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    • 6. 发明授权
    • Phenylene, furyl, and thienyl leukotriene B.sub.4 analogues
    • 亚苯基,呋喃基和噻吩基白三烯B4类似物
    • US4791133A
    • 1988-12-13
    • US67526
    • 1987-06-26
    • Stevan W. DjuricRichard A. HaackJulie M. Miyashiro
    • Stevan W. DjuricRichard A. HaackJulie M. Miyashiro
    • C07C59/48C07D307/54C07D309/30C07D333/24A61K31/38A61K31/34C07C69/76C07C103/26C07D211/08C07D333/22C07D409/00
    • C07D309/30C07C59/48C07D307/54C07D333/24
    • This invention relates to leukotriene B.sub.4 antagonists having the structure ##STR1## and the pharmaceutically acceptable addition salts thereof; wherein R.sup.1 is lower alkyl having 1-10 carbon atoms; or lower alkenyl or alkynyl having 2-10 carbon atoms; or lower alkadienyl having 3-10 carbon atoms; or lower alkadiynyl or alkenynyl having 4-10 carbon atoms;wherein R.sup.2 and R.sup.3 are the same or different and represent hydrogen or lower alkyl having 1-6 carbon atoms;wherein X is CH.dbd.CH, S, or O;wherein Y is CH.dbd.CH or C.tbd.C;wherein Z is OR.sup.4 or NR.sup.5 R.sup.6, and wherein R.sup.4 represent H, lower alkyl having 1-6 carbon atoms, or a pharmaceutically acceptable cation, and wherein R.sup.5 and R.sup.6 act independently and represent H or lower alkyl having 1-6 carbon atoms, or R.sup.5 and R.sup.6 may act together with N to form a cycloamine of the formula: ##STR2## wherein q is an integer from 2-5; wherein m and n are the same or different and either 1 or 0; andwherein p is an integer from 1 to 5.
    • 本发明涉及具有以下结构的白细胞三烯B4拮抗剂及其药学上可接受的加成盐; 其中R1是具有1-10个碳原子的低级烷基; 或具有2-10个碳原子的低级烯基或炔基; 或具有3-10个碳原子的低级链二烯基; 或具有4-10个碳原子的低级炔二炔基或烯炔基; 其中R2和R3相同或不同并且表示氢或具有1-6个碳原子的低级烷基; 其中X为CH = CH,S或O; 其中Y为CH = CH或C 3BOND C; 其中Z是OR 4或NR 5 R 6,并且其中R 4表示H,具有1-6个碳原子的低级烷基或药学上可接受的阳离子,并且其中R5和R6独立地表示H代表具有1-6个碳原子的低级烷基或R5 并且R6可以与N一起起作用以形成下式的环胺:其中q是2-5的整数; 其中m和n相同或不同,为1或0; 并且其中p为1至5的整数。