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2. 发明公开

EP0008154A1 Ureylene phenylene anionic naphthalene-sulfonic acids, their use as complement system inhibitors in a body fluid and process for their preparation 失效
标题翻译：阴离子Ureylenphenylen萘酸，它们作为Komplementsystemhemmer体液和它们的制备方法使用。
公开(公告)号：EP0008154A1
公开(公告)日：1980-02-20
申请号：EP79301036.4
申请日：1979-06-01
申请人： AMERICAN CYANAMID COMPANY
发明人： Siuta, Gerald Joseph , Poletto, John Frank , Conrow, Ransom Brown , Bernstein, Seymour
IPC分类号： C07C143/675 , C07C143/80 , A61K31/18 , A61K31/185
CPC分类号： C07C309/59 , A61K31/185 , C07C309/47 , C07C311/46 , C07C311/47
摘要： The present invention provides novel ureylene phenylene anionic naphthalenesulfonic acids, which have complement-inhibiting properties and which may be represented by the general formula:
wherein X and Y are each selected from the group consisting of -CO- and -SO 2 -; R and R 3 are each selected from the group consisting of hydrogen, methyl and -S0 3 A, wherein A is a pharmaceutically acceptable salt cation; R, and R 4 are each selected from the group consisting of hydrogen and -COOB. wherein B is selected from the group consisting of hydrogen and a pharmaceutically acceptable salt cation; R 2 and R s are each selected from the group consisting of hydrogen and methyl; with the proviso that R. R,, R 2 , R 3 , R 4 and R 5 may not all be hydrogen; with the second proviso that when X and Y are both -CO- and R 2 is methyl, then R, R,, R 3 , R. and R s may not all be hydrogen; and with the third proviso that no phenyl moiety can contain both -SO 3 A and -COOB.
The corresponding amine compounds of the formula below are novel intermediates for the novelureylene compounds above:
摘要翻译：本发明提供了新颖的亚脲基苯基阴离子萘磺酸，具有补体抑制特性-并且其可以是由以下通式表示：各自选自-CO-和-SO 2 - 中选出worin X和Y; 被选自氢，甲基和-SO3A各自选择的R和R3，worin A是药学上可接受的盐的阳离子; R1和R4各自选自氢和-COOB的选择，worin B被选自氢和药学上可接受的盐的阳离子的选择; R1和R5各自选自氢和甲基中选择; 其条件没有R，R1，R2，R3，R4和R5可以不全部是氢; 与所述第二条件做了当X和Y均为-CO-且R 2为甲基时，则R，R1，R3，R4和R5可以不全部是氢; 和与第三条件确实没有苯基部分可以同时包含-SO3A和-COOB。下式的相应的胺化合物可用于上述novelureylene化合物的新的中间体：ð

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