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1. 发明申请

WO2010005740A2 METHODS FOR THE PREPARATION OF TARGETING AGENT FUNCTIONALIZED DIBLOCK COPOLYMERS FOR USE IN FABRICATION OF THERAPEUTIC TARGETED NANOPARTICLES 审中-公开
标题翻译：制备用于制备治疗性靶向纳米颗粒的靶向功能性二嵌段共聚物的方法
公开(公告)号：WO2010005740A2
公开(公告)日：2010-01-14
申请号：PCT/US2009/047554
申请日：2009-06-16
申请人： BIND BIOSCIENCES, INC. , ALI, Mir, M. , HRKACH, Jeff , ZALE, Stephen, E.
发明人： ALI, Mir, M. , HRKACH, Jeff , ZALE, Stephen, E.
IPC分类号： A61K9/16 , A61K47/34 , A61P35/00
CPC分类号： A61K47/34 , A61K9/5153 , A61K47/60 , A61K47/6911
摘要： This application provides methods of making nanoparticles using pre-functionalized poly(ethylene glycol)(also referred to as PEG) as a macroinitiator for the synthesis of diblock copolymers. These diblock copolymers comprise a poly(ethylene glycol) block bearing a targeting agent at its terminus and a second biocompatible and biodegradable hydrophobic polymer block (e.g. a poly(ester)). The poly(ethylene glycol) is hetero-bifunctional with a targeting moiety (agent) covalently bound to its α terminus and a polymerization initiating functional group (e.g., a hydroxyl group) present on its ω terminus. Ring opening polymerization yields the desired poly(ester)-poly(ethylene glycol)-targeting agent polymer that is used to impart targeting capability to therapeutic nanoparticles. This "polymerization from" approach typically employs precursors of the targeting agent wherein the reactivity of functional groups of the targeting agent is masked using protecting groups. Also described is a "coupling to" that utilized the poly(ethylene glycol)-targeting agent conjugate where the targeting agent remains in its native un-protected form. This method uses "orthogonal" chemistry that exhibit no cross reactivity towards functional groups typically found within targeting agents of interest. Nanoparticles produced according to the disclosed methods as well as their use in the treatment of various diseases are also provided.
摘要翻译：本申请提供了使用预官能化聚（乙二醇）（也称为PEG）作为二嵌段共聚物合成的大分子引发剂制备纳米颗粒的方法。这些二嵌段共聚物包含在其末端具有靶向剂的聚（乙二醇）嵌段和第二生物相容性和可生物降解的疏水性聚合物嵌段（例如聚（酯））。聚（乙二醇）与共价结合到其末端的靶向部分（试剂）和存在于其末端的聚合引发官能团（例如羟基）是异双官能的。总站。开环聚合产生用于赋予治疗性纳米颗粒靶向能力的所需聚（酯） - 聚（乙二醇） - 靶向剂聚合物。这种“聚合”方法通常使用靶向剂的前体，其中靶向剂的官能团的反应性使用保护基掩蔽。还描述了使用聚（乙二醇） - 靶向剂缀合物的“偶联”，其中靶向剂保持其天然未保护形式。该方法使用对正常感兴趣的靶向剂中通常发现的官能团没有交叉反应性的“正交”化学。还提供了根据所公开的方法制备的纳米颗粒及其在治疗各种疾病中的用途。

2. 发明申请

WO2010005726A2 THERAPEUTIC POLYMERIC NANOPARTICLES WITH MTOR INHIBITORS AND METHODS OF MAKING AND USING SAME 审中-公开
标题翻译：具有MTOR抑制剂的治疗性聚合物纳米颗粒及其制备方法和使用方法
公开(公告)号：WO2010005726A2
公开(公告)日：2010-01-14
申请号：PCT/US2009/047518
申请日：2009-06-16
申请人： BIND BIOSCIENCES INC. , ZALE, Stephen, E. , TROIANO, Greg , ALI, Mir Mukkaram , HRKACH, Jeff , WRIGHT, James
发明人： ZALE, Stephen, E. , TROIANO, Greg , ALI, Mir Mukkaram , HRKACH, Jeff , WRIGHT, James
IPC分类号： A61K9/16 , A61K47/34 , A61K31/435 , A61P35/00
CPC分类号： A61K9/14 , A61K9/19 , A61K9/5146 , A61K9/5153 , A61K31/00 , A61K31/435 , A61K31/436 , C07C59/08 , Y10S977/773
摘要： The present disclosure generally relates to therapeutic nanoparticles. Exemplary nanoparticles disclosed herein may include about 1 to about 20 weight percent of a mTOR inhibitor; and about 70 to about 99 weight percent biocompatible polymer.
摘要翻译：本公开一般涉及治疗性纳米颗粒。本文公开的示例性纳米颗粒可包括约1至约20重量％的mTOR抑制剂; 和约70至约99重量％的生物相容性聚合物。

