Method for decreasing opioid metabolism

By replacing the 8- or 3-hydroxyl group in opioid receptor-binding compounds with carboxamide or related residues, the compounds achieve enhanced bioavailability and therapeutic efficacy, addressing the limitations of existing opioid receptor-binding agents.
US20060030580A1Inactive Publication Date: 2006-02-09RENESSELAER POLYTECHNIC INST
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Patent Information

Authority / Receiving Office
US · United States
Patent Type
Applications(United States)
Current Assignee / Owner
RENESSELAER POLYTECHNIC INST
Publication Date
2006-02-09
Estimated Expiration
Not applicable · inactive patent
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Abstract

8-Substituted-2,6-methano-3-benzazocines of general streucture I in which A is —CH2—OH, —CH2NH2, —NHSO2CH3, and Y is O, S or NOH are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications. 8-Carboxamides, thiocarboxamides, hydroxyamidines and formamides are preferred.
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Description

CROSS REFERENCE TO RELATED APPLICATIONS

[0001] This application is a continuation of copending U.S. application Ser. No. 10 / 987,527, filed Nov. 12, 2004, which was a continuation of U.S. application Ser. No. 10 / 409,803, filed Apr. 9, 2003, now U.S. Pat. No. 6,887,998, which was a divisional of Ser. No. 10 / 305,287, filed Nov. 26, 2002, now U.S. Pat. No. 6,784,187. U.S. Ser. No. 10 / 305,287 was a continuation-in-part of PCT International application PCT / USO1 / 45581, filed Oct. 31, 2001, and published under PCT Article 21(2) in English on May 10, 2002, as WO 02 / 36573. PCT US01 / 45581 claimed benefit from U.S. provisional application 60 / 244,438, filed Oct. 31, 2000. The entire contents of each of the prior applications are incorporated herein by reference.STATEMENT AS TO RIGHTS UNDER FEDERALLY-SPONSORED RESEARCH

[0002] This invention was made with Government support under Contract No. RO1 DA12180, awarded by the National Institutes of Health. Accordingly, the U.S. Government has certain ri...

Claims

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