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    Dibenz [b,e] oxepin derivatives
    5.
    发明授权
    Dibenz [b,e] oxepin derivatives 失效
    二苯并[b，e]氧杂七环衍生物

    公开(公告)号：US4465835A

    公开(公告)日：1984-08-14

    申请号：US486425

    申请日：1983-04-19

    申请人： Hiroshi Takizawa ,  Osamu Morita ,  Yoshimasa Oiji ,  Tamotsu Hashimoto

    发明人： Hiroshi Takizawa ,  Osamu Morita ,  Yoshimasa Oiji ,  Tamotsu Hashimoto

    IPC分类号： C07D313/12 ,  C07D453/02 ,  C07D491/10 ,  C07D405/04

    CPC分类号： C07D491/10 ,  C07D313/12 ,  C07D453/02

    摘要： Novel dibenz [b,e] oxepin derivatives represented by the general formula: ##STR1## wherein R.sub.11 represents an alkyl group containing 1 to 5 carbon atoms, an alkoxy group containing 1 to 5 carbon atoms, a halogen atom, a cyclohexyl group or a phenyl group; and R.sub.21 represents ##STR2## wherein X represents a hydrogen atom, a hydroxy group, an amino group or a substituted aralkyl group containing 7 to 20 carbon atoms, and n represents 0 or an integer of 1 to 3 ##STR3## wherein Y represents an alkylamino group containing 1 to 5 carbon atoms, an aralkyl group containing 7 to 20 carbon atoms, a substituted aralkyl group, an aralkyloxy group containing 7 to 20 carbon atoms, an aralkylamino group containing 7 to 20 carbon atoms, a heterocyclic ring or a substituted heterocyclic ring, and n has the same meaning as defined before; provided that when R.sub.11 represents an alkyl group, an alkoxy group or a halogen atom, X does not represent a hydrogen atom; and the pharmaceutically acceptable acid addition salts thereof.Also disclosed are pharmaceutical compositions comprising a pharmaceutical carrier and, as an active ingredient, an effective amount of dibenz [b,e] oxepin derivative represented by the following general formula: ##STR4## wherein R.sub.1 represents an alkyl group containing 1 to 5 carbon atoms, an alkoxy group containing 1 to 5 carbon atoms, a halogen atom, a cyclohexyl group or a phenyl group; and R.sub.2 represents ##STR5## wherein X represents a hydrogen atom, a hydroxy group, an amino group or a substituted aralkyl group containing 7 to 20 carbon atoms, and n has the same meaning as defined before ##STR6## wherein Y and n have the same meaning as defined above; and the pharmaceutically acceptable acid addition salts thereof. Compound I, represented by the general formula (I), has antichlolinergic, antihistaminergic, antiasthmatic and antiplatelet aggregation activities, and is therefore useful as a sposmolysant, an antihistaminic, an antiasthmatic agent and as a medicament for cardiovascular or cerebrovascular diseases, respectively.This is a division of application Ser. No. 256,037, filed Apr. 21, 1981, now U.S. Pat. No. 4,396,550.

    Dibenz [b,e] oxepin derivatives
    6.
    发明授权
    Dibenz [b,e] oxepin derivatives 失效

