Patent ID: 8722654
Filing Date: 2014-05-13
Classification: A61K,C07C

Abstract:
1. A method to treat corneal neovascularization comprising administering a composition comprising a lipoxin compound to the corneal tissue of a subject in need thereof, wherein the lipoxin compound comprises the formula wherein X is R1, OR.1, or SR1; wherein R1 is (i) a hydrogen atom; (ii) an alkyl of 1 to 8 carbons atoms, inclusive, which can be straight chain or branched; (iii) a cycloalkyl of 3 to 10 carbon atoms, inclusive; (iv) an aralkyl of 7 to 12 carbon atoms; (v) phenyl; (vi) substituted phenyl wherein Zi, Zii, Ziii, Ziv and Zv are each independently selected from —NO2, —CN, —C(═O)—R1, —SO3H, a hydrogen atom, halogen, methyl, —ORx, wherein Rx is 1 to 8 carbon atoms, inclusive, which can be a straight chain or branched, and hydroxyl; or (vii) a straight or branched chain alkenyl of 2 to 8 carbon atoms, inclusive; wherein Q1 is (C═O), SO2 or (CN); wherein Q3 is O, S or NH; wherein one of R2 and R3 is a hydrogen atom and the other is (a) a hydrogen atom; (b) an alkyl of 1 to 8 carbon atoms, inclusive, which can be straight chain or branched; (c) a cycloalkyl of 3 to 6 carbon atoms, inclusive; (d) an alkenyl of 2 to 8 carbon atoms, inclusive, which can be straight chain or branched; or (e) Ra Q2Rb wherein Q2 is —O— or —S—; wherein Ra is alkylene of 0 to 6 carbons atoms, inclusive, which can be straight chain or branched; and wherein Rb is alkyl of 0 to 8 carbon atoms, inclusive, which can be straight chain or branched; wherein R4 is (a) a hydrogen atom; (b) an alkyl of 1 to 6 carbon atoms, inclusive, which can be straight chain or branched; wherein Y1 or Y2 is —OH, methyl, or —SH and wherein the other is (a) a hydrogen atom (b) CHaZb where a+b=3, a=0 to 3, b=0 to 3; and each Z, independently, is a cyano, a nitro, or a halogen atom; (c) an alkyl of 2 to 4 carbon atoms, inclusive, straight chain or branched; or (d) an alkoxy of 1 to 4 carbon atoms, inclusive; or Y1 and Y2 taken together are (a) ═NH; or (b) ═O; wherein R5 is (a) an alkyl of 1 to 9 carbon atoms which can be straight chain or branched; (b) —(CH2)n-Ri wherein n=0 to 4 and Ri is (i) a cycloalkyl of 3 to 10 carbon atoms, inclusive; (ii) a phenyl; or (iii) substituted phenyl wherein Zi, Zii, Ziii, Ziv and Zv are each independently selected from —NO2, —CN, —C(═O)—R1, —SO3H, a hydrogen atom, halogen, methyl, —ORx, wherein Rx is 1 to 8 carbon atoms, inclusive, which can be a straight chain or branched, and hydroxyl; (c) RaQaRb wherein Qa is O or S; wherein Ra is alkylene of 0 to 6 carbons atoms, inclusive, which can be straight chain or branched; wherein Rb is alkyl of 0 to 8 carbon atoms, inclusive, which can be straight chain or branched; (d) —C(Riii)(Riv)-Ri wherein Riii and Riv are each, independently: (i) a hydrogen atom; (ii) CHaZb where a+b=3, a=0 to 3, b=0+3, and wherein each Z, independently, is a cyano, a nitro, or a halogen atom; (e) a haloalkyl of 1 to 8 carbon atoms, inclusive, and 1 to 6 halogen atoms, inclusive, straight chain or branched; and wherein R6 is (a) a hydrogen atom; (b) an alkyl from 1 to 4 carbon atoms, inclusive, straight chain or branched; (c) a halogen.