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    N.sup.6 -disubstituted purine derivatives, and pharmaceutical compositions containing them, useful for treating allergic diseases, bronchospastic and bronchoconstrictory conditions
    24.
    发明授权
    N.sup.6 -disubstituted purine derivatives, and pharmaceutical compositions containing them, useful for treating allergic diseases, bronchospastic and bronchoconstrictory conditions 失效
    N6-二取代嘌呤衍生物和含有它们的药物组合物，其可用于治疗过敏性疾病，支气管痉挛和支气管收缩条件

    公开(公告)号：US4853386A

    公开(公告)日：1989-08-01

    申请号：US897109

    申请日：1986-08-15

    申请人： Walter-Gunar Friebe ,  Otto-Henning Wilhelms

    发明人： Walter-Gunar Friebe ,  Otto-Henning Wilhelms

    IPC分类号： A61K31/52 ,  A61P11/08 ,  A61P37/08 ,  C07D473/00 ,  C07D473/16 ,  C07D473/34 ,  C07D473/40

    CPC分类号： C07D473/00 ,  C07D473/16 ,  C07D473/34

    摘要： The present invention provides N.sup.6 -disubstituted purine derivatives of the general formula: ##STR1## wherein R.sub.1 and R.sub.4 are the same or different and each represents a hydrogen or halogen atom or an --NR.sub.6 R.sub.7 group, R.sub.2 and R.sub.3 are the same or different and each represents a C.sub.1 -C.sub.6 alkyl radical, a C.sub.2 -C.sub.6 alkenyl radical, a C.sub.3 -C.sub.7 cycloalkyl radical, a phenalkyl radical containing up to 4 carbon atoms in the alkyl moiety, which can be straight-chained or branched, the phenyl moiety of which can be substituted one or more times by halogen, hydroxyl, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylthio or trifluoromethyl; a furylmethyl or furylethyl radical, a thiophenemethyl or thiopheneethyl radical, a pyridylmethyl or pyridylethyl radical optionally substituted by a C.sub.1 -C.sub.4 alkyl radical, an indanyl radical or a tetrahydronaphthyl radical, R.sub.5 is a hydrogen atom, a tetrahydrofuranyl or tetrahydropyranyl radical or a C.sub.1 -C.sub.10 radical which is optionally substituted one or more times by hydroxyl, C.sub.1 -C.sub.6 alkanoyloxy, C.sub.1 -C.sub.6 alkoxycarbonyl, C.sub.2 -C.sub.6 carboxyalkanoyloxy, C.sub.2 -C.sub.6 hydroxyalkoxy, C.sub.3 -c.sub.6 dihydroxyalkoxy, carboxyl, cyano or 1H-tetrazol-5-yl radical, R.sub.6 and R.sub.7 are the same or different and each represents a hydrogen atom or a C.sub.1 -C.sub.6 alkyl radical or together represent a C.sub.2 -C.sub.5 alkylene radical optionally interrupted by oxygen, sulphur or an NR.sub.8 group and R.sub.8 is a hydrogen atom or a C.sub.1 -C.sub.6 alkyl radical; as well as the pharmacologically acceptable salts thereof.

    摘要翻译： 本发明提供以下通式的N6-二取代的嘌呤衍生物：其中R 1和R 4相同或不同，并且各自表示氢或卤素原子或-NR 6 R 7基团，R 2和R 3相同或不同， 各自表示C1-C6烷基，C2-C6链烯基，C3-C7环烷基，在烷基部分含有至多4个碳原子的苯烷基，其可以是直链或支链的，苯基 其部分可以被卤素，羟基，C 1 -C 6烷基，C 1 -C 6烷氧基，C 1 -C 6烷硫基或三氟甲基取代一次或多次; 呋喃基甲基或呋喃乙基，噻吩甲基或噻吩乙基，任选被C 1 -C 4烷基，茚满基或四氢萘基取代的吡啶基甲基或吡啶基，R5是氢原子，四氢呋喃基或四氢吡喃基或C1- C 1 -C 6烷氧基，C 1 -C 6烷氧基羰基，C 2 -C 6羧基烷酰氧基，C 2 -C 6羟基烷氧基，C 3 -C 6二羟基烷氧基，羧基，氰基或1H-四唑-5-基 ，R6和R7相同或不同，各自表示氢原子或C1-C6烷基，或一起代表任选被氧，硫或NR8基中断的C2-C5亚烷基，R8是氢原子或C1 -C6烷基; 以及其药理学上可接受的盐。

    Dibenz�b,e!oxepin derivatives and pharmaceutical agents which contain them
    28.
    发明授权
    Dibenz�b,e!oxepin derivatives and pharmaceutical agents which contain them 失效
    二苯并[b，e] oxepin衍生物和含有它们的药剂

