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公开(公告)号：US09149540B2
公开(公告)日：2015-10-06
申请号：US12991041
申请日：2009-04-28
申请人： Takeshi Nakanishi , Kazuhisa Hara , Chieko Seno
发明人： Takeshi Nakanishi , Kazuhisa Hara , Chieko Seno
CPC分类号： A61K47/48315 , A61K31/785 , A61K47/34 , A61K47/60 , A61K47/645 , C08G69/10 , C08G69/40 , C08G69/48
摘要： Disclosed is a polymer conjugate of folic acid or a folic acid derivative, wherein an amide bond is not used. The compound has chemical stability and adequate drug release rate in the living organism. Specifically disclosed is a polymer conjugate of folic acid or a folic acid derivative, wherein a substituent represented by formula (I) is bonded to a carboxy group of a block copolymer which is composed of a polyethylene glycol and a polymer having a carboxy group in a side chain, or a pharmacologically acceptable salt thereof. [In the formula, A represents a monocyclic or fused aromatic group; G represents an optionally substituted (C1-C6) alkylene group; Y represents a hydrogen atom or a substituent; and E represents a residue of folic acid or a folic acid derivative.]
摘要翻译： 公开了叶酸或叶酸衍生物的聚合物缀合物，其中不使用酰胺键。 该化合物在生物体中具有化学稳定性和足够的药物释放速率。 具体公开的是叶酸或叶酸衍生物的聚合物缀合物，其中由式（I）表示的取代基与由聚乙二醇和具有羧基的聚合物组成的嵌段共聚物的羧基键合 侧链或其药理学上可接受的盐。 [式中，A表示单环或稠合芳基; G表示任选取代的（C 1 -C 6）亚烷基; Y表示氢原子或取代基; E表示叶酸或叶酸衍生物的残基。]
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公开(公告)号：US20110294980A1
公开(公告)日：2011-12-01
申请号：US12991041
申请日：2009-04-28
申请人： Takeshi Nakanishi , Kazuhisa Hara , Chieko Seno
发明人： Takeshi Nakanishi , Kazuhisa Hara , Chieko Seno
CPC分类号： A61K47/48315 , A61K31/785 , A61K47/34 , A61K47/60 , A61K47/645 , C08G69/10 , C08G69/40 , C08G69/48
摘要： Disclosed is a polymer conjugate of folic acid or a folic acid derivative, wherein an amide bond is not used. The compound has chemical stability and adequate drug release rate in the living organism. Specifically disclosed is a polymer conjugate of folic acid or a folic acid derivative, wherein a substituent represented by formula (I) is bonded to a carboxy group of a block copolymer which is composed of a polyethylene glycol and a polymer having a carboxy group in a side chain, or a pharmacologically acceptable salt thereof. [In the formula, A represents a monocyclic or fused aromatic group; G represents an optionally substituted (C1-C6) alkylene group; Y represents a hydrogen atom or a substituent; and E represents a residue of folic acid or a folic acid derivative.]
摘要翻译： 公开了叶酸或叶酸衍生物的聚合物缀合物，其中不使用酰胺键。 该化合物在生物体中具有化学稳定性和足够的药物释放速率。 具体公开的是叶酸或叶酸衍生物的聚合物缀合物，其中由式（I）表示的取代基与由聚乙二醇和具有羧基的聚合物组成的嵌段共聚物的羧基键合 侧链或其药理学上可接受的盐。 [式中，A表示单环或稠合芳基; G表示任选取代的（C 1 -C 6）亚烷基; Y表示氢原子或取代基; E表示叶酸或叶酸衍生物的残基。]
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公开(公告)号：US06500816B1
公开(公告)日：2002-12-31
申请号：US09786874
申请日：2001-03-12
申请人： Hisao Ekimoto , Masao Onishi , Chieko Seno , Teruyuki Sakai
发明人： Hisao Ekimoto , Masao Onishi , Chieko Seno , Teruyuki Sakai
IPC分类号： A61K31555
CPC分类号： C07D487/22 , A61K41/0057 , A61K41/0076 , C09B23/0066 , C09B23/02 , C09B23/10
摘要： Effective treatment of tumors, especially carcinomas, can be achieved by administering to man a photochemotherapeutic agent containing as an active ingredient a compound showing maximum absorption in the wavelength region of 800 to 1,200 nm, and then applying light rays of a wavelength of 800 to 1,200 nm.
