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US 6,720,327 B2Granted
Lactone integrin antagonists
AssigneePharmacia Corporation
InventorsPeter Ruminski, Thomas D. Penning, Lan Jiang, Balekudru Devadas, Thomas Rogers, Jennifer VanCamp, Chester Yuan
Life of this patent
Estimating the term…
Abstract
The present invention relates to a class of compounds represented by the Formula I. or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula I, and methods of selectively inhibiting or antagonizing the αvβ3 and/or the αvβ5 integrin.
Claims5
A compound of the Formula:
- wherein:
- y is zero;
- z is 1;
- A is C;
- R2, R3, and R4 are H, OH, or haloalkyl;
- Y is N—R1;
- R9 is H;
- R1 taken together with R8 forms a 4-12 membered dinitrogen containing heterocycle optionally substituted with one or more substituent selected from the group consisting of lower alkyl, hydroxy, keto, alkoxy, halogen, phenyl, amino, carboxyl or carboxyl ester, and fused phenyl;
- and
- R5, R6 and R7 are independently selected from the group consisting of hydrogen, alkyl, alkenyl, alkynyl, phenyl, carboxyl derivatives, haloalkyl, cycloalkyl, monocyclic heterocycles optionally substituted with alkyl, halogen, haloalkyl, cyano, hydroxy, nitro, alkoxy, aryloxy, alkylsulfonyl, arylsulfonyl, sulfonamide, thio, alkylthio, carboxyl derivatives, amino, amido, about C1 to about C10 alkyl optionally substituted with one or more of halo, haloalkyl, hydroxy, alkoxy, aryloxy, thio, alkylthio, alkynyl, alkenyl, alkyl, arylthio, alkylsulfoxide, alkylsulfonyl, arylsulfoxide, arylsulfonyl, cyano, nitro, amino, alkylamino, dialkylamino, alkylsulfonamide, phenylsulfonamide, acylamide, carboxyl derivatives, sulfonamide, sulfonic acid, phosphonic acid derivatives, phosphinic acid derivatives, phenyl, phenylthio, phenylsulfoxide, or phenylsulfone all optionally substituted on the phenyl ring with halo, alkyl, haloalkyl, cyano, nitro, hydroxy, carboxyl derivatives, alkoxy, phenyloxy, amino, alkylamino, dialkylamino, amido, phenyl, fused phenyl, monocyclic heterocycles, and fused monocyclic heterocycles, monocyclic heterocyclicthio, monocyclic heterocycliesulfoxide, and monocyclic heterocyclic sulfone, which can be optionally substituted with halo, haloalkyl, nitro, hydroxy, alkoxy, fused phenyl, or alkyl, alkylcarbonyl, haloalkylcarbonyl, and phenylcarbonyl, phenyl optionally substituted in one or more positions with halo, haloalkyl, alkyl, alkoxy, phenyloxy, methylenedioxy, ethylenedioxy, alkylthio, haloalkylthio, thio, hydroxy, cyano, nitro, acyloxy, carboxyl derivatives, carboxyalkoxy, amido, acylamino, amino, alkylamino, dialkylamino, trifluoroalkoxy, trifluoromethylsulfonyl, alkylsulfonyl, sulfonic acid, sulfonamide, phenyl, fused phenyl, monocyclic heterocycles and fused monocyclic heterocycles.
7 more elements
A compound selected from the group consisting of
- or isomers or enantiomers or tautomers or polymorphs thereof.
Dependencies are inferred from the claim text.