3. 发明申请

WO2010005725A2 THERAPEUTIC POLYMERIC NANOPARTICLES COMPRISING VINCA ALKALOIDS AND METHODS OF MAKING AND USING SAME 审中-公开
标题翻译：包含VINCA生物碱的治疗性聚合物纳米颗粒及其制备和使用方法
公开(公告)号：WO2010005725A2
公开(公告)日：2010-01-14
申请号：PCT/US2009/047517
申请日：2009-06-16
申请人： BIND BIOSCIENCES, INC. , ZALE, Stephen, E. , TROIANO, Greg , ALI, Mir Mukkaram , HRKACH, Jeff , WRIGHT, James
发明人： ZALE, Stephen, E. , TROIANO, Greg , ALI, Mir Mukkaram , HRKACH, Jeff , WRIGHT, James
IPC分类号： A61K9/16 , A61K31/475 , A61K47/34 , A61P35/00
CPC分类号： A61K9/1647 , A61K9/14 , A61K9/1694 , A61K9/19 , A61K9/5153 , A61K31/4745 , A61K31/475 , A61K31/55 , A61K47/26
摘要： The present disclosure generally relates to therapeutic nanoparticles. Exemplary nanoparticles disclosed herein may include about 1 to about 20 weight percent of a vinca alkaloid; and about 50 to about 99 weight percent biocompatible polymer.
摘要翻译：本公开总体上涉及治疗性纳米颗粒。本文公开的示例性纳米粒子可以包括约1至约20重量百分比的长春花生物碱; 和约50至约99重量％的生物相容性聚合物。

4. 发明申请

WO2010005721A3 DRUG LOADED POLYMERIC NANOPARTICLES AND METHODS OF MAKING AND USING SAME 审中-公开
公开(公告)号：WO2010005721A3
公开(公告)日：2010-01-14
申请号：PCT/US2009/047513
申请日：2009-06-16
申请人： BIND BIOSCIENCES, INC. , ZALE, Stephen, E. , TROIANO, Greg , ALI, Mir Mukkaram , HRKACH, Jeff , WRIGHT, James
发明人： ZALE, Stephen, E. , TROIANO, Greg , ALI, Mir Mukkaram , HRKACH, Jeff , WRIGHT, James
IPC分类号： A61K9/16 , A61K47/34 , A61K33/24 , A61K31/337
摘要： The present disclosure generally relates to nanoparticles having about 0.2 to about 35 weight percent of a therapeutic agent; and about 10 to about 99 weight percent of biocompatible polymer such as a diblock poly(lactic) acid-poly(ethylene)glycol. Other aspects of the invention include methods of making such nanoparticles.

5. 发明公开

EP2509634A2 STABLE FORMULATIONS FOR LYOPHILIZING THERAPEUTIC PARTICLES 有权转让
标题翻译：稳定的制剂对于治疗冻干颗粒
公开(公告)号：EP2509634A2
公开(公告)日：2012-10-17
申请号：EP10836748.3
申请日：2010-12-10
申请人： Bind Biosciences, Inc.
发明人： TROIANO, Greg , ZALE, Stephen, E. , WRIGHT, James , VAN GEEN UOVEN, Tina , SONG, Young-ho
IPC分类号： A61K47/40 , A61K47/30 , A61K47/36 , A61K47/02 , A61K31/335 , A61P35/00
CPC分类号： A61K31/337 , A61K9/0019 , A61K9/16 , A61K9/19 , A61K9/5123 , A61K9/5153 , A61K9/5161 , A61K9/5192 , A61K31/335 , A61K47/26 , A61K47/34 , A61K47/40 , C08G63/664 , Y10S977/906
摘要： The present disclosure generally relates to lyophilized pharmaceutical compositions comprising polymeric nanoparticles which, upon reconstitution, have low levels of greater than 10 micron size particles. Other aspects of the invention include methods of making such nanoparticles.

