Title:
SUSTAINED-RELEASE ANALGESIC COMPOUNDS
Document Type and Number:
WIPO Patent Application WO2002098427
Kind Code:
A3
Abstract:
A pharmaceutically active inventive compound comprises two independently active analgesic moieties covalently conjoined through a physiologically labile linker. A preferred embodiment comprises an opioid, such as morphine, covalently linked to at least one analgesic compound selected from the group consisting of an opioid or a no-opioid compound through a physiologically labile linker. Suitable covalent linkers are covalently bonded to the two independently active analgesic compounds through one or more lactone, lactam, or sulfonamido linkages. Suitable linkers include endogenous carboxylate, amido, and sulfonamido moieties, and exogenous moieties that form the aforementioned lactone, lactam or sulfonamido linkages.
Inventors:
ASHTON PAUL
SMITH THOMAS J
CYNKOWSKI TADEUSZ
CYNKOWSKA GRAZYNA
MICKUNAS EDMUND
SMITH THOMAS J
CYNKOWSKI TADEUSZ
CYNKOWSKA GRAZYNA
MICKUNAS EDMUND
Application Number:
PCT/US2002/017613
Publication Date:
February 20, 2003
Filing Date:
June 05, 2002
Export Citation:
Assignee:
CONTROL DELIVERY SYSTEMS (US)
International Classes:
A61K31/16; A61K31/19; A61K31/21; A61K31/216; A61K31/485; A61K31/57; A61K31/60; A61K31/616; A61K47/48; A61P25/04; A61P29/00; A61P43/00; C07D489/00; C07D489/02; C07D489/08; C07D519/00; (IPC1-7): A61K31/485; A61K31/16; A61K31/216; A61K31/60; C07D489/00; C07D489/02; C07D489/04; C07C65/10; A61P25/04; A61P29/00
Domestic Patent References:
| WO1998017673A1 | 1998-04-30 |
Foreign References:
| FR2708611A1 | 1995-02-10 | |||
| US6156764A | 2000-12-05 | |||
| US5190947A | 1993-03-02 | |||
| US5869498A | 1999-02-09 |
Other References:
DATABASE WPI Section Ch Week 199011, Derwent World Patents Index; Class B04, AN 1990-079188, XP002213507
BIDLACK J M ET AL: "N-methyl and N-cyclopropylmethyl-14alpha,14'beta-[dithiobis[2-oxo-2,1 -ethanediyl)imino]]bis(7, 8-dihydro-5beta-methyl-morphinone) MET-TAMO and N-CPM-MET-TAMO: synthesis and opioid binding properties", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, OXFORD, GB, vol. 5, no. 15, 3 August 1995 (1995-08-03), pages 1695 - 1700, XP004135410, ISSN: 0960-894X
KAMEI J ET AL: "EFFECTS OF DOUBLE-ENKEPHALIN (BIPHALIN) AN ENKEPHALIN ANALOGUE ON RESPIRATION AND THE COUGH REFLEX IN RATS", JOURNAL OF PHARMACOBIODYNAMICS, vol. 11, no. 9, 1988, pages 645 - 650, XP001105321, ISSN: 0386-846X
LISO P A ET AL: "Polymeric drugs derived from ibuprofen with improved antiinflammatory profile.", JOURNAL OF BIOMEDICAL MATERIALS RESEARCH, vol. 32, no. 4, 1996, pages 553 - 560, XP001105352, ISSN: 0021-9304
PORTOGHESE P S: "BIVALENT LIGANGDS AND THE MESSAGE-ADDRESS CONCEPT IN THE DESIGN OF SELECTIVE OPIOID RECEPTOR ANTAGONISTS", TRENDS IN PHARMACOLOGICAL SCIENCES, ELSEVIER, AMSTERDAM,, NL, vol. 10, no. 6, 1 June 1989 (1989-06-01), pages 230 - 235, XP000567745, ISSN: 0167-7691
LIPKOWSKI A W ET AL: "BIFUNCTIONAL PHARMACOPHORES. BIOLOGICAL ACTIVITIES OF THE PEPTIDE ANALOG CONTAINING BOTH CASOMORPHINE-LIKE AND SUBSTANCE P ANTAGONIST-LIKE ACTIVE ELEMENTS", POLISH JOURNAL OF PHARMACOLOGY AND PHARMACY, POLISH ACADEMY OF SCIENCES INSTITUTE OF, PL, vol. 44, 1992, pages 25 - 32, XP000995776, ISSN: 0301-0244
PORTOGHESE P S: "The bivalent ligand approach in the design of highly selective opioid receptor antagonists.", NIDA RESEARCH MONOGRAPH. UNITED STATES 1990, vol. 96, 1990, pages 3 - 20, XP002213506, ISSN: 1046-9516
BIDLACK J M ET AL: "N-methyl and N-cyclopropylmethyl-14alpha,14'beta-[dithiobis[2-oxo-2,1 -ethanediyl)imino]]bis(7, 8-dihydro-5beta-methyl-morphinone) MET-TAMO and N-CPM-MET-TAMO: synthesis and opioid binding properties", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, OXFORD, GB, vol. 5, no. 15, 3 August 1995 (1995-08-03), pages 1695 - 1700, XP004135410, ISSN: 0960-894X
KAMEI J ET AL: "EFFECTS OF DOUBLE-ENKEPHALIN (BIPHALIN) AN ENKEPHALIN ANALOGUE ON RESPIRATION AND THE COUGH REFLEX IN RATS", JOURNAL OF PHARMACOBIODYNAMICS, vol. 11, no. 9, 1988, pages 645 - 650, XP001105321, ISSN: 0386-846X
LISO P A ET AL: "Polymeric drugs derived from ibuprofen with improved antiinflammatory profile.", JOURNAL OF BIOMEDICAL MATERIALS RESEARCH, vol. 32, no. 4, 1996, pages 553 - 560, XP001105352, ISSN: 0021-9304
PORTOGHESE P S: "BIVALENT LIGANGDS AND THE MESSAGE-ADDRESS CONCEPT IN THE DESIGN OF SELECTIVE OPIOID RECEPTOR ANTAGONISTS", TRENDS IN PHARMACOLOGICAL SCIENCES, ELSEVIER, AMSTERDAM,, NL, vol. 10, no. 6, 1 June 1989 (1989-06-01), pages 230 - 235, XP000567745, ISSN: 0167-7691
LIPKOWSKI A W ET AL: "BIFUNCTIONAL PHARMACOPHORES. BIOLOGICAL ACTIVITIES OF THE PEPTIDE ANALOG CONTAINING BOTH CASOMORPHINE-LIKE AND SUBSTANCE P ANTAGONIST-LIKE ACTIVE ELEMENTS", POLISH JOURNAL OF PHARMACOLOGY AND PHARMACY, POLISH ACADEMY OF SCIENCES INSTITUTE OF, PL, vol. 44, 1992, pages 25 - 32, XP000995776, ISSN: 0301-0244
PORTOGHESE P S: "The bivalent ligand approach in the design of highly selective opioid receptor antagonists.", NIDA RESEARCH MONOGRAPH. UNITED STATES 1990, vol. 96, 1990, pages 3 - 20, XP002213506, ISSN: 1046-9516
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