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    • 1. 发明公开
    • Dibenz (b,e) oxepin derivative and antiallergic agent
    • Dibenz(b,e)oxepin-Derivat和antiallergisches Mittel。
    • EP0188802A2
    • 1986-07-30
    • EP85116465.7
    • 1985-12-23
    • KYOWA HAKKO KOGYO CO., LTD.
    • Kumazawa, ToshiakiOshima, EtsuoObase, HiroyukiOhmori, KanjiIshii, HideeShuto, Katsuichi
    • C07D313/12A61K31/335A61K31/495A61K31/55
    • C07D405/04C07D313/12
    • A dibenz[b,e]oxepin derivative represented by the formula (I):
      {wherein A 1 is a hydrogen atom, a methyl group, (CH 2 ) m OR 1 [where m is an integer of 1 to 4, and R 1 is a hydrogen atom, CH 2 CH(OH)CH 2 OCH 2 CH 3 , CH 2 CH(OAc)CH 2 OCH 2 CH 3 or CH 2 OCH 2 CH 2 OCH 3 ], CH(CH 3 )CH 2 OR 1 (where R 1 has the same meaning as defined above), CH = CHC0 2 R 2 (where R 2 is a hydrogen atom or a lower alkyl group), (CH 2 ) n CO 2 R 2 (where n is an integer of 1 to 3, and R has the same meaning as defined above), CH(CH 3 )CO 2 R 2 (where R 2 has the same meaning as defined above), CO 2 (CH 2 )NR 3 R 4 (where is an integer of 1 to 6, and R 3 and R 4 are the same or different lower alkyl groups), CONHR 5 (where R 5 is a lower alkyl group). CO 2 CH 2 CH(OR 6 ),CH 2 OCH 2 CH 3 (where R 6 is a hydrogen atom or an acetyl group), C0 2 CH 2 CH 2 0CH 2 CH 2 0H or CO 2 X 1 (where X 1 is a hydrogen atom or a lower alkyl group). A 2 is a 4-lower alkylpiperazino group, a 4-lower alkylhomopiperazino group or Y-(CH 2 ) p NR 7 R 8 (where Y is NH, O or S, p is an integer of 2 to 5, and R 7 and R 8 are the same or different hydrogen atoms or lower alkyl groups). One of A3 and A4 is COR [where R 9 is a hydroxyl group, a lower alkoxy group, an 1-(ethoxycarbony- loxy)ethoxy group or an amino group] or a cyano group, and the other is a hydrogen atom; or A3 is a hydrogen atom or an alkyl group having 1 to 3 carbon atoms and is a substituent at the 4-position, and A4 is a hydrogen atom.} has antiallergic activity such as antiasthmatic activity.
    • 由式(I)表示的二苯并[b,e]氧杂七环衍生物:其中A 1是氢原子,甲基,(CH 2)m OR 1 [其中m是整数1 至4,R 1为氢原子,CH 2 CH(OH)CH 2 OCH 2 CH 3,CH 2 CH(OAc)CH 2 OCH 2 CH 3或CH 2 OCH 2 CH 2 OCH 3,CH(CH 3)CH 2 OH(其中R 1具有与上述相同的含义) CH = CHCO 2 R 2(其中R 2是氢原子或低级烷基),(CH 2)n CO 2 R 2(其中n是1至3的整数,并且R 2具有相同的含义 如上定义),CH(CH 3)CO 2 R 2(其中R 2具有与上述相同的含义),CO 2(CH 2)n NR 3 R 4(其中@是1至 6,R 3和R 4是相同或不同的低级烷基),CONHR 5(其中R 5是低级烷基),CO 2 CH 2 CH(OR 6),CH 2 OCH 2 CH 3(其中 R 6是氢原子或乙酰基),CO 2 CH 2 CH 2 OCH 2 CH 2 OH或CO 2 X 1(其中X 1是氢原子或低级烷基)。 A 2是4-低级烷基哌嗪基,4-低级烷基高哌啶子基或Y-(CH 2)p NR R R 8(其中Y是NH,O或S,p是2至5的整数 R 7和R 8是相同或不同的氢原子或低级烷基)。 A 3和A 4中的一个是COR 9,其中R 9是羟基,低级烷氧基,1-(乙氧羰基氧基)乙氧基或氨基或氰基, 另一个是氢原子; 或A 3为氢原子或碳原子数为1〜3的烷基,为4位的取代基,A 4为氢原子。}具有抗过敏活性,例如抗哮喘活性。
    • 3. 发明公开
    • Dibenz (b,e) oxepin derivative and antiallergic agent
    • DIBENZ(B,E)OXEPIN衍生物和抗癌剂
    • EP0188802A3
    • 1986-08-20
    • EP85116465
    • 1985-12-23
    • KYOWA HAKKO KOGYO CO., LTD.
    • Kumazawa, ToshiakiOshima, EtsuoObase, HiroyukiOhmori, KanjiIshii, HideeShuto, Katsuichi
    • C07D313/12A61K31/335A61K31/495A61K31/55
    • C07D405/04C07D313/12
    • A dibenz[b,e]oxepin derivative represented by the formula (I):
      {wherein A 1 is a hydrogen atom, a methyl group, (CH 2 ) m OR 1 [where m is an integer of 1 to 4, and R 1 is a hydrogen atom, CH 2 CH(OH)CH 2 OCH 2 CH 3 , CH 2 CH(OAc)CH 2 OCH 2 CH 3 or CH 2 OCH 2 CH 2 OCH 3 ], CH(CH 3 )CH 2 OR 1 (where R 1 has the same meaning as defined above), CH = CHC0 2 R 2 (where R 2 is a hydrogen atom or a lower alkyl group), (CH 2 ) n CO 2 R 2 (where n is an integer of 1 to 3, and R has the same meaning as defined above), CH(CH 3 )CO 2 R 2 (where R 2 has the same meaning as defined above), CO 2 (CH 2 )NR 3 R 4 (where is an integer of 1 to 6, and R 3 and R 4 are the same or different lower alkyl groups), CONHR 5 (where R 5 is a lower alkyl group). CO 2 CH 2 CH(OR 6 ),CH 2 OCH 2 CH 3 (where R 6 is a hydrogen atom or an acetyl group), C0 2 CH 2 CH 2 0CH 2 CH 2 0H or CO 2 X 1 (where X 1 is a hydrogen atom or a lower alkyl group). A 2 is a 4-lower alkylpiperazino group, a 4-lower alkylhomopiperazino group or Y-(CH 2 ) p NR 7 R 8 (where Y is NH, O or S, p is an integer of 2 to 5, and R 7 and R 8 are the same or different hydrogen atoms or lower alkyl groups). One of A3 and A4 is COR [where R 9 is a hydroxyl group, a lower alkoxy group, an 1-(ethoxycarbony- loxy)ethoxy group or an amino group] or a cyano group, and the other is a hydrogen atom; or A3 is a hydrogen atom or an alkyl group having 1 to 3 carbon atoms and is a substituent at the 4-position, and A4 is a hydrogen atom.} has antiallergic activity such as antiasthmatic activity.