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    • 37. 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。
    • 38. 发明公开
    • Quinoline-n-oxide derivative and pharmaceutical composition
    • 喹啉N-氧化物衍生物和药物制剂。
    • EP0177764A1
    • 1986-04-16
    • EP85111243.3
    • 1985-09-05
    • KYOWA HAKKO KOGYO CO., LTD.
    • Teranishi, MasayukiSuzuki, KojiKase, HiroshiKitamura, ShigetoShuto, KatsuichiOmori, Kenji
    • C07D215/60C07D405/12A61K31/47
    • C07D405/12C07D215/60
    • A quinoline-N-oxide derivative represented by the formula:
      [wherein X is hydroxy, lower alkoxy, lower alkylthio, unsubstituted or substituted aralkyloxy, or unsubstituted or substituted aralkylthio; Y is a hydrogen atom or halogen atom; R, is alkylene or alkenylene having 3 to 15 carbon atoms; Z is hydroxymethyl, lower alkoxymethyl, unsubstituted or substituted aryloxymethyl, tetrahydropyranyloxymethyl, tetrahydrofuranyloxymethyl, unsubstituted or substituted arylsulfonyloxymethyl, lower alkylthiomethyl, unsubstituted or substituted arylthiomethyl, lower alkylsulfinylmethyl, unsubstituted or substituted arylsulfinylmethyl, lower alkylsulfonylmethyl, unsubstituted or substituted arylsulfonylmethyl, aminomethyl, -CH 2 NHR 2 (wherein R 2 is lower alkyl, unsubstituted or substituted aralkyl, or unsubstituted or substituted aryl), -CH 2 NR 3 R 4 , (wherein R 3 and R 4 are lower alkyl, unsubstituted or substituted aralkyl, or unsubstituted or substituted aryl), -CH 2 N + R 5 R 6 R 7 (wherein R 5 , R 6 , and R 7 are lower alkyl, unsubstituted or substituted aralkyl, or unsubstituted or substituted aryl, where the counterion is an anion of acid or a hydroxyl ion), -COR 8 (wherein R. is a hydrogen atom, lower alkyl or hydroxy), -CH(OR 9 ) 2 (wherein R. is lower alkyl), iminomethyl, hydroxyiminomethyl, or a halogen atom] and its salts, can very strongly inhibit the lipoxygenase and considerably suppress production and release of its metabolites, and thus are useful as preventive and healing agents for the diseases caused by the lipoxygenase metabolites.
    • 40. 发明公开
    • Novel piperidine derivatives and pharmaceutical compositions containing same
    • 哌啶 - 衍生物和药物制剂Zusammensetzungen。
    • EP0092391A2
    • 1983-10-26
    • EP83302123.1
    • 1983-04-14
    • KYOWA HAKKO KOGYO CO., LTD
    • Teranishi, MasayukiObase, HiroyukiNomoto, YujiShuto, KatsuichiKarasawa, AkiraKasuya, Yutaka
    • C07D401/06C07D401/04A61K31/445
    • C07D401/04C07D211/26C07D211/58C07D401/06
    • Novel piperidine derivatives are disclosed having hypotensive activity, as well as pharmaceutical preparations containing them. The novel compounds are of the formula
      wherein A is a hydroxyl group, a halogen atom, a C,-C 5 alkyl group, a C 1 -C 5 alkoxy group, a C 2 -C 5 alkenyloxy group, a C 1 -C 5 alkinyloxy group, a C 1 -C 5 alkylthio group, a carboxyl group, a C 1 -C 5 alkoxycarbonyl group, a nitro group, an amino group, a C 1 -C 5 alkylamino group, a C,-C 5 alkanoylamino group, a sulfamoyl group, a mono- or di- (C 1 -C 5 alkyl) aminosulfonyl group, a C 1 -C 5 alkylsulfonyl group, a carbamoyl group, a cyano group or a trifluoromethyl group; when m is 2 or more, A may be the same or different groups, or two A groups may combine to form a C,-C 5 alkylenedioxy group; m is 0 or an integer of 1-5; Q is a carbonyl group or a hydroxymethylene group; R is a hydrogen atom or an alkyl group having 1-4 carbon atoms; X and Y are defined as follows: i) when Y = H, X represents
      ii) when Y = CH 3 , X represents
      and when
      X represents a hydrogen atom and their pharmacologically acceptable acid addition salts.
    • 公开了具有降血压活性的新型哌啶衍生物,以及含有它们的药物制剂。 该新化合物具有式CHEM,其中A为羟基,卤原子,C1-C5烷基,C1-C5烷氧基,C7-C5链烯氧基,C1-C5烷氧基, C1-C5烷硫基,羧基,C1-C5烷氧基羰基,硝基,氨基,C1-C5烷基氨基,C1-C5烷酰基氨基,氨磺酰基,一或二( C1-C5烷基)氨基磺酰基,C1-C5烷基磺酰基,氨基甲酰基,氰基或三氟甲基; 当m为2以上时,A可以相同或不同,或两个A基团可以结合形成C1-C5亚烷基二氧基; m为0或1-5的整数; Q是羰基或羟基亚甲基; R是氢原子或具有1-4个碳原子的醇酸基; X和Y定义如下:i)当Y = H时,X表示 ii)当Y = CH 3时,X表示,当Y = CHEM时,X表示氢原子及其药理学上可接受的酸加成盐 。