公开(公告)号：US08685383B2

公开(公告)日：2014-04-01

申请号：US13493899

申请日：2012-06-11

申请人： 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

发明人： 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分类号： A61K31/74 ,  A61K47/48 ,  A61K38/04 ,  C08G63/48 ,  C08G63/91 ,  C08G65/32 ,  C08L67/00 ,  C08G65/333 ,  C08G65/334

CPC分类号： A61K47/59 ,  A61K31/4745 ,  A61K47/64 ,  A61K47/6803 ,  A61K47/6849 ,  A61K47/6883 ,  C07K7/02 ,  C07K16/32 ,  C08G65/33396 ,  C08G65/334

摘要： 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.

公开(公告)号：US20120321583A1

公开(公告)日：2012-12-20

申请号：US13493899

申请日：2012-06-11

申请人： 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

发明人： 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分类号： C08G65/333 ,  C08G65/332 ,  A61P35/00 ,  A61P35/02 ,  A61K47/48 ,  C07K5/103

CPC分类号： A61K47/59 ,  A61K31/4745 ,  A61K47/64 ,  A61K47/6803 ,  A61K47/6849 ,  A61K47/6883 ,  C07K7/02 ,  C07K16/32 ,  C08G65/33396 ,  C08G65/334

摘要： 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.

摘要翻译： 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。