Inhibitors of (α-v)(β-6) integrin
Disclosed are small molecule inhibitors of αvβ6 integrin, and methods of using them to treat a number of diseases and conditions.
1. A compound of formula (I):
A-B—C (I)
wherein:
A is
B is -alkylene-C(O)N(R)—;
C is
R is H;
R 1 is H;
R 2 is H, alkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, cycloalkyl, -alkylene-alkoxy, alkylene-aryl, or heterocycloalkyl; and
R 3 is H;
or a pharmaceutically acceptable salt thereof.
2. The compound of claim 1 , wherein R 2 is H, (C 1 -C 4 )alkyl, cyclopropyl, CH 2 OMe, phenyl, —CH 2 Ph, pyridinyl, or indolyl.
3. The compound of claim 1 , wherein R 2 is unsubstituted phenyl.
4. The compound of claim 1 , wherein R 2 is substituted phenyl.
5. The compound of claim 4 , wherein the substituted phenyl is substituted with one or more independent instances of alkoxy, OH, halide, —N(H)C(O)alkyl, —C(O)NH 2 , or —C(O)alkyl.
6. The compound of claim 5 , wherein the substituted phenyl is substituted with at least one halide.
7. The compound of claim 6 , wherein the halide is Cl.
8. The compound of claim 1 , wherein the compound is selected from the group consisting of:
9. The compound of claim 1 , wherein the compound is:
10. The compound of claim 1 , wherein the compound is selected from the group consisting of:
11. The compound of claim 1 , wherein the compound is:
12. The compound of claim 1 , wherein the compound is selected from the group:
13. The compound of claim 1 , wherein the compound is:
14. The compound of claim 1 , wherein
a. alkylene in B is n-propyl or n-butyl; and
b. R 2 is selected from unsubstituted phenyl, or phenyl substituted with one or more of alkoxy, alkyl, cycloalkyl, or halide.
15. The compound of claim 1 , wherein
R 2 is H.
16. The compound of claim 1 , wherein the compound is:
17. The compound of claim 1 , wherein the compound is:
18. The compound of claim 1 , wherein R 2 is selected from H, Me, unsubstituted phenyl, or phenyl substituted with one or more of alkoxy, alkyl, cycloalkyl, or halide.
19. The compound of claim 1 , wherein R 2 is H, alkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl.
20. The compound of claim 1 , wherein R 2 is selected from H, Me, unsubstituted phenyl, or phenyl substituted with one or more of methoxy, methyl, cyclopropyl, or halide.
21. The compound of claim 1 , wherein alkylene in B is propyl or butyl.
22. The compound of claim 1 , wherein alkylene in B is n-propyl or n-butyl.
23. The compound of claim 1 , wherein C is
24. The compound of claim 23 , wherein R 2 is H, alkyl, or aryl.
25. The compound of claim 24 , wherein alkylene in B is propyl or butyl.
26. The compound of claim 24 , wherein R 2 is H, methyl or unsubstituted phenyl and alkylene in B is n-propyl or n-butyl.
27. The compound of claim 1 , wherein alkylene in B is n-propyl or n-butyl.
28. The compound of claim 1 , wherein C is
29. The compound of claim 28 , wherein R 2 is H, alkyl, or aryl.
30. The compound of claim 28 , wherein R 2 is unsubstituted phenyl and alkylene in B is n-propyl or n-butyl.
31. The compound of claim 1 , wherein C is
32. The compound of claim 31 , wherein R 2 is H, alkyl, or aryl.
33. The compound of claim 32 , wherein alkylene in B is propyl or butyl.
34. The compound of claim 31 , wherein R 2 is unsubstituted phenyl or phenyl substituted with alkoxy, alkyl or halogen, and the alkylene in B is n-propyl or n-butyl.
35. The compound of claim 34 , wherein R 2 is unsubstituted phenyl or phenyl substituted with methoxy, and alkylene in B is n-propyl.