摘要翻译： 肿瘤特别是癌的有效治疗可以通过给人一种光化学治疗剂来实现，该光化学治疗剂含有在800至1,200nm的波长区域显示最大吸收的化合物作为活性成分，然后施加波长为800至1,200的光线 nm。
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公开(公告)号：US20120116051A1
公开(公告)日：2012-05-10
申请号：US13319175
申请日：2010-05-12
CPC分类号： C08G69/10 , A61K31/167 , A61K31/19 , A61K31/195 , A61K31/337 , A61K31/365 , A61K31/4745 , A61K31/52 , A61K31/573 , A61K31/704 , A61K31/7052 , A61K31/7068 , A61K47/60 , A61K47/645 , C08G69/40 , C08G69/48
摘要： A polymer conjugate of a physiologically active substance, which enables drug release independent of a biological enzyme and can be expected to have a high therapeutic effect, is demanded.Provided is a polymer conjugate of a physiologically active substance, comprising a block copolymer of a polyethylene glycol moiety and a polymer having two or more carboxy groups, in which a substituent represented by general formula (I) or general formula (II) is linked to at least one of the side-chain carboxy groups of the block copolymer via an amide bond [in the formula, R8 and R9 each independently are hydrogen atom or (C1-C6)alkyl which may have a substituent, R10 is hydrogen atom, (C1-C40)alkyl which may have a substituent, (C1-C40) aralkyl group which may have a substituent, an aromatic group which may have a substituent, an amino acid residue having a protected carboxy group, or a sugar residue which may have a substituent, CX—CY represents CH—CH or C═C (double bond), and A represents a residue obtained by removing, from a physiologically active substance having one or more hydroxy groups, one of the one or more hydroxy groups].
摘要翻译： 需要生物活性物质的聚合物缀合物，其使药物释放与生物酶无关并且可以预期具有高治疗效果。 提供了一种生理活性物质的聚合物缀合物，其包含聚乙二醇部分和具有两个或更多个羧基的聚合物的嵌段共聚物，其中由通式（I）或通式（II）表示的取代基与 嵌段共聚物中的至少一个侧链羧基通过酰胺键[在式中，R8和R9各自独立地为氢原子或可具有取代基的（C1-C6）烷基，R10为氢原子（ 可以具有取代基的C 1 -C 40的烷基，可以具有取代基的（C 1〜C 40）芳烷基，可以具有取代基的芳香族基，具有被保护的羧基的氨基酸残基， 取代基，CX-CY表示CH-CH或C = C（双键），A表示通过从具有一个或多个羟基的生理活性物质除去一个或多个羟基之一而获得的残基]。
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公开(公告)号：US08920788B2
公开(公告)日：2014-12-30
申请号：US12922747
申请日：2009-03-17
申请人： Masayuki Kitagawa , Chieko Seno
发明人： Masayuki Kitagawa , Chieko Seno
IPC分类号： A61K31/74 , A61K31/352 , A61K31/197 , A61K31/405 , A61K31/407 , A61K31/704 , A61K47/48 , C08G69/10 , C08G69/40 , C08G69/48
CPC分类号： A61K31/352 , A61K31/197 , A61K31/405 , A61K31/407 , A61K31/704 , A61K47/60 , A61K47/645 , C08G69/10 , C08G69/40 , C08G69/48
摘要： Disclosed is a water-soluble high-molecular weight conjugate of physiologically active substances which enable medicament to release without depending on the enzymes in a living body and which is expected to have a useful therapeutic effect. A high-molecular weight conjugate of a physiologically active substance has a substituent group represented by a general formula (1) bonded to a side-chain carboxy group of a block copolymer which has a polyethylene glycol moiety and either a polyaspartic acid moiety or a polyglutamic acid moiety. Formula (1): —Ar—CR15R16-O—C(═O)-A [In the formula: Ar represents an aromatic hydrocarbon group optionally a substituent group, or an aromatic heterocyclic group optionally having a substituent group; R15 and R16 independently represent a hydrogen atom or a (C1-C6) alkyl group optionally having a substituent group; and A represents a residual group of a physiologically active substance that has an carboxy group, or a residual group of a physiologically active substance that has an amino group].
摘要翻译： 公开了一种生理活性物质的水溶性高分子量缀合物，其能够使药物在不依赖于活体内的酶的情况下释放并且预期具有有用的治疗效果。 生理活性物质的高分子量缀合物具有与通式（1）表示的通式（1）所表示的取代基，该通式（1）与具有聚乙二醇部分和聚天冬氨酸部分或聚谷氨酸的嵌段共聚物的侧链羧基键合 酸部分。 式（1）：-Ar-CR 15 R 16 -O-C（= O）-A [式中，Ar表示可以具有取代基的芳香族烃基或任选具有取代基的芳香族杂环基， R 15和R 16独立地表示氢原子或任选具有取代基的（C1-C6）烷基; A表示具有羧基的生理活性物质或具有氨基的生理活性物质的残基的残基。
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公开(公告)号：US08808749B2
公开(公告)日：2014-08-19
申请号：US13319175
申请日：2010-05-12
IPC分类号： A61K9/14 , A61K31/365 , A61K31/19 , A61K31/195 , A61K31/337 , C08G69/10 , A61K47/48 , A61K31/167 , C08G69/48 , A61K31/573 , A61K31/7068 , A61K31/704 , A61K31/52 , C08G69/40 , A61K31/4745 , A61K31/7052
CPC分类号： C08G69/10 , A61K31/167 , A61K31/19 , A61K31/195 , A61K31/337 , A61K31/365 , A61K31/4745 , A61K31/52 , A61K31/573 , A61K31/704 , A61K31/7052 , A61K31/7068 , A61K47/60 , A61K47/645 , C08G69/40 , C08G69/48
摘要： A polymer conjugate of a physiologically active substance, which enables drug release independent of a biological enzyme and can be expected to have a high therapeutic effect, is demanded.Provided is a polymer conjugate of a physiologically active substance, comprising a block copolymer of a polyethylene glycol moiety and a polymer having two or more carboxy groups, in which a substituent represented by general formula (I) or general formula (II) is linked to at least one of the side-chain carboxy groups of the block copolymer via an amide bond [in the formula, R8 and R9 each independently are hydrogen atom or (C1-C6)alkyl which may have a substituent, R10 is hydrogen atom, (C1-C40)alkyl which may have a substituent, (C1-C40) aralkyl group which may have a substituent, an aromatic group which may have a substituent, an amino acid residue having a protected carboxy group, or a sugar residue which may have a substituent, CX—CY represents CH—CH or C═C (double bond), and A represents a residue obtained by removing, from a physiologically active substance having one or more hydroxy groups, one of the one or more hydroxy groups].
