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US 7,759,502 B2Granted
Stilbene derivatives and their use for binding and imaging amyloid plaques
AssigneeThe Trustees of the University of Pennsylvania
InventorsHank F. Kung, Mei-Ping Kung, Zhi-Ping Zhuang
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Abstract
This invention relates to a method of imaging amyloid deposits and to labeled compounds, and methods of making labeled compounds useful in imaging amyloid deposits. This invention also relates to compounds, and methods of making compounds for inhibiting the aggregation of amyloid proteins to form amyloid deposits, and a method of delivering a therapeutic agent to amyloid deposits.
Claims9
A compound of general Formula II:
- or a pharmaceutically acceptable salt thereof, wherein:
- Z is O;
- R9, R10 and R11, in each instance, is independently selected from the group consisting of hydrogen, halogen, C1-4 alkyl, cyano, carboxy(C1-5)alkyl, trifluoromethyl, nitro, methylamino, dimethylamino, halo(C1-4)alkyl, and formyl;
- R12 is selected from the group consisting of:
- a. C1-4 alkylthio,
- b. C1-4 alkylsulfonyl,
- c. hydroxy,
- d. C1-4 alkoxy,
- e. NR13R14, wherein
- R13 and R14 are hydrogen or C1-4 alkyl,
- f. phenyl(C1-4)alkyl,
- g. C6-10 aryl,
- h. heteroaryl,
- i. heterocycle,
- j. heterocycle(C1-4)alkyl, and
- k. C3-6 cycloalkyl,
- wherein said phenyl(C1-4)alkyl, C6-10 aryl, heteroaryl, heterocycle, heterocycle(C1-4)alkyl or C3-6 cycloalkyl are substituted with one of the following:
- C1-4 alkylthio, C1-4 alkyl sulfonyl, methoxy, hydroxy, dimethylamino or methylamino;
- and
- X′ is 125I, 123I, 131I, 18F, 76Br, 77Br or Sn(alkyl)3.
17 more elements
A compound of general Formula II:
- or a pharmaceutically acceptable salt thereof, wherein:
- Z is O or S;
- R9 is hydrogen;
- R10 is hydrogen;
- R11 is hydrogen, halogen, C1-4 alkyl, cyano, carboxy(C1-5)alkyl, trifluoromethyl, nitro, methylamino, dimethylamino, halo(C1-4)alkyl, or formyl;
- R12 is C1-4 alkylthio, C1-4 alkylsulfonyl, hydroxy, C1-4 alkoxy or NR13R14;
- and
- x′ is 125I, 123I, 131I, 18F, 76Br, 77Br or Sn(alkyl)3.
5 more elements
Dependencies are inferred from the claim text.