Patent ID: 8383825

Claim:
A method of treating an ocular condition of an eye of a patient, comprising the step of placing a biodegradable intraocular implant in an eye of the patient, the implant comprising a tyrosine kinase inhibitor and a biodegradable polymer matrix, wherein the implant degrades at a rate effective to sustain release of an amount of the tyrosine kinase inhibitor from the implant effective to treat the ocular condition, wherein said ocular condition is diabetic retinopathy, and wherein the tyrosine kinase inhibitor is a compound of formula I or a prodrug, pharmaceutically acceptable salt, racemic mixture or enantiomer of said compound, wherein: X is CR 4 or N; Y is CR 1 or N; R′ is selected from the group consisting of hydrogen, alkyl, halogen, OR 4 , CN, NO 2 , COR 4 , (CH 2 ) a OR 4 , (CH 2 ) a 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 ,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 ; 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; 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 ; R 6 is selected from the group consisting of hydrogen, carboalkyl, alkylamine, alkylhydroxy, and alkyloxyalkyl or R 6 is a 5 or 6 membered carbocvclic 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; and e is 0 or an integer of from 1 to 2.