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    • 2. 发明申请
    • PRODUCTS FOR THE DELIVERY OF THERAPEUTIC/DIAGNOSTIC COMPOUNDS TO THE HEART
    • 用于向心脏递送治疗/诊断化合物的产品
    • WO2016102576A1
    • 2016-06-30
    • PCT/EP2015/080991
    • 2015-12-22
    • CONSIGLIO NAZIONALE DELLE RICERCHEISTITUTO NAZIONALE ASSICURAZIONE CONTRO GLI INFORTUNI SUL LAVORO
    • CATALUCCI, DanieleMIRAGOLI, MicheleIAFISCO, MicheleTAMPIERI, Anna
    • A61K9/14A61K9/51
    • A61K9/5115A61K9/007A61K9/143A61K9/5192A61K31/7105A61K38/03A61K47/52A61K47/6929C12N15/113C12N2310/141C12N2320/32
    • The invention relates to a process for the preparation of a product comprising one or more nanoparticles of calcium phosphate (CaP-NP) with negative surface charge having a ζ-potential in the range from -41.0 mV to -27.0 mV comprising the steps of: a) maintaining a mixture having a pH in the range from 7 to 10 and comprising an aqueous solution of calcium, an aqueous solution of phosphate and a solution of citrate ions at a temperature in the range from 20 °C to 40 °C for a time in the range from 30 seconds to 10 minutes; b) removing non-reacted ions from the solution of step a), thus obtaining a suspension of one or more nanoparticles of calcium phosphate (CaP-NP); c) recovering the product of one or more nanoparticles of calcium phosphate (CaP-NP) from the suspension of step b). In an advantageous embodiment, the process of the invention provides, in the mixture of step a), also an aqueous solution of one or more therapeutic/diagnostic compounds. The product of the invention may be used as a vehicle for one or more diagnostic/therapeutic compounds for the treatment of cardiovascular diseases through inhalation administration.
    • 本发明涉及一种制备包含一种或多种具有负电荷的磷酸钙(CaP-NP)的纳米颗粒的产品的方法,所述磷酸钙(CaP-NP)具有-41.0mV至-27.0mV范围内的ζ电位,包括以下步骤: a)保持pH在7至10范围内的混合物,并在20℃至40℃的温度范围内包含钙水溶液,磷酸盐水溶液和柠檬酸根离子溶液,用于 时间范围从30秒到10分钟; b)从步骤a)的溶液中除去未反应的离子,从而获得一种或多种磷酸钙(CaP-NP)纳米颗粒的悬浮液; c)从步骤b)的悬浮液中回收一种或多种磷酸钙(CaP-NP)纳米颗粒的产物。 在有利的实施方案中,本发明的方法在步骤a)的混合物中还提供一种或多种治疗/诊断化合物的水溶液。 本发明的产品可以用作一种或多种用于通过吸入给药治疗心血管疾病的诊断/治疗化合物的载体。
    • 3. 发明申请
    • MIMETIC PEPTIDES AND THEIR USE IN MEDICINE
    • 甲基纤维素及其在医学中的应用
    • WO2015110589A1
    • 2015-07-30
    • PCT/EP2015/051376
    • 2015-01-23
    • CONSIGLIO NAZIONALE DELLE RICERCHE
    • CATALUCCI, DanieleCONDORELLI, Gianluigi
    • C07K14/705C07K7/04G01N33/50A61K38/00A61P27/02A61P25/16A61P9/00
    • C07K14/705A61K38/00G01N33/5008G01N33/6872G01N2333/705G06F19/70G06F19/709
    • The present invention concerns the field of ion channels, and in particular relates to peptides which are suitable for use in the treatment of conditions where the L-type calcium channel (LTCC) density and function is altered. LTCCs are located on the membrane of all excitable cells and control the small voltage gradient across the plasma membrane by allowing the flow of Ca 2+ ions down their electrochemical gradient. This Ca 2+ flux is critical for numerous processes including cardiac action potential propagation, muscle contraction, Ca 2+ -dependent gene expression, synaptic efficacy, and cell survival by contributing to various signaling cascades. Reduction of the inward calcium current (I Ca ) conducted through the LTCCs is seen in several diseases and medications to improve or restores impaired intracellular Ca 2+ homeostasis are limited. The present invention reports mimetic peptides (MPs) that through a novel mechanism directly targets LTCCs and, by modulation of LTCC density and function, increases I Ca . This invention supports a therapeutic role for MP to treat human diseases associated with altered cellular Ca 2+ homeostasis.
    • 本发明涉及离子通道领域,特别涉及适用于治疗L型钙通道(LTCC)密度和功能改变的病症的肽。 LTCC位于所有可兴奋细胞的膜上,并通过允许Ca 2+离子沿其电化学梯度流动来控制横跨质膜的小电压梯度。 这种Ca2 +通量对于许多过程是至关重要的,包括心脏动作电位传播,肌肉收缩,Ca2 +依赖性基因表达,突触功效和通过促成各种信号级联的细胞存活。 在几种疾病中观察到通过LTCC进行的向内钙电流(I Ca)的减少,以改善或恢复受损的细胞内Ca2 +体内平衡的药物是有限的。 本发明报道模拟肽(MP),其通过新型机制直接靶向LTCC,并且通过调节LTCC密度和功能来增加ICa。 本发明支持MP治疗与改变的细胞Ca2 +体内平衡相关的人类疾病的治疗作用。