Conjugates of mycophenolic acid
View Patent ↗The present invention provides a method for the measurement of an analyte in biological samples whereby an uncompetitive inhibitor is coupled to a ligand and utilized in a homogeneous assay. The analyte can be a drug or drug derivative, hormone, polypeptide, or oligonucleotide. The present invention also provides novel compounds, assay reagents and packaged kits useful for performing such measurements.
1. A ligand-inhibitor conjugate with the structure
wherein n=1 and X is selected from the group consisting of —O—CONH—(CH 2 ) 2 -NH-thyroxine, —O—CONH—(CH 2 ) 2 —NHC(═C)—(CH 2 ) 4 -theophylline, —NH—CO—(CH 2 ) 3 -phenytoin, —O—CO[NH-gentamicin], —NH—CO-Ph-CO[NH-gentamicin] wherein Ph is phenyl, 5′-[[[(digoxin(1,4-oxazepin))-4-yl]-phenyl-4-carbonyl]amino]-, 5′-[[[(digitoxin(1,4-oxazepin))-4-yl]-phenyl-4-carbonyl]amino]-, and
2. The conjugate of claim 1 wherein X is —O—CONH—(CH 2 ) 2 —NH-thyroxine.
3. The conjugate of claim 1 wherein X is —O—CONH—(CH 2 ) 2 —NHC(═C)—(CH 2 ) 4 -theophylline.
4. The conjugate of claim 1 wherein X is
5. The conjugate of claim 1 wherein X is —NH—CO—(CH 2 ) 3 -phenytoin.
6. The conjugate of claim 1 wherein X is —O—CO[NH-gentamicin].
7. The conjugate of claim 1 wherein X is —NH—CO-Ph-CO[NH-gentamicin] and Ph is phenyl.
8. The conjugate of claim 1 wherein X is 5′-[[[(digoxin(1,4-oxazepin))-4-yl]-phenyl-4-carbonyl]amino]-.
9. The conjugate of claim 1 wherein X is 5′-[[[(digitoxin(1,4-oxazepin))-4-yl]-phenyl-4-carbonyl]amino]-.
10. The compound of claim 1 that is 5′-[(theophylline-8-butyramidoethylaminocarbonyloxy)isoprenyl]-MPA.