Prostaglandin transporter inhibitors
AssigneesAlbert Einstein College of Medicine of Yeshiva University, New York University
InventorsVictor L. Schuster, Yuling Chi, Young-Tae Chang, Jaeki Min
Life of this patent
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Abstract
The present invention generally relates to prostaglandin transport. More specifically, the invention is directed to compounds that inhibit prostaglandin transport and subsequent COX-2 induction, and methods relating thereto.
Claims18
1-12. (canceled)
A method of determining whether a test compound is an inhibitor of a prostaglandin transporter, the method comprising contacting the test compound with the prostaglandin transporter, then determining whether the prostaglandin transporter has less transporter activity when contacted with the test compound than when not so contacted, wherein the test compound is
- or a pharmaceutically acceptable salt, ester, or tautomer thereof, wherein R1 and R2 are independently a C1-C15 straight or branched alkyl, a substituted alkyl, a cycloalkyl, a carboxyalkyl, a substituted cycloalkyl, a C1-C15 straight or branched alkenyl, a substituted alkenyl, a cycloalkenyl, a substituted cycloalkenyl, a C1-C15 straight or branched alkinyl, a substituted alkinyl, a cycloalkinyl, a substituted cycloalkinyl, a C1-C10 straight or branched ether, a substituted ether, a cycloether, an ester, an amide, an acetyl, an aminal, an anhydride, an aryl, a substituted aryl, a heteroaryl, a substituted heteroaryl, a carboxyaryl, a heterocyclic group, a substituted heterocyclic group, a fused cycloalkyl, a substituted fused cycloalkyl, a fused heterocyclic group, a substituted fused heterocyclic group, a fused aryl, a substituted fused aryl, a fused heteroaryl, a substituted fused heteroaryl ring, or any combination thereof, optionally further comprising a hydroxy, an alkoxy, an aryloxy, an oxo, an ester, an ether, an amine, an azo, an azido, a nitro, an imine, an isothionate, a carbonyl, a peroxide, a halogen, a formyl, an acyl, a carboxy, an amido, a carbamoyl, a guanidino, a ureido, a amidino, a thiol, a mercapto, a sulfinyl, a sulfonyl and/or a sulfonamide,
- or is
- or a pharmaceutically acceptable salt, ester, or tautomer thereof, wherein R1, R2 and R3 are independently a C1-C15 straight or branched alkyl, a substituted alkyl, a cycloalkyl, a carboxyalkyl, a substituted cycloalkyl, a C1-C15 straight or branched alkenyl, a substituted alkenyl a cycloalkenyl, a substituted cycloalkenyl, a C1-C15, straight or branched alkinyl, a substituted alkinyl, a cycloalkinyl, a substituted cycloalkinyl, a C1-C10 straight or branched ether, a substituted ether, a cycloether, an ester, an amide, an acetyl, an aminal, an anhydride, an aryl, a substituted aryl, a heteroaryl, a substituted heteroaryl, a carboxyaryl, a heterocylic group, a substituted heterocyclic group, a fused cycloalkyl, a substituted fused cycloalkyl, a fused heterocyclic group, a substituted fused heterocyclic group, a fused aryl, a substituted fused aryl, a fused heteroaryl, a substituted fused heteroaryl ring, or any combination thereof, optionally further comprising a hydroxy, an alkoxy, an aryloxy, an oxo, an ester, an ether, an amine, an azo, an azido, a nitro, an imine, an isothionate, a carbonyl, a peroxide, a halogen, a formyl, an acyl, a carboxy, an amido, a carbamoyl, a guanidino, a ureido, a amidino, a thiol, a mercapto, a sulfinyl, a sulfonyl and/or a sulfonamide and wherein R3 is not
- or is
- or a pharmaceutically acceptable salt ester, or tautomer thereof, wherein R1 and R3 are independently a C1-C15 straight or branched alkyl, a substituted alkyl, a cycloalkyl, a carboxyalkyl, a substituted cycloalkyl, a C1-C15 straight or branched alkenyl, a substituted alkenyl a cycloalkenyl, a substituted cycloalkenyl, a C1-C15 straight or branched alkinyl, a substituted alkinyl, a cycloalkinyl, a substituted cycloalkinyl, a C1-C10 straight or branched ether, a substituted ether, a cycloether, an ester, an amide, an acetyl, an aminal, an anhydride, an aryl, a substituted aryl, a heteroaryl, a substituted heteroaryl, a carboxyaryl, a heterocyclic group, a substituted heterocyclic group, a fused cycloalkyl, a substituted fused cycloalkyl, a fused heterocyclic group a substituted fused heterocyclic group, a fused aryl, a substituted fused aryl, a fused heteroaryl, a substituted fused heteroaryl ring, or any combination thereof, optionally further comprising a hydroxy, an alkoxy, an aryloxy, an oxo, an ester, an ether, an amine, an azo, an azido, a nitro, an imine, an isothionate, a carbonyl, a peroxide, a halogen, a formyl, an acyl, a carboxy, an amido, a carbamoyl, a guanidino, a ureido, a amidino, a thiol, a mercapto, a sulfinyl, a sulfonyl and/or a sulfonamide, and wherein R2 is
14-45. (canceled)
A method of inhibiting COX-2 in a mammal, the method comprising administering an inhibitor of prostaglandin transporter activity to the mammal.
A method of treating pain or inflammation in a mammal, the method comprising administering an inhibitor of prostaglandin transporter activity to the mammal.
60-87. (canceled)
Dependencies are inferred from the claim text.