摘要翻译： 需要生物活性物质的聚合物缀合物，其使药物释放与生物酶无关并且可以预期具有高治疗效果。 提供了一种生理活性物质的聚合物缀合物，其包含聚乙二醇部分和具有两个或更多个羧基的聚合物的嵌段共聚物，其中由通式（I）或通式（II）表示的取代基与 嵌段共聚物中的至少一个侧链羧基通过酰胺键[在式中，R8和R9各自独立地为氢原子或可具有取代基的（C1-C6）烷基，R10为氢原子（ 可以具有取代基的C 1 -C 40的烷基，可以具有取代基的（C 1〜C 40）芳烷基，可以具有取代基的芳香族基，具有被保护的羧基的氨基酸残基， 取代基，CX-CY表示CH-CH或C = C（双键），A表示通过从具有一个或多个羟基的生理活性物质除去一个或多个羟基之一而获得的残基]。
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公开(公告)号：US20110201754A1
公开(公告)日：2011-08-18
申请号：US12922747
申请日：2009-03-17
申请人： Masayuki Kitagawa , Chieko Seno
发明人： Masayuki Kitagawa , Chieko Seno
CPC分类号： A61K31/352 , A61K31/197 , A61K31/405 , A61K31/407 , A61K31/704 , A61K47/60 , A61K47/645 , C08G69/10 , C08G69/40 , C08G69/48
摘要： Disclosed is a water-soluble high-molecular weight conjugate of physiologically active substances which enable medicament to release without depending on the enzymes in a living body and which is expected to have a useful therapeutic effect. A high-molecular weight conjugate of a physiologically active substance has a substituent group represented by a general formula (1) bonded to a side-chain carboxy group of a block copolymer which has a polyethylene glycol moiety and either a polyaspartic acid moiety or a polyglutamic acid moiety. Formula (1): —Ar—CR15R16-O—C(═O)-A [In the formula: Ar represents an aromatic hydrocarbon group optionally a substituent group, or an aromatic heterocyclic group optionally having a substituent group; R15 and R16 independently represent a hydrogen atom or a (C1-C6) alkyl group optionally having a substituent group; and A represents a residual group of a physiologically active substance that has an carboxy group, or a residual group of a physiologically active substance that has an amino group].
摘要翻译： 公开了一种生理活性物质的水溶性高分子量缀合物，其能够使药物在不依赖于活体中的酶的情况下释放并且预期具有有用的治疗效果。 生理活性物质的高分子量缀合物具有与通式（1）表示的通式（1）表示的取代基，该通式结合到具有聚乙二醇部分和聚天冬氨酸部分或聚谷氨酸的嵌段共聚物的侧链羧基上 酸部分。 式（1）：-Ar-CR 15 R 16 -O-C（= O）-A [式中，Ar表示可以具有取代基的芳香族烃基或任选具有取代基的芳香族杂环基， R 15和R 16独立地表示氢原子或任选具有取代基的（C1-C6）烷基; A表示具有羧基的生理活性物质或具有氨基的生理活性物质的残基的残基。
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公开(公告)号：US20090239782A1
公开(公告)日：2009-09-24
申请号：US12311086
申请日：2007-09-27
CPC分类号： A61K31/787 , C08G69/10 , C08G73/1092 , C08G81/00 , C08G2650/38
摘要： Provided is a high-molecular weight conjugate of resorcinol derivatives which is excellent in water solubility and stability and has high antitumor activity even when used in a smaller total drug amount than the resorcinol derivatives. The high-molecular weight conjugate of resorcinol derivatives comprises a structure in which a carboxyl group of polymer moiety having a carboxyl group in the side chain and polyethylene glycol moiety is linked to a hydroxyl group of resorcinol derivatives via an ester bond.
摘要翻译： 提供了间苯二酚衍生物的高分子量缀合物，其水溶性和稳定性优异，并且即使以比间苯二酚衍生物更小的总药物量使用也具有高抗肿瘤活性。 间苯二酚衍生物的高分子量缀合物包括其侧链中具有羧基的聚合物部分的羧基和聚乙二醇部分通过酯键与间苯二酚衍生物的羟基连接的结构。
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