Claims for Patent: 7,601,740

Summary for Patent: 7,601,740

Title:	Selective serotonin 2A/2C receptor inverse agonists as therapeutics for neurodegenerative diseases
Abstract:	Behavioral pharmacological data with the compound of formula (I), a novel and selective 5HT2A/2C receptor inverse agonist, demonstrate in vivo efficacy in models of psychosis and dyskinesias. This includes activity in reversing MK-801 induced locomotor behaviors, suggesting that this compound may be an efficacious anti-psychotic, and activity in an MPTP primate model of dyskinesias, suggesting efficacy as an anti-dyskinesia agent. These data support the hypothesis that 5HT2A/2C receptor inverse agonism may confer antipsychotic and anti-dyskinetic efficacy in humans, and indicate a use of the compound of formula (I) and related agents as novel therapeutics for Parkinson's Disease, related human neurodegenerative diseases, and psychosis.
Inventor(s):	Weiner; David M. (San Diego, CA), Davis; Robert E. (San Diego, CA), Brann; Mark R. (Rye, NH), Andersson; Carl-Magnus A. (Hjarup, SE), Uldam; Allan K. (Ballerup, DK)
Assignee:	Acadia Pharmaceuticals, Inc. (San Diego, CA)
Application Number:	10/759,561
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 7,601,740
Patent Claims:	1. A composition comprising a compound of Formula (I): ##STR00010## or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier. 2. The composition of claim 1, further comprising an additional therapeutic agent. 3. The composition of claim 2, wherein the additional therapeutic agent is selected from the group consisting of levodopa bromocriptine, pergolide, ephenedrine sulfate, pemoline, mazindol, d,1-.alpha.-methylphenethylamine, methylphenidate, pramipexole, modafinil, and ropinirole. 4. The composition of claim 2, wherein the additional therapeutic agent is an anti-dyskinesia agent. 5. The composition of claim 4, wherein the additional therapeutic agent is an anti-dyskinesia agent selected from the group consisting of baclofen, botulinum toxin, clonazepam, and diazepam. 6. The composition of claim 2, wherein the additional therapeutic agent is an anti-dystonia, anti-myoclonus, or anti-tremor agent selected from the group consisting of baclofen, botulinum toxin, clonazepam, and diazepam. 7. The composition of claim 2, wherein the additional therapeutic agent is an anti-psychotic agent with dopaminergic receptor antagonism. 8. The composition of claim 2, wherein the additional therapeutic agent is an anti-psychotic agent selected from the group consisting of chlorpromazine, haloperodol, molindone, thiordazine, a phenothiazine, a butyrophenone, diphenylbutylpiperidine (pimozide), thioxanthines (fluphenthixol), substituted benzamides (sulpiride), sertindole, amisulpride, ziprasidone, aripiprazole, clozapine, olanzapine, riserpidone, N-desmethylclozapine, N-desmethylolanzapine, and 9-OH-respirdone. 9. The composition of claim 1, wherein the compound of formula (I) is the free base. 10. The composition of claim 1, wherein the salt is a hydrochloride salt. 11. The composition of claim 1, wherein the salt is a tartrate salt. 12. The composition of claim 1, wherein the composition is in a single unit dosage form. 13. The composition of claim 12, wherein the composition is in a single unit dosage form suitable for oral administration to a human. 14. The composition of claim 12, wherein the dosage form is solid. 15. The composition of claim 13, wherein the composition is in the form of a tablet or a capsule. 16. The composition of claim 15, wherein the composition is in the form of a tablet. 17. The composition of claim 12, wherein the amount of the compound of Formula (I), or a salt thereof, is from about 0.001 mg to about 50 mg. 18. The composition of claim 12, wherein the amount of the compound of Formula (I), or a salt thereof, is from about 1 mg to about 10 mg. 19. The composition of claim 12, wherein the amount of the compound of Formula (I), or a salt thereof, is about 10 mg. 20. The composition of claim 12, wherein the amount of the compound of Formula (I), or a salt thereof, is about 25 mg. 21. The composition of claim 12, wherein the amount of the compound of Formula (I), or a salt thereof, is about 50 mg. 22. A compound having the structure of Formula (I): ##STR00011## or a pharmaceutically acceptable salt thereof. 23. A compound of claim 22, wherein the compound of formula (I) is in solid form. 24. A compound of claim 22, wherein the compound of formula (I) is the free base. 25. A compound of claim 22, wherein the salt is a hydrochloride salt. 26. A compound of claim 22, wherein the salt is a tartrate salt.