Patent ID: 6803055
Filing Date: 2004-10-12
Classification: A61K,A61P,Y10S

Abstract:
A sustained-release microparticle composition, comprising:a microparticle comprising a 1,2 benzazole of the formula â€ƒand the pharmaceutically acceptable acid addition salts thereof, wherein R is hydrogen or alkyl of 1 to 6 carbon atoms; R1 and R2 are independently selected from the group consisting of hydrogen, halo, hydroxy, alkyloxy of 1 to 6 carbon atoms, and C alkyl of 1 to 6 carbon atoms; X is O or S; Alk is C1-4 alkanediyl; and Q is a radical of formula whereinR3 is hydrogen or alkyl of 1 to 6 carbon atoms; Z is â€”Sâ€”, â€”CH2â€”, or â€”CR4&boxH;CR5â€”; where R4 and R5 are independently selected from the group consisting of hydrogen or alkyl of 1 to 6 carbon atoms; A is a bivalent radical â€”CH2â€”CH2â€”, â€”CH2â€”CH2â€”CH2â€” or CR6&boxH;CR7â€”; where R6 and R7 are independently selected from the group consisting of hydrogen, halo, amino or alkyl of 1 to 6 carbon atoms; and R8 a hydrogen or hydroxyl; and a biodegradable and biocompatible polymeric matrix that exhibits diffusional release of said 1,2 benzazole; and a microparticle comprising a 1,2 benzazole of the formula â€ƒand the pharmaceutically acceptable acid addition salts thereof, wherein R is hydrogen or alkyl of 1 to 6 carbon atoms; R1 and R2 are independently selected from the group consisting of hydrogen, halo, hydroxy, alkyloxy of 1 to 6 carbon atoms, and C alkyl of 1 to 6 carbon atoms; X is O or S; Alk is C14 alkanediyl; and Q is a radical of formula whereinR3 is hydrogen or alkyl of 1 to 6 carbon atoms; Z is â€”Sâ€”, â€”CH2â€”, or â€”CR4&boxH;CR5â€”; where R4 and R5 are independently selected from the group consisting of hydrogen or alkyl of 1 to 6 carbon atoms; A is bivalent radical â€”CH2â€”CH2â€”, â€”CH2â€”CH2â€”CH2â€” or CR6&boxH;CR7â€”; where R6 and R7 are independently selected from the group consisting of hydrogen, halo, amino or alkyl of 1 to 6 carbon atoms; and R8 is hydrogen or hydroxyl; and a biodegradable and biocompatible polymeric matrix that exhibits biodegradation release of said 1,2 benzazole;.