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US 8,143,302 B2Granted
Methods and compositions for diagnostic and therapeutic targeting of COX-2
AssigneeVanderbilt University
InventorsLawrence J. Marnett, Md. Jashim Uddin, Brenda C. Crews
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Abstract
The presently disclosed subject matter provides compositions that selectively bind cyclooxygenase-2 and comprise a therapeutic and/or diagnostic moiety. Also provided are methods for using the disclosed compositions for diagnosing (i.e., by imaging) a target cell and/or treating a disorder associated with a cyclooxygenase-2 biological activity.
Claims43
A therapeutic and/or diagnostic agent having a structural formula:
- wherein:
- R3═C1 to C3 alkyl or branched alkyl, NH2, or a dipolar N3 group;
- X is an active agent;
- A is a tether, wherein the tether is selected from the group consisting of an alkylamide tether, a PEG tether, an alkylpiperazine tether, and a phenylene tether;
- B is O or —NH;
- n is 0-4.
3 more elements
A method for synthesizing a therapeutic and/or diagnostic agent, the method comprising:
- (a) providing a derivative of a non-steroidal anti-inflammatory drug (NSAID), said derivative comprising a carboxylic acid moiety, and wherein the NSAID is an indolyl amine or a celecoxib analog;
- (b) derivatizing the carboxylic acid moiety to a secondary amide or an ester;
- and
- (c) complexing an active agent to the secondary amide or the ester,
- wherein:
- (i) the active agent comprises a therapeutic moiety, a diagnostic moiety, or both a therapeutic moiety and a diagnostic moiety;
- (ii) the active agent is complexed to the derivative of the NSAID via a tether;
- and
- (iii) the therapeutic and/or diagnostic agent selectively binds to cyclooxygenase-2 (COX-2), and further wherein the therapeutic and/or diagnostic agent has a structural formula:
- where:
- R3═C1 to C3 alkyl or branched alkyl, NH2, or a dipolar N3 group;
- X is an active agent;
- A is a tether selected from the group consisting of an alkylamide tether, a PEG tether, an alkylpiperazine tether, and a phenylene tether;
- B is O or —NH;
- n is 0-4.
12 more elements
A method for imaging a target cell in a subject, the method comprising:
- (a) administering to the subject a diagnostic agent under conditions sufficient for contacting the diagnostic agent with the target cell, wherein the diagnostic agent has a structural formula:
- where:
- R3═C1 to C3 alkyl or branched alkyl, NH2, or a dipolar N3 group;
- X is a detectable moiety;
- A is a tether, wherein the tether is selected from the group consisting of an alkylamide tether, a PEG tether, an alkylpiperazine tether, and a phenylene tether;
- B is O or —NH;
- n is 0-4;
- and
- (b) detecting the detectable moiety.
6 more elements
Dependencies are inferred from the claim text.