公开(公告)号：US06602981B2

公开(公告)日：2003-08-05

申请号：US09798114

申请日：2001-03-01

申请人： Alan M. Ezrin ,  Dominique P. Bridon ,  Darren L. Holmes ,  Peter G. Milner

发明人： Alan M. Ezrin ,  Dominique P. Bridon ,  Darren L. Holmes ,  Peter G. Milner

IPC分类号： C07K700

CPC分类号： C07K14/70 ,  A61K38/00 ,  A61K47/64 ,  C07K14/665 ,  C07K2319/00

摘要： Conjugates are prepared from antinociceptive agents, particularly opioids or opioid analogs, more particularly dynorphins, endorphins, deltorphins, enkephalins or analogs thereof, by combining said antinociceptive agent with a material providing a functionally reactive group capable of reacting with a blood component (preferably a blood cell or protein). Said conjugates permit extension of the therapeutic life of the antinociceptive agent. They may be administered to patients to alleviate pain, produce analgesic effects, or assist in cases of narcotics withdrawal, and may also be used as probes for receptor activity. The administration to the patient may be made either in vivo or ex vivo and may be performed by either introducing the derivative including the reactive functional group into the patient's vascular system or preparing such a conjugate externally (or in vitro) and introducing that conjugate to the patient's vascular system

公开(公告)号：US06500918B2

公开(公告)日：2002-12-31

申请号：US09798121

申请日：2001-03-01

申请人： Alan M. Ezrin ,  Dominique P. Bridon ,  Darren L. Holmes ,  Peter G. Milner

发明人： Alan M. Ezrin ,  Dominique P. Bridon ,  Darren L. Holmes ,  Peter G. Milner

IPC分类号： C07K700

CPC分类号： C07K14/70 ,  A61K38/00 ,  A61K47/64 ,  C07K14/665 ,  C07K2319/00

摘要： Conjugates are prepared from antinociceptive agents, particularly opioids or opioid analogs, more particularly dynorphins, endorphins, deltorphins, enkephalins or analogs thereof, by combining said antinociceptive agent with a material providing a functionally reactive group capable of reacting with a blood component (preferably a blood cell or protein). Said conjugates permit extension of the therapeutic life of the antinociceptive agent. They may be administered to patients to alleviate pain, produce analgesic effects, or assist in cases of narcotics withdrawal, and may also be used as probes for receptor activity. The administration to the patient may be made either in vivo or ex vivo and may be performed by either introducing the derivative including the reactive functional group into the patient's vascular system or preparing such a conjugate externally (or in vitro) and introducing that conjugate to the patient's vascular system.

摘要翻译： 通过将所述抗伤害感受剂与提供能够与血液成分（优选血液）反应的功能反应性基团的材料组合，由抗伤害感受剂，特别是阿片样物质或阿片样物质类似物，更具体地说是强啡肽，内啡肽，delphphins，脑啡肽或其类似物制备缀合物 细胞或蛋白质）。 所述缀合物允许延长抗伤害感受剂的治疗寿命。 可以向患者施用以缓解疼痛，产生镇痛作用或辅助麻醉药物撤出的情况，也可用作受体活性的探针。 对患者的施用可以在体内或体外制备，并且可以通过将包含反应性官能团的衍生物引入患者的血管系统或者在外部（或体外）中制备这种缀合物并将该缀合物引入到 患者血管系统。

公开(公告)号：US06440417B1

公开(公告)日：2002-08-27

申请号：US09434605

申请日：1999-11-05

申请人： Karen Thibaudeau ,  Dominique Blanchard ,  Dominique P. Bridon ,  Alan M. Ezrin ,  Margaret Hardy ,  Nissab Boudjellab

发明人： Karen Thibaudeau ,  Dominique Blanchard ,  Dominique P. Bridon ,  Alan M. Ezrin ,  Margaret Hardy ,  Nissab Boudjellab

IPC分类号： C07K1644

CPC分类号： C07K16/44 ,  A61K2039/505

摘要： Antibodies to a therapeutic agent and its derivatives and conjugates are disclosed, including antibodies to argatroban and its derivatives and conjugates. The antibodies are useful as reagents in assays and diagnostic kits for determining the concentration of a therapeutic agent or its derivatives and conjugates in biological samples, and further have therapeutic uses in treatment for potential toxicity associated with stable therapeutic conjugates and derivatives, both in vivo and ex vivo.

摘要翻译： 公开了治疗剂及其衍生物和缀合物的抗体，包括阿加曲班及其衍生物和缀合物的抗体。 该抗体可用作用于测定和诊断试剂盒中的试剂，用于确定生物样品中治疗剂或其衍生物和缀合物的浓度，并且还具有用于治疗与稳定的治疗性缀合物和衍生物相关的潜在毒性的治疗用途，包括体内和 离体