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Claims for Patent: 5,688,801

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Claims for Patent: 5,688,801

Title: Method of inhibiting neurotransmitter activity using microencapsulated 3-piperidiny2-substituted 1,2-benzisoxazoles and 1,2-benzisothiazoles
Abstract:A pharmaceutical composition comprising a biodegradable and biocompatible composition comprising a 1,2 benzazole within a polymeric matrix. The 1,2 benzazole composition, pharmaceutically acceptable acid addition salts thereof, are potent antagonists of a series of neurotransmitters, particularly serotonin and dopamine. A method of inhibiting both serotonergic overactivity and dopaminergic overstimulation in animals is provided by administration of a biodegradable and biocompatible microparticle composition comprising a 1,2 benzazole or a pharmaceutically acceptable acid addition salt thereof. A method of treating warm blooded animals suffering from psychotic disorders, and a method of preparing the biodegradable and biocompatible composition are also described.
Inventor(s): Mesens; Jean (Wechelderzande, BE), Rickey; Michael E. (Loveland, OH), Atkins; Thomas J. (Cincinnati, OH)
Assignee: Janssen Pharmaceutica (BE) Alkermes Controlled Therapeutics Inc. II (MA)
Application Number:08/403,432
Patent Claims: 1. A method of inhibiting serotonergic activity or dopaminergic activity in animals wherein said method comprises administering a microparticle composition comprising a 1,2-benzazole of the formula ##STR15## or a pharmaceutically acceptable acid addition salt 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 ##STR16## 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 biocompatibly acceptable microparticle polymer carrier.

2. The method of claim 1, wherein the microparticle polymer carrier polymeric matrix is selected from the group consisting of poly(glycolic acid), poly-D,L-lactic add, 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 about 35 to 40 wt. % of said microparticles.

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

5. 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)-1piperidinyl]ethyl]-6,7,8,9-tetra hydro-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one or a pharmaceutically acceptable acid addition salt thereof.
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