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1. 发明申请

WO1987003281A1 PROPANE-1,3-DIOL DERIVATIVES, A METHOD FOR THEIR PRODUCTION AND A PHARMACEUTICAL COMPOSITION 审中-公开
标题翻译：丙-1,3-二醇衍生物，其生产方法和药物组合物
公开(公告)号：WO1987003281A1
公开(公告)日：1987-06-04
申请号：PCT/DK1986000128
申请日：1986-11-20
申请人： LEO PHARMACEUTICAL PRODUCTS LTD. A/S , GRUE-SORENSEN, Gunnar , NIELSEN, Christian, Kaergaard
发明人： LEO PHARMACEUTICAL PRODUCTS LTD. A/S
IPC分类号： C07C93/04
CPC分类号： C07D277/24 , C07C271/06 , C07C333/02
摘要： A derivative of 2-methylenepropane-1,3-diol of general formula (I), where O-A and O-A , which can be the same or different, each represents O, O-C(O), O-C(O)NH, O-C(S)NH or O-C(O)O, R represents an alkyl or alkenyl group of 10 - 22 carbon atoms, n is an integer from 1 to 11, B represents a quaternary ammonium group, either NR R R , or N(Het), where R , R and R are similar or different alkyl groups of 1 - 4 carbon atoms, or two or all of R , R and R may be incorporated into a cyclic or bicyclic structure, which may contain additional hetero atoms; X means the anion of a pharmaceutically acceptable inorganic or organic acid; and R and R are the same or different, and represent hydrogen or alkyl groups of 1 - 4 carbon atoms. The present compounds have been shown to possess a PAF antagonistic effect and an inhibitory effect on the growth of tumor cells, and are thus valuable in the human and veterinary practice as platelet aggregation inhibitors, anti-thrombotic agents, anti-asthmatic agents, anti-allergic agents, anti-inflammatory agents, anti-hypotensive agents, anti-ulcer agents, anti-psoriatic agents, anti-graft rejection agents, anti-conception agents and anti-tumor agents.
摘要翻译：通式（I）的2-亚甲基丙烷-1,3-二醇的衍生物，其中OA 1和OA 2可以相同或不同，各自表示O，OC（O），OC（O ）NH，OC（S）NH或OC（O）O，R 1表示10-22个碳原子的烷基或烯基，n是1至11的整数，B +表示季铵基 NR 4 R 5 R 6或N（Het），其中R 4，R 5和R 6是相同或不同的1-4个碳原子的烷基，或 R 4，R 5和R 6中的两个或全部可以并入环状或双环结构，其可以含有另外的杂原子; 是指药学上可接受的无机酸或有机酸的阴离子; R 2和R 3相同或不同，代表氢或1-4个碳原子的烷基。本发明化合物已被证明具有PAF拮抗作用和对肿瘤细胞生长的抑制作用，因此在人和兽医学实践中作为血小板聚集抑制剂，抗血栓形成剂，抗哮喘药，抗 - 过敏剂，抗炎剂，抗低血压剂，抗溃疡剂，抗牛皮癣剂，抗移植物排斥剂，抗受孕剂和抗肿瘤剂。

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