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    • 7. 发明授权
    • Cyclic amine compounds as CCR5 antagonists
    • 环胺化合物作为CCR5拮抗剂
    • US07348324B2
    • 2008-03-25
    • US10273111
    • 2002-10-18
    • Shinichi ImamuraShohei HashiguchiTaeko HattoriOsamu NishimuraNaoyuki KanzakiMasanori BabaYoshihiro Sugihara
    • Shinichi ImamuraShohei HashiguchiTaeko HattoriOsamu NishimuraNaoyuki KanzakiMasanori BabaYoshihiro Sugihara
    • A61P31/18A61K31/535A61K31/4965A61K31/44A61K31/47C07D413/00C07D241/00C07D211/00
    • C07D401/12C07D211/58C07D211/62C07D401/14C07D405/14C07D409/14C07D413/14C07D417/14C07D471/04C07D487/14
    • A compound of formula (I) (wherein R1 is a hydrogen atom, a hydrocarbon group which may be substituted, a non-aromatic heterocyclic group which may be substituted, R2 is a hydrocarbon group which may be substituted, a non-aromatic heterocyclic group which may be substituted, or R1 and R2 may combine to each other together with A to form a heterocyclic group which may be substituted; A is N or N+—R5.Y− (R5 is a hydrocarbon group; Y− is a counter anion); R3 is a cyclic hydrocarbon group which may be substituted or a heterocyclic group which may be substituted; n is 0 or 1; R4 is a hydrogen atom, a hydrocarbon group which may be substituted, a heterocyclic group which may be substituted, an alkoxy group which may be substituted, an aryloxy group which may be substituted, or an amino group which may be substituted, E is a divalent aliphatic hydrocarbon group which may be substituted by group(s) other than oxo; G1 is a bond, CO or SO2; G2 is CO, SO2, NHCO, CONH or OCO; J is methine or a nitrogen atom; and each of Q and R is a bond or a divalent C1-3 aliphatic hydrocarbon which may be substituted; provided that J is methine when G2 is OCO, that one of Q and R is not a bond when the other is a bond and that each of Q and R is not substituted by oxo group(s) when G1 is a bond) or a salt thereof has a potent CCR5 antagonistic activity and can be advantageously used for the treatment or prevention of infectious disease of various HIV in human (e.g. AIDS).
    • 式(I)化合物(其中R 1为氢原子,可被取代的烃基,可被取代的非芳香族杂环基,R 2 O 2 >可以被取代的烃基,可以被取代的非芳族杂环基,或者R 1和R 2可以彼此结合形成A至 形成可以被取代的杂环基; A是N或N + - - - - - - - (R 5) SUP>为烃基; Y为 - 抗衡阴离子); R 3为可被取代的环状烃基或可被取代的杂环基; n 为0或1; R 4为氢原子,可被取代的烃基,可被取代的杂环基,可被取代的烷氧基,可被取代的芳氧基 ,或可以被取代的氨基,E是可以是二价脂族烃基 被除氧基以外的基团取代; G 1是一个键,CO或SO 2; G 2是CO,SO 2,NHCO,CONH或OCO; J为次甲基或氮原子; 并且Q和R中的每一个是可被取代的键或二价C 1-3烷基脂族烃; 条件是当G 2 O是OCO时J为次甲基,当另一个为键并且Q和R各自不被氧代基取代时,Q和R中的一个不为键, 当G 1是一个键时)或其盐具有强的CCR5拮抗活性,并且可以有利地用于治疗或预防人类各种HIV感染性疾病(如艾滋病)。