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    • 1. 发明公开
    • DRUG FOR RESPIRATORY DISEASES
    • 药物治疗呼吸道疾病
    • EP2974730A1
    • 2016-01-20
    • EP14763747.4
    • 2014-03-13
    • Daiichi Sankyo Company, Limited
    • TAKAHASHI, SakikoDOMON, YukiKITANO, YutakaSHINOZUKA, Tsuyoshi
    • A61K31/506A61P11/00A61P11/06A61P11/08A61P11/14
    • A61K31/506A61K31/433A61K31/496
    • It is intended to provide a therapeutic agent and/or a preventive agent for a respiratory disease or a therapeutic agent and/or a preventive agent for a sodium channel associated disease. The present invention provides a pharmaceutical comprising a compound represented by the following formula (I) or a pharmacologically acceptable salt thereof as an active ingredient:

      Ar 1 and Ar 2 : a heteroaryl group or an aryl group; R 1 , R 2 and R 3 : a hydrogen atom, a halogen atom, a C1-C6 alkyl group, a halogenated C1-C6 alkyl group, a hydroxy C1-C6 alkyl group, a C1-C6 alkoxy C1-C6 alkyl group or a C3-C7 cycloalkyl group or a cyano group; R 4 and R 5 : a hydrogen atom, a halogen atom, a C1-C6 alkyl group, a halogenated C1-C6 alkyl group, a hydroxyl group, a hydroxy C1-C6 alkyl group, a C1-C6 alkoxy C1-C6 alkyl group, a C3-C7 cycloalkyl group or a C1-C6 alkoxy group;
      n: an integer of 1 to 3; and
      the heteroaryl or aryl group optionally has one or two groups independently selected from a halogen atom, a C1-C6 alkyl group, a halogenated C1-C6 alkyl group, a hydroxyl group, a hydroxy C1-C6 alkyl group, a C1-C6 alkoxy C1-C6 alkyl group, a C3-C7 cycloalkyl group, a carboxyl group, a cyano group, an amino group, a C1-C3 alkylamino group and a di-C1-C3 alkylamino group, and when the heteroaryl or aryl group has two such groups, the two groups are the same as or different from each other.
    • 旨在提供用于呼吸系统疾病或钠通道相关疾病的治疗剂和/或预防剂的治疗剂和/或预防剂。 本发明提供药物,其含有下式(I)所示的化合物或其药理学上可接受的盐作为有效成分:Ar 1和Ar 2:杂芳基或芳基; R 1,R 2和R 3:氢原子,卤素原子,C 1 -C 6烷基,卤代C 1 -C 6烷基,羟基C 1 -C 6烷基,C 1 -C 6烷氧基C 1 -C 6烷基或C 3 -C7环烷基或氰基; R 4和R 5:氢原子,卤素原子,C 1 -C 6烷基,卤代C 1 -C 6烷基,羟基,羟基C 1 -C 6烷基,C 1 -C 6烷氧基C 1 -C 6烷基, C3-C7环烷基或C1-C6烷氧基; n:1〜3的整数; 并且杂芳基或芳基任选具有一个或两个独立地选自卤素原子,C1-C6烷基,卤代C1-C6烷基,羟基,羟基C1-C6烷基,C1-C6烷基 烷氧基C 1 -C 6烷基,C 3 -C 7环烷基,羧基,氰基,氨基,C 1 -C 3烷基氨基和二-C 1 -C 3烷基氨基,并且当杂芳基或芳基具有 两个这样的组,两组彼此相同或不同。
    • 3. 发明授权
    • DRUG FOR RESPIRATORY DISEASES
    • 药物治疗呼吸道疾病
    • EP2974730B1
    • 2018-01-31
    • EP14763747.4
    • 2014-03-13
    • Daiichi Sankyo Company, Limited
    • TAKAHASHI, SakikoDOMON, YukiKITANO, YutakaSHINOZUKA, Tsuyoshi
    • A61K31/506A61P11/00A61P11/06A61P11/08A61P11/14
    • A61K31/506A61K31/433A61K31/496
    • It is intended to provide a therapeutic agent and/or a preventive agent for a respiratory disease or a therapeutic agent and/or a preventive agent for a sodium channel associated disease. The present invention provides a pharmaceutical comprising a compound represented by the following formula (I) or a pharmacologically acceptable salt thereof as an active ingredient: Ar 1 and Ar 2 : a heteroaryl group or an aryl group; R 1 , R 2 and R 3 : a hydrogen atom, a halogen atom, a C1-C6 alkyl group, a halogenated C1-C6 alkyl group, a hydroxy C1-C6 alkyl group, a C1-C6 alkoxy C1-C6 alkyl group or a C3-C7 cycloalkyl group or a cyano group; R 4 and R 5 : a hydrogen atom, a halogen atom, a C1-C6 alkyl group, a halogenated C1-C6 alkyl group, a hydroxyl group, a hydroxy C1-C6 alkyl group, a C1-C6 alkoxy C1-C6 alkyl group, a C3-C7 cycloalkyl group or a C1-C6 alkoxy group; n: an integer of 1 to 3; and the heteroaryl or aryl group optionally has one or two groups independently selected from a halogen atom, a C1-C6 alkyl group, a halogenated C1-C6 alkyl group, a hydroxyl group, a hydroxy C1-C6 alkyl group, a C1-C6 alkoxy C1-C6 alkyl group, a C3-C7 cycloalkyl group, a carboxyl group, a cyano group, an amino group, a C1-C3 alkylamino group and a di-C1-C3 alkylamino group, and when the heteroaryl or aryl group has two such groups, the two groups are the same as or different from each other.
    • 4. 发明公开
    • METHODS OF PRODUCING 4-CYCLOALKYLOXYBENZENESULFONAMIDES
    • 生产4-环烷氧基苯磺酰胺的方法
    • EP3144300A1
    • 2017-03-22
    • EP16193142.3
    • 2013-02-08
    • Daiichi Sankyo Company, Limited
    • SHINOZUKA, TsuyoshiKOBAYASHI, HiroyukiSUZUKI, SayakaTANAKA, KyosukeKIMOTO, HirokoDOMON, Yuki
    • C07D285/08C07D417/12C07D403/12C07D401/12
    • C07D403/12C07B2200/13C07D285/08C07D401/12C07D417/12Y02P20/55
    • A method of producing a compound of formula (I) or a pharmacologically acceptable salt thereof, useful as a therapeutic agent and/or a preventive agent for pain or for a sodium channel associated disease:

