Details for Patent: 7,659,285

Which drugs does patent 7,659,285 protect, and when does it expire?

Patent 7,659,285 protects NUPLAZID and is included in two NDAs.

This patent has thirty-five patent family members in twenty-one countries.

Summary for Patent: 7,659,285

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):	David M. Weiner, Robert E. Davis, Mark R. Brann, Carl-Magnus A. Andersson, Allan K. Uldam
Assignee:	Acadia Pharmaceuticals Inc
Application Number:	US11/416,855
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 7,659,285
Patent Claim Types: see list of patent claims	Use; Composition;

United States Patent 7,659,285: Pimavanserin Patent Scope, Claims, Expiration, and Generic Risk

US Patent 7,659,285 protects the use of pimavanserin, including pharmaceutically acceptable salts such as pimavanserin tartrate, to treat Parkinson's disease psychosis. The patent is a method-of-treatment patent rather than a composition-of-matter patent. Its strongest commercial coverage is directed to once-daily pimavanserin treatment in the 10 mg to 50 mg range, including the dosing regimen used for Nuplazid.

The patent does not broadly prevent all manufacture or sale of pimavanserin. Infringement generally depends on whether a competing product is marketed, prescribed, or used for the claimed Parkinson's disease psychosis indication and dosing conditions.

What drug does US Patent 7,659,285 protect?

US 7,659,285 covers pimavanserin, also known by the development code ACP-103. The chemical name recited in the claims is:

N-(1-methylpiperidin-4-yl)-N-(4-fluorophenylmethyl)-N'-(4-(2-methylpropyloxy)phenylmethyl)carbamide.

The claim text supplied contains typographical errors, including "flourophenyl" and inconsistent use of "N-" and "N'-". The patent's chemical identity is understood from the complete patent specification and claim context to be pimavanserin.

Item	Description
Active ingredient	Pimavanserin
Commercial product	Nuplazid
Original developer	Acadia Pharmaceuticals
Approved product	Pimavanserin tartrate
Dosage forms	Tablets and capsules
Primary FDA indication	Hallucinations and delusions associated with Parkinson's disease psychosis
Patent type	Method of treatment
Patent number	US 7,659,285
Patent grant date	February 9, 2010
FDA approval of Nuplazid	April 29, 2016

The FDA-approved product is pimavanserin tartrate, although labeling expresses dosage in terms of pimavanserin. The standard Nuplazid dose is 34 mg once daily, equivalent to 20 mg of pimavanserin free base. The approved regimen falls within the broader dosing concepts described in the patent, although the precise milligram expression in the patent claims and the marketed salt formulation must be analyzed separately. [1]

What are the independent claims in US 7,659,285?

Claims 1 and 2 are the principal independent claims supplied.

Claim 1: Treatment of Parkinson's disease psychosis

Claim 1 covers:

1. A patient who has Parkinson's disease;
2. Treatment of Parkinson's disease psychosis;
3. Administration of a therapeutically effective amount;
4. Pimavanserin or a pharmaceutically acceptable salt.

The claim does not expressly require a particular dose, dosage form, frequency, route, or salt. This makes claim 1 the broadest claim in the set. A product or regimen could fall within claim 1 even if it does not use the 10 mg, 25 mg, or 50 mg amounts recited in dependent claims 3 through 5.

The disease limitation is material. Treatment of schizophrenia, Alzheimer's disease psychosis, or general psychosis without the Parkinson's disease limitation would not literally satisfy claim 1. The claim also requires treatment of psychosis, not merely treatment of Parkinson's disease symptoms.

Claim 2: Pharmaceutical composition containing 10 mg to 50 mg

Claim 2 covers administration to a Parkinson's disease patient of a pharmaceutical composition containing approximately 10 mg to approximately 50 mg of pimavanserin or a pharmaceutically acceptable salt.

The claim is narrower than claim 1 because it introduces a dose range. It remains broad as to:

• Tablet, capsule, or other dosage form;
• Excipients;
• Release profile;
• Manufacturing process;
• Specific salt, unless a dependent claim applies;
• Route of administration, unless limited elsewhere in the patent.

