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)—, wherein the alkylene is propylene or butylene;
C is
R 2 is H, alkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, cycloalkyl, -alkylene-alkoxy, alkylene-aryl, or heterocycloalkyl;
R 3 , is H, halide, methyl or OMe;
R is H or methyl; and
each R 1 is independently H, alkyl, halide, alkoxy, CF 3 , OH, alkylene-OH, NO 2 , —N(H)R, or NH 2 , provided at least one instance of R 1 is Me, halide, OMe, OH, alkylene-OH, or NH 2 ;
or a pharmaceutically acceptable salt thereof.
2. The compound of claim 1 , wherein R 3 is H.
3. The compound of claim 1 , wherein at least one instance of R 1 is alkyl, or halide.
4. The compound of claim 1 , wherein R 2 is H.
5. The compound of claim 1 , wherein R 2 is (C 1 -C 4 )alkyl, cyclopropyl, CH 2 OMe, phenyl, —CH 2 Ph, pyridinyl, or indolyl.
6. The compound of claim 5 , wherein R 2 is Me.
7. The compound of claim 5 , wherein R 2 is phenyl or pyridinyl.
8. The compound of claim 7 , wherein the phenyl at R 2 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; and wherein the pyridinyl at R 2 is substituted with NH 2 , or OH.
9. The compound of claim 5 , wherein R 2 is