Patent ID: 8143410

Claim:
An ocular implant comprising: a tyrosine kinase inhibitor and a polymer matrix that releases drug at a rate effective to sustain release of an amount of the tyrosine kinase inhibitor from the implant for at least about one week after the implant is placed in an eye, wherein said tyrosine kinase inhibitor is a compound represented by the following general formula I: Wherein X is N; Y is CR 1 or N; R 1 is selected from the group consisting of hydrogen, alkyl, halogen, OR4, CN, NO 2 , COR 4 , (CH 2 ) a OR 4 , (CH 2 ) a N(R 4 ) 2 , C(O)N(R 4 ) 2 and N(R 4 ) 2 ; R 2 is selected from the group consisting of hydrogen, halogen, alkyl, OR 4 , CN, NO 2 , SO 2 N(R 4 ) 2 , COR 4 , (CH 2 ) a OR 4 , (CH 2 ) a N(R 4 ) 2 , C(O)N(R 4 ) 2 , N(R 4 ) 2 and N(R 6 )(CR 7 R 8 ) a R 10 ; R 3 is selected from the group consisting of hydrogen, halogen, alkyl, OR 4 , CN, NO 2 , SO 2 N(R 4 ) 2 , COR 4 , (CH 2 ) a OR 4 , (CH 2 ) a N(R 4 ) 2 , C(O)N(R 4 ) 2 , N(R 4 ) 2 and N(R 6 )(CR 7 R 8 ) a R 10 ; R 4 is hydrogen or C 1 to C 4 alkyl; A is selected from the group consisting of C≡C, CH═CH, CH 2 CH 2 , CH 2 O, CF 2 O, OCH 2 , OCF 2 , O, N(R 4 ), C(O), S(O) e , NR 7 C(O), C(O)NR 7 and N(R 7 )C(O)NR 7 ; B is selected from the group consisting of hydrogen, alkyl and alkyloxyalkyl or B may be a 5 or 6 membered carbocyclic aryl or heterocyclic aryl group; E is a 5 or 6 membered carbocyclic aryl or heterocyclic aryl group; E′ is selected from the group consisting of alkyl, CF 3 , (CR 7 R 8 ) a C(O)OR 10 , (CR 7 R 8 ) a C(O)N(R 10 ) 2 , (CR 7 R 8 ) a C(O)N(OR 10 )(R 10 ), (CR 7 R 8 ) a (OR 10 ), (CR 7 R 8 ) a N(R 10 ) 2 , and (CR 7 R 8 ) a R 10 ; wherein R 7 and R 8 are selected from the group consisting of H, halogen, hydroxyl, and alkyl or CR 7 R 8 may represent a carbocyclic ring of from 3 to 6 carbons; and R 10 is selected from the group consisting of hydrogen, halogen, alkyl, hydroxyl, hydroxymethyl, carbocyclic aryl, heterocyclic aryl, (CR 7 R 8 ) a C(O)OR 6 , (CR 7 R 8 ) a C(O)R 6 , (CR 7 R 8 ) a C(O)N(R 6 ) 2 , (CR 7 R 8 ) a C(O)N(OR 6 )(R 6 ), (CR 7 R 8 ) a (OR 6 ), (CR 7 R 8 ) a N(R 6 ) 2 and (CR 7 R 8 ) a R 6 , wherein R 6 is selected from the group consisting of hydrogen, carboalkyl, alkylamine, alkylhydroxy, and alkyloxyalkyl or R 6 is a 5 or 6 membered carbocyclic or heterocyclic group; a is 0 or an integer of from 1 to 5; b is an integer of from 2 to 5; c is 0 or an integer of from 1 to 4; d is 0 or an integer of from 1 to 5; e is 0 or an integer of from 1 to 2 and further including prodrugs, pharmaceutically acceptable salts, racemic mixtures and enantiomers of said compound.