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1.发明授权
公开(公告)号：US5204352A
公开(公告)日：1993-04-20
申请号：US102445
申请日：1987-09-29
申请人： Richard J. Sundberg , Daniel J. Dahlhausen , Govindarajan Manikumar , Babu J. Mavunkel , Hikmat A. Musallam , Atanu Biswas , Srinivasan Varadarajan
发明人： Richard J. Sundberg , Daniel J. Dahlhausen , Govindarajan Manikumar , Babu J. Mavunkel , Hikmat A. Musallam , Atanu Biswas , Srinivasan Varadarajan
IPC分类号： C07D213/53 , C07D233/54 , C07D471/04 , C07D513/04
CPC分类号： C07D213/53 , C07D233/64 , C07D471/04 , C07D513/04
摘要： Novel compounds are provided which exhibit high levels of anti-parasitic activity, specifically against parasites of the genus Trypanosoma. The compounds are comprised of aryl-substituted quaternary heteroaromatic salts which include a positively charged imidazolium or other heterocyclic ring, a linking group, a phenyl ring, and a polar functional group. The polar functional group is preferably a quanylhydrazone or a heterocyclic hydrazone. A method is also provided for treating the diseases associated with Trypanosoma parasites which comprises administering to infected animals or humans an effective amount of a compound of the present invention.
摘要翻译： 提供新的化合物，其具有高水平的抗寄生虫活性，特别是针对锥虫属的寄生虫。 该化合物包括芳基取代的季芳香盐，其包括带正电荷的咪唑鎓或其它杂环，连接基，苯环和极性官能团。 极性官能团优选为anyl腙或杂环腙。 还提供了一种治疗与锥虫属寄生虫相关的疾病的方法，其包括向受感染的动物或人施用有效量的本发明化合物。
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公开(公告)号：US5130438A
公开(公告)日：1992-07-14
申请号：US825711
申请日：1985-11-20
IPC分类号： C07D213/50 , C07D213/53 , C07D213/81
CPC分类号： C07D213/53 , C07D213/50 , C07D213/81
摘要： An illustrative embodiment of the invention substitutes solid, non-carcinogenic bis(methanesulfonoxymethyl) ether for bis-chloromethyl ether in a low temperature reaction of about 0.degree.-5.degree. C. for the production of bis-methylene ether pyridinium quaternary compounds. In this way, the production of important nerve agent antidotes (toxogonin, HI-6 and HGG-12) by a method of synthesis using the reactant bis-mesylmethyl ether, is carried out in appreciably greater safety.
摘要翻译： 本发明的说明性实施方案在约0-5℃的低温反应中将固体，非致癌双（甲磺酰氧甲基）醚替代双氯甲基醚用于生产双 - 亚甲基醚吡啶鎓季铵化合物。 以这种方式，通过使用反应物双甲基甲基醚的合成方法生产重要的神经毒素解毒剂（毒素，HI-6和HGG-12）以显着更大的安全性进行。
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公开(公告)号：US4978782A
公开(公告)日：1990-12-18
申请号：US402755
申请日：1989-09-05
IPC分类号： C07C323/64
CPC分类号： C07C323/64
摘要： A novel symmetrical organic disulfide sulfonate compound is disclosed as useful as an anti-radiation agent. The compound is disodium (1,4-butylenedithio)bis(4-butanesulfinate).
摘要翻译： 公开了一种新颖的对称有机二硫化磺酸盐化合物作为抗辐射剂。 该化合物是二（1,4-丁二硫代）双（4-丁磺酰亚胺）二钠。
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4.发明授权
公开(公告)号：US4943657A
公开(公告)日：1990-07-24
申请号：US365891
申请日：1989-06-14
IPC分类号： C07C323/64
CPC分类号： C07C323/64
摘要： Unsymmetrical organic disulfide sulfinate compounds, useful as an antiradiation agents, having the general formula: ##STR1## wherein A is one or of the following polar groups, OH, COOH, SO.sub.3 Na, --C(O)--, or derivatives such as esters and nonamino nitrogen derivatives such as amides or nitriles; k is an integer of one to eight; Y is a straight or substituted aliphatic chain having from two to eight carbon atoms which may have one or more S--S groups interposed therebetween; m signifies the number of carbon atoms in an aliphatic chain Y containing 2 to 8 carbon atoms which may have S--S interposed; aliphatic chain Y, substituted with one or more polar groups of the number k is attached to one of the two sulfur atoms shown. The second sulfur atom is attached through an aliphatic chain of 2 to 5 carbon atoms to the sulfinate function SO.sub.2 M wherein R.sup.1 and R.sup.2 may be hydrogen, aryl, cycloalkyl or various polar groups such as OH, COOH, SO.sub.3 Na, --C(O)--, or derivatives such as esters and nonamino derivatives such as amides or nitriles. The system ##STR2## also may comprise an aromatic ring; n may be the integers 2 through 6; M of the sulfinate function is hydrogen, a metallic element selected from group 1 A of the Periodic Table such as Li, Na, or K, or the equivalent R.sub.4 N+; or an organic group such as a straight or substituted aliphatic chain having up to 4 carbon atoms, designed to promote stability. The synthesis of the compounds occurs by subjecting 1,1-dioxides of cyclic disulfides to the action of a thiolate ion, whereby cleavage is effected between the sulfur and sulfonyl units.
