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    • 9. 发明申请
    • ERGOLINE DERIVATIVES AND THEIR USE AS CHEMOKINE RECEPTOR LIGANDS
    • ERGOLINE衍生物及其作为化合物受体配体使用
    • WO2006128658A1
    • 2006-12-07
    • PCT/EP2006/005106
    • 2006-05-29
    • NOVARTIS AGNOVARTIS PHARMA GMBHBAENTELI, RolfGLICKMAN, FraserKOVARIK, JiriLEWIS, IanSTREIFF, MarkusTHOMA, GebhardZERWES, Hans-Günter
    • BAENTELI, RolfGLICKMAN, FraserKOVARIK, JiriLEWIS, IanSTREIFF, MarkusTHOMA, GebhardZERWES, Hans-Günter
    • C07D457/06C07D457/08A61K31/48
    • C07D457/06C07D457/08
    • Disclosed are ergoline derivatives, Formula (I), wherein either each of R 1 and R 2 , independently, is H; optionally R 10 and/or R 11 -substituted-phenyl or - phenyl-C 1-4 alkyl; optionally R 10 and/or R 11 -substituted-heteroaryl or -heteroaryl-C 1-4 alkyl; optionally R 10 and/or R 11 -substituted heteroaryl N-oxide; optionally R 10 -substituted C 1 -C 8 alkyl; optionally R 10 -substituted C 2 -C 8 alkenyl, optionally R 10 -substituted C 2 -C 8 alkynyl; optionally R 10 -substituted C 3 -C 8 cycloalkyl, or optionally R 10 -substituted C 4 -C 8 cycloalkenyl; or R 1 and R 2 form together with the nitrogen atom to which they are attached an optionally R 10 -substituted 3-8 membered ring containing in addition to the nitrogen atom up to 2 heteroatoms selected independently from N, O and S; R 3 is H; OR 1 ; CH 2 R 1 R 2 ; (CH 2 ) 1-2 NR 1 R 2 ; CH 2 -CH 2 -OR 1 ; CH 2 -CO-NR 1 R 2 ; or CO-CH 2 R 1 R 2 ; R 4 is F; CI; Br; I; OR 1 ; NR 1 R 2 or has one of the significances given for R 1 ; and R 5 has one of the significances given for R 1 , 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中的每一个独立地是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链烯基,任选地R 10取代的C 2 C 8 -C 15炔基; 任选的R 10取代的C 3 -C 8环烷基,或任选地R 10取代的C 1 -C 10 - 4 -C 8环烯基; 或R 1和R 2 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,其含有 除了氮原子多达2个独立于N,O和S选择的杂原子; R 3是H; OR 1 ; CH 2 - [R 1 - [R 2 ; (CH 2 1-2 NR 1 - [R 2 ; CH 2 -CH 2 -OR 1 ; CH 2 -CO-NR 1 - [R 2 ; 或CO-CH 2 R 1 R 2 R 2; R 4是F; CI; BR; 一世; OR 1 ; NR 1 R 2 R 2或具有对R 1 1给出的含义之一; 和R 5具有游离形式或盐形式的R 1 1给出的意义之一,用于预防或治疗由趋化因子受体及其配体之间的相互作用介导的疾病或疾病 。