    公开(公告)号：US4396550A

    公开(公告)日：1983-08-02

    申请号：US256037

    申请日：1981-04-21

    申请人： Hiroshi Takizawa ,  Osamu Morita ,  Yoshimasa Oiji ,  Tamotsu Hashimoto

    发明人： Hiroshi Takizawa ,  Osamu Morita ,  Yoshimasa Oiji ,  Tamotsu Hashimoto

    IPC分类号： C07D313/12 ,  C07D453/02 ,  C07D491/10 ,  C07D301/00 ,  A61K31/36 ,  C07D303/00 ,  C07D305/00

    CPC分类号： C07D491/10 ,  C07D313/12 ,  C07D453/02

    摘要： Novel dibenz [b,e] oxepin derivatives represented by the general formula: ##STR1## wherein R.sub.11 represents an alkyl group containing 1 to 5 carbon atoms, an alkoxy group containing 1 to 5 carbon atoms, a halogen atom, a cyclohexyl group or a phenyl group; and R.sub.21 represents ##STR2## wherein X represents a hydrogen atom, a hydroxy group, an amino group or a substituted aralkyl group containing 7 to 20 carbon atoms, and n represents 0 or an integer of 1 to 3 ##STR3## or (3) --NH--(CH.sub.2).sub.n --Y, wherein Y represents an alkylamino group containing 1 to 5 carbon atoms, an aralkyl group containing 7 to 20 carbon atoms, a substituted aralkyl group, an aralkyloxy group containing 7 to 20 carbon atoms, an aralkylamino group containing 7 to 20 carbon atoms, a heterocyclic ring or a substituted heterocyclic ring, and n has the same meaning as defined before; provided that when R.sub.11 represents an alkyl group, an alkoxy group or a halogen atom, X does not represent a hydrogen atom; and the pharmaceutically acceptable acid addition salts thereof.Also disclosed are pharmaceutical compositions comprising a pharmaceutical carrier and, as an active ingredient, an effective amount of a dibenz [b,e] oxepin derivative represented by the following general formula: ##STR4## wherein R.sub.1 represents an alkyl group containing 1 to 5 carbon atoms, an alkoxy group containing 1 to 5 carbon atoms, a halogen atom, a cyclohexyl group or a phenyl group; and R.sub.2 represents ##STR5## wherein X represents a hydrogen atom, a hydroxy group, an amino group or a substituted aralkyl group containing 7 to 20 carbon atoms, and n has the same meaning as defined before ##STR6## or (3) --NH--(CH.sub.2).sub.n --Y, wherein Y and n have the same meaning as defined above; and the pharmaceutically acceptable acid addition salts thereof. Compound I, represented by the general formula (I), has antichlolinergic, antihistaminergic, antiasthmatic and antiplatelet aggregation activities, and is therefore useful as a sposmolysant, an antihistaminic, an antiasthmatic agent and as a medicament for cardiovascular or cerebrovascular diseases, respectively.

    Antiulcer [1] benzepino[3,4-b]pyridine and compositions
    7.
    发明授权
    Antiulcer [1] benzepino[3,4-b]pyridine and compositions 失效
    抗溃疡[1]苯并[3,4-b]吡啶和组合物

    公开(公告)号：US4547496A

    公开(公告)日：1985-10-15

    申请号：US623084

    申请日：1984-06-21

    申请人： Toshiaki Kumazawa ,  Yoshimasa Oiji ,  Hiroshi Tanaka ,  Katsuichi Shuto

    发明人： Toshiaki Kumazawa ,  Yoshimasa Oiji ,  Hiroshi Tanaka ,  Katsuichi Shuto

    IPC分类号： C07D491/04 ,  C07D491/044 ,  C07D495/04 ,  C07D519/00 ,  A61K31/44 ,  A61K31/535

    CPC分类号： C07D491/04 ,  C07D495/04

    摘要： A novel [1] benzepino[3,4-b]pyridine derivative having antiulcer activity is represented by the formula (I): ##STR1## wherein R.sup.1 represents a hydrogen atom, an alkyl group, a halogenated alkyl group, an alkoxy group or a halogen atom; R.sup.2 represents ##STR2## wherein Y represents an amino group, a substituted amino group, a heterocyclic group or a substituted heterocyclic group; Z represents a hydrogen atom, an alkyl group or an acyl group; and m is an integer of 1-3, ##STR3## wherein Z' represents a hydrogen atom or an alkyl group; Y has the same meaning as defined above, and n is 0, 1 or 2; or ##STR4## wherein Z and n have the same meanings as defined above; X represents an oxygen atom or a sulfur atom. Also disclosed are pharmaceutically acceptable acid addition salts of the compound represented by the formula (I).

    摘要翻译： 具有抗溃疡活性的新型[1]苯并[3,4-b]吡啶衍生物由式（I）表示：其中R 1表示氢原子，烷基，卤代烷基， 烷氧基或卤素原子; R2表示，其中Y表示氨基，取代氨基，杂环基或取代的杂环基; Z表示氢原子，烷基或酰基; m为1-3的整数，其中Z'表示氢原子或烷基; Y具有与上述相同的含义，n为0,1或2; 或其中Z和n具有与上述相同的含义; X表示氧原子或硫原子。 还公开了由式（I）表示的化合物的药学上可接受的酸加成盐。