Functionalization of polyglycolides by “click” chemistry
    1.
    发明授权
    Functionalization of polyglycolides by “click” chemistry 有权
    通过“点击”化学功能化聚乙交酯

    公开(公告)号:US08927682B2

    公开(公告)日:2015-01-06

    申请号:US12229544

    申请日:2008-08-25

    IPC分类号: C08G63/08 C08G63/82

    CPC分类号: C08G63/08 C08G63/823

    摘要: Poly(glycolide) polymers are disclosed. The polymers generally include a polymerized alkynyl-substituted glycolide having a polymer backbone with one or more alkynyl groups appended thereto. The alkynyl groups provide reactive sites for further functionalization of the polymer, for example by reaction with azide derivatives (e.g., azide-substituted organic compounds). Alkynyl and azide groups react via the “click” chemistry mechanism to form functional groups covalently bonded to the polymer via a triazole link. The polymers are biodegradable and can be used to deliver drugs or other therapeutic substances (e.g., large biomolecules such as single strand RNA) at targeted locations in a patient's body and/or at controlled release rates.

    摘要翻译: 公开了聚(乙交酯)聚合物。 聚合物通常包括聚合的炔基取代的乙交酯,其具有带有一个或多个炔基的聚合物主链。 炔基提供用于聚合物进一步官能化的反应位点,例如通过与叠氮化物衍生物(例如叠氮取代的有机化合物)反应。 炔基和叠氮基通过“点击”化学机理反应以形成通过三唑连接共价键合到聚合物上的官能团。 聚合物是可生物降解的,并且可以用于在患者身体的目标位置和/或以控制释放速率递送药物或其它治疗物质(例如大的生物分子,例如单链RNA)。

    "> Functionalization of polyglycolides by
    2.
    发明申请
    Functionalization of polyglycolides by "click" chemistry 有权
    通过“点击”化学功能化聚乙交酯

    公开(公告)号:US20090054619A1

    公开(公告)日:2009-02-26

    申请号:US12229544

    申请日:2008-08-25

    IPC分类号: C08G63/08

    CPC分类号: C08G63/08 C08G63/823

    摘要: Poly(glycolide) polymers are disclosed. The polymers generally include a polymerized alkynyl-substituted glycolide having a polymer backbone with one or more alkynyl groups appended thereto. The alkynyl groups provide reactive sites for further functionalization of the polymer, for example by reaction with azide derivatives (e.g., azide-substituted organic compounds). Alkynyl and azide groups react via the “click” chemistry mechanism to form functional groups covalently bonded to the polymer via a triazole link. The polymers are biodegradable and can be used to deliver drugs or other therapeutic substances (e.g., large biomolecules such as single strand RNA) at targeted locations in a patient's body and/or at controlled release rates.

    摘要翻译: 公开了聚(乙交酯)聚合物。 聚合物通常包括聚合的炔基取代的乙交酯,其具有带有一个或多个炔基的聚合物主链。 炔基提供用于聚合物进一步官能化的反应位点,例如通过与叠氮化物衍生物(例如叠氮取代的有机化合物)反应。 炔基和叠氮基通过“点击”化学机理反应以形成通过三唑连接共价键合到聚合物上的官能团。 聚合物是可生物降解的,并且可以用于在患者身体的目标位置和/或以控制释放速率递送药物或其它治疗物质(例如大的生物分子,例如单链RNA)。

    Functional polyglycolide nanoparticles derived from unimolecular micelles
    3.
    发明申请
    Functional polyglycolide nanoparticles derived from unimolecular micelles 有权
    衍生自单分子胶束的功能聚乙交酯纳米颗粒

    公开(公告)号:US20090325292A1

    公开(公告)日:2009-12-31

    申请号:US12460655

    申请日:2009-07-22

    IPC分类号: C12N5/06 C08G63/08 A61K9/00

    摘要: Poly(glycolide) polymers are disclosed. The polymers generally include a glycolide-based polymer backbone that includes one or more functional groups such as alkynyl groups, hydrophilic organic triazole groups, hydrophobic organic triazole groups (also including amphiphilic organic triazole groups), di-triazole organic crosslinking groups, and triazole-substituted drug derivatives. The alkynyl groups provide reactive sites for further functionalization of the polymer, for example by reaction with azide derivatives. The polymers can further encapsulate a drug for delivery to a patient (i.e., as compared to drug derivatives that are covalently attached to the polymer). The polymers can be in the form of thermodynamically stable unimolecular micelles or crosslinked nanoparticles. The polymer compositions are completely biodegradable and hold great potential for use in biomedical applications.

    摘要翻译: 公开了聚(乙交酯)聚合物。 聚合物通常包括基于乙交酯的聚合物主链,其包括一个或多个官能团,例如炔基,亲水有机三唑基,疏水性有机三唑基团(也包括两亲性有机三唑基团),二 - 三唑有机交联基团和三唑 - 取代的药物衍生物。 炔基提供用于聚合物进一步官能化的反应位点,例如通过与叠氮化物衍生物反应。 聚合物可以进一步包封用于递送给患者的药物(即,与共价连接到聚合物上的药物衍生物相比)。 聚合物可以是热力学稳定的单分子胶束或交联纳米颗粒的形式。 聚合物组合物是完全可生物降解的,并且具有用于生物医学应用的巨大潜力。

    Process for the preparation of polymers of dimeric cyclic esters
    7.
    发明授权
    Process for the preparation of polymers of dimeric cyclic esters 有权
    制备二聚环酯聚合物的方法

    公开(公告)号:US06469133B2

    公开(公告)日:2002-10-22

    申请号:US09736991

    申请日:2000-12-13

    IPC分类号: C08G6308

    CPC分类号: C08G63/08 C08G63/823

    摘要: The present invention provides a process for the direct synthesis of high melting polymers made from dimeric cyclic esters. In particular, the present invention provides a process for synthesis of polylactic acid (PLA) from racemic materials such as racemic lactide and polymandelide from mandelide. The process further provides racemic metal organic ligand catalysts such as racemic salbinap that catalyzes the polymerization of racemic dimeric cyclic ester monomers to a polylactide stereocomplex. Polymandelide and mixed dimeric cyclic esters are also prepared in the presence of low amounts of water.

    摘要翻译: 本发明提供直接合成由二聚环酯制成的高熔点聚合物的方法。 特别地,本发明提供从外消旋材料如外消旋丙交酯和来自扁桃体的聚扁桃酸酯合成聚乳酸(PLA)的方法。 该方法进一步提供外消旋金属有机配位体催化剂,例如外消旋萨拉宾酸,其催化外消旋二聚环状酯单体聚合成聚丙交酯立体络合物。 聚山梨糖苷和混合的二聚环状酯也是在少量水存在下制备的。