The phrase "about 10 mg to about 50 mg" creates a range with potential tolerance at the boundaries. The exact scope would depend on claim construction, specification support, prosecution history, and the factual dose measurement used by the accused product.

How do claims 3 through 11 narrow the patent?

Claim	Limitation	Commercial significance
3	About 10 mg	Covers a low-dose regimen
4	About 25 mg	Covers an intermediate dose
5	About 50 mg	Covers a high-dose regimen
6	Once-daily administration	Relevant to commercial maintenance dosing
7	About 0.01 mg/kg to about 1.5 mg/kg	Weight-based dosing alternative
8	Tartrate salt under claim 1	Directly relevant to Nuplazid
9	Tartrate salt under claim 2	Combines tartrate with the 10 mg to 50 mg composition range
10	Hydrochloride salt under claim 1	Covers a different salt form
11	Hydrochloride salt under claim 2	Combines hydrochloride with the composition range

Claims 8 and 9 are commercially important because Nuplazid uses pimavanserin tartrate. Claims 10 and 11 expand the salt coverage beyond the marketed tartrate form.

Claim 6 is also significant because Nuplazid is administered once daily. A generic manufacturer could attempt to avoid a once-daily dependent claim by labeling a different dosing frequency, but that strategy would not avoid claim 1 or claim 2 if the other claim elements remained satisfied.

What is the scope of protection for pimavanserin tartrate?

Claims 8 and 9 expressly cover pimavanserin tartrate.

Claim 8 applies the tartrate limitation to the broad treatment method in claim 1. It therefore covers administration of pimavanserin tartrate to a patient with Parkinson's disease psychosis, without requiring a particular dose.

Claim 9 applies the tartrate limitation to claim 2. It requires:

• Parkinson's disease psychosis;
• A pharmaceutical composition;
• About 10 mg to about 50 mg of pimavanserin or its salt;
• The tartrate salt.

These claims are potentially relevant to generic products containing pimavanserin tartrate, even where the generic manufacturer does not copy the Nuplazid brand formulation. The claims do not appear, based on the supplied language, to require a particular excipient system, tablet hardness, dissolution profile, coating, or manufacturing process.

That distinction matters. A generic product may avoid a formulation patent while still facing an asserted method-of-use patent.

What doses and regimens are protected?

The patent contains three principal dosing concepts:

1. Fixed doses of approximately 10 mg, 25 mg, and 50 mg;
2. A weight-based dose of approximately 0.01 mg/kg to 1.5 mg/kg;
3. Once-daily administration.

The claims are not limited to the exact commercial 34 mg pimavanserin tartrate capsule strength because the patent describes amounts of the active compound or salt in different ways. Dose conversion between pimavanserin free-base equivalent and pimavanserin tartrate must be performed carefully.

A product labeled for 34 mg of pimavanserin tartrate may be expressed in labeling as 20 mg pimavanserin. The legal analysis should therefore distinguish:

• Salt weight;
• Pimavanserin free-base equivalent;
• Dosage-unit strength;
• Total daily dose;
• Amount administered to the patient.

The patent's use of "about" may create factual disputes over whether a particular dose falls within a claimed range. A dose materially outside the stated range would have a stronger non-infringement position against claims 2 through 5 and 9 through 11, but not necessarily against claim 1.

What is the FDA and Orange Book status of US 7,659,285?

Nuplazid was approved by FDA under the 505(b)(1) pathway as a new drug for hallucinations and delusions associated with Parkinson's disease psychosis. FDA lists relevant patents for approved products in the Orange Book, including patents that cover the drug substance, formulation, or method of use. [2]

US 7,659,285 is associated with the Parkinson's disease psychosis use of pimavanserin. The Orange Book listing is important because an ANDA applicant must address listed patents through one of four certifications:

• Paragraph I: No patent information is listed;
• Paragraph II: The patent has expired;
• Paragraph III: The applicant will wait until patent expiration;
• Paragraph IV: The patent is invalid, unenforceable, or will not be infringed.

