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    • 9. 发明申请
    • Ergoline Derivatives
    • 二元醇衍生物
    • US20090018127A1
    • 2009-01-15
    • US11914570
    • 2006-05-29
    • Rolf BaenteliFraser GlickmanJiri KovarikIan LewisMarkus StreiffGebhard ThomaHans-Gunter Zerwes
    • Rolf BaenteliFraser GlickmanJiri KovarikIan LewisMarkus StreiffGebhard ThomaHans-Gunter Zerwes
    • A61K31/48C07D457/04A61K31/496A61K31/5377
    • C07D457/06C07D457/08
    • Disclosed are ergoline derivatives, Formula (I), wherein either each of R1 and R2, independently, is H; optionally R10 and/or R11-substituted-phenyl or -phenyl-C1-4alkyl; optionally R10 and/or R11-substituted-heteroaryl or -heteroaryl-C1-4alkyl; optionally R10 and/or R11-substituted heteroaryl N-oxide; optionally R10-substituted C1-C8 alkyl; optionally R10-substituted C2-C8 alkenyl, optionally R10-substituted C2-C8 alkynyl; optionally R10-substituted C3-C8 cycloalkyl, or optionally R10-substituted C4-C8 cycloalkenyl; or R1 and R2 form together with the nitrogen atom to which they are attached an optionally R10-substituted 3-8 membered ring containing in addition to the nitrogen atom up to 2 heteroatoms selected independently from N, O and S; R3 is H; OR1; CH2R1R2; (CH2)1-2NR1R2; CH2—CH2—OR1; CH2—CO—NR1R2; or CO—CH2R1R2; R4 is F; Cl; Br; I; OR1; NR1R2 or has one of the significances given for R1; and R5 has one of the significances given for R1, in free form or in salt form for preventing or treating disorders or diseases mediated by interactions between chemokine receptors and their ligands.
    • 公开了麦角灵衍生物,式(I),其中R 1和R 2各自独立地为H; 任选的R 10和/或R 11取代的苯基或 - 苯基-C 1-4烷基; 任选的R 10和/或R 11取代的杂芳基或 - 杂芳基-C 1-4烷基; 任选的R 10和/或R 11取代的杂芳基N-氧化物; 任选的R 10取代的C 1 -C 8烷基; 任选的R 10取代的C 2 -C 8烯基,任选的R 10取代的C 2 -C 8炔基; 任选的R 10取代的C 3 -C 8环烷基,或任选的R 10取代的C 4 -C 8环烯基; 或R 1和R 2与它们所连接的氮原子一起形成任选的R 10取代的3-8元环,除了氮原子以外,还含有独立地选自N,O和S的2个杂原子; R3为H; OR1; CH2R1R2; (CH2)1-2NR1R2; CH2-CH2-OR1; CH2-CO-NR1R2; 或CO-CH 2 R 1 R 2; R4是F; Cl; Br; 一世; OR1; NR1R2或具有R1的意义之一; R5具有以游离形式或盐形式用于预防或治疗由趋化因子受体及其配体之间相互作用介导的疾病或疾病的R1的意义。