Anti-alphavbeta1 integrin compounds and methods

1. A compound, or a salt thereof, having the formula:

wherein,

Ring A is cycloalkyl, heterocycloalkyl, aryl, or heteroaryl;

L 1 is a bond;

L 2 is unsubstituted methylene;

L 3 is substituted or unsubstituted C 1 -C 10 alkylene, substituted or unsubstituted 2 to 10 membered heteroalkylene, substituted or unsubstituted C 3 -C 6 cycloalkylene, or substituted or unsubstituted alkylarylene;

X is a bond, —C—, —C—C—, —C═C—, —C—C—C—, —C═C—C—, —C—C═C—, —O—C—, —C—O—, —C—O—C, —S—C—, —C—S—, —C—S—C—;

Y is a —C(O)N(R 4 )—, substituted or unsubstituted arylene, or substituted or unsubstituted heteroarylene;

R 1 is independently hydrogen, halogen, oxo, —N 3 , —CF 3 , —CCl 3 , —CBr 3 , —CI 3 , —CN, —CHO, —OH, —NH 2 , —COOH, —CONH 2 , —NO 2 , —SH, —SO 2 , —SO 2 Cl, —SO 2 CH 3 —SO 3 H, —OSO 3 H, —SO 2 NH 2 , —NHNH 2 , —ONH 2 , —NHC(O)NHNH 2 , substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, or a detectable moiety;

R 2 is independently hydrogen, halogen, —N 3 , —CF 3 , —CCl 3 , —CBr 3 , —CI 3 , —CN, —CHO, —OH, —NH 2 , —COOH, —CONH 2 , —NO 2 , —SH, —SO 2 , —SO 2 Cl, —SO 2 CH 3 —SO 3 H, —OSO 3 H, —SO 2 NH 2 , —NHNH 2 , —ONH 2 , —NHC(O)NHNH 2 , substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, or a detectable moiety, or wherein if z2 an integer of 2 to 5, two R 2 substituents attached to adjacent ring carbons are optionally joined to form a substituted or unsubstituted aryl or substituted or unsubstituted heteroaryl;

R 3A is hydrogen, —C(NH)NH 2 , —C(NH)R 3D , —C(NR 3C )NH 2 , —C(NR 3C )R 3D , —C(NCN)NH 2 , NH, NH 2 , —C(NH)NHR 3D , —C(NR 3C )NHR 3D , —C(NCN)NHR 3D , substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl;

R 3B is —C(NH)NH 2 , —C(NH)R 3D , —C(NR 3C )NH 2 , —C(NR 3C )R 3D , —C(NCN)NH 2 , NH, NH 2 , —C(NH)NHR 3D , —C(NR 3C )NHR 3D , —C(NCN)NHR 3D , substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl;

R 3A and R 3B are optionally joined to form a substituted or unsubstituted heterocycloalkyl or substituted or unsubstituted heteroaryl;

R 3C and R 3D are independently hydrogen, halogen, oxo, —N 3 , —CF 3 , —CCl 3 , —CBr 3 , —CI 3 , —CN, —CHO, —OH, —NH 2 , —COOH, —CONH 2 , —NO 2 , —SH, —SO 2 , —SO 2 Cl, —SO 2 CH 3 —SO 3 H, —SO 4 H, —SO 2 NH 2 , —NHNH 2 , —ONH 2 , —NHC(O)NHNH 2 , substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl;

R 4 is independently hydrogen or unsubstituted C 1 -C 5 alkyl;

z1 is an integer from 1 to 9; and

z2 is an integer from 1 to 5.

2. The compound of claim 1 , wherein L 3 is substituted or unsubstituted C 1 -C 5 alkylene, substituted or unsubstituted 2 to 6 membered heteroalkylene, or substituted or unsubstituted alkylarylene.

