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    • 4. 发明公开
    • NITROGENOUS TRICYCLIC COMPOUNDS AND DRUGS COMPRISING THE SAME
    • 医疗器械制造商维吾尔自行车
    • EP0889037A1
    • 1999-01-07
    • EP97907297.2
    • 1997-03-13
    • Eisai Co., Ltd.
    • MIYAMOTO, MitsuakiYOSHIUCHI, TatsuyaSATO, KeizoKAINO, MakotoTANAKA, MasayukiSOEJIMA, MotoharuMORIYA, KatsuhiroSAKUMA, YoshinoriYAMADA, KojiHARADA, KokichiNISHIZAWA, YukioKOBAYASHI, SeiichiOKITA, MakotoKATAYAMA, Koichi
    • C07D219/14C07D243/38C07D279/24C07D279/34C07D417/06C07D417/12C07D417/14A61K31/54A61K31/645
    • C07D417/06C07D279/22C07D279/24C07D417/12C09B21/00C09B57/08
    • To provide a novel phenothiazine, acridan, acridone oxime, acridone hydrazone and dibenzodiazepine derivative efficacious against diseases in which histamine, leukotrienes, etc. participate.
      A phenothiazine, acridan, acridone oxime, acridone hydrazone and dibenzodiazepine derivative represented by the following formula are efficacious in preventing or treating diseases in which chemical mediators such as histamine and leukotrienes participate, for example, asthma, allergic rhinitis, atopic dermatitis, urticaria, hay fever, gastrointestinal allergy and food allergy.
      A nitrogen-containing tricyclic compound represented by the following formula (I), a hydrate thereof or a pharmacologically acceptable salt thereof:
         (wherein D represents alkylene, etc.)
      wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 and R 8 are the same or different from each other and each represents hydrogen, hydroxy, cyano, nitro, optionally substituted carbamoyl, halogeno, optionally halogenated lower alkyl, etc.; Z represents -S-, -SO-, -SO 2 -, =NO-substituent, -NC(O)- or =NN-substituent; and Q represents, for example, -NR 20 R 21 (wherein R 20 and R 21 are the same or different from each other and each represents hydrogen, optionally halogenated lower alkyl, optionally substituted aryl, optionally substituted arylalkyl, optionally substituted heteroaryl or optionally substituted heteroarylalkyl, or R 20 and R 21 may form together with the nitrogen atom to which they are bonded a 3- to 8-membered ring).
    • 提供对组胺,白三烯等参与的疾病有效的新型吩噻嗪,吖啶酮,吖啶酮肟,吖啶酮腙和二苯并二氮杂衍生物。 由下式表示的吩噻嗪,吖啶酮,吖啶酮肟,吖啶酮腙和二苯并二氮杂衍生物可有效预防或治疗化学介质如组胺和白三烯参与的疾病,例如哮喘,过敏性鼻炎,特应性皮炎,荨麻疹,干草 发烧,胃肠道过敏和食物过敏。 由下式(I)表示的含氮三环化合物,其水合物或其药理学上可接受的盐:(其中D表示亚烷基等,其中R 1,R 2, R 3,R 4,R 5,R 6,R 7和R 8彼此相同或不同,各自表示氢,羟基,氰基,硝基,任选取代的氨基甲酰基, 卤代,任选卤代的低级烷基等; Z表示-S-,-SO-,-SO 2 - ,= NO-取代基,-NC(O) - 或= N - 取代基; Q表示例如-NR R 20和R 21彼此相同或不同,各自表示氢,任选卤代的低级烷基,任选取代的芳基,任选取代的芳烷基,任选取代的杂芳基或任选取代的 杂芳基烷基或R 20和R 21可以与它们所键合的氮原子一起形成3-至8-元环)。
    • 8. 发明公开
    • Pharmaceutical composition for the treatment of underlying nonpharmacologically induced nervous system cholinergic deficit state comprising monoamine acridine derivatives
    • 用于处理含单aminakridin衍生物胆碱能神经系统的非pharmacologischer Unsprungender缺乏症的药物组合物。
    • EP0595365A1
    • 1994-05-04
    • EP93117982.4
    • 1987-09-28
    • Summers, William Koopmans
    • Summers, William Koopmans
    • A61K31/47A61K31/495C07D401/06C07D219/14
    • A61K31/00A61K31/47A61K31/495C07D219/10
    • A pharmaceutical composition for treatment of underlying nonpharmacologically induced central or peripheral nervous system cholinergic deficit state in humans comprising a monoamine acridine derivative of the formula:

      wherein R₁ represents hydrogen, hydroxy, methyl, methoxy, ethyl or ethoxy; R₁ and R₂ together may form a double bond, R₃ and R₄ together may form a double bond, or R₁, R₂, R₃ and R₄ are all hydrogen; R₅ represents hydrogen, hydroxy, methoxy or ethoxy; R₆ represents hydrogen, hydroxy, methoxy or ethoxy; and R₇ is without a substituent or R₇ represents an oxygen atom, a C₁-C₂₀ alkyl radical or a radical selected from the group consisting of
         -R-N(R)₂,

      wherein each R is independently selected from C₁-C₂₀ alkyl; or a pharmaceutically acceptable salts thereof, and a pharmaceutically acceptable inert carrier therefor; with the provisos that the monoamine acridine derivative is a compound in which (i) if R₁, R₂, R₃, R₄, R₅ and R₆ are each hydrogen, then R₇ cannot be without a substituent, (ii) if R₁ and R₂ together form a double bond, R₃ and R₄ together form a double bond and R₅ and R₆ are each hydrogen, then R₇ cannot be without a substituent, and (iii) if R₃ and R₄ together form a double bond and R₇ is without a substituent, then R₁ cannot be a hydrogen atom is provided.
    • 用于治疗的药物组合物底层nonpharmacologically诱导人类,包括下式的一元胺衍生物吖中枢或外周神经系统胆碱能缺乏状态: worin氢R1 darstellt,羟基,甲基,甲氧基,乙基或乙氧基; R1和R2可一起形成一个双键,R 3和R 4一起可以形成双键,或R1,R2,R3和R4都是氢; R5氢darstellt,羟基,甲氧基或乙氧基; 氢R6 darstellt,羟基,甲氧基或乙氧基; 和R 7是不具有取代基或氧原子的R7 darstellt,一个C1-C20烷基或基团选自下组的R-N(R)2中选择, worin每个R是unabhängig从C1-C20烷基; 或其药学上可接受的盐,和药学上可接受的隋性载体; 与DASS死单胺吖啶衍生物,条件是,其中(i)如果R1,R2,R3,R4,R5和R6各自为氢,则R 7不能是化合物不具有取代基的,(ⅱ)如果R 1和R 2一起形成一个 双键,R 3和R 4一起形成双键且R 5和R 6各自为氢时,则R 7不能没有取代基,以及(iii)如果R 3和R 4一起形成双键,R 7是不具有取代基时,则R 1不能 是提供一种氢原子。