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1. 发明授权

US09018323B2 Polymer derivative of cytidine metabolic antagonist 有权
标题翻译：胞苷代谢拮抗剂的聚合物衍生物
公开(公告)号：US09018323B2
公开(公告)日：2015-04-28
申请号：US13884413
申请日：2011-11-16
申请人： Keiichirou Yamamoto , Manami Okazaki , Dai Kawamura
发明人： Keiichirou Yamamoto , Manami Okazaki , Dai Kawamura
IPC分类号： C08G81/00 , A61K31/513 , C07D407/04 , C08G69/40 , C08G69/48 , A61K31/77 , A61K31/785 , A61K47/48 , C08G85/00
CPC分类号： C08G81/00 , A61K31/513 , A61K31/77 , A61K31/785 , A61K47/60 , A61K47/645 , C07D407/04 , C08G69/40 , C08G69/48
摘要： [Problem]To provide a novel polymer derivative of a cytidine metabolic antagonist which allows release of a medicament irrespective of enzymes of the living body and is expected to have high therapeutic effects. [Solution]The polymer derivative of a cytidine metabolic antagonist in which a substituent represented by the general formula (I) or the general formula (II) [wherein R7 and R8 each independently represent a hydrogen atom or an optionally substituted (C1-C6)alkyl group, R6 represents a hydrogen atom, an optionally substituted (C1-C40)alkyl group, an optionally substituted (C1-C40)aralkyl group, an optionally substituted aromatic group, an amino acid residue in which the carboxy group is protected, or an optionally substituted sugar residue, CX—CY represents CH—CH or C═C (double bond), and A represents the residue of the cytidine metabolic antagonist except the amino group at the position 4] is bonded to the side-chain carboxy group of a block copolymer of a polyethylene-glycol structural moiety and a polymer having 10 or more carboxy groups.
摘要翻译： [问题]提供一种胞苷代谢拮抗剂的新型聚合物衍生物，其允许不管生物体的酶释放药物并且预期具有高治疗效果。 [溶液]通式（I）或通式（II）表示的取代基的胞苷代谢拮抗剂的聚合物衍生物[其中，R7和R8各自独立地表示氢原子或可以具有取代基的（C1-C6）烷基，R 6表示氢原子，任选取代的（C 1 -C 40）烷基，任选取代的（C 1 -C 40）芳烷基，任选取代的芳族基团，其中羧基被保护的氨基酸残基，或任选取代的糖残基，CX-CY表示CH-CH或C = C（双键），A表示胞苷代谢拮抗剂的残基，除了位置4]上的氨基键合到侧链羧基的聚乙二醇结构部分和具有10个或更多个羧基的聚合物的嵌段共聚物。

2. 发明申请

US20130331517A1 Novel Polymer Derivative Of Cytidine Metabolic Antagonist 有权
标题翻译：胞苷代谢拮抗剂的新型聚合物衍生物
公开(公告)号：US20130331517A1
公开(公告)日：2013-12-12
申请号：US13884413
申请日：2011-11-16
申请人： Keiichirou Yamamoto , Manami Okazaki , Dai Kawamura
发明人： Keiichirou Yamamoto , Manami Okazaki , Dai Kawamura
IPC分类号： C08G81/00
CPC分类号： C08G81/00 , A61K31/513 , A61K31/77 , A61K31/785 , A61K47/60 , A61K47/645 , C07D407/04 , C08G69/40 , C08G69/48
摘要： [Problem]To provide a novel polymer derivative of a cytidine metabolic antagonist which allows release of a medicament irrespective of enzymes of the living body and is expected to have high therapeutic effects.[Solution]The polymer derivative of a cytidine metabolic antagonist in which a substituent represented by the general formula (I) or the general formula (II) [wherein R7 and R8 each independently represent a hydrogen atom or an optionally substituted (C1-C6)alkyl group, R6 represents a hydrogen atom, an optionally substituted (C1-C40)alkyl group, an optionally substituted (C1-C40)aralkyl group, an optionally substituted aromatic group, an amino acid residue in which the carboxy group is protected, or an optionally substituted sugar residue, CX—CY represents CH—CH or C═C (double bond), and A represents the residue of the cytidine metabolic antagonist except the amino group at the position 4] is bonded to the side-chain carboxy group of a block copolymer of a polyethylene-glycol structural moiety and a polymer having 10 or more carboxy groups.
摘要翻译： [问题]提供一种胞苷代谢拮抗剂的新型聚合物衍生物，其允许不管生物体的酶释放药物并且预期具有高治疗效果。 [溶液]通式（I）或通式（II）表示的取代基的胞苷代谢拮抗剂的聚合物衍生物[其中，R7和R8各自独立地表示氢原子或可以具有取代基的（C1-C6）烷基，R 6表示氢原子，任选取代的（C 1 -C 40）烷基，任选取代的（C 1 -C 40）芳烷基，任选取代的芳族基团，其中羧基被保护的氨基酸残基，或任选取代的糖残基，CX-CY表示CH-CH或C = C（双键），A表示胞苷代谢拮抗剂的残基，除了位置4]上的氨基键合到侧链羧基的聚乙二醇结构部分和具有10个或更多个羧基的聚合物的嵌段共聚物。

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