      Ar 1 and Ar 2 : a heteroaryl group or an aryl group, each optionally substituted; R 1 , R 2 and R 3 : a hydrogen atom, a halogen atom, a C1-C6 alkyl group, a halogenated C1-C6 alkyl group, a hydroxy C1-C6 alkyl group, a C1-C6 alkoxy C1-C6 alkyl group or a C3-C7 cycloalkyl group or a cyano group; R 4 and R 5 : a hydrogen atom, a halogen atom, a C1-C6 alkyl group, a halogenated C1-C6 alkyl group, a hydroxyl group, a hydroxy C1-C6 alkyl group, a C1-C6 alkoxy C1-C6 alkyl group, a C3-C7 cycloalkyl group or a C1-C6 alkoxy group; and n: an integer of 1 to 3, comprising a step of removing a protecting group P from the compound of formula (VI):

      or a step of reacting a compound of formula (X) and a compound of formula (XI) :

      wherein X represents a halogen atom.
    • 制备用作疼痛或钠通道相关疾病的治疗剂和/或预防剂的式(I)化合物或其药理学上可接受的盐的方法:Ar 1和Ar 2:杂芳基或芳基 ,各自任选被取代; R 1,R 2和R 3:氢原子,卤素原子,C 1 -C 6烷基,卤代C 1 -C 6烷基,羟基C 1 -C 6烷基,C 1 -C 6烷氧基C 1 -C 6烷基或C 3 -C7环烷基或氰基; R 4和R 5:氢原子,卤素原子,C 1 -C 6烷基,卤代C 1 -C 6烷基,羟基,羟基C 1 -C 6烷基,C 1 -C 6烷氧基C 1 -C 6烷基, C3-C7环烷基或C1-C6烷氧基; 并且n为1至3的整数,所述方法包括从式(VI)化合物除去保护基团P的步骤或使式(X)化合物与式(XI)化合物反应的步骤:其中 X代表卤素原子。