Thioxopyrazolo[1,5-c]quinazoline derivatives, anti-allergic compositions
and methods for treating allergic conditions by parenteral
administration, aerosol or insufflation
    3.
    发明授权
    Thioxopyrazolo[1,5-c]quinazoline derivatives, anti-allergic compositions and methods for treating allergic conditions by parenteral administration, aerosol or insufflation 失效
    噻唑并[1,5-c]喹唑啉衍生物,抗过敏组合物和通过胃肠外给药,气雾剂或吹入剂治疗过敏症状的方法

    公开(公告)号:US4282226A

    公开(公告)日:1981-08-04

    申请号:US148433

    申请日:1980-05-09

    IPC分类号: C07D487/04 A61K31/505

    CPC分类号: C07D487/04

    摘要: Compounds are provided having the structure ##STR1## wherein R.sup.1 is hydrogen or lower alkyl of 1-3 carbons, R.sup.2 is carboxyl, hydroxymethyl, lower alkanoyloxymethyl, or lower alkoxycarbonyl, R.sup.3 is hydrogen, lower alkyl or benzyl, and R.sup.4 and R.sup.5 are the same or different and represent hydrogen, lower alkyl, lower alkoxy, alkanoyloxy, benzyloxy, hydroxy, halogen (Cl, Br and F), nitro, and trifluoromethyl. These compounds are useful as anti-allergics when administered parenterally or by insufflation but have poor activity when administered orally.

    摘要翻译: 提供具有以下结构的化合物,其中R 1是氢或1-3个碳的低级烷基,R 2是羧基,羟甲基,低级烷酰氧基甲基或低级烷氧基羰基,R 3是氢,低级烷基或苄基,R 4和R 5是 代表氢,低级烷基,低级烷氧基,烷酰氧基,苄氧基,羟基,卤素(Cl,Br和F),硝基和三氟甲基。 这些化合物在肠胃外或吹入时可用作抗过敏剂,但口服时具有差的活性。

    Pyrazolo[1,5-c]quinazoline derivatives and related compounds
    7.
    发明授权
    Pyrazolo[1,5-c]quinazoline derivatives and related compounds 失效
    吡唑并[8,1,5-c {9]喹唑啉衍生物及相关化合物

    公开(公告)号:US4164578A

    公开(公告)日:1979-08-14

    申请号:US925738

    申请日:1978-07-19

    申请人: B. Richard Vogt

    发明人: B. Richard Vogt

    摘要: Compounds are provided having the structure ##STR1## wherein R.sup.1 is hydrogen, alkyl of 1-3 carbons, phenyl optionally substituted by R.sup.4 ; R.sup.2 is cyano; ##STR2## (wherein Z is a single bond or ##STR3## (wherein R.sup.9. is hydrogen or alkyl, Q is CH or N); ##STR4## wherein R.sup.6 is amino, alkylamino, dialkylamino, haloalkyl or ##STR5## and R.sup.4 and R.sup.5 are the same or different and represent hydrogen, lower alkyl, lower alkoxy, alkanoyloxy, benzyloxy, substituted benzyloxy, hydroxy, halogen (Cl, Br and F), nitro and trifluoromethyl; and R.sup.7, R.sup.8, m and n are as defined hereinafter. These compounds are useful as anti-allergy agents.

    摘要翻译: 提供了具有其中R 1是氢,1-3个碳的烷基,任选被R 4取代的苯基的结构的化合物; R2是氰基; (其中Z是单键或 (其中R9是氢或烷基,Q是CH或N);其中R6是氨基,烷基氨基,二烷基氨基,卤代烷基或 和R 4和R 5相同或不同,表示氢,低级烷基,低级烷氧基,烷酰氧基,苄氧基,取代的苄氧基,羟基,卤素(Cl,Br和F),硝基和三氟甲基; R7,R8,m和n分别为 这些化合物可用作抗过敏剂。

    4H-s-triazolo[4,3-a][1,5]benzodiazepin-5-ones
    8.
    发明授权
    4H-s-triazolo[4,3-a][1,5]benzodiazepin-5-ones 失效
    4H-s-三唑并{8,43-a {9 {8,5 {9 benzodiazepin-5-ones

    公开(公告)号:US4164498A

    公开(公告)日:1979-08-14

    申请号:US944531

    申请日:1978-09-21

    申请人: B. Richard Vogt

    发明人: B. Richard Vogt

    IPC分类号: C07D243/12 C07D487/14

    CPC分类号: C07D243/12 Y10S514/906

    摘要: Compounds of the following formula ##STR1## are useful as central nervous system depressants, tranquilizers, sedatives, growth promotors, anti-convulsants and muscle relaxants in mammalian species.

    摘要翻译: 以下式的化合物可用作哺乳动物物种中的中枢神经系统抑制剂,镇静剂,镇静剂,生长促进剂,抗惊厥药和肌肉松弛剂。

    Pyrazolo[1,5-c]quinazoline derivatives and related compounds
    9.
    发明授权
    Pyrazolo[1,5-c]quinazoline derivatives and related compounds 失效
    吡唑并[8,1,5-c {9]喹唑啉衍生物及相关化合物

    公开(公告)号:US4112098A

    公开(公告)日:1978-09-05

    申请号:US842718

    申请日:1977-10-17

    申请人: B. Richard Vogt

    发明人: B. Richard Vogt

    摘要: Compounds are provided having the structure ##STR1## wherein R.sup.1 is hydrogen, alkyl of 1 to 3 carbons, 1-(hydroxyimino)alkyl, alkanoylamino, amino, or ##STR2## wherein alkyl in the above groups contains 1 to 4 carbons; R.sup.2 is 1-(hydroxyimino)alkyl, alkanoylamino, amino, ##STR3## hydrogen, lower alkyl or phenyl (optionally substituted by R.sup.4) wherein alkyl in the above groups contains 1 to 4 carbons; R.sup.3 is hydrogen, lower alkyl, benzyl or phenyl (optionally substituted with R.sup.4), dialkylaminoalkyl, hydroxyalkyl, ##STR4## (wherein R.sup.6 is hydrogen or alkyl, and R.sup.7 is alkyl); with the proviso that R.sup.1 or R.sup.2 is 1-(hydroxyimino)alkyl, alkanoylamino or amino, when R.sup.3 is hydrogen, lower alkyl, benzyl or phenyl; and R.sup.4 and R.sup.5 are the same or different and represent hydrogen, lower alkyl, lower alkoxy, alkanoyloxy, benzyloxy, hydroxy, halogen (Cl, Br and F), nitro and trifluoromethyl. The above compounds are useful as anti-allergy agents and antiinflammatory agents.

    摘要翻译: 提供具有其中R 1是氢,1至3个碳的烷基,1-(羟基亚氨基)烷基,烷酰基氨基,氨基或者其中上述基团中的烷基含有1至4个碳原子的结构的化合物; R 2是1-(羟基亚氨基)烷基,烷酰基氨基,氨基,氢,低级烷基或苯基(任选被R 4取代),其中上述基团中的烷基含有1至4个碳; R3是氢,低级烷基,苄基或苯基(任选被R4取代),二烷基氨基烷基,羟烷基,(其中R6是氢或烷基,R7是烷基)。 条件是当R 3为氢时,R 1或R 2为1-(羟基亚氨基)烷基,烷酰基氨基或氨基,低级烷基,苄基或苯基; 和R 4和R 5相同或不同,代表氢,低级烷基,低级烷氧基,烷酰氧基,苄氧基,羟基,卤素(Cl,Br和F),硝基和三氟甲基。 上述化合物可用作抗过敏剂和抗炎剂。