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    • 2. 发明申请
    • Controlled Release Formulations for the Delivery of HIF-1 Inhibitors
    • 用于输送HIF-1抑制剂的控制释放制剂
    • US20150141359A1
    • 2015-05-21
    • US14599853
    • 2015-01-19
    • The Johns Hopkins University
    • Justin Scot HanesPeter Anthony CampochiaroJie Fu
    • A61K47/48A61K9/00A61K31/704
    • A61K47/60A61K9/0048A61K9/14A61K9/16A61K31/704A61K47/50A61K47/59A61K47/6907
    • Controlled release dosage formulations for the delivery of one or more HIF-1 inhibitors are provided. The controlled release formulations contain one or more HIF-1 inhibitors conjugated to or dispersed in a polymeric vehicle. The one or more HIF-1 inhibitors can be dispersed or encapsulated in a polymeric matrix. In some embodiments, the one or more HIF-1 inhibitors are covalently bound to a polymer, forming a polymer-drug conjugate. Polymeric vehicles can be formed into implants, microparticles, nanoparticles, or combinations thereof. Controlled release HIF-1 formulations provide prolonged therapeutic benefit while lowering side effects by releasing low levels of one or more HIF-1 inhibitors and/or HIF-1 inhibitor conjugates over a prolonged period of time. Controlled release dosage formulations can be used to treat or prevent a disease or disorder in a patient associated with vascularization, including cancer, obesity, and ocular diseases such as wet AMD.
    • 提供用于递送一种或多种HIF-1抑制剂的控制释放剂量制剂。 控制释放制剂含有一种或多种与聚合物载体共轭或分散在其中的HIF-1抑制剂。 一种或多种HIF-1抑制剂可以分散或包封在聚合物基质中。 在一些实施方案中,一种或多种HIF-1抑制剂与聚合物共价结合,形成聚合物 - 药物缀合物。 聚合物载体可以形成植入物,微粒,纳米颗粒或其组合。 受控释放的HIF-1制剂通过在长时间内释放低水平的一种或多种HIF-1抑制剂和/或HIF-1抑制剂缀合物来提供延长的治疗益处,同时降低副作用。 控制释放剂量制剂可用于治疗或预防与血管形成相关的患者(包括癌症,肥胖症和眼部疾病如湿性AMD)中的疾病或病症。
    • 6. 发明授权
    • Controlled release formulations for the delivery of HIF-1 inhibitors
    • 用于递送HIF-1抑制剂的控制释放制剂
    • US08962577B2
    • 2015-02-24
    • US13797506
    • 2013-03-12
    • The Johns Hopkins University
    • Justin Scot HanesPeter Anthony CampochiaroJie Fu
    • A61K31/70C07H15/24A61K47/48A61K9/00
    • A61K47/60A61K9/0048A61K9/14A61K9/16A61K31/704A61K47/50A61K47/59A61K47/6907
    • Controlled release dosage formulations for the delivery of one or more HIF-1 inhibitors are provided. The controlled release formulations contain one or more HIF-1 inhibitors conjugated to or dispersed in a polymeric vehicle. The one or more HIF-1 inhibitors can be dispersed or encapsulated in a polymeric matrix. In some embodiments, the one or more HIF-1 inhibitors are covalently bound to a polymer, forming a polymer-drug conjugate. Polymeric vehicles can be formed into implants, microparticles, nanoparticles, or combinations thereof. Controlled release HIF-1 formulations provide prolonged therapeutic benefit while lowering side effects by releasing low levels of one or more HIF-1 inhibitors and/or HIF-1 inhibitor conjugates over a prolonged period of time. Controlled release dosage formulations can be used to treat or prevent a disease or disorder in a patient associated with vascularization, including cancer, obesity, and ocular diseases such as wet AMD.
    • 提供用于递送一种或多种HIF-1抑制剂的控制释放剂量制剂。 控制释放制剂含有一种或多种与聚合物载体共轭或分散在其中的HIF-1抑制剂。 一种或多种HIF-1抑制剂可以分散或包封在聚合物基质中。 在一些实施方案中,一种或多种HIF-1抑制剂与聚合物共价结合,形成聚合物 - 药物缀合物。 聚合物载体可以形成植入物,微粒,纳米颗粒或其组合。 受控释放的HIF-1制剂通过在长时间内释放低水平的一种或多种HIF-1抑制剂和/或HIF-1抑制剂缀合物来提供延长的治疗益处,同时降低副作用。 控制释放剂量制剂可用于治疗或预防与血管形成相关的患者(包括癌症,肥胖症和眼部疾病如湿性AMD)中的疾病或病症。