公开(公告)号：US20060039891A1

公开(公告)日：2006-02-23

申请号：US10493354

申请日：2001-10-29

申请人： Navid Malik ,  Ruth Duncan ,  Donald Tomalia ,  Roseita Esfand

发明人： Navid Malik ,  Ruth Duncan ,  Donald Tomalia ,  Roseita Esfand

IPC分类号： A61K31/765

CPC分类号： A61K31/765

摘要： Antineoplastic dendritic polymer conjugates which are useful drug delivery systems for carrying antineoplastic agents to malignant tumors are prepared. The antineoplastic agent is encapsulated within the dendritic polymer using an ionic charge shunt mechanism, whereby, the antineoplastic agent interacts with the anionic functional groups on the surface of the dendritic polymer allowing the antineoplastic agent to be uptaken by the dendritic polymer through an association with the functional groups of the interior of the dendritic polymer. The antineoplastic dendritic polymer conjugates may be administered intravenously, orally, parentally, subcutaneously, intraarterially or topically to an animal having a malignant tumor in an amount which is effective to inhibit growth of the malignant tumor. The antineoplastic dendritic polymer conjugates exhibit high drug efficiency, high drug carrying capacity, good water solubility, good stability on storage, and reduced toxicity.

摘要翻译： 制备用于将抗肿瘤药物携带到恶性肿瘤中的有用的药物递送系统的抗肿瘤树突状聚合物缀合物。 使用离子电荷分流机制将抗肿瘤剂包封在树突状聚合物内，由此，抗肿瘤剂与树突状聚合物表面上的阴离子官能团相互作用，允许抗肿瘤剂被树状聚合物吸收，通过与 树枝状聚合物内部的官能团。 抗肿瘤性树突状聚合物缀合物可以以有效抑制恶性肿瘤生长的量静脉内，口服，亲本，皮下，动脉内或局部给予具有恶性肿瘤的动物。 抗肿瘤树突状聚合物缀合物具有药效高，药物携带能力强，水溶性好，储存稳定性好，毒性降低。

公开(公告)号：US06585956B2

公开(公告)日：2003-07-01

申请号：US09111232

申请日：1998-07-07

申请人： Navid Malik ,  Ruth Duncan

发明人： Navid Malik ,  Ruth Duncan

IPC分类号： A61K4748

CPC分类号： B82Y5/00 ,  A61K47/6949 ,  C08G69/00 ,  C08G69/02 ,  C08G83/003 ,  Y10S424/16

摘要： Dendritic polymer conjugates which are useful drug delivery systems for carrying platinum containing anti-tumor agents to malignant tumors are prepared by obtaining a dendritic polymer having functional groups which are accessible to a platinum containing compound capable of interacting with the functional groups, contacting the dendritic polymer with the platinum containing compound, and reacting the dendritic polymer with the platinum containing compound. The dendritic polymer platinates may be administered intravenously, orally, parentally, subcutaneously or topically to an animal having a malignant tumor in an amount which is effective to inhibit growth of the malignant tumor. The dendritic polymer platinates exhibit high drug efficiency, high drug carrying capacity, good water solubility, good stability on storage, reduced toxicity, and improved anti-tumor activity in vivo.

摘要翻译： 作为携带含有抗肿瘤剂的含铂药物的有用的药物递送系统的树突状聚合物缀合物通过获得具有官能团的树枝状聚合物来制备，所述树枝状聚合物具有能够与所述官能团相互作用的含铂化合物，所述树枝状聚合物接触所述树枝状聚合物 与含铂化合物反应，并使树枝状聚合物与含铂化合物反应。 树突状聚合物平板可以静脉内，口服，亲本，皮下或局部给予具有有效抑制恶性肿瘤生长的恶性肿瘤的动物。 树状聚合物平板显示出高的药物效率，高的药物携带能力，良好的水溶性，良好的储存稳定性，降低的毒性和改善的体内抗肿瘤活性。

公开(公告)号：US06790437B2

公开(公告)日：2004-09-14

申请号：US09881126

申请日：2001-06-14

申请人： Navid Malik ,  Ruth Duncan

发明人： Navid Malik ,  Ruth Duncan

IPC分类号： A61P3500

CPC分类号： B82Y5/00 ,  A61K47/6949 ,  C08G69/00 ,  C08G69/02 ,  C08G83/003 ,  Y10S424/16

摘要： Dendritic polymer conjugates which are useful drug delivery systems for carrying platinum containing anti-tumor agents to malignant tumors are prepared by obtaining a dendritic polymer having functional groups which are accessible to a platinum containing compound capable of interacting with the functional groups, contacting the dendritic polymer with the platinum containing compound, and reacting the dendritic polymer with the platinum containing compound. The dendritic polymer platinates may be administered intravenously, orally, parentally, subcutaneously or topically to an animal having a malignant tumor in an amount which is effective to inhibit growth of the malignant tumor. The dendritic polymer platinates exhibit high drug efficiency, high drug carrying capacity, good water solubility, good stability on storage, reduced toxicity, and improved anti-tumor activity in vivo.

