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    • 2. 发明公开
    • BORON-DIPYRRIN COMPLEX AND PHARMACEUTICAL PRODUCT CONTAINING SAME
    • 硼 - 双甘氨酸络合物和含有该化合物的药物产品
    • EP3266765A1
    • 2018-01-10
    • EP16761669.7
    • 2016-03-04
    • Japan Science and Technology Agency
    • KANAI, MotomuSOMA, YoheiSHIMIZU, YusukeTANIGUCHI, AtsuhikoOISAKI, KounosukeKUNINOBU, Yoichiro
    • C07D207/44A61K31/69A61P25/28C07D207/456C07D401/14C07D455/04C07F5/02A61K41/00
    • A61K31/69A61K31/4025A61K31/4725A61K41/00C07D207/44C07D207/456C07D207/46C07D215/06C07D401/14C07D455/04C07F5/02
    • Provided are a compound which is useful as an in vivo applicable, amyloid-oxygenating catalyst selective for amyloid and applicable not only to an Aβ peptide, but also to other amyloids and a drug containing the compound for preventing and/or treating amyloid-related diseases.
      Disclosed is a boron-dipyrrin complex represented by the following formula (1)

      wherein X 1 and X 2 are the same or different and each represent a halogenoalkyl group or a halogen atom;
      R 1 represents a hydrogen atom, an alkyl group, or a group represented by formula (b):

      R 2 and R 6 are the same or different and each represent a hydrogen atom or a halogen atom;
      R 3 , R 4 , R 5 , and R 7 are the same or different and each represent a hydrogen atom, a halogen atom, or an alkyl group;
      R 8 represents a hydrogen atom or -(CH 2 ) l -(Y) m -(CH 2 ) n -Z wherein Y represents -CO-, -CONH-, or a triazole ring, Z represents a carboxyl group, a sulfonic acid group, or a -CO-peptide residue, 1 and n each represent an integer of 1 to 6, and m represents 0 or 1;
      R 9 and R 10 are the same or different and each represent a hydrogen atom, an alkyl group, an alkoxy group, a halogen atom, an amino group, a nitro group, or a cyano group; and
      R 8 and R 10 together optionally form an alkylene group.
    • 本发明提供可用作淀粉样蛋白选择性体内适用的淀粉样蛋白增氧催化剂的化合物,不仅适用于Aβ肽,而且适用于其他淀粉状蛋白和含有该淀粉样蛋白相关疾病的预防和/或治疗用化合物的药物 。 公开了由下式(1)表示的硼 - 双联吡啶配合物,其中X 1和X 2相同或不同并且各自表示卤代烷基或卤素原子; R 1表示氢原子,烷基或由式(b)表示的基团:R 2和R 6相同或不同并且各自表示氢原子或卤素原子; R3,R4,R5和R7相同或不同,各自表示氢原子,卤素原子或烷基; R8代表氢原子或 - (CH2)l-(Y)m-(CH2)nZ,其中Y代表-CO - , - CONH-或三唑环,Z代表羧基,磺酸基或 -CO-肽残基,1和n各自表示1至6的整数,并且m表示0或1; R9和R10相同或不同,分别表示氢原子,烷基,烷氧基,卤素原子,氨基,硝基或氰基。 并且R 8和R 10一起任选地形成亚烷基。