Symm. phenyltris(sulfonylimino)tri-benzene sulfonic acids and salts, a method of inhibiting the complement system in a body fluid with such a compound, a method for the preparation of such compounds and a pharmaceutical composition comprising such a compound
申请人:AMERICAN CYANAMID COMPANY
公开号:EP0013079A1
公开(公告)日:1980-07-09
There are provided s-phenyltris (sulfonylimino) tri- benzene mono- and di-sulfonic acids and their salts which are useful as complement inhibitors. The novel compounds have the general formula:
wherein each R is selected from the group consisting of hydrogen and alkali metal; each R1, R2 and R3 is selected from the group consisting of hydrogen and SO3A, wherein A is selected from the group consisting of hydrogen and a pharmaceutically acceptable salt cation; provided that at least one of the R1, R2 and R3 groups on each phenyl is SO3A; and further provided that when R2 is SO3A. R1 and R, may not be SO3A. E.g., these compounds may be prepared according to the following flowchart:
wherein R' stands for
These compounds find utility as complement inhibitors in body fluids and as such may be used to ameliorate or prevent those pathological reactions requiring the function of complement and in the therapeutic treatment of warm-blooded animals having immunologic diseases.
本发明提供了可用作补体抑制剂的 s-苯基三(磺酰亚胺)三苯单磺酸和二磺酸及其盐。这些新型化合物具有通式:
其中每个 R 选自氢和碱金属组成的组;每个 R1、R2 和 R3 选自氢和 SO3A 组成的组,其中 A 选自氢和药学上可接受的阳离子盐组成的组;条件是每个苯基上的 R1、R2 和 R3 基团中至少有一个是 SO3A;进一步条件是当 R2 是 SO3A 时。R1和R可以不是SO3A。例如,这些化合物可按以下流程图制备:
其中 R' 代表
这些化合物可用作体液中的补体抑制剂,因此可用于改善或预防需要补体功能的病理反 应,以及对患有免疫疾病的温血动物进行治疗。