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US 5,965,168 AGranted
Microencapsulated 3-piperidinyl-substituted 1,2-benzisoxazoles and 1,2-benzisothiazoles
AssigneesAlkermes Controlled Therapeutics Inc. II, Janssen Pharmaceutica NV
InventorsJean Mesens, Michael E. Rickey, Thomas J. Atkins
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Abstract
The invention relates to a pharmaceutical composition comprising a biodegradable and biocompatible microparticle composition comprising a 1,2-benzazole of the formula ##STR1## and the pharmaceutically acceptable acid addition salts thereof, within a polymeric matrix.
Claims12
A sustained-release microparticle comprising:
- a 1,2-benzazole of the formula ##STR16## and the pharmaceutically acceptable acid addition salts thereof, wherein R is hydrogen or alkyl of 1 to 6 carbon atoms;
- R.sup.1 and R.sup.2 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 C.sub.1-4 alkanediyl;
- and
- Q is a radical of formula ##STR17## wherein R.sup.3 is hydrogen or alkyl of 1 to 6 carbon atoms;
- Z is --S--, --CH.sub.2 --, or --CR.sup.4 .dbd.CR.sup.5 --;
- where R.sup.4 and R.sup.5 are independently selected from the group consisting of hydrogen or alkyl of 1 to 6 carbon atoms;
- A is a bivalent radical --CH.sub.2 --CH.sub.2 --, --CH.sub.2 --CH.sub.2 --CH.sub.2 -- or CR.sup.6 .dbd.CR.sup.7 --;
- where R.sup.6 and R.sup.7 are independently selected from the group consisting of hydrogen, halo, amino or alkyl of 1 to 6 carbon atoms;
- and
- R.sup.8 is hydrogen or hydroxyl;
- and a biodegradable and biocompatible polymeric matrix.
10 more elements
Dependencies are inferred from the claim text.