Korea Research Institute of Chemical Technology, Pharmacology Research Center, Division of Drug Discovery Research, Laboratory of Translational Therapeutics , P.O.Box 107, Yuseong-gu, Daejeon 305-600 , Republic of Korea +82 42 860 7687 ;
Expert Opin Ther Pat. 2013 Dec;23(12):1591-610. doi: 10.1517/13543776.2013.842556. Epub 2013 Oct 4.
Mononuclear macrophage/monocyte-lineage hematopoietic precursors differentiate into multinucleated osteoclasts. Abnormally increased numbers and/or overactivation of osteoclasts can lead to bone loss. Therefore, pharmaceutical inhibition of osteoclast differentiation is one therapeutic strategy for mitigating the occurrence of bone loss-associated disorders and related fractures.
This review surveys the patents and patent applications from 2008 to 2012 that are related to inventions of therapeutics and/or methods for inhibiting osteoclast differentiation.
Over the past 20 years, the identification and validation of signaling molecules involved in osteoclast differentiation has led to a better understanding of the molecular mechanism, and to the development of new therapeutic agents for treating bone loss-associated disorders. Since 2008, 34 WO patents or patent applications have been filed that relate to inventions of therapeutics and/or methods for chemical-based, natural product-based, or biological-based inhibitors of osteoclast differentiation. Here, analysis of these patents and patent applications is presented, and summarize the disclosed osteoclast differentiation-inhibiting target molecules. This report can support further advances in the development of anti-osteoclastogenic therapeutics for bone loss-associated disorders, including osteoporosis, rheumatoid arthritis, Paget's disease, periodontal disease, osteosarcoma, and cancer bone metastasis.
单核巨噬细胞/单核细胞系造血前体细胞分化为多核破骨细胞。破骨细胞数量异常增加和/或过度激活可导致骨丢失。因此，抑制破骨细胞分化的药物治疗是减轻与骨丢失相关疾病和相关骨折发生的一种治疗策略。
本文综述了 2008 年至 2012 年与破骨细胞分化抑制治疗和/或方法相关的专利和专利申请。
在过去的 20 年中，对参与破骨细胞分化的信号分子的鉴定和验证，使人们对分子机制有了更好的理解，并开发了治疗与骨丢失相关疾病的新治疗剂。自 2008 年以来，已提交了 34 项 WO 专利或专利申请，涉及基于化学、天然产物或生物的破骨细胞分化抑制剂的治疗和/或方法的发明。在此，对这些专利和专利申请进行了分析，并总结了所披露的破骨细胞分化抑制靶分子。本报告可以支持进一步开发用于治疗与骨丢失相关疾病的抗破骨细胞生成治疗剂，包括骨质疏松症、类风湿关节炎、佩吉特病、牙周病、骨肉瘤和癌症骨转移。
