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发明授权
US5011959A 1,2-diaminocyclohexane-platinum complexes with antitumor activity 失效
具有抗肿瘤活性的1,2-二氨基环己烷 - 铂配合物

1,2-diaminocyclohexane-platinum complexes with antitumor activity
摘要：
The present invention comprises a water-soluble square-planar cis-platinum(II) four-coordinate complex having the formula:trans-R,R-DACH Pt(II) X.sub.2ortrans-R,R-DACH Pt(II) Ywherein X is a monovalvent cation, two of which are present, selected from the group consisting of cyclopropanecarboxylato, shikimato, saccharatolactone, galacturonato and N,N-dimethyglycinato; wherein Y is a divalent cation selected from the group consisting of citraconato, 1,1-cyclobutanedicarboxylato, 1,1-cyclopropanedicarboxylato, isocitratolactone and Z-iminodiacetato where Z is bound to the nitrogen and is ethyl, propyl, Isopropyl, n-butyl, sec-butyl, ter-butyl, n-amyl, isoamyl or OH.In one preferred aspect the water-soluble square-planar cis-platinum(II) four-coordinate complex has the formula:trans-R,R-DACH Pt(II) X.sub.2wherein X is a monovalent cation. Two X substituents are present in the platinum complex. These X substituents are preferably selected from the group consisting of cyclopropanecarboxylato, shikimato, saccharatolactone, galacturonato and N,N-dimethylglycinato. Both X substituents are usually identical butmay be different.
摘要（中）：

本发明包括具有下式的水溶性正方形顺式 - 铂（II）四配位络合物：反式-R，R-DACH Pt（II）X2或反式-R，R-DACH Pt（II）Y 其中X是单价阳离子，其中两个存在，选自环丙烷羧酸盐，莽草酸，蔗糖内酯，半乳糖醛酸和N，N-二甲基甘氨酸; 其中Y是选自柠康酸，1,1-环丁烷二羧酸，1,1-环丙烷二羧酸，异柠檬酸内酯和Z-亚氨基二乙酸的二价阳离子，其中Z与氮结合，是乙基，丙基，异丙基，正丁基， 仲丁基，叔丁基，正戊基，异戊基或OH。 在一个优选的方面，水溶性正方形顺式 - 铂（II）四配位络合物具有下式：反式-R，R-DACH Pt（II）X2，其中X是一价阳离子。 铂络合物中存在两个X取代基。 这些X取代基优选选自环丙烷羧酸，莽草酸，蔗糖内酯，半乳糖醛酸和N，N-二甲基甘氨酸。 两个X取代基通常是相同的，但可以是不同的。

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