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公开(公告)号：US08524214B2
公开(公告)日：2013-09-03
申请号：US12789047
申请日：2010-05-27
Applicant: Aleksandr Yurkovetskiy , Mao Yin , Gui Liu , Laura C. Akullian , John J. Kane , Cheri A. Stevenson , Charles E. Hammond , Russell C. Petter , John H. Van Duzer , Timothy B. Lowinger
Inventor： Aleksandr Yurkovetskiy , Mao Yin , Gui Liu , Laura C. Akullian , John J. Kane , Cheri A. Stevenson , Charles E. Hammond , Russell C. Petter , John H. Van Duzer , Timothy B. Lowinger
IPC: A61K31/045 , A61K31/04 , A61K31/13 , A61K31/21 , A61K31/33 , A61K31/695 , A61K31/765
CPC classification number: C07D519/04 , A61K47/59 , C07D491/22 , G01N2500/00 , Y10T436/145555
Abstract: Polyal-Drug conjugates comprising a variable rate-releasing linker are described along with methods of making such conjugates. Uses for such Polyal-Drug conjugates is also described.
Abstract translation: 描述包含可变速率释放连接体的多价 - 药物共轭物以及制备这种缀合物的方法。 也描述了这种多种药物共轭物的用途。
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公开(公告)号：US20130158046A1
公开(公告)日：2013-06-20
申请号：US13769024
申请日：2013-02-15
Applicant: Laura C. Akullian , Russell C. Petter , John J. Kane , Charles E. Hammond , Mao Yin , Aleksandr Yurkovetskiy , Cheri A. Stevenson
Inventor： Laura C. Akullian , Russell C. Petter , John J. Kane , Charles E. Hammond , Mao Yin , Aleksandr Yurkovetskiy , Cheri A. Stevenson
IPC: C07D303/40 , C07D303/18
CPC classification number: C07D303/40 , A61K47/59 , C07D303/18 , C07D303/22 , C07D303/36 , C07D405/14 , C07D487/08
Abstract: Fumagillin analog polymer conjugates, methods of making fumagillin analog polymer conjugates, compositions comprising a polymer conjugate of a fumagillin analog, and methods for treating cancer, or treating angiogenic diseases comprising administering to a subject in need thereof an effective amount of a polymer conjugate of a fumagillin analog, are described. Also described are novel fumagillin analogs, methods of making fumagillin analogs, compositions comprising at least one fumagillin analog, and methods for treating cancer, or treating angiogenic diseases comprising administering to a subject in need thereof an effective amount of a fumagillin analog.
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公开(公告)号：US20120321583A1
公开(公告)日：2012-12-20
申请号：US13493899
申请日：2012-06-11
Applicant: Aleksandr Yurkovetskiy , Mao Yin , Timothy B. Lowinger , Joshua D. Thomas , Charles E. Hammond , Cheri A. Stevenson , Natalya D. Bodyak , Patrick R. Conlon , Dmitry R. Gumerov
Inventor： Aleksandr Yurkovetskiy , Mao Yin , Timothy B. Lowinger , Joshua D. Thomas , Charles E. Hammond , Cheri A. Stevenson , Natalya D. Bodyak , Patrick R. Conlon , Dmitry R. Gumerov
IPC: C08G65/333 , C08G65/332 , A61P35/00 , A61P35/02 , A61K47/48 , C07K5/103
CPC classification number: A61K47/59 , A61K31/4745 , A61K47/64 , A61K47/6803 , A61K47/6849 , A61K47/6883 , C07K7/02 , C07K16/32 , C08G65/33396 , C08G65/334
Abstract: A drug conjugate is provided herein. The conjugate comprises a protein based recognition-molecule (PBRM) and a polymeric carrier substituted with one or more -LD-D, the protein based recognition-molecule being connected to the polymeric carrier by LP. Each occurrence of D is independently a therapeutic agent having a molecular weight ≦5 kDa. LD and LP are linkers connecting the therapeutic agent and PBRM to the polymeric carrier respectively. Also disclosed are polymeric scaffolds useful for conjugating with a PBRM to form a polymer-drug-PBRM conjugate described herein, compositions comprising the conjugates, methods of their preparation, and methods of treating various disorders with the conjugates or their compositions.
