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How Many 'New' entities Can Be Created from One Active Substance? The Case of Cyclosporin A

机译:一个活性物质可以创建多少个“新”实体?环孢菌素A的情况

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摘要

The existence of various crystalline forms of active substances, which can potentially differ in their pharmacokinetic profile, bioavailability or stability, creates the possibility of extending the patent protection of "old" substances utilizing the structures of new crystalline forms. Using cyclosporin A as an example, this report points to the fact that even with relatively small molecules, having about 60 non-hydrogen atoms, the number of "new" entities that can be generated can be at times nearly infinite.
机译:活性物质的各种晶形的存在,可能在其药代动力学特征,生物利用度或稳定性方面可能存在差异,从而有可能利用新晶形的结构扩展对“旧”物质的专利保护。以环孢菌素A为例,该报告指出了这样一个事实,即使对于具有约60个非氢原子的相对较小的分子,可以产生的“新”实体的数量有时也可以接近无限。

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