4-Imidazoline derivatives and their use in preparing pharmaceutical compositions
    3.
    发明公开
    4-Imidazoline derivatives and their use in preparing pharmaceutical compositions 失效
    4-咪唑啉衍生物和它们用于制备药物制剂的用途。

    公开(公告)号:EP0396973A1

    公开(公告)日:1990-11-14

    申请号:EP90107993.9

    申请日:1990-04-26

    IPC分类号: C07D233/70 A61K31/415

    CPC分类号: C07D233/70

    摘要: 4-lmidazoline derivatives represented by the formula (I) and/or formula (II):
    wherein R 1 represents C 1 -C 8 alkyl, C 3 -C 8 alkenyl, C 3 -Cs alkynyl, C 3 -C 8 cycloalkyl, or optionally substituted aralkyl; R 2 and R 3 independently represent hydrogen, C 3 -C 20 alkyl, C 3 -C 20 alkenyl, C 3 -C 20 alkynyl, C 3 -C 20 alkoxy, C 3 -C 20 alkenyloxy, C 3 -C 20 alkynyloxy, C 3 -C S cycloalkyl, C 1 -C 10 alkylthio, or optionally substituted aralkyl or aralkyloxy; R 4 represents C 1 -C 6 alkyl, C 3 -C 8 cycloalkyl, or optionally substituted aralkyl; provided that R 2 and R 3 cannot be hydrogen at the same time, and pharmaceutically acceptable salts thereof. A pharmaceutical formulation containing the compound is also provided.

    摘要翻译: 由式(I)和/或式表示的4-咪唑啉衍生物(II):其中,R <1>表示C1-C8烷基,C3-C8链烯基,C3-C8炔基,C3-C8环烷基,或任选 取代的芳烷基; [R <3>代表氢unabhängig<2>和R,C3-C20烷基,C3-C20链烯基,C3-C20炔基,C3-C20烷氧基,C3-C20链烯氧基,C3-C20炔氧基,C3-C8环烷基,C1 C10烷硫基,或任选取代的芳烷基或芳烷氧基; [R <4> darstellt C1-C6烷基,C3-C8环烷基,或任选取代的芳烷基; 提供确实ř<2>和R <3>不能同时为氢,以及它们药学上可接受的盐。 因此,提供含有该化合物的药物制剂。

    Heterocyclic compounds having lipoxygenase inhibiting activity
    5.
    发明公开

    公开(公告)号:EP0420762A3

    公开(公告)日:1991-07-31

    申请号:EP90402692.9

    申请日:1990-09-28

    摘要: A novel heterocyclic compound represented by the following formula (I):
    wherein X represents an oxygen atom or sulfur atom; R¹ represents a hydrogen atom or halogen atom; R² represents a C₄-C₆ alkyl group, C₂-­C₁₀ alkoxyalkyl group, C₃-C₁₅ alkenyl group, C₇-C₁₂ aralkyl group, C₈-­C₁₈ aralkyloxyalkyl group, C₇-C₁₂ aryloxyalkyl group, C₃-C₁₀ alkynyl group, C₄-C₁₂ alkadienyl group, C₆-C₁₈ alkatrienyl group, C₆-C₁₂ alkadiynyl group, or C₆-C₁₂ alkatriynyl group, said aryloxyalkyl group, alkynyl group, alkadienyl group, alkatrienyl group, alkadiynyl group and alkatriynyl group being capable of having at least one substituent selected from the group consisting of halogen atoms, C₁-C₄ alkyl group, C₁-C₄ halogenated alkyl group, phenyl group, hydroxyl group and C₁-­C₄ alkoxy group; and each of R³ and R⁴ independently represents a hydrogen atom, C₁-C₆ alkyl group, phenyl group or tolyl group, or R³ and R⁴ may be combined together to from a benzene ring which may have at least one halogen atom; or a pharmaceutically acceptable salt thereof. The compound according to the present invention has an effect of inhibiting lipoxygenase and suppresses the formation of leukotrienes and, accordingly, useful for the prevention and treatment of inflammation, rheumatism and various allergic diseases.