6. 发明公开

EP2309991A2 THERAPEUTIC POLYMERIC NANOPARTICLES COMPRISING VINCA ALKALOIDS AND METHODS OF MAKING AND USING SAME 审中-公开
标题翻译：长春花生物碱疗效的聚合物纳米粒子，和方法的生产和使用
公开(公告)号：EP2309991A2
公开(公告)日：2011-04-20
申请号：EP09794917.6
申请日：2009-06-16
申请人： Bind Biosciences, Inc.
发明人： ZALE, Stephen, E. , TROIANO, Greg , ALI, Mir Mukkaram , HRKACH, Jeff , WRIGHT, James
IPC分类号： A61K9/16 , A61K31/475 , A61K47/34 , A61P35/00
CPC分类号： A61K9/1647 , A61K9/14 , A61K9/1694 , A61K9/19 , A61K9/5153 , A61K31/4745 , A61K31/475 , A61K31/55 , A61K47/26
摘要： The present disclosure generally relates to therapeutic nanoparticles. Exemplary nanoparticles disclosed herein may include about 1 to about 20 weight percent of a vinca alkaloid; and about 50 to about 99 weight percent biocompatible polymer.

7. 发明公开

EP2136788A1 CANCER CELL TARGETING USING NANOPARTICLES 有权
标题翻译：癌细胞靶向纳米
公开(公告)号：EP2136788A1
公开(公告)日：2009-12-30
申请号：EP08744752.0
申请日：2008-03-31
申请人： Bind Biosciences, Inc.
发明人： ZALE, Stephen, E. , ALI, Mir Mukkaram
IPC分类号： A61K9/14 , B82B1/00
CPC分类号： A61K9/1647 , A61K9/146 , A61K9/5153 , A61K9/5192 , A61K31/136 , A61K31/197 , A61K31/337 , A61K31/704 , A61K47/34 , A61K47/542 , A61K47/60 , A61K47/6935 , A61K47/6937 , B82Y5/00 , C07C275/16 , C07C275/24 , C08G63/664 , C08G63/6852 , C08G63/6922 , Y10S977/904 , Y10S977/905 , Y10S977/906 , Y10S977/911 , Y10S977/915
摘要： The present invention generally relates to polymers and macromolecules, in particular, to polymers useful in particles such as nanoparticles. One aspect of the invention is directed to a method of developing nanoparticles with desired properties. In one set of embodiments, the method includes producing libraries of nanoparticles having highly controlled properties, which can be formed by mixing together two or more macromolecules in different ratios. One or more of the macromolecules may be a polymeric conjugate of a moiety to a biocompatible polymer. In some cases, the nanoparticle may contain a drug. Other aspects of the invention are directed to methods using nanoparticle libraries.

8. 发明公开

EP2309989A2 DRUG LOADED POLYMERIC NANOPARTICLES AND METHODS OF MAKING AND USING SAME 有权转让
公开(公告)号：EP2309989A2
公开(公告)日：2011-04-20
申请号：EP09794913.5
申请日：2009-06-16
申请人： Bind Biosciences, Inc.
发明人： ZALE, Stephen, E. , TROIANO, Greg , ALI, Mir Mukkaram , HRKACH, Jeff , WRIGHT, James
IPC分类号： A61K9/16 , A61K47/34 , A61K33/24 , A61K31/337
CPC分类号： A61K47/34 , A61J3/00 , A61K9/10 , A61K9/107 , A61K9/1647 , A61K9/19 , A61K9/5146 , A61K9/5153 , A61K31/337 , A61K31/4355 , A61K31/436 , A61K31/437 , A61K31/439 , A61K31/475 , A61K31/704 , A61K31/7068 , A61K47/6915 , A61K47/6925 , A61K47/6937 , B82Y5/00 , C07C59/08 , Y10S977/773
摘要： The present disclosure generally relates to methods of making nanoparticles having about 0.2 to about 35 weight percent of a therapeutic agent; and about 10 to about 99 weight percent of biocompatible polymer such as a diblock poly(lactic) acid-poly(ethylene)glycol.