3. The compound of claim 1 , wherein

L 3 is R 6 -substituted C 1 -C 3 alkylene;

R 6 is —NHC(O)R 6A ;

R 6A is —C(NCN)R 6c , —C(NH)R 6C , R 6C -substituted or unsubstituted alkyl, or R 6C -substituted or unsubstituted heteroalkyl;

R 6C is hydrogen, halogen, oxo, —N 3 , —CF 3 , —CCl 3 , —CBr 3 , —CI 3 , —CN, —COR 6D , —OR 6D , —NR 6D R 6E , —COOR 6E , —CONR 6D R 6E , —NHC(O)R 6D , —NO 2 , —SR 6D , —SO n6 R 6D , —NHNR 6D R 6E , —ONR 6D R 6E , —NHC(O)NHNR 6D R 6E , —C(NCN)R 6D , —C(NH)R 6D , R 6F -substituted or unsubstituted alkyl, R 6F -substituted or unsubstituted heteroalkyl, R 6F -substituted or unsubstituted cycloalkyl, R 6F -substituted or unsubstituted heterocycloalkyl, R 6F -substituted or unsubstituted aryl, or R 6F -substituted or unsubstituted heteroaryl;

n6 is 2, 3, or 4; and

R 6D , R 6E and R 6F are independently hydrogen, halogen, oxo, —N 3 , —CF 3 , —CCl 3 , —CBr 3 , —CI 3 , —CN, —CHO, —OH, —NH 2 , —COOH, —CONH 2 , —NO 2 , —SH, —SO 2 , —SO 2 Cl, —SO 2 CH 3 —SO 3 H, —SO 4 H, —SO 2 NH 2 , —NHNH 2 , —ONH 2 , —NHC(O)NHNH 2 , substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, or a detectable moiety.

4. The compound of claim 1 , wherein Y is —NHC(O)—, —NCH 3 —, —NC(O)CH 3 —, —NC(O)OCH 3 —, 4 to 6 membered unsubstituted heteroarylene, or unsubstituted 5 or 6 membered arylene.

5. The compound of claim 1 , wherein R 2 is independently hydrogen, halogen, —CF 3 , —CCl 3 , —CBr 3 , —CI 3 , —NH 2 , —NO 2 , —SO 2 CH 3 , substituted or unsubstituted C 1 -C 5 alkyl, substituted or unsubstituted 2 to 5 membered heteroalkyl, substituted or unsubstituted 5 or 6 membered aryl, or a detectable moiety.

6. The compound of claim 1 , wherein R 3A is hydrogen, —C(NH)NH 2 , —C(NCN)NH 2 , substituted or unsubstituted heterocycloalkyl, or substituted or unsubstituted heteroaryl.

7. The compound of claim 1 having the formula:

8. The compound of claim 7 having the formula:

9. The compound of claim 7 , wherein R 2 is hydrogen, halogen, —SO 2 CH 3 , —NO 2 , —NH 2 , substituted or unsubstituted C 1 -C 3 alkyl, or substituted or unsubstituted 2 to 5 membered heteroalkyl.

10. The compound of claim 7 , wherein R 3A is independently hydrogen, —C(NH)NH 2 , —C(NCN)NH 2 , or substituted or unsubstituted heterocycloalkyl, or substituted or unsubstituted heteroaryl.

11. The compound of claim 1 having the formula:

12. The compound of claim 1 having the formula:

wherein

R 6A is R 6C -substituted or unsubstituted alkyl or R 6C -substituted or unsubstituted heteroalkyl;

R 6C is —NR 6D R 6E , —NHC(O)R 6D , —C(NCN)R 6D , —C(NH)R 6D , R 6F -substituted or unsubstituted alkyl, R 6F -substituted or unsubstituted heteroalkyl, R 6F -substituted or unsubstituted cycloalkyl, R 6F -substituted or unsubstituted heterocycloalkyl, R 6F -substituted or unsubstituted aryl, or R 6F -substituted;

R 6D is a detectable moiety;

R 6E and R 6F are independently hydrogen, halogen, oxo, —N 3 , —CF 3 , —CCl 3 , —CBr 3 , —CI 3 , —CN, —CHO, —OH, —NH 2 , —COOH, —CONH 2 , —NO 2 , —SH, —SO 2 , —SO 2 Cl, —SO 2 CH 3 —SO 3 H, —OSO 3 H, —SO 2 NH 2 , —NHNH 2 , —ONH 2 , —NHC(O)NHNH 2 , substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, or a detectable moiety.

13. The compound of claim 7 having the formula:

14. The compound of claim 7 having formula:

15. The compound of claim 7 having the formula:

16. The compound of claim 7 having formula:

17. A pharmaceutical composition comprising the compound of claim 1 , or a salt thereof.

18. A method for treating fibrosis, said method comprising administering to a subject in need thereof a therapeutically effective amount of the compound of claim 1 .