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Details for Patent: 7,858,072

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Details for Patent: 7,858,072

Title:Stilbene derivatives and their use for binding and imaging amyloid plaques
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.
Inventor(s): Kung; Hank F. (Wynnewood, PA), Kung; Mei-Ping (Wynnewood, PA), Zhuang; Zhi-Ping (Lansdale, PA)
Assignee: The Trustees of the University of Pennsylvania (Philadelphia, PA)
Filing Date:Dec 19, 2005
Application Number:11/305,350
Claims:1. A compound of Formula Ib, ##STR00055## wherein, n is an integer from one to six; R.sup.1 is selected from the group consisting of: (a) NR.sup.aR.sup.b, wherein R.sup.a and R.sup.b are independently hydrogen, C.sub.1-4 alkyl or (CH.sub.2).sub.dX, where X is halogen, and d is an integer between 1 and 4, (b) hydroxy, (c) C.sub.1-4 alkoxy, and (d) hydroxy(C.sub.1-4)alkyl; R.sup.2 is selected from the group consisting of: ##STR00056## wherein q is an integer from one to 10; Z is selected from the group consisting of -Ch, halogen, halogen substituted benzoyloxy, halogen substituted benzyloxy, halogen substituted phenyl(C.sub.1-4alkyl, halogen substituted aryloxy, and a halogen substituted C.sub.6-10 aryl; and R.sup.30, R.sup.31, R.sup.32 and R.sup.33 are in each instance independently selected from the group consisting of hydrogen, hydroxy, C.sub.1-4 alkoxy, C.sub.1-4 alkyl, hydroxy(C.sub.1-4)alkyl and ##STR00057## wherein X is -Ch or halogen; ##STR00058## wherein Z, R.sup.30, R.sup.31.sub., R.sup.32 and R.sup.33 are as described above, and ##STR00059## wherein Y is selected from the group consisting of halogen, halogen substituted benzoyloxy, halogen substituted phenyl(C.sub.1-4)alkyl, halogen substituted aryloxy, and halogen substituted C.sub.6-10 aryl; U is selected from the group consisting of hydrogen, hydroxy, halogen, halogen substituted benzoyloxy, halogen substituted phenyl(C.sub.1-4)alkyl, halogen substituted aryloxy, and halogen substituted C.sub.6-10 aryl; and R.sup.34, R.sup.35, R.sup.36, R.sup.37, R.sup.38, R.sup.39 and R.sup.40 are in each instance independently selected from the group consisting of hydrogen, halogen, hydroxy, C.sub.1-4 alkoxy, C.sub.1-4 alkyl, and hydroxy(C.sub.1-4)alkyl; R.sup.7 and R.sup.8 are in each instance independently selected from the group consisting of hydrogen, hydroxy, amino, methylamino, dimethylamino, C.sub.1-4 alkoxy, C.sub.1-4 alkyl, and hydroxy(C.sub.1-4)alkyl; provided that if n is one, then said halogen is other than F or .sup.18F.

2. The compound of claim 1, wherein said halogen, in each instance, is a radiolabeled halogen.

3. The compound of claim 1, wherein said halogen, in each instance, is selected from the group consisting of .sup.123I, .sup.125I, .sup.131I, .sup.76Br and .sup.18F.

4. The compound of claim 3, wherein R.sup.1 is NR.sup.aR.sup.b, wherein R.sup.a and R.sup.b are independently hydrogen or C.sub.1-4 alkyl.

5. The compound of claim 1, wherein n is one and wherein R.sup.2 is ##STR00060##

6. The compound of claim 5, wherein q is an integer from 2 to 5.

7. The compound of claim 6, wherein R.sup.7 and R.sup.8 are each hydrogen.

8. The compound of claim 7, wherein R.sup.30, R.sup.31, R.sup.32 and R.sup.33 are, in each instance, hydrogen.

9. The compound of claim 8, having the following formula: ##STR00061## wherein Z is -Ch, .sup.123I, .sup.125I, .sup.131I.

10. The compound of claim 9, having the following formula: ##STR00062##

11. The compound of claim 7, having the following formula: ##STR00063## wherein Z is -Ch, .sup.123I, .sup.125I, .sup.131I.

