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    • 5. 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)。
    • 9. 发明授权
    • Cyclic amine compounds as CCR5 antagonists
    • 环胺化合物作为CCR5拮抗剂
    • US06562978B1
    • 2003-05-13
    • US10089374
    • 2002-03-29
    • Shinichi ImamuraShohei HashiguchiTaeko HattoriOsamu NishimuraNaoyuki KanzakiMasanori BabaYoshihiro Sugihara
    • Shinichi ImamuraShohei HashiguchiTaeko HattoriOsamu NishimuraNaoyuki KanzakiMasanori BabaYoshihiro Sugihara
    • C07D21128
    • 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)的化合物(其中R 1为氢原子,可被取代的烃基,可被取代的非芳族杂环基,R 2为可被取代的烃基,非芳香族杂环基 或者R 1和R 2可以与A相互结合形成可被取代的杂环基; A是N或-N + -R 5 .Y-(R 5是烃基; Y-是抗衡阴离子 ); R3是可以被取代的环状烃基或可以被取代的杂环基; n是0或1; R4是氢原子,可以被取代的烃基,可以被取代的杂环基, 可被取代的烷氧基,可被取代的芳氧基或可被取代的氨基,E是可被除氧以外的基团取代的二价脂族烃基; G 1是键,CO 或SO 2; G2是CO,SO 2,NHCO,CONH或OCO; J是次甲基或硝基 原子 Q和R分别为可以被取代的键或二价C 1-3脂族烃; 条件是当G2是OCO时J是次甲基,当另一个是键时Q和R中的一个不是键,并且当G 1是键时,Q和R各自不被氧代基取代)或 其盐具有有效的CCR5拮抗活性,可有利地用于治疗或预防人类各种HIV感染性疾病(如艾滋病)。
    • 10. 发明授权
    • Fused heterocycle derivatives and use thereof
    • 稠合杂环衍生物及其用途
    • US08304557B2
    • 2012-11-06
    • US12133063
    • 2008-06-04
    • Yuya OguroShinichi Imamura
    • Yuya OguroShinichi Imamura
    • C07D277/62A61K31/428
    • C07D471/04C07D417/12C07D471/14C07D513/04
    • A compound represented by the formula (I): wherein Z1, Z2, Z3 and Z4 are the following combination, (Z1,Z2,Z3,Z4)=(CR4,N,CR5,C), (N,N,CR5,C), (N,C,CR5,N), (S,C,CR5,C) or (S,C,N,C); R1 and R2 are the same or different and each is (1) a hydrogen atom, (2) a halogen atom, (3) a group bonded via a carbon atom, (4) a group bonded via a nitrogen atom, (5) a group bonded via an oxygen atom or (6) a group bonded via a sulfur atom; R3 is an amino optionally having substituent(s); R4 and R5 are the same or different and each is (1) a hydrogen atom, (2) a halogen atom, (3) a group bonded via a carbon atom, (4) a group bonded via a nitrogen atom, (5) a group bonded via an oxygen atom or (6) a group bonded via a sulfur atom; R3 and R4 optionally form a ring optionally having substituent(s); and a group represented by the formula is a cyclic group optionally having substituent(s), or a salt thereof.
    • 由式(I)表示的化合物:其中Z 1,Z 2,Z 3和Z 4是以下组合:(Z 1,Z 2,Z 3,Z 4)=(CR 4,N,CR 5,C),(N,N, C),(N,C,CR5,N),(S,C,CR5,C)或(S,C,N,C) R1和R2相同或不同,分别为(1)氢原子,(2)卤素原子,(3)通过碳原子键合的基团,(4)通过氮原子键合的基团,(5) 通过氧原子键合的基团或(6)通过硫原子键合的基团; R3是任选具有取代基的氨基; R4和R5相同或不同,分别为(1)氢原子,(2)卤素原子,(3)通过碳原子键合的基团,(4)通过氮原子键合的基团,(5) 通过氧原子键合的基团或(6)通过硫原子键合的基团; R3和R4任选地形成任选具有取代基的环; 并且由下式表示的基团是任选具有取代基的环状基团或其盐。