    Heterocyclic compounds having lipoxygenase inhibiting activity
    6.
    发明公开
    Heterocyclic compounds having lipoxygenase inhibiting activity 失效
    Heterocyclische Derivate mit lipoxygenase hemmender Wirkung。

    公开(公告)号:EP0420762A2

    公开(公告)日:1991-04-03

    申请号:EP90402692.9

    申请日:1990-09-28

    摘要: A novel heterocyclic compound represented by the following formula (I):
    wherein X represents an oxygen atom or sulfur atom; R¹ represents a hydrogen atom or halogen atom; R² represents a C₄-C₆ alkyl group, C₂-­C₁₀ alkoxyalkyl group, C₃-C₁₅ alkenyl group, C₇-C₁₂ aralkyl group, C₈-­C₁₈ aralkyloxyalkyl group, C₇-C₁₂ aryloxyalkyl group, C₃-C₁₀ alkynyl group, C₄-C₁₂ alkadienyl group, C₆-C₁₈ alkatrienyl group, C₆-C₁₂ alkadiynyl group, or C₆-C₁₂ alkatriynyl group, said aryloxyalkyl group, alkynyl group, alkadienyl group, alkatrienyl group, alkadiynyl group and alkatriynyl group being capable of having at least one substituent selected from the group consisting of halogen atoms, C₁-C₄ alkyl group, C₁-C₄ halogenated alkyl group, phenyl group, hydroxyl group and C₁-­C₄ alkoxy group; and each of R³ and R⁴ independently represents a hydrogen atom, C₁-C₆ alkyl group, phenyl group or tolyl group, or R³ and R⁴ may be combined together to from a benzene ring which may have at least one halogen atom; or a pharmaceutically acceptable salt thereof. The compound according to the present invention has an effect of inhibiting lipoxygenase and suppresses the formation of leukotrienes and, accordingly, useful for the prevention and treatment of inflammation, rheumatism and various allergic diseases.

    摘要翻译: 由下式(I)表示的新型杂环化合物:其中X表示氧原子或硫原子; R 1表示氢原子或卤素原子; R 2表示C4-C6烷基,C2-C10烷氧基烷基,C3-C15烯基,C7-C12芳烷基,C8-C18芳烷氧基烷基,C7-C12芳氧基烷基,C3-C10炔基,C4- C12链二烯基,C6-C18链三烯基,C6-C12烷二炔基或C6-C12烷基三炔基,所述芳氧基烷基,炔基,链二烯基,链三烯基,炔二炔基和烷基三炔基能够具有至少一个取代基 由卤素原子,C1-C4烷基,C1-C4卤代烷基,苯基,羟基和C1-C4烷氧基组成的组; R 3和R 4各自独立地表示氢原子,C 1 -C 6烷基,苯基或甲苯基,或者R 3和R 4可以一起结合成苯环, 可以具有至少一个卤素原子; 或其药学上可接受的盐。 根据本发明的化合物具有抑制脂氧合酶的作用,抑制白细胞三烯的形成,因此可用于预防和治疗炎症,风湿病和各种过敏性疾病。

    (2-Chloro-3-oxo-1-alkenyl)bicyclo (3.3.0.) octene derivative and process for preparing the same
    10.
    发明公开
    (2-Chloro-3-oxo-1-alkenyl)bicyclo (3.3.0.) octene derivative and process for preparing the same 失效
    (2-氯-3-氧代-1-烯基)-bicyclo¬3.3.0octenderivat和过程及其制备

    公开(公告)号:EP0234158A1

    公开(公告)日:1987-09-02

    申请号:EP86402925.1

    申请日:1986-12-23

    IPC分类号: C07C177/00

    CPC分类号: C07C405/0083

    摘要: There are disclosed a (2-chloro-3-oxo-l-alkenyl)bicyclo[3.3.0]octene derivative represented by the formula:
    wherein R' represents -CH 2 CH 2 CH 2 CH 2 COOR 5 , -CH 2 CH 2 -O-CH 2 COOR 5 , -CH=CHCH 2 CH 2 COOR 5 or -CH 2 CH 2 C≡C-COOR 5 group where R 5 in the groups represents a hydrogen atom or an alkyl group having I to 6 carbon atoms; R 2 represents a hydrogen atom, an acyl group having I to 7 carbon atoms, a tri(I to 7 carbon atoms)hydrocarbylsilyl group or a group forming an acetal bonding with an oxygen atom of a hydroxy group; R 3 represents a straight or branched alkyl group having 3 to 10 carbon atoms, a cycloalkyl group having 4 to 7 carbon atoms, which may be substituted by at least one alkyl group having I to 4 carbon atoms, a straight or branched alkenyl group having 3 to 12 carbon atoms, a straight or branched alkynyl group having 3 to 8 carbon atoms, a phenyl group or a phenoxy group which may have substituents, an alkoxy group having I to 6 carbon atoms or an alkyl group substituted by a cycloalkyl group having 5 to 8 carbon atoms, and a process for preparing the same which comprises reacting an aldehyde represented by the formula:
    wherein R 1 and R 2 have the same meanings as defined above, with kotophosphonate represented by the formula:
    wherein R 3 has the same meaning as defined above and R 4 represents an alkyl group having I to 10 carbon atoms, in the presence of a base.