螺环吲哚类和螺环茚满类化合物作为趋化因子 C-C 型受体 2 的拮抗剂：WO 2009023754.
Spiroindenes and spiroindanes as antagonists of CC chemokine receptor 2: WO 2009023754.
机构信息
Bristol-Myers Squibb Company, Research & Development, Rt. 206 & Province Line Road, Princeton, NJ 08543, USA.
出版信息
Expert Opin Ther Pat. 2010 Feb;20(2):283-9. doi: 10.1517/13543770903490437.
BACKGROUND
CC chemokine receptor 2 (CCR2) is a GPCR involved in the migration and activation of inflammatory monocytes. A number of studies have highlighted a role for CCR2 in preclinical animal models of atherosclerosis, restenosis, multiple sclerosis, rheumatoid arthritis and insulin resistance. Accordingly, pharmaceutical scientists have been investigating the antagonism of CCR2 as a potential therapy.
OBJECTIVE
This patent evaluation examines the report of a new chemical subseries of CCR2 antagonists.
METHODS
The compounds of the title invention are compared to the related earlier work in the area of CCR2 antagonism.
CONCLUSIONS
The compounds disclosed in PCT application WO 2009023754 extend previous work in a dipiperidine series of CCR2 antagonists through the introduction of both a 1,2-disubstituted ethanol spacer and a 1'H-spiro[indene-1,4'-piperin]-1'-yl group. These compounds may represent a means of treating diseases driven by CCR2-bearing leukocytes.
背景
CC 趋化因子受体 2（CCR2）是一种 G 蛋白偶联受体，参与炎症性单核细胞的迁移和激活。许多研究强调了 CCR2 在动脉粥样硬化、再狭窄、多发性硬化症、类风湿关节炎和胰岛素抵抗的临床前动物模型中的作用。因此，制药科学家一直在研究 CCR2 的拮抗作用作为一种潜在的治疗方法。
目的
本专利评估检查了一种新型 CCR2 拮抗剂的化学亚系列报告。
方法
将本发明的化合物与 CCR2 拮抗领域的相关早期工作进行比较。
结论
PCT 申请 WO 2009023754 中披露的化合物通过引入 1,2-二取代乙醇间隔基和 1'H-螺[茚并-1,4'-哌啶]-1'-基，扩展了之前在 CC 趋化因子受体 2 拮抗剂二哌啶系列中的工作。这些化合物可能代表了治疗由 CCR2 阳性白细胞驱动的疾病的一种手段。
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