Abstract translation: 本文提供药物缀合物。 缀合物包含基于蛋白质的识别分子（PBRM）和被一个或多个-LD-D取代的聚合物载体，基于蛋白质的识别分子通过LP连接到聚合物载体上。 每次出现的D独立地是具有分子量＆nlE; 5kDa的治疗剂。 LD和LP分别是将治疗剂和PBRM分别连接到聚合物载体的接头。 还公开了可用于与PBRM缀合以形成本文所述的聚合物 - 药物-PBRM缀合物的聚合物支架，包含缀合物的组合物，其制备方法，以及用缀合物或其组合物治疗各种病症的方法。
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4.发明申请MODIFIED POLYMERS FOR DELIVERY OF POLYNUCLEOTIDES, METHOD OF MANUFACTURE, AND METHODS OF USE THEREOF 失效用于输送多核苷酸的改性聚合物，其制造方法及其使用方法公开(公告)号：US20110243880A1
公开(公告)日：2011-10-06
申请号：US13073815
申请日：2011-03-28
Applicant: Aleksandr Yurkovetskiy , Mao Yin , Timothy B. Lowinger , Carolina B. Cabral , Charles E. Hammond , Cheri A. Stevenson
Inventor： Aleksandr Yurkovetskiy , Mao Yin , Timothy B. Lowinger , Carolina B. Cabral , Charles E. Hammond , Cheri A. Stevenson
CPC classification number: C08L59/00 , A61K47/59 , A61K48/0041 , C12N15/111 , C12N2310/11 , C12N2310/12 , C12N2310/14 , C12N2320/32
Abstract: A polynucleotide delivery vehicle comprising a modified polymer is provided herein, the modified polymer having the following formula: in which W1, W2, W3, W4, W5, W6, Z1, Z2, Z3, Z4, Z5, Z9, R1, R2, R3, R4, R5, n1, n2, n3, n4, n5, and n6 are defined herein. Also disclosed are methods of delivering a polynucleotide to the cytoplasm of a selected tissue type or cell type and methods of reducing expression of a gene in a cell or a subject in need thereof with the modified polymer.
Abstract translation: 本文提供了包含改性聚合物的多核苷酸递送载体，所述改性聚合物具有下式：其中W1，W2，W3，W4，W5，W6，Z1，Z2，Z3，Z4，Z5，Z9，R1，R2， R3，R4，R5，n1，n2，n3，n4，n5和n6在本文中定义。 还公开了将多核苷酸递送至所选组织类型或细胞类型的细胞质的方法以及在有需要的细胞或受试者中用改性聚合物降低基因表达的方法。
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5.发明申请PHARMACEUTICAL FORMULATIONS OF BIODEGRADABLE BIOCOMPATIBLE CAMPTOTHECIN-POLYMER CONJUGATES 失效生物可降解生物活性聚合物共聚物的药物制剂公开(公告)号：US20100179181A1
公开(公告)日：2010-07-15
申请号：US12635027
申请日：2009-12-10
Applicant: James ROLKE , Russell C. PETTER , Mao YIN , Aleksandr YURKOVETSKIY , Gui LIU , Emile FARHAN
Inventor： James ROLKE , Russell C. PETTER , Mao YIN , Aleksandr YURKOVETSKIY , Gui LIU , Emile FARHAN
IPC: A61K31/4375 , A61K35/00
CPC classification number: A61K47/48215 , A61K31/44 , A61K47/59
Abstract: A camptothecin/polymer dual phase drug release system is described that is stable in both liquid and lyophilized states. The polymer contains acetals and/or ketals.