摘要翻译： 作为携带含有抗肿瘤剂的含铂药物的有用的药物递送系统的树突状聚合物缀合物通过获得具有官能团的树枝状聚合物来制备，所述树枝状聚合物具有能够与所述官能团相互作用的含铂化合物，所述树枝状聚合物接触所述树枝状聚合物 与含铂化合物反应，并使树枝状聚合物与含铂化合物反应。 树突状聚合物平板可以静脉内，口服，亲本，皮下或局部给予具有有效抑制恶性肿瘤生长的恶性肿瘤的动物。 树状聚合物平板显示出高的药物效率，高的药物携带能力，良好的水溶性，良好的储存稳定性，降低的毒性和改善的体内抗肿瘤活性。

公开(公告)号：US07005124B2

公开(公告)日：2006-02-28

申请号：US10016733

申请日：2001-10-29

申请人： Navid Malik ,  Ruth Duncan ,  Donald A. Tomalia ,  Roseita Esfand

发明人： Navid Malik ,  Ruth Duncan ,  Donald A. Tomalia ,  Roseita Esfand

IPC分类号： A61K47/48 ,  A61K33/24 ,  A61K31/80

CPC分类号： B82Y5/00 ,  A61K47/6949 ,  C08G69/00 ,  C08G69/02 ,  C08G83/003 ,  Y10S424/16

摘要： Antineoplastic dendritic polymer conjugates which are useful drug delivery systems for carrying antineoplastic agents to malignant tumors are prepared by obtaining a dendritic polymer having functional groups which are accessible to an antineoplastic agent capable of interacting with the functional groups, and contacting the dendritic polymer with the antineoplastic agent. The preferred platin-based analogues of the antineoplastic agents conjugated to the dendritic polymer may be administered intravenously, orally, parentally, subcutaneously, intramuscularly, intraarterially or topically to an animal having a malignant tumor in an amount which is effective to inhibit growth of the malignant tumor. The antineoplastic dendritic polymer conjugates exhibit high drug efficiency, high drug carrying capacity, good water solubility, good stability on storage, reduced toxicity, and improved anti-tumor activity in vivo.

公开(公告)号：US08058344B2

公开(公告)日：2011-11-15

申请号：US10511317

申请日：2003-03-18

申请人： Sunil Shaunak ,  Elisabetta Gianasi ,  Ruth Duncan

发明人： Sunil Shaunak ,  Elisabetta Gianasi ,  Ruth Duncan

IPC分类号： A61K31/785 ,  C08G63/48 ,  C08G63/91

CPC分类号： A61K47/595

摘要： The present invention relates to new anionic glycodendrimers having new biological activity, processes for preparing them and their use in medicine including veterinary medicine.

摘要翻译： 本发明涉及具有新的生物活性的新型阴离子型糖团聚体，其制备方法及其在包括兽医学的药物中的应用。

公开(公告)号：US5985916A

公开(公告)日：1999-11-16

申请号：US62372

申请日：1998-04-17

申请人： Ruth Duncan ,  Paolo Ferruti ,  Evagoras G. Evagorou

发明人： Ruth Duncan ,  Paolo Ferruti ,  Evagoras G. Evagorou

IPC分类号： A61K47/48 ,  A61K31/28

CPC分类号： A61K47/48207 ,  A61K47/48192

摘要： A polymer-platinum compound for use in tumor treatment is described. The compound is composed of a biodegradable diamido-diamine polymer linked to a platinum species. The platinum species is released from the polymer to yield a platinum species having anti-tumor activity.

摘要翻译： 描述了用于肿瘤治疗的聚合物 - 铂化合物。 该化合物由与铂族物质连接的可生物降解的二酰氨基二胺聚合物组成。 铂族物质从聚合物中释放出来，产生具有抗肿瘤活性的铂族物质。

公开(公告)号：US5965118A

公开(公告)日：1999-10-12

申请号：US60455

申请日：1998-04-14

申请人： Ruth Duncan ,  Evagoras G. Evagorou ,  Robert G. Buckley ,  Elisabetta Gianasi

发明人： Ruth Duncan ,  Evagoras G. Evagorou ,  Robert G. Buckley ,  Elisabetta Gianasi

IPC分类号： A61K31/282 ,  A61K33/24 ,  A61K47/32 ,  A61K47/48 ,  A61P35/00 ,  A61K31/78 ,  C07K5/103 ,  C08F8/42

CPC分类号： A61K47/48176

摘要： A polymer-platinum compound for use in tumor treatment is described. The compound is composed of a polymer backbone having platinum-containing side chains spaced along the polymer backbone. The side chains are composed of an oligopeptide attached at one end to the backbone and at the other end to the platinum compound.