9. 发明公开

EP2285350A2 METHODS FOR THE PREPARATION OF TARGETING AGENT FUNCTIONALIZED DIBLOCK COPOLYMERS FOR USE IN FABRICATION OF THERAPEUTIC TARGETED NANOPARTICLES 有权转让
标题翻译：过程与靶向药物的官能嵌段共聚物FOR USE在治疗的纳米粒子的生产PRODUCING
公开(公告)号：EP2285350A2
公开(公告)日：2011-02-23
申请号：EP09794932.5
申请日：2009-06-16
申请人： Bind Biosciences, Inc.
发明人： ALI, Mir, M. , HRKACH, Jeff , ZALE, Stephen, E. , ALVAREZ DE CIENFUEGOS, Luis
IPC分类号： A61K9/16 , A61K47/34 , A61P35/00
CPC分类号： A61K47/34 , A61K9/5153 , A61K47/60 , A61K47/6911
摘要： This application provides methods of making nanoparticles using pre-functionalized poly(ethylene glycol)(also referred to as PEG) as a macroinitiator for the synthesis of diblock copolymers. These diblock copolymers comprise a poly(ethylene glycol) block bearing a targeting agent at its terminus and a second biocompatible and biodegradable hydrophobic polymer block (e.g. a poly(ester)). The poly(ethylene glycol) is hetero-bifunctional with a targeting moiety (agent) covalently bound to its α terminus and a polymerization initiating functional group (e.g., a hydroxyl group) present on its ω terminus. Ring opening polymerization yields the desired poly(ester)-poly(ethylene glycol)-targeting agent polymer that is used to impart targeting capability to therapeutic nanoparticles. This "polymerization from" approach typically employs precursors of the targeting agent wherein the reactivity of functional groups of the targeting agent is masked using protecting groups. Also described is a "coupling to" that utilized the poly(ethylene glycol)-targeting agent conjugate where the targeting agent remains in its native un-protected form. This method uses "orthogonal" chemistry that exhibit no cross reactivity towards functional groups typically found within targeting agents of interest. Nanoparticles produced according to the disclosed methods as well as their use in the treatment of various diseases are also provided.
摘要翻译：（因此，通过被称为PEG），本申请提供了使用官能化的预聚（乙二醇）作为二嵌段共聚物的合成中的宏引发剂制备纳米颗粒的方法。这些二嵌段共聚物包含聚（乙二醇）嵌段轴承在其末端和靶向剂的第二生物相容的和生物可降解的疏水性聚合物嵌段（例如，聚（酯））。的聚（乙二醇）是异双功能与靶向部分（剂）共价结合到其α末端和聚合引发官能团（E. G.，羟基）存在于它的ω末端。开环聚合反应得到所需的聚（酯）聚（乙二醇）靶向剂的聚合物并用于赋予靶向能力对治疗纳米颗粒。这种方法“从聚合”采用典型地，靶向剂的前体worin靶向剂的官能团的反应性，使用的保护基团掩蔽。如此描述为“耦合于”所使用的聚（乙二醇）靶向剂缀合物，其中所述靶向剂保持在其天然的未保护的形式。该方法使用“正交”化学确实表现出对通常发现的官能团没有交叉反应中的定位感兴趣的代理商。纳米颗粒产生的雅丁到盘游离缺失的方法以及它们在各种疾病的治疗中的用途因此被提供。

10. 发明公开

EP2379064A2 LONG CIRCULATING NANOPARTICLES FOR SUSTAINED RELEASE OF THERAPEUTIC AGENTS 审中-公开
标题翻译：长循环纳米粒子治疗药物的延迟释放
公开(公告)号：EP2379064A2
公开(公告)日：2011-10-26
申请号：EP09835578.7
申请日：2009-12-15
申请人： Bind Biosciences, Inc.
发明人： ZALE, Stephen, E. , TROIANO, Greg , ALI, Mir, Mukkaram , HRKACH, Jeff , WRIGHT, James , LOW, Susan
IPC分类号： A61K9/32 , A61K9/51 , A61K9/22 , A61K9/16 , A61P35/00
CPC分类号： A61K9/5153 , A61K9/0019 , A61K9/1641 , A61K31/337 , A61K31/436 , A61K31/475 , A61K31/519 , A61K47/542 , A61K47/593 , A61K47/60 , A61K47/6925 , A61K47/6937 , B82Y5/00
摘要： The present disclosure is directed in part to a biocompatible nanoparticle composition comprising a plurality of non-colloidal long circulating nanoparticles, each comprising a α-hydroxy polyester-co-polyether and a therapeutic agent, wherein such disclosed compositions provide a therapeutic effect for at least 12 hours.

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