Abstract translation: 描述了在液体和冻干状态下稳定的喜树碱/聚合物双相药物释放系统。 聚合物含有缩醛和/或缩酮。
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Patent Agency Ranking
公开(公告)号：US20090148396A1
公开(公告)日：2009-06-11
申请号：US12276856
申请日：2008-11-24
Applicant: Laura C. AKULLIAN , Russell C. PETTER , John J. KANE , Charles E. HAMMOND , Mao YIN , Aleksandr YURKOVETSKIY , Cheri A. STEVENSON
Inventor： Laura C. AKULLIAN , Russell C. PETTER , John J. KANE , Charles E. HAMMOND , Mao YIN , Aleksandr YURKOVETSKIY , Cheri A. STEVENSON
IPC: A61K31/77 , C08F24/00 , C08F26/06 , A61P35/00 , A61K31/787
CPC classification number: C07D303/40 , A61K47/59 , C07D303/18 , C07D303/22 , C07D303/36 , C07D405/14 , C07D487/08
Abstract: Fumagillin analog polymer conjugates, methods of making fumagillin analog polymer conjugates, compositions comprising a polymer conjugate of a fumagillin analog, and methods for treating cancer, or treating angiogenic diseases comprising administering to a subject in need thereof an effective amount of a polymer conjugate of a fumagillin analog, are described. Also described are novel fumagillin analogs, methods of making fumagillin analogs, compositions comprising at least one fumagillin analog, and methods for treating cancer, or treating angiogenic diseases comprising administering to a subject in need thereof an effective amount of a fumagillin analog.
Abstract translation: 烟曲霉素类似物聚合物缀合物，制备烟曲霉素类似物聚合物共轭物的方法，包含烟曲霉素类似物的聚合物缀合物的组合物，以及用于治疗癌症的方法或治疗血管发生疾病的方法，包括向有需要的受试者施用有效量的 烟曲霉素类似物。 还描述了新的烟曲霉素类似物，制备烟曲霉素类似物的方法，包含至少一种烟曲霉素类似物的组合物，以及用于治疗癌症的方法或治疗血管发生疾病，包括向有需要的受试者施用有效量的烟曲霉素类似物。
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公开(公告)号：US08685383B2
公开(公告)日：2014-04-01
申请号：US13493899
申请日：2012-06-11
Applicant: Aleksandr Yurkovetskiy , Mao Yin , Timothy B. Lowinger , Joshua D. Thomas , Charles E. Hammond , Cheri A. Stevenson , Natalya D. Bodyak , Patrick R. Conlon , Dmitry R. Gumerov
Inventor： Aleksandr Yurkovetskiy , Mao Yin , Timothy B. Lowinger , Joshua D. Thomas , Charles E. Hammond , Cheri A. Stevenson , Natalya D. Bodyak , Patrick R. Conlon , Dmitry R. Gumerov
IPC: A61K31/74 , A61K47/48 , A61K38/04 , C08G63/48 , C08G63/91 , C08G65/32 , C08L67/00 , C08G65/333 , C08G65/334
CPC classification number: A61K47/59 , A61K31/4745 , A61K47/64 , A61K47/6803 , A61K47/6849 , A61K47/6883 , C07K7/02 , C07K16/32 , C08G65/33396 , C08G65/334
Abstract: A drug conjugate is provided herein. The conjugate comprises a protein based recognition-molecule (PBRM) and a polymeric carrier substituted with one or more -LD-D, the protein based recognition-molecule being connected to the polymeric carrier by LP. Each occurrence of D is independently a therapeutic agent having a molecular weight ≦5 kDa. LD and LP are linkers connecting the therapeutic agent and PBRM to the polymeric carrier respectively. Also disclosed are polymeric scaffolds useful for conjugating with a PBRM to form a polymer-drug-PBRM conjugate described herein, compositions comprising the conjugates, methods of their preparation, and methods of treating various disorders with the conjugates or their compositions.
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8.发明授权Modified polymers for delivery of polynucleotides, method of manufacture, and methods of use thereof 失效用于递送多核苷酸的改性聚合物，其制备方法及其使用方法公开(公告)号：US08349308B2
公开(公告)日：2013-01-08
申请号：US13073815
申请日：2011-03-28
Applicant: Aleksandr Yurkovetskiy , Mao Yin , Timothy B. Lowinger , Carolina B. Cabral , Charles E. Hammond , Cheri A. Stevenson
Inventor： Aleksandr Yurkovetskiy , Mao Yin , Timothy B. Lowinger , Carolina B. Cabral , Charles E. Hammond , Cheri A. Stevenson
CPC classification number: C08L59/00 , A61K47/59 , A61K48/0041 , C12N15/111 , C12N2310/11 , C12N2310/12 , C12N2310/14 , C12N2320/32
Abstract: A polynucleotide delivery vehicle comprising a modified polymer is provided herein, the modified polymer having the following formula: in which W1, W2, W3, W4, W5, W6, Z1, Z2, Z3, Z4, Z5, Z9, R1, R2, R3, R4, R5, n1, n2, n3, n4, n5, and n6 are defined herein. Also disclosed are methods of delivering a polynucleotide to the cytoplasm of a selected tissue type or cell type and methods of reducing expression of a gene in a cell or a subject in need thereof with the modified polymer.
