低级烷基; 低级烷基氨基; 羧基; 硝基 氰基; 羰; 亚氨基 或被取代或未取代的苯基,苯硫基,苯基氨基或苯氧基取代; 并且R 2和R 3或R 3和R 4或R 4和R 5一起可以是与其所连接的碳原子形成环的1至5个碳原子的亚烷基二氧基; 或其药学上可接受的盐。

    Benzoguanamine derivatives, their production and pharmaceutical
compositions containing the same
    9.
    发明授权
    Benzoguanamine derivatives, their production and pharmaceutical compositions containing the same 失效
    苯胍胺衍生物,其生产和含有相同的药物组合物

    公开(公告)号:US4333933A

    公开(公告)日:1982-06-08

    申请号:US266483

    申请日:1981-05-22

    CPC分类号: C07D251/16 C07D251/18

    摘要: Novel 2-amino-4-nicotinoylamino-6-halogenophenyl-s-triazines and acid addition salts thereof, possessing strong anti-inflammatory action when the phenyl group is mono- or di-halogen substituted. The compounds are formulated into pharmaceutical compositions in bulk or dosage form, and are administered to humans and animals having inflammatory conditions or disorders until the same are reduced or overcome. The novel compounds are prepared by various procedures such as reacting a benzoguanamine which is halogen-substituted with an active derivative of nicotinic acid, and recovering the 2-amino-4-nicotinoylamino-6-halogenophenyl-s-triazines thus formed.

    摘要翻译: 新的2-氨基-4-烟酰氨基-6-卤代苯基-s-三嗪及其酸加成盐,当苯基是单 - 或二 - 卤素取代时具有强的抗炎作用。 化合物以体积或剂型形式配制成药物组合物,并且给予具有炎性病症或障碍的人和动物,直到减少或克服。 通过各种方法制备新化合物,例如使被卤素取代的苯并胍胺与烟酸的活性衍生物反应,并回收由此形成的2-氨基-4-烟酰氨基-6-卤代苯基-s-三嗪。