- Document Number:
20160347725
- Appl. No:
15/116764
- Application Filed:
February 04, 2015
- نبذة مختصرة :
This disclosure relates to small molecule inhibitors of paxillin and paxillin binding, and related compositions and methods of treatment.
- Claim:
1. A compound having the structure of Formula (I): [chemical expression included] or a pharmaceutically acceptable salt thereof, wherein: X is O or S; Z is O or NH; R1 is selected from the group consisting of hydrogen, alkyl and arylalkyl; R2 is aryl, wherein the aryl group is optionally substituted one or more times with a substituent selected from the group consisting of halogen and alkoxy; R3, independently for each occurrence, is selected from the group consisting of alkyl, alkenyl, alkoxy, trifluoromethoxy, acetyl, aryl, hydroxy, halogen, cyano, nitro, amino, alkylamino, diakylamino, amido, alkylamido and arylamido; or wherein any two adjacent R3 may combine to form a fused aromatic ring, wherein said fused aromatic ring can be substituted one or more times with R4; R4, independently for each occurrence, are selected from the group consisting of alkyl, alkenyl, alkoxy, trifluoromethoxy, acetyl, aryl, hydroxy, halogen, cyano, nitro, amino, alkylamino, diakylamino, amido, alkylamido and arylamido; and m is 0, 1, 2, 3 or 4.
- Claim:
2. The compound of claim 1, wherein R3, independently for each occurrence, is selected from the group consisting of alkyl, alkenyl, alkoxy, trifluoromethoxy, acetyl, aryl, hydroxy, halogen, cyano, nitro, amino, alkylamino, diakylamino, amido, alkylamido and arylamido.
- Claim:
3. The compound of claim 1 having the structure of Formula (II): [chemical expression included] or a pharmaceutically acceptable salt thereof, wherein: R3 and R4, independently for each occurrence, are selected from the group consisting of alkyl, alkenyl, alkoxy, trifluoromethoxy, acetyl, aryl, hydroxy, halogen, cyano, nitro, amino, alkylamino, diakylamino, amido, alkylamido and arylamido; m is 0, 1 or 2; and n is 0, 1, 2, 3 or 4.
- Claim:
4. The compound of claim 1 wherein R1 is hydrogen.
- Claim:
5. The compound of claim 2, wherein: R1 is hydrogen; R2 is aryl, wherein the aryl group is optionally substituted one or more times with a substituent selected from the group consisting of halogen and alkoxy; R3, independently for each occurrence, is selected from the group consisting of alkoxy and hydroxy; and m is 0, 1 or 2.
- Claim:
6. The compound of claim 3, wherein: R3, independently for each occurrence, is selected from the group consisting of alkoxy and halide; and R4 is hydrogen.
- Claim:
7. The compound of claim 1, wherein: R2 is selected from the group consisting of phenyl, methoxyphenyl, trimethoxyphenyl, bromomethoxyphenyl and dibromomethoxyphenyl.
- Claim:
8. The compound of any one of the preceding claims, wherein R2 is 3,4,5-trimethoxyphenyl.
- Claim:
9. (canceled)
- Claim:
10. (canceled)
- Claim:
11. (canceled)
- Claim:
12. (canceled)
- Claim:
13. The compound of claim 1, wherein X is O and Z is O.
- Claim:
14. The compound of claim 1, wherein X is O and Z is NH.
- Claim:
15. The compound of claim 1, wherein X is S and Z is O.
- Claim:
16. The compound of claim 1, wherein X is S and Z is NH.
- Claim:
17. The compound of claim 2, selected from the group consisting of: [chemical expression included] or pharmaceutically acceptable salts thereof.
- Claim:
18. The compound of claim 3, selected from the group consisting of: [chemical expression included] or pharmaceutically acceptable salts thereof.
- Claim:
19. The compound: [chemical expression included] or a pharmaceutically acceptable salt thereof.
- Claim:
20. The compound of claim 1, wherein the compound has (R) stereochemistry.
- Claim:
21. The compound of claim 1, wherein the compound has (S) stereochemistry.
- Claim:
22. A pharmaceutical composition comprising a compound of claim 1 and a pharmaceutically acceptable carrier.
- Claim:
23. A method for the treatment of a disorder selected from the group consisting of metastatic cancer, retinal neovascularization, radiation retinopathy, diabetic retinopathy and polycystic kidney disease in a mammal, comprising administering to the mammal an effective amount of a compound of claim 1.
- Claim:
24. (canceled)
- Claim:
25. (canceled)
- Claim:
26. (canceled)
- Claim:
27. (canceled)
- Claim:
28. (canceled)
- Claim:
29. (canceled)
- Claim:
30. (canceled)
- Claim:
31. (canceled)
- Claim:
32. (canceled)
- Claim:
33. (canceled)
- Claim:
34. (canceled)
- Claim:
35. (canceled)
- Claim:
36. (canceled)
- Claim:
37. A method of inhibiting paxillin function in a mammal, comprising administering to the mammal an effective amount of a compound of claim 1.
- Current International Class:
07; 07; 07
- الرقم المعرف:
edspap.20160347725
Processing Request
No Comments.