公开(公告)号：US06602981B2

公开(公告)日：2003-08-05

申请号：US09798114

申请日：2001-03-01

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

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

IPC: C07K700

CPC classification number: C07K14/70 ,  A61K38/00 ,  A61K47/64 ,  C07K14/665 ,  C07K2319/00

Abstract: 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

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

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

IPC: C07K700

CPC classification number: C07K14/70 ,  A61K38/00 ,  A61K47/64 ,  C07K14/665 ,  C07K2319/00

Abstract: 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.

Abstract translation: 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：US06387914B2

公开(公告)日：2002-05-14

申请号：US09841738

申请日：2001-04-24

Applicant: Pascal Druzgala ,  Peter G. Milner

Inventor： Pascal Druzgala ,  Peter G. Milner

IPC: C07D23962

CPC classification number: C07D239/62 ,  C07D239/66

Abstract: The subject invention concerns novel compounds that are useful as ultrashort acting hypnotic barbiturates. Specifically exemplified are derivatives of barbituric and thiobarbituric acids. They are rapidly metabolized by blood and tissue enzymes to form polar metabolites with no hypnotic activity and which are rapidly eliminated.

Abstract translation: 本发明涉及可用作超短效催眠巴比妥酸盐的新型化合物。 具体举例说明的是巴比妥酸和硫代巴比妥酸的衍生物。 它们被血液和组织酶快速代谢，以形成无催眠活性的极性代谢物，并迅速消除。

公开(公告)号：US5668139A

公开(公告)日：1997-09-16

申请号：US470113

申请日：1995-06-06

Applicant: Luiz Belardinelli ,  Ray Olsson ,  Stephen Baker ,  Peter J. Scammells ,  Peter G. Milner ,  Jurg R. Pfister ,  George F. Schreiner

Inventor： Luiz Belardinelli ,  Ray Olsson ,  Stephen Baker ,  Peter J. Scammells ,  Peter G. Milner ,  Jurg R. Pfister ,  George F. Schreiner

IPC: A61K31/52 ,  A61K31/522 ,  A61K31/7076 ,  A61P1/16 ,  A61P3/10 ,  A61P9/00 ,  A61P9/06 ,  A61P11/00 ,  A61P11/06 ,  A61P11/08 ,  A61P13/02 ,  A61P13/12 ,  A61P43/00 ,  C07D473/06 ,  C07D473/08 ,  C07D519/00 ,  C07H19/16 ,  C07H19/167 ,  C07D473/34

CPC classification number: C07H19/16 ,  C07D473/06

Abstract: Adenosine and xanthine derivatives, and compositions comprising those compounds, are potent selective agonists and antagonists of adenosine receptors. The derivatives and compositions are used to treat conditions, including certain cardiac arrhythmias.

Abstract translation: 腺苷和黄嘌呤衍生物以及包含这些化合物的组合物是腺苷受体的有效选择性激动剂和拮抗剂。 衍生物和组合物用于治疗包括某些心律失常的病症。