    公开(公告)号：US5696155A

    公开(公告)日：1997-12-09

    申请号：US632473

    申请日：1996-09-10

    申请人： Walter-Gunar Friebe ,  Werner Scheuer ,  Ulrich Tibes

    发明人： Walter-Gunar Friebe ,  Werner Scheuer ,  Ulrich Tibes

    IPC分类号： A61K31/335 ,  C07D313/12 ,  C07D493/04

    CPC分类号： C07D493/04 ,  C07D313/12

    摘要： Compounds of formula I ##STR1## in which Q denotes hydrogen, a hydroxy group or a C.sub.1 to C.sub.8 alkoxy group which can be substituted if desired, by carboxyl or C.sub.1 to C.sub.6 alkoxycarbonyl and either Y and Z together form a group ##STR2## and X represents hydrogen, C.sub.1 to C.sub.6 alkyl or C.sub.2 to C.sub.6 alkenyl or Y and X together form a group ##STR3## or an alkylene residue of 2-4 carbon atoms and Z represents hydrogen, C.sub.1 to C.sub.6 alkyl or C.sub.1 to C.sub.6 alkanoyl, where R denotes hydrogen or a C.sub.1 to C.sub.6 alkyl residue as well as physiologically tolerated salts thereof, processes for their production and pharmaceutical agents containing these compounds for the treatment of inflammatory diseases and allergic diseases.

    摘要翻译： PCT No.PCT / EP94 / 03479 371日期：1996年9月10日 102（e）1996年9月10日PCT PCT日期：1994年10月22日PCT公布。 公开号WO95 / 11906 日期：1995年5月4日，式I的化合物（I）其中Q表示氢，羟基或可根据需要被取代的C 1至C 8烷氧基，由羧基或C 1至C 6烷氧基羰基以及Y和Z一起 形成基团，X表示氢，C 1至C 6烷基或C 2至C 6烯基或Y和X一起形成基团Z表示氢，C 1至C 6烷基或C 1至C 6烷酰基，其中R表示氢或 C1至C6烷基残基以及其生理上耐受的盐，其制备方法和含有这些化合物用于治疗炎症性疾病和过敏性疾病的药剂。

    Pyrrolobenzimidazoles and pharmaceutical compositions containing them
    29.
    发明授权
    Pyrrolobenzimidazoles and pharmaceutical compositions containing them 失效
    吡咯并苯并咪唑和含有它们的药物组合物

    公开(公告)号：US4863945A

    公开(公告)日：1989-09-05

    申请号：US131367

    申请日：1987-12-10

    申请人： Walter-Gunar Friebe ,  Alfred Mertens ,  Klaus Strein ,  Erwin Boehm

    发明人： Walter-Gunar Friebe ,  Alfred Mertens ,  Klaus Strein ,  Erwin Boehm

    IPC分类号： A61K31/40 ,  A61P7/02 ,  A61P9/04 ,  A61P9/12 ,  C07D487/04

    CPC分类号： C07D487/04

    摘要： Pyrrolobenzimidazoles of the formula: ##STR1## are useful for treatment of heart and circulatory diseases. R.sub.1 is substituted phenyl; or optionally substituted naphthyl or a five- or six-membered heterocyclic group which can be condensed with a phenyl ring to form a bicyclic radical. R.sub.2 is hydrogen, alkyl, alkenyl or cycloalkenyl; R.sub.3 is alkyl, alkenyl or hydroxyalkyl or with R.sub.2 together forms cycloakylene; or R.sub.2 and R.sub.3 together form alkylidene or cycloalkylidene. R.sub.4 is hydrogen or lower alkanoyl. X is a valency bond, alkylene, vinylene, imino or carbonylamino. T stands for two hydrogen atoms. When X is a valency bond, R.sub.1 can also be hydrogen, hydrocarbyl which may also contain oxygen, amino, sulfur, carbonyl and sulfonyl groups. When X is imino or carbonylamino or when R.sub.1 is a bicyclic radical, T can also be oxygen. The compounds also include the tautomers and physiologically acceptable salts with inorganic and organic acids.

    摘要翻译： 下式的吡咯并苯并咪唑：可用于治疗心脏和循环系统疾病。 R1是取代的苯基; 或任选取代的萘基或可与苯环缩合形成双环基团的五元或六元杂环基。 R2是氢，烷基，烯基或环烯基; R3是烷基，烯基或羟基烷基或与R2一起形成亚环烷基; 或者R 2和R 3一起形成亚烷基或亚环烷基。 R4是氢或低级烷酰基。 X是价键，亚烷基，亚乙烯基，亚氨基或羰基氨基。 T代表两个氢原子。 当X是价键时，R 1也可以是氢，也可以含有氧，氨基，硫，羰基和磺酰基的烃基。 当X是亚氨基或羰基氨基时，或当R1是双环基时，T也可以是氧。 化合物还包括与无机和有机酸形成的互变异构体和生理上可接受的盐。