Chemistry: natural resins or derivatives; peptides or proteins; – Proteins – i.e. – more than 100 amino acid residues – Chemical modification or the reaction product thereof – e.g.,...
Reexamination Certificate
2005-04-19
2005-04-19
Brumback, Brenda (Department: 1647)
Chemistry: natural resins or derivatives; peptides or proteins;
Proteins, i.e., more than 100 amino acid residues
Chemical modification or the reaction product thereof, e.g.,...
C530S350000, C530S300000
Reexamination Certificate
active
06881829
ABSTRACT:
The present invention provides composition of matter for and methods of treating pain and drug abuse using novel chimeric hybrid molecules containing an opioid moiety of chemically modified morphine (3) that binds to and activates the human mu (μ) opioid receptor, with the opioid moiety linked through a novel linker-hinge (4) to a substance P peptide fragment moiety (5) that binds to and activates the human substance P receptor. The hybrid alkaloid/peptide chimeric molecules produce clinically efficacious opioid analgesia with little or no development of opioid tolerance or formation of opioid dependence. The hybrid alkaloid/peptide analgesics may be administered intrathecally, systemically or orally.
REFERENCES:
patent: 5891842 (1999-04-01), Kream
patent: 6063758 (2000-05-01), Lappi et al.
patent: 6310072 (2001-10-01), Smith et al.
patent: WO 0130371 (2001-05-01), None
Lipkowski, et al, Neuropeptides: Peptide and Nonpeptide Analogs, Peptides: Synthesis, Structures and Applications. 1995, pp 287-320. Academic Press.
Reuler, et al.,The Chronic Pain Syndrone: Misconceptions&Management ,Ann Intern Med. 93:588-596 (1980).
Sriwatankul, et al,Analysis of Narcotic Analgesic usage in the Treatment of Postopertive Pain,JAMA 250:926-929 (1983).
Schechter,Pain&Pain Control in Children,Current Problems in Pediatrics 15 (1985).
Goodman & Gilman,The Pharmacological Basis of Therapeutics511 (7thed. 1985).
Foran, et al,A Substance P-opioid chimeric peptide as a unique nontolerance-forming analgesic,97 PNAS 13:7621-26 (2000).
Egelton, et al,Transport of Opioid Peptides into the Central Nervous System,J Pharm Sci 1998, 87(11):1433-39.
Borchard,Optimizing oral absorption of peptides using prodrug strategies,J Control Release 1999; 62(1-2):231-38.
Stain-Texier,Elevated concentrations of morphine 6-beta-D-glucuronide in brain extracellular fluid despite low blood-brain barrier permeability,Br J Pharmacol 1999; 128(4):917-24.
Merrifield,Solid Phase Synthesis,Science 232: 241-47 (1986).
Barany, et al,Solid-phase peptide synthesis; a silver anniversary report,Int'l J Peptide Protein Res 30:705-39 (1987).
Kent,Chemical Synthesis of Peptides and Proteins,Ann Rev Biochem 57:857-989 (1988).
Kaiser, et al,Peptide&Protein Synthesis by Segment Synthesis-Condensation,Science 243:187-98 (1989).
Kream,Substance P markedly potentiates the antinocicpetive effects of morphine sulphate administered at the spinal level,90 PNAS 5564-68 (1993).
Masczynska, et al,Alternative forms of interaction of substance P and opioids innocicpetive transmission,LTRS Peptide Sci 298, 5:395-98 (1998).
Masczynska, et al,Dual Functional Interactions of Substance P Opioids in Nociceptive Transmission,Analgesia 3:259-68 (1998).
Watson, et al,Tissue Selectivity of Substance P Alkyl Esters Suggesting Multiple Receptors,Euro J Pharmacol 87:77-84 (1983).
Sizheng, et al,Opioid and neurokinin activities of substance P fragments and their analogs,Euro J Pharamcol 193:209-15 (1991).
Lipkowski, et al,An Approach to the Self Regulatory Mechanism of Substance P Actions,33 Life Sciences 141-44 (1983).
Foran, et al,Inhibition of Morphine tolerance Development by a Substance P-Opioid Peptide Chimera,J Pharamcol & Ex Thera 295:3:1142-48 (2000).
Lipkowski, et al,Opioid Peptide Analogues: Reconsideration as a Potentially New Generation of Analgesics,Polish J Chem, 68:907 12 (1994).
Misterek, et al,Spinal Co-Administration of Peptide Substnace P Antagonist Increases Antinociceptive Effect of the Opioid Peptide Biphalin,54 Life Sciences, 14:939-44 (1994).
Foran, et al,Chimeric Peptide for the Treatment of Acute&Chronic PainAnesthesiology 91:3A:A944 (1999).
Langel, et al,Design of chimeric peptide ligands to galanin receptors and substance P receptors,Intl J Peptide & Protein Res 39:6:516-522 (1992).
Cavagnero, et al,Delta opioid Receptor Selectivity Ligands,49 Life Sciences 495-503 (1991).
Carr, et al,Mechanisms of Opioid Analgetic Actions,1 Principles & Practice of Anesthesiology, Ch 32 (1993).
Brumback Brenda
Chimeracom, L.L.C.
Landsman Robert S.
LandOfFree
Chimeric hybrid analgesics does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Chimeric hybrid analgesics, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Chimeric hybrid analgesics will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-3371678