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    • 8. 发明授权
    • Fused heterocyclic compounds
    • US09029536B2
    • 2015-05-12
    • US13814073
    • 2011-08-03
    • Joseph RakerTakahiko TaniguchiMasato YoshikawaTomoaki HasuiJun Kunitomo
    • Joseph RakerTakahiko TaniguchiMasato YoshikawaTomoaki HasuiJun Kunitomo
    • C07D471/04C07D471/14C07D519/00
    • C07D471/04C07D471/14C07D519/00
    • The present invention provides a compound which has the effect of PDE 10A inhibition, and which is useful as a medicament for preventing or treating schizophrenia or so on. A compound represented by the formula (1′): wherein, Ring A′ represents an optionally substituted pyridine ring, an optionally substituted pyridazine ring, a pyrimidine ring, or 10 a pyrazine ring, R1′ represents (1) wherein, R1a′ represents an optionally substituted phenyl group, or an optionally substituted 5- to 10-membered heterocyclic group, Ring B2 represents a bond, —S—, -0-, —CO—, an optionally substituted methylene group, or —NRa′— (Ra′ represents a hydrogen atom, or an optionally substituted C1-6 alkyl group), and Ring B1′ represents an optionally further substituted 6- to 10-membered aromatic hydrocarbon ring, or an optionally further substituted 5- to 10-membered aromatic heterocyclic ring, or alternatively, L′ and R1a′ may be taken together to form an optionally substituted bicyclic or tricyclic fused heterocyclic group, or (2), wherein, R1b′ represents an optionally substituted phenyl group, or an optionally substituted 5- to 10-membered heterocyclic group, Ring B2′ represents an optionally substituted benzene ring, an optionally substituted pyridine ring, an optionally substituted pyrimidine ring, an optionally substituted pyrazine ring, or an optionally substituted pyridazine ring, Ring D′ represents an optionally further substituted 5- or 6-membered ring, R2′ represents a hydrogen atom, or a substituent, X′ represents ═N— or ═CRb′—(Rb′ represents a hydrogen atom, or a substituent), - - - - - represents that Rb′ and R2′ may form, taken together with the carbon atom and the nitrogen atom to which they are each adjacent, an optionally substituted 5- to 7-membered ring when.X′ is ═CRb′, or a salt thereof.
    • 9. 发明申请
    • FUSED HETEROCYCLIC COMPOUNDS
    • 熔融杂环化合物
    • US20130172292A1
    • 2013-07-04
    • US13814073
    • 2011-08-03
    • Joseph RakerTakahiko TaniguchiMasato YoshikawaTomoaki HasuiJun Kunitomo
    • Joseph RakerTakahiko TaniguchiMasato YoshikawaTomoaki HasuiJun Kunitomo
    • C07D471/04C07D471/14C07D519/00
    • C07D471/04C07D471/14C07D519/00
    • The present invention provides a compound which has the effect of PDE 10A inhibition, and which is useful as a medicament for preventing or treating schizophrenia or so on. A compound represented by the formula (1′): wherein, Ring A′ represents an optionally substituted pyridine ring, an optionally substituted pyridazine ring, a pyrimidine ring, or 10 a pyrazine ring, R1′ represents (1) wherein, R1a′ represents an optionally substituted phenyl group, or an optionally substituted 5- to 10-membered heterocyclic group, Ring B2 represents a bond, —S—, -0-, —CO—, an optionally substituted methylene group, or —NRa′-(Ra′ represents a hydrogen atom, or an optionally substituted C1-6 alkyl group), and Ring B1′ represents an optionally further substituted 6- to 10-membered aromatic hydrocarbon ring, or an optionally further substituted 5- to 10-membered aromatic heterocyclic ring, or alternatively, L′ and R1a′ may be taken together to form an optionally substituted bicyclic or tricyclic fused heterocyclic group, or (2), wherein, R1b′ represents an optionally substituted phenyl group, or an optionally substituted 5- to 10-membered heterocyclic group, Ring B2′ represents an optionally substituted benzene ring, an optionally substituted pyridine ring, an optionally substituted pyrimidine ring, an optionally substituted pyrazine ring, or an optionally substituted pyridazine ring, Ring D′ represents an optionally further substituted 5- or 6-membered ring, R2′ represents a hydrogen atom, or a substituent, X′ represents ═N— or ═CRb′—(Rb′ represents a hydrogen atom, or a substituent), - - - - - represents that Rb′ and R2′ may form, taken together with the carbon atom and the nitrogen atom to which they are each adjacent, an optionally substituted 5- to 7-membered ring when.X′ is ═CRb′, or a salt thereof.
    • 本发明提供了具有PDE 10A抑制作用的化合物,其可用作预防或治疗精神分裂症等的药物。 由式(1')表示的化合物:其中环A'表示任选取代的吡啶环,任选取代的哒嗪环,嘧啶环或吡嗪环,R1'表示(1)其中R1a'表示 任选取代的苯基或任选取代的5至10元杂环基,环B2表示键,-S - , - O-,-CO-,任选取代的亚甲基或-NR a' - (R a '表示氢原子或任选取代的C 1-6烷基),并且环B1'表示任选进一步取代的6至10元芳族烃环或任选进一步取代的5至10元芳族杂环 ,或者可选地,L'和R 1a'可以一起形成任选取代的双环或三环稠合杂环基,或(2),其中,R 1b'表示任选取代的苯基,或任选取代的5-至10- 环B2'表示 任选取代的苯环,任选取代的吡啶环,任选取代的嘧啶环,任选取代的吡嗪环或任选取代的哒嗪环,环D'表示任选进一步取代的5-或6-元环,R 2' 表示氢原子或取代基,X'表示= N-或= CRb' - (Rb'表示氢原子或取代基), - - - 表示Rb'和R2'可以一起形成 与它们各自相邻的碳原子和氮原子,当X'= CRb'或其盐时,任选取代的5-至7-元环。