3,5-二羟基戊酸的类似物用于成骨作用

專利類型

發明

專利國別 (專利申請國家)

大陸

專利申請案號

201610051593.3

專利證號

4615153

專利獲證名稱

3,5-二羟基戊酸的类似物用于成骨作用

專利所屬機關 (申請機關)

高雄醫學大學

獲證日期

2021/08/13

技術說明

由於骨折和骨質疏鬆影響社會經濟成本之付出甚鉅，加上現今臨床使用的促骨生成藥物之選擇不如抑骨吸收劑來得多，且多屬賀爾蒙產品，然而其副作用的產生需格外留意，因此開發具臨床使用潛力之促骨生成藥物有其重要性。他汀類化合物具有高度肝細胞選擇性，為臨床降血脂用藥。雖被揭露具有造骨能力，但不具有骨組織選擇性，導致人體實驗中所呈現的骨密度增加能力並不一致。本項發明以HMG 基團（3,5-Dihydroxypentanoate）為主架構，利用非寡肽分子或具骨親和寡肽修飾3,5-Dihydroxypentanoate，開發在骨頭組織具選擇性的衍生物。本發明的產物對HMG-CoA還原酶呈現低抑制，具有效地提升細胞礦化與促骨頭生長的能力，提升骨密度，克服他汀類藥物在生物體上無法達成的促骨頭生成活性。 The treatment of bone disease meaningfully affects social economy. In addition, bone formation agents are more frequently chosen than bone resorption agents. Among bone formation agents, hormones are key therapeutics but cause side effects. Hence, it is important and necessary to develop drugs for bone formation. Statins are known as hepatocyte selective lipid lowering agents in clinical. Their bone formation ability have been reported, however, they are not specific distribution to bone. It may be the reason to answer the bone formation of statins is controversial in human. This invention explores the derivatives of 3,5-Dihydroxypentanoate, which were modified by non-peptide molecules or bone affinity peptides. The products exist lower inhibition of HMG-CoA reductase, significantly increase the abilities of cell mineralization and bone formation to enhance bone density, and improve the anabolic effects of statins in biological system.

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智財保護與科技管理組

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07-3138030

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