Patent EP0415693A1 successfully refreshed from Google Patents.
EP0415693A1
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EP
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Composition and method for selective enhancement of opiate activity and reduction of opiate tolerance and dependence
Assignee: Arizona Technology Development Corp
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Filing: 1990-08-28
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Granted: —
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Expires: 2010-08-28
Abstract
Abstract A composition for selectively enhancing opiate activity, including analgesic, anti-tussive, and sedative activity, as well as opiate activity in the treatment of dyspena and modulation of intestinal motility, while reducing tolerance and dependence associated with chronic use of opiate analgesics. More specifically, a composition and method which selectively enhances opiate analgesia induced at mu (µ) receptors by direct or indirect action at the delta (δ) receptor sites of the central nervous system.
Inventors
- 👤 Frank c/o The University of Arizona Porreca
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-11-03 07:34
CPC Classifications
A; A61; A61K; A61K38/00; A61K38/04; A61P; A61P25/00; A61P25/04; A61P25/30; A61P43/00
Claims Analysis
Total Claims: 14
Claim 1
Independent Claim
37 words
The use of a pharmaceutical composition comprising a δ receptor agonist and an opiate analgesic in the manufacture of a medicament for selective enhancement of the efficacy of opiate activity and reduction of opiate tolerance and dependence.
Claim 2
Dependent Claim
37 words
The use of a pharmaceutical composition comprising a δ receptor agonist and an opiate analgesic in the manufacture of a medicament for selective enhancement of the efficacy of opiate activity and reduction of opiate tolerance and dependence.
Claim 3
Dependent Claim
16 words
A use according to Claim 1, wherein said δ receptor agonist is a direct acting agonist.
Claim 4
Dependent Claim
16 words
A use according to Claim 1, wherein said & receptor agonist is an indirect acting agonist.
Claim 5
Dependent Claim
18 words
A use according any one of the preceding claims, wherein said δ receptor agonist is an endogenous agonist.
Claim 6
Dependent Claim
20 words
A use according to any one of Claims 1 to 3, wherein said δ receptor agonist is an exogenous agonist.
Claim 7
Dependent Claim
18 words
A use according to any one of the preceding claims, wherein said δ receptor agonist is a prodrug.
Claim 8
Dependent Claim
19 words
A use according to any one of the preceding claims, wherein said composition further comprises any pharmaceutically acceptable carrier.
Claim 9
Dependent Claim
42 words
A use according to Claim 1, wherein said δ receptor agonist is selected from the group consisting of [D-Pen², D-Pen⁵] Enkephalin], [D-Pen², L-Pen⁵] Enkephalin, [D-Ala², D-Leu⁵] Enkephalin, [D-Ser², Leu⁵, Thr⁶] Enkephalin, [D-Thr², Leu, Thr⁶] Enkephalin, Leucine-enkephalin, thiorphan, kelatorphan, (R)-3-(N-hydroxy-carboxamido-2-benzylpropanoyl)-L-phenylalanine, (S)-N-[N-1-[[2-2-dimethyl-1,3-dioxolan-4yl)methoxy]carbonyl]-2-phenylethyl]-L-phenylalanine]-β-alanine, and N-[L-(-1-carboxy-2-phenyl)ethyl]-L-phenylalanyl-β-alanine.
Claim 10
Dependent Claim
38 words
A use according to Claim 1 or 8, wherein said opiate analgesic is selected from the group consisting of morphine, heroin, hydromorphone, oxymorphine, metopon, codeine, hydrocodone, drocode, oxycodone, tramadol, pholcodine, levorphanol, methadone, dextromoramide, dipipanone, phenadoxone, meperidine and alphaprodine.
Claim 11
Dependent Claim
34 words
A use according to any one of the preceding claims wherein the composition is intended for administration to patients as a long term treatment or to patients dependent on or tolerant to an opiate.
Claim 12
Dependent Claim
82 words
A kit comprising a pharmaceutical formulation of a µ receptor agonist and, separate or as part of the same formulation, a pharmaceutical formulation of a delta receptor agonist and means to administer the formulation or formulations to a patient, wherein there are respective said formulations for the µ and δ receptor agonists and the kit is adapted for administration of said δ receptor agonist through a different and distinct route of administration from the route of administration of said µ receptor agonist.
Claim 13
Dependent Claim
82 words
A kit comprising a pharmaceutical formulation of a µ receptor agonist and, separate or as part of the same formulation, a pharmaceutical formulation of a delta receptor agonist and means to administer the formulation or formulations to a patient, wherein there are respective said formulations for the µ and δ receptor agonists and the kit is adapted for administration of said δ receptor agonist through a different and distinct route of administration from the route of administration of said µ receptor agonist.
Claim 14
Dependent Claim
25 words
A kit according to Claim 10, 11 or 12, wherein said kit is adapted for intracerebroventricular, subcutaneous or intraperitoneal administration of one or both formulations.
References Cited (Backward Citations)
US4361553A
Cited
WO1989003211A1
Cited
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