12. The compound of claim 11, having the following formula: ##STR00064##

13. The compound of claim 4, wherein n is 3.

14. The compound of claim 13, wherein R.sup.2 is ##STR00065##

15. The compound of claim 14, wherein q is an integer from 2 to 5.

16. The compound of claim 15, wherein R.sup.7 and R.sup.8 are each hydrogen.

17. The compound of claim 16, wherein R.sup.30, R.sup.31, R.sup.32 and R.sup.33 are, in each instance, hydrogen.

18. The compound of claim 17, having the following formula: ##STR00066## wherein R.sup.a and R.sup.b are each independently hydrogen or methyl.

19. The compound of claim 17, having the following formula: ##STR00067## wherein Z is -Ch, .sup.123I, .sup.125I, .sup.131I or .sup.18F.

20. The compound of claim 19, having the following formula: ##STR00068##

21. The compound of claim 17, having the following formula: ##STR00069## wherein Z is -Ch, .sup.123I, .sup.125I, .sup.131I or .sup.18F.

22. The compound of claim 21, having the following formula: ##STR00070##

23. The compound of claim 4, wherein R.sup.2 is ##STR00071## wherein U is hydroxy.

24. The compound of claim 23, wherein R.sup.34, R.sup.35R.sup.36, R.sup.37, R.sup.38, R.sup.39 and R.sup.40 are in each instance, hydrogen.

25. The compound of claim 24, having the following structure: ##STR00072## wherein Z is -Ch, .sup.123I, .sup.125I, or .sup.131I.

26. A compound of Formula Ib, having the following structure: ##STR00073## wherein, n is an integer from one to six; R.sup.1 is selected from the group consisting of: (a) NR.sup.aR.sup.b, wherein R.sup.a and R.sup.b are independently hydrogen, C.sub.1-4 alkyl or (CH.sub.2).sub.dX, where X is halogen, and d is an integer between 1 and 4, (b) hydroxy, (c) C.sub.1-4 alkoxy, and (d) hydroxy(C.sub.1-4)alkyl; R.sup.2 is selected from the group consisting of: ##STR00074## wherein q is an integer from 2 to 10; and Z is -Ch; ##STR00075## wherein Z is -Ch, and R.sup.30, R.sup.31, R.sup.32 and R.sup.33 are as described above, and ##STR00076## wherein Y is -Ch; U is selected from the group consisting of hydrogen, hydroxy, halogen, halogen substituted benzoyloxy, halogen substituted phenyl(C.sub.1-4)alkyl, halogen substituted aryloxy, and halogen substituted C.sub.6-10 aryl; and R.sup.34, R.sup.35, R.sup.36, R.sup.37, R.sup.38, R.sup.39 and R.sup.40 are in each instance independently selected from the group consisting of hydrogen, halogen, hydroxy, C.sub.1-4 alkoxy, C.sub.1-4 alkyl, and hydroxy(C.sub.1-4)alkyl; wherein -Ch is a ##STR00077## wherein R.sup.P is hydrogen or a sulfhydryl protecting group, and R.sup.9, R.sup.10, R.sup.11, R.sup.12, R.sup.13, R.sup.14, R.sup.15, R.sup.16, R.sup.43 and R.sup.44 are in each instance independently selected from the group consisting of hydrogen, hydroxy, amino, methylamino, dimethylamino, C.sub.1-4 alkoxy, C.sub.1-4 alkyl, and hydroxy(C.sub.1-4alkyl, and R.sup.7 and R.sup.8 are in each instance independently selected from the group consisting of hydrogen, hydroxy, amino, methylamino, dimethylamino, C.sub.1-4 alkoxy, C.sub.1-4 alkyl, and hydroxy(C.sub.1-4)alkyl.

27. A derivative of a compound of claim 26, wherein said -Ch has the following structure: ##STR00078##

28. A pharmaceutical composition comprising a compound of claim 1.

29. A diagnostic composition for imaging amyloid deposits, comprising a radiolabeled compound of claim 1.

30. A method of imaging amyloid deposits, comprising: (a) introducing into a mammal a detectable quantity of a diagnostic composition of claim 29; (b) allowing sufficient time for the labeled compound to bind to be associated with amyloid deposits; and (c) detecting the labeled compound associated with one or more amyloid deposits.
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