US6500918B2
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Conjugate comprising an antinociceptive agent covalently bonded to a blood component
Assignee: Conjuchem LLC
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Filing: 2001-03-01
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Granted: 2002-12-31
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Expires: 2021-03-01
Abstract
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.
Inventors
- 👤 Alan M. Ezrin
- 👤 Dominique P. Bridon
- 👤 Darren L. Holmes
- 👤 Peter G. Milner
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 10:56
CPC Classifications
C; C07; C07K; C07K14/00; C07K14/435; C07K14/665; C07K14/70; A; A61; A61K; A61K47/00; A61K47/50; A61K47/51; A61K47/62; A61K47/64; A61K38/00; C07K2319/00
Claims Analysis
Total Claims: 19
Claim 1
Independent Claim
51 words
A conjugate comprising an antinociceptive agent derivative covalently bonded to albumin, the antinociceptive agent derivative comprising an antinociceptive agent coupled thereto to a reactive entity that reacts with a functionality on albumin to covalently bond the antinociceptive agent derivative to albumin, the ratio of antinociceptive agent derivative to albumin being 1:1.
Claim 2
Dependent Claim
51 words
A conjugate comprising an antinociceptive agent derivative covalently bonded to albumin, the antinociceptive agent derivative comprising an antinociceptive agent coupled thereto to a reactive entity that reacts with a functionality on albumin to covalently bond the antinociceptive agent derivative to albumin, the ratio of antinociceptive agent derivative to albumin being 1:1.
Claim 3
Dependent Claim
18 words
A conjugate as claimed in claim 1 wherein the albumin is an isolated albumin taken from a patient.
Claim 4
Dependent Claim
15 words
A conjugate as claimed in claim 1 wherein the albumin is from a commercial source.
Claim 5
Dependent Claim
21 words
A conjugate as claimed in claim 1 wherein the reactive entity is coupled to the antinociceptive agent via a linking group.
Claim 6
Dependent Claim
14 words
A conjugate as claimed in claim 1 wherein the antinociceptive agent is an opioid.
Claim 7
Dependent Claim
22 words
A conjugate as claimed in claim 5 wherein the opioid is selected from the group consisting of dynorphins, endorphins, enkephalins and deltorphins.
Claim 8
Dependent Claim
17 words
A conjugate as claimed in claim 6 wherein the opioid is dynorphin A or an analog thereof.
Claim 9
Dependent Claim
14 words
A conjugate as claimed in claim 1 wherein the reactive entity is a maleimide.
Claim 10
Dependent Claim
45 words
A conjugate comprising an opioid derivative covalently bonded to albumin, the opioid derivative comprising an opioid coupled to a reactive entity that reacts with a functionality on albumin to covalently bond the opioid derivative to albumin, the ratio of opioid derivative to albumin being 1:1.
Claim 11
Dependent Claim
45 words
A conjugate comprising an opioid derivative covalently bonded to albumin, the opioid derivative comprising an opioid coupled to a reactive entity that reacts with a functionality on albumin to covalently bond the opioid derivative to albumin, the ratio of opioid derivative to albumin being 1:1.
Claim 12
Dependent Claim
22 words
A conjugate as claim in claim 9 wherein the opioid is selected from the group consisting of dynorphins, endorphins, enkephalins and deltorphins.
Claim 13
Dependent Claim
17 words
A conjugate as claimed in claim 10 wherein the opioid is dynorphin A or an analog thereof.
Claim 14
Dependent Claim
14 words
A conjugate as claimed in claim 9 wherein the reactive entity is a maleimide.
Claim 15
Dependent Claim
13 words
A conjugate comprising a compound of formula covalently bonded to albumin ex vivo.
Claim 16
Dependent Claim
13 words
A conjugate comprising a compound of formula covalently bonded to albumin ex vivo.
Claim 17
Dependent Claim
19 words
A conjugate as claimed in claim 13 wherein the compound is bonded to albumin in a ratio of 1:1.
Claim 18
Dependent Claim
18 words
A conjugate as claimed in claim 13 wherein the albumin is an isolated albumin taken from a patient.
Claim 19
Dependent Claim
15 words
A conjugate as claimed in claim 13 wherein the albumin is from a commercial source.
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USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 2005-12-30 | 2006-07-01 | 2006-12-31 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 2009-12-30 | 2010-07-01 | 2010-12-31 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2013-12-30 | 2014-07-01 | 2014-12-31 | $7700.00 | Window Closed / Lapsed |