Novel anthranilic acid derivatives
    1.
    发明授权
    Novel anthranilic acid derivatives 失效
    新型邻氨基苯甲酸衍生物

    公开(公告)号:US4337270A

    公开(公告)日:1982-06-29

    申请号:US152217

    申请日:1980-05-21

    IPC分类号: A61K31/245 C07C101/72

    CPC分类号: C07C235/38 C07C235/56

    摘要: Novel anthranilic acid derivatives of the general formula: ##STR1## wherein X is a halogen atom, an alkoxyl group having 1-3 carbon atoms, an alkyl group having 1-3 carbon atoms or a nitro group, n is an integer of 1-2, Y is an alkoxyl group having 1-3 carbon atoms, m is an integer of 2-3, Z is --COCH.dbd.CH-- or --CO--, R.sub.1 is a hydrogen atom or an alkyl group having 1-4 carbon atoms, and pharmaceutically acceptable salts thereof, which derivatives and salts possess a strong antiallergic action and are thus useful as therapeutically active agents for diseases caused by allergies, such as asthma, hay fever, urticaria and atopic dermatitis; an antiallergic composition comprising the same; and a method of alleviating diseases caused by allergies using the same.

    摘要翻译: 新型的下式的邻氨基苯甲酸衍生物:其中X为卤素原子,具有1-3个碳原子的烷氧基,具有1-3个碳原子的烷基或硝基,n为1- 2,Y是具有1-3个碳原子的烷氧基,m是2-3的整数,Z是-COCH = CH-或-CO-,R1是氢原子或具有1-4个碳原子的烷基 和其药学上可接受的盐,其衍生物和盐具有强的抗过敏作用,因此可用作由过敏引起的疾病如哮喘,花粉症,荨麻疹和特应性皮炎的治疗活性剂; 包含其的抗过敏组合物; 以及减轻由使用其引起的过敏引起的疾病的方法。

    Pyrido(2,3-d) pyrimidinones
    2.
    发明授权
    Pyrido(2,3-d) pyrimidinones 失效
    吡啶(2,3-d)嘧啶酮

    公开(公告)号:US4009166A

    公开(公告)日:1977-02-22

    申请号:US582889

    申请日:1975-06-02

    IPC分类号: C07D471/04

    CPC分类号: C07D471/04 Y10S514/916

    摘要: The compounds of the present invention can be represented by the following formula: ##STR1## wherein R is selected from the group consisting of phenyl and substituted phenyl; R' is selected from the group consisting of hydrogen, lower alkyl, unsaturated lower alkyl, substituted lower alkyl, lower alkoxycarbonyl and aralkyl; Y and Z are selected from the group consisting of carbonyl and methylene, but Y and Z are always dissimilar.The compounds of the present invention possess a high degree of pharmacological activities such as anti-inflammatory, anti-ulcerative, analgetic, antipyretic, antihistaminic and central nervous system depressive activities, and certain of them are useful as new anti-inflammatory agents, analgesics and central nervous system depresssants.

    摘要翻译: 本发明的化合物可以由下式表示:其中R选自苯基和取代的苯基; R'选自氢,低级烷基,不饱和低级烷基,取代的低级烷基,低级烷氧基羰基和芳烷基; Y和Z选自羰基和亚甲基,但Y和Z总是不相似的。

    Novel process for preparing isoindoline derivatives
    3.
    发明授权
    Novel process for preparing isoindoline derivatives 失效
    异二氢吲哚衍生物的新方法

    公开(公告)号:US4400520A

    公开(公告)日:1983-08-23

    申请号:US299432

    申请日:1981-09-04

    IPC分类号: C07D209/46

    CPC分类号: C07D209/46

    摘要: A process for the preparation of an isoindoline derivative of the following general formula (II): ##STR1## wherein R.sup.2 is a hydrogen atom or lower alkyl group and X is a carboxyl group, carboalkoxy group, amide group or cyano group, which comprisescycling a benzylidene derivative of the following general formula (I) ##STR2## wherein R.sup.1 is a hydrogen atom or lower alkyl group, and R.sup.2 and X are as defined above, in the presence of a reducing agent such as sodium boron hydride. In one embodiment, the benzylidene derivative may be substituted by a reaction mixture containing the same, the reaction mixture being prepared by reacting o-phthalaldehydic acid or its ester with an aniline derivative.

    摘要翻译: 制备下列通式(II)的异二氢吲哚衍生物的方法:其中R2是氢原子或低级烷基,X是羧基,烷氧羰基,酰胺基或氰基, 其包括在还原剂例如钠的存在下,使下列通式(I)的亚苄基衍生物(其中R1是氢原子或低级烷基,R2和X如上所定义) 硼氢化物。 在一个实施方案中,亚苄基衍生物可以被含有该亚苄基衍生物的反应混合物取代,反应混合物通过邻邻邻苯二甲醛或其酯与苯胺衍生物反应来制备。