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    Substituted isoquinolines as ultra short acting neuromuscular blockers
    1.
    发明授权
    Substituted isoquinolines as ultra short acting neuromuscular blockers 失效
    取代的异喹啉作为超短效神经肌肉阻滞剂

    公开(公告)号：US06177445B1

    公开(公告)日：2001-01-23

    申请号：US09381721

    申请日：1999-12-22

    申请人： Eric Cleveland Bigham ,  Grady Evan Boswell ,  John Joseph Savarese ,  Roy Archibald Swaringen, Jr. ,  Sanjay Shashikant Patel ,  Eric Eugene Boros ,  Robert Anthony Mook, Jr. ,  Vincente Samano

    发明人： Eric Cleveland Bigham ,  Grady Evan Boswell ,  John Joseph Savarese ,  Roy Archibald Swaringen, Jr. ,  Sanjay Shashikant Patel ,  Eric Eugene Boros ,  Robert Anthony Mook, Jr. ,  Vincente Samano

    IPC分类号： A61K3147

    CPC分类号： C07D217/16 ,  C07D217/20

    摘要： Ultra short acting neuromuscular blocking agents of Formula (I) which are useful as skeletal muscle relaxants during emergency intubation procedures, routine surgery and post-operative settings are disclosed, wherein q and t are independently from 0 to 4; X1 and X2 are independently halogen; ha and hb are independenity from 0 to 2; Z1 and Z2 are indepentdently hydrogen, C1-6 alkyl, C2-6 alkenyl or C2-6 alkynyl with the proviso that Z1 and Z2 are not both hydrogen; Y1, Y2, and Y3 and Y4 are independently hydrogen, halogen or C1-3 alkoxy; m and p are independently 1 to 6; n and r are independently 0 to 4; with the proviso the if ha and hb are both 0, then r is 0 and n is 0 to 2; R1 to R14 are independently hydrogen, halogen, C1-3 alkoxy, or R2 and R3 together with the carbon atoms to which they are bonded, R5 and R6 together with the carbon atoms to which they are bonded, R9 and R10 together with the carbon atoms to which they are bonded, R12 and R13 together with the carbon atoms to which they are bonded, may independently form a methylenedioxy or ethylenedioxy moiety contained in five- or six-membered ring; W1 and W2 are carbon; and A is a pharmaceutically acceptable anion.

    摘要翻译： 公开了在紧急插管程序，常规手术和术后设置中可用作骨骼肌松弛剂的式（I）的超短效神经肌肉阻滞剂，其中q和t独立地为0至4; X1和X2独立地为卤素; ha和hb是从0到2的独立性; Z1和Z2独立地为氢，C1-6烷基，C2-6烯基或C2-6炔基，条件是Z1和Z2不同时为氢; Y1，Y2和Y3和Y4独立地是氢，卤素或C1-3烷氧基; m和p独立地为1至6; n和r分别为0〜4; 条件是如果ha和hb均为0，则r为0且n为0至2; R 1至R 14独立地为氢，卤素，C 1-3烷氧基或R 2和R 3与它们所键合的碳原子一起，R 5和R 6与它们所键合的碳原子一起，R 9和R 10与碳 R12和R13与它们所键合的碳原子一起可以独立地形成五元或六元环中所含的亚甲二氧基或亚乙二氧基部分; W1和W2是碳; A是药学上可接受的阴离子。