摘要翻译： 可用作抗辐射剂的非对称有机二硫化物亚磺酸盐化合物，具有以下通式：其中A是一个或以下极性基团，OH，COOH，SO 3 Na，-C（O） - 或衍生物，例如酯和 非氨基氮衍生物如酰胺或腈; k是1到8的整数; Y是具有2至8个碳原子的直链或取代的脂肪族链，它们之间可以具有一个或多个S-S基团; m表示可插入S-S的含有2〜8个碳原子的脂族链Y中的碳原子数; 由数个k的一个或多个极性基团取代的脂族链Y连接到所示的两个硫原子中的一个上。 第二硫原子通过2至5个碳原子的脂族链连接到亚磺酸盐官能团SO 2 M上，其中R 1和R 2可以是氢，芳基，环烷基或各种极性基团，例如OH，COOH，SO 3 N a，-C（O） - ，或衍生物如酯和非氨基衍生物如酰胺或腈。 系统
还可以包括芳环; n可以是整数2到6; 亚硫酸盐官能团的M为氢，选自元素周期表的一种元素的金属元素如Li，Na或K，或当量的R4N +; 或有机基团，例如具有至多4个碳原子的直链或取代的脂族链，旨在促进稳定性。 化合物的合成通过使环状二硫化物的1,1-二氧化物发生硫醇盐离子的作用而发生，从而在硫磺和磺酰基单元之间进行切割。 -
5.发明授权
公开(公告)号：US4883890A
公开(公告)日：1989-11-28
申请号：US228010
申请日：1988-08-03
IPC分类号： C07C323/64
CPC分类号： C07C323/64
摘要： Unsymmetrical organic disulfide sulfinate compounds, useful as an antiradiation agents, having the general formula: ##STR1## wherein A is one or of the following polar groups, OH, COOH, SO.sub.3 Na, --C(O)--, or derivatives such as esters and nonamino nitrogen derivatives such as amides or nitriles; k is an integer of one to eight; Y is a straight or substituted aliphatic chain having from two to eight carbon atoms which may have one or more S--S groups interposed therebetween; m signifies the number of carbon atoms in an aliphatic chain Y containing 2 to 8 carbon atoms which may have S--S interposed; aliphatic chain Y, substituted with one or more polar groups of the number k is attached to one of the two sulfur atoms shown. The second sulfur atom is attached through an aliphatic chain of 2 to 5 carbon atoms to the sulfinate function SO.sub.2 M wherein R.sup.1 and R.sup.2 may be hydrogen, aryl, cycloalkyl or various polar groups such as OH, COOH, SO.sub.3 Na, --C(O)--, or derivatives such as esters and nonamino derivatives such as amides or nitriles. The system ##STR2## also may comprise an aromatic ring; n may be the integers 2 through 6; M of the sulfinate function is hydrogen, a metallic element selected from group 1 A of the Periodic Table such as Li, Na, or K, or the equivalent R.sub.4 N+; or an organic group such as a straight or substituted aliphatic chain having up to 4 carbon atoms, designed to promote stability. The synthesis of the compounds occurs by subjecting 1,1-dioxides of cyclic disulfides to the action of a thiolate ion, whereby cleavage is effected between the sulfur and sulfonyl units.
摘要翻译： 可用作抗辐射剂的非对称有机二硫化物亚磺酸盐化合物，具有以下通式：其中A是一个或以下极性基团，OH，COOH，SO 3 Na，-C（O） - 或衍生物，例如酯和 非氨基氮衍生物如酰胺或腈; k是1到8的整数; Y是具有2至8个碳原子的直链或取代的脂肪族链，它们之间可以具有一个或多个S-S基团; m表示可插入S-S的含有2〜8个碳原子的脂族链Y中的碳原子数; 由数个k的一个或多个极性基团取代的脂族链Y连接到所示的两个硫原子中的一个上。 第二硫原子通过2至5个碳原子的脂族链连接到亚磺酸盐官能团SO 2 M上，其中R 1和R 2可以是氢，芳基，环烷基或各种极性基团，例如OH，COOH，SO 3 N a，-C（O） - ，或衍生物如酯和非氨基衍生物如酰胺或腈。 系统
还可以包括芳环; n可以是整数2到6; 亚硫酸盐官能团的M为氢，选自元素周期表的一种元素的金属元素如Li，Na或K，或当量的R4N +; 或有机基团，例如具有至多4个碳原子的直链或取代的脂族链，旨在促进稳定性。 化合物的合成通过使环状二硫化物的1,1-二氧化物发生硫醇盐离子的作用而发生，从而在硫磺和磺酰基单元之间进行切割。
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