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Claims for Patent: 6,110,921

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Claims for Patent: 6,110,921

Title: Microencapsulated 3-piperidinyl-substituted 1,2-benzisoxazoles and 1,2-benzisothiazoles
Abstract:The invention relates to a method of treating psychotic disorders comprising a biodegradable and biocompatible microparticle composition comprising a 1,2-benzazole of the formula ##STR1## and the pharmaceutically acceptable acid addition salts thereof.
Inventor(s): Mesens; Jean (Wechelderzande, BE), Rickey; Michael E. (Loveland, OH), Atkins; Thomas J. (York, PA)
Assignee: Alkermes Controlled Therapeutics Inc. II (Cambridge, MA) Janssen Pharmaceutica (BE)
Application Number:09/252,486
Patent Claims: 1. A method of treating warm blooded animals suffering from psychotic disorders comprising the administration thereto of a pharmaceutically effective amount of a sustained-release microparticle composition 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.

2. The method of claim 1, wherein the polymeric matrix material of said microparticle is selected from the group consisting of poly(glycolic acid), poly-D,L-lactic acid, poly-L-lactic acid, copolymers of the foregoing, poly(aliphatic carboxylic acids), copolyoxalates, polycaprolactone, polydioxonone, poly(ortho carbonates), poly(acetals), poly(lactic acid-caprolactone), polyorthoesters, poly(glycolic acid-caprolactone), polyanhydrides, albumin, casein, and waxes.

3. The method of claim 1, wherein said 1,2-benzazole comprises 1 to 90 wt. % of said microparticles.

4. The method of claim 1, wherein said 1,2-benzazole comprises about 35 to 40 wt. % of said microparticles.

5. The method of claim 1, wherein said microparticles range in size from 1 to 500 microns.

6. The method of claim 1, wherein said microparticles range in size from 25 to 180 microns.

7. The method of claim 1, wherein said microparticles are formulated in a liquid injection vehicle.

8. The method of claim 7, wherein said liquid vehicle is selected from the group consisting of

A. physiological saline solution and

B. an aqueous solution of carboxymethyl cellulose with a surfactant.

9. The method of claim 1, wherein said microparticles are administered by intra-muscular injection.

10. The method of claim 1, wherein said microparticles are administered by subcutaneous injection.

11. The method of claim 1, wherein the 1,2-benzazole is selected from the group consisting of 3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl)ethyl]-6,7,8,9-tetr ahydro-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one and the pharmaceutically acceptable acid addition salts thereof.

12. The method of claim 1, wherein the 1,2-benzazole is selected from the group consisting of 3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl)ethyl]-6,7,8,9-tetr ahydro-9-hydroxy-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one and the pharmaceutically acceptable acid addition salts thereof.

13. The method of claim 12, wherein the 1,2-benzazole is 3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl)ethyl]-6,7,8,9-tetr ahydro-9-hydroxy-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one.
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