Inflammation and Immunology Medicinal Chemistry Pfizer, Cambridge, MA, USA.
Expert Opin Ther Pat. 2010 Dec;20(12):1703-22. doi: 10.1517/13543776.2010.534459. Epub 2010 Nov 14.
Discovery of small molecule inhibitors for treatment of rheumatoid arthritis is a major ongoing effort within the pharmaceutical industry. Spleen tyrosine kinase (SYK) is one of the leading small molecular targets with regard to clinical developments due to the efforts of Rigel and Portola.
Diaminopyrimidines are one of the most prominent structural elements incorporated into the design of kinase inhibitors. This review provides an extensive overview of the patent estates for the leading discovery programs at Portola and Rigel on diaminopyrimidines and how their patent estates are in relationship with the competition and prior art.
An overview of the patent landscape for diaminopyrimidines. In addition, the reader will be updated on what modifications in these scaffolds lead to very potent SYK inhibitors as judged by the applications. Finally, the authors will provide their best guess on what the structure is of Portola's recently announced clinical candidate.
The Rigel and the Portola research organizations have filed a series of patent applications on diaminopyrimidines as inhibitors of SYK. The scope of these applications is broad in a crowded chemical space. These applications contain very broad claims and the future will tell how much of the generic space claimed will be allowed in granted patents.
在制药行业，发现用于治疗类风湿性关节炎的小分子抑制剂是一项主要的持续努力。由于 Rigel 和 Portola 的努力，脾酪氨酸激酶 (SYK) 是临床开发方面主要的小分子靶标之一。
二氨基嘧啶类化合物是激酶抑制剂设计中最突出的结构单元之一。本篇综述广泛概述了 Portola 和 Rigel 在二氨基嘧啶类化合物方面的领先发现计划的专利情况，以及它们的专利与竞争和现有技术的关系。
二氨基嘧啶类化合物的专利格局概述。此外，读者将了解到这些支架中的哪些修饰可使 SYK 抑制剂具有很强的活性，这是通过应用程序来判断的。最后，作者将对 Portola 最近宣布的临床候选药物的结构做出最佳猜测。
Rigel 和 Portola 研究机构已就二氨基嘧啶类化合物作为 SYK 抑制剂提交了一系列专利申请。这些申请在拥挤的化学空间中具有广泛的范围。这些申请包含非常广泛的权利要求，未来将说明在授予的专利中允许主张多少通用空间。