Abstract translation: 本文提供了包含改性聚合物的多核苷酸递送载体，所述改性聚合物具有下式：其中W1，W2，W3，W4，W5，W6，Z1，Z2，Z3，Z4，Z5，Z9，R1，R2， R3，R4，R5，n1，n2，n3，n4，n5和n6在本文中定义。 还公开了将多核苷酸递送至所选组织类型或细胞类型的细胞质的方法以及在有需要的细胞或受试者中用改性聚合物降低基因表达的方法。
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公开(公告)号：US20100305149A1
公开(公告)日：2010-12-02
申请号：US12789047
申请日：2010-05-27
Applicant: Aleksandr Yurkovetskiy , Mao Yin , Gui Liu , Laura C. Akullian , John J. Kane , Cheri A. Stevenson , Charles E. Hammond , Russell C. Petter , John H. Van Duzer , Timothy B. Lowinger
Inventor： Aleksandr Yurkovetskiy , Mao Yin , Gui Liu , Laura C. Akullian , John J. Kane , Cheri A. Stevenson , Charles E. Hammond , Russell C. Petter , John H. Van Duzer , Timothy B. Lowinger
IPC: A61K31/439 , A61P35/00 , A61P35/04 , C07D487/18 , C07D491/22 , G01N33/50
CPC classification number: C07D519/04 , A61K47/59 , C07D491/22 , G01N2500/00 , Y10T436/145555
Abstract: Polyal-Drug conjugates comprising a variable rate-releasing linker are described along with methods of making such conjugates. Uses for such Polyal-Drug conjugates is also described.
Abstract translation: 描述包含可变速率释放连接体的多价 - 药物共轭物以及制备这种缀合物的方法。 也描述了这种多种药物共轭物的用途。
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10.发明申请PHARMACEUTICAL FORMULATIONS FOR FUMAGILLIN DERIVATIVE-PHF CONJUGATES 审中-公开FUMAGILLIN衍生物 - PHF结合物的药物制剂公开(公告)号：US20130189218A1
公开(公告)日：2013-07-25
申请号：US13725900
申请日：2012-12-21
Applicant: Laura Akullian , Gui Liu , Timothy B. Lowinger , Dennis McGillicuddy , Cheri Stevenson , John Van Duzer , Mao Yin , Aleksandr Yurkovetskiy
Inventor： Laura Akullian , Gui Liu , Timothy B. Lowinger , Dennis McGillicuddy , Cheri Stevenson , John Van Duzer , Mao Yin , Aleksandr Yurkovetskiy
IPC: A61K47/48
CPC classification number: A61K47/60 , C07D303/22
Abstract: The invention described herein provides a mixture comprising polymer molecules or salts thereof, wherein a polymer molecule in the mixture comprises covalently bound subunits L, K, and M wherein the average molecular weight of the polymer molecules in the mixture is about 50 kDa to about 200 kDa, wherein the mole percentage of subunit M, K and L, relative to the total amount of subunits in the mixture, is about 90.5 to about 96 mol %, about 2.8 to about 7.3 mol %, and about 1.2 to about 2.2 mol %, respectively.
Abstract translation: 本文描述的本发明提供了包含聚合物分子或其盐的混合物，其中该混合物中的聚合物分子包含共价结合的亚单位L，K和M，其中混合物中聚合物分子的平均分子量为约50kDa至约200 kDa，其中亚单位M，K和L相对于混合物中亚单位总量的摩尔百分比为约90.5至约96摩尔％，约2.8至约7.3摩尔％，约1.2至约2.2摩尔％ ， 分别。
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