摘要翻译： 描述了用于肿瘤治疗的聚合物 - 铂化合物。 该化合物由聚合物主链组成，其具有沿着聚合物主链间隔开的含铂侧链。 侧链由一端连接于骨架的寡肽和另一端与铂化合物组成。

公开(公告)号：US5622718A

公开(公告)日：1997-04-22

申请号：US406876

申请日：1995-04-28

申请人： Aymen Al-Shamkhani ,  Ruth Duncan

发明人： Aymen Al-Shamkhani ,  Ruth Duncan

IPC分类号： A61K47/48

CPC分类号： C08B37/0084 ,  A61K47/4823

摘要： The invention is an alginate-bioactive agent conjugate connected via an acid labile biodegradable spacer linkage. The conjugate is effective for delivering bioactive agents to targets existing in low-pH environments, either at the target surface or in the target interior.

摘要翻译： PCT No.PCT / GB93 / 01999 Sec。 371日期：1995年4月28日 102（e）日期1995年4月28日PCT 1993年9月23日PCT公布。 公开号WO94 / 07536 日期1994年04月14日本发明是通过酸不稳定的生物可降解间隔物连接物连接的藻酸盐 - 生物活性剂缀合物。 该缀合物有效地将生物活性剂递送至目标表面或目标内部的低pH环境中存在的靶标。

公开(公告)号：US20050214247A1

公开(公告)日：2005-09-29

申请号：US10511317

申请日：2003-03-18

申请人： Sunil Shaunak ,  Elisabetta Gianasi ,  Ruth Duncan

发明人： Sunil Shaunak ,  Elisabetta Gianasi ,  Ruth Duncan

IPC分类号： C07H13/02 ,  A61K31/7028 ,  A61K47/48 ,  A61P1/04 ,  A61P17/00 ,  A61P19/02 ,  A61P29/00 ,  A61P31/04 ,  A61P35/04 ,  A61P37/06 ,  C08B37/00 ,  C08G73/00 ,  A61K31/785 ,  C08G63/48 ,  C08G63/91

CPC分类号： A61K47/595

摘要： The present invention relates to new anionic glycodendrimers having new biological activity, processes for preparing them and their use in medicine including veterinary medicine.

摘要翻译： 本发明涉及具有新的生物活性的新型阴离子型糖团聚体，其制备方法及其在包括兽医学的药物中的应用。

公开(公告)号：US5037883A

公开(公告)日：1991-08-06

申请号：US438352

申请日：1989-11-17

申请人： Jindrich Kopecek ,  Pavla Rejmanova ,  Jiri Strohalm ,  Karel Ulbrich ,  Blanka Rihova ,  Vladimir Chytry ,  John B. Lloyd ,  Ruth Duncan

发明人： Jindrich Kopecek ,  Pavla Rejmanova ,  Jiri Strohalm ,  Karel Ulbrich ,  Blanka Rihova ,  Vladimir Chytry ,  John B. Lloyd ,  Ruth Duncan

IPC分类号： A61K38/00 ,  A61K20060101 ,  A61K31/00 ,  A61K31/70 ,  A61K45/00 ,  A61K47/00 ,  A61K47/48 ,  A61P35/00

CPC分类号： A61K47/48692 ,  A61K47/48176 ,  Y10S530/811 ,  Y10S530/812 ,  Y10S530/815 ,  Y10S530/816

摘要： A polymeric drug comprising an inert synthetic polymeric carrier combined through aminoacid or peptide spacers with a bioactive molecule, a targeting moiety, and an optional cross-linkage, comprises:(a) 5.0 to 99.7 mol % of units derived from N-(2-hydroxypropyl)methacrylamide,(b) 0.2 to 20.0 mol % of units derived from an N-methylacrylcylated peptide, the peptide groups being bound to a bioactive moiety,(c) 0.1 to 94.8 mol % of units derived from N-methacrylamide, N-methacrylic acid or an N-methacrylolated aminoacid or peptide, to which are bound a determinant capable of interacting with specific receptors on cell surfaces,(d) optionally, 0 to 5 mol % of units derived from an N-methacryloylated peptide, the peptide groups being bound to a linking group which is similarly to a similar peptide group attached to another polymer chain, and(e) optionally, as a bioassay label, 0 to 2 mol % units derived from N-methyacryloylated tyrosinamide.

摘要翻译： 包含通过氨基酸或肽间隔物与生物活性分子，靶向部分和任选的交联结合的惰性合成聚合物载体的聚合物药物包括：（a）5.0-99.7mol％衍生自N-（2- 羟丙基）甲基丙烯酰胺，（b）衍生自N-甲基丙烯酰化肽的单元的0.2〜20.0摩尔％，所述肽基团与生物活性部分结合，（c）0.1〜94.8摩尔％的来源于N-甲基丙烯酰胺，N- 甲基丙烯酸或N-甲基丙烯酰化的氨基酸或肽，其结合能够与细胞表面上的特异性受体相互作用的决定簇，（d）任选地0至5摩尔％的衍生自N-甲基丙烯酰基化肽的单元，所述肽基团 与类似于连接于另一聚合物链的肽基团的连接基团结合，和（e）任选地，作为生物测定标记物，衍生自N-甲基丙烯酰基化酪氨酰胺的0至2摩尔％的单位。