A Paragraph IV certification can trigger patent litigation if the NDA holder sues within the statutory period. Under the Hatch-Waxman framework, timely litigation can create a 30-month stay of final ANDA approval, subject to statutory exceptions and court developments. [3]

The controlling current patent status should be taken from the FDA Orange Book and USPTO patent records rather than from commercial patent databases. The patent's effective term may differ from its ordinary 20-year term because of patent-term adjustment and any FDA patent-term extension.

When does US 7,659,285 lose exclusivity?

The ordinary patent term is calculated from the relevant nonprovisional filing or international application date, subject to the patent-term rules applicable to the patent. FDA patent-term extension can extend the term for a qualifying patent covering an approved product.

Public commercial references have associated US 7,659,285 with an expiration in the 2027 period after regulatory term adjustment. The legally operative date is the expiration date recorded in the USPTO patent file and reflected in the applicable Orange Book entry.

Exclusivity type	Relevance to Nuplazid
New chemical entity exclusivity	Protected the product from ANDA approval for five years after FDA approval
Orphan-drug exclusivity	Parkinson's disease psychosis approval received orphan-drug protection
Patent exclusivity	Determined by the applicable pimavanserin patents
Pediatric exclusivity	Applies only if FDA awarded the statutory six-month extension
Regulatory exclusivity	Does not necessarily prevent a 505(b)(2) application from relying on published data in the same manner as a patent

Orphan-drug exclusivity and patent exclusivity are separate. Orphan exclusivity generally blocks approval of the same drug for the same disease or condition for seven years, while a patent may continue beyond or expire before that period. FDA approved Nuplazid in 2016, so its original orphan period was distinct from the patent term. [1]

Which later patents are relevant to the pimavanserin patent estate?

US 7,659,285 is one part of the pimavanserin estate. Later patent families may address:

• Additional methods of treating psychosis;
• Dosing regimens;
• Patient populations;
• Combination therapy;
• Formulations;
• Solid-state forms or salts;
• Manufacturing processes;
• Expanded indications, including dementia-related psychosis.

A generic entrant must analyze the entire Orange Book-listed estate, not only US 7,659,285. A later formulation or method patent can delay commercial launch even after an earlier use patent expires.

The principal patent-estate distinction is:

Estate category	Protection target	Relevance to generic risk
Composition-of-matter patents	Pimavanserin molecule	Highest early-life barrier, if unexpired
Salt or solid-state patents	Tartrate, hydrochloride, crystal forms	Can constrain the selected API form
Formulation patents	Tablet, capsule, release profile, excipients	May be avoided by design-around
Method-of-use patents	Parkinson's disease psychosis and other indications	Often addressed through Paragraph IV or skinny-label strategy
Manufacturing patents	Synthesis, purification, crystallization	Can affect API sourcing, but often does not block finished-dose approval
Pediatric and orphan exclusivity	Regulatory approval timing	Separate from patent infringement

The claims supplied for US 7,659,285 are method claims. They do not, on their face, claim the pimavanserin molecule itself or a specific tablet formulation.

Which companies could challenge Nuplazid patents?

Potential ANDA challengers would include companies with established CNS generic operations and the capacity to develop pimavanserin tartrate products. Publicly reported patent litigation and Paragraph IV activity involving Nuplazid has included multiple generic applicants, including entities associated with Teva, Zydus, Aurobindo, Alembic, Amneal, Dr. Reddy's, and other generic manufacturers.

The relevant legal question is not simply whether a company can manufacture pimavanserin. The company must determine whether its proposed label will include Parkinson's disease psychosis, whether it will use pimavanserin tartrate, and whether its dose and frequency fall within the claims.

A generic applicant can pursue several strategies:

• Paragraph III certification and delayed launch;
• Paragraph IV certification against listed patents;
• A section viii statement carving out patented indications;
• A redesigned dosing regimen;
• A formulation design-around;
• Launch after a settlement date;
• A declaratory judgment or litigation defense based on invalidity or non-infringement.

What is the Paragraph IV risk for a pimavanserin generic?

The core Paragraph IV issues for US 7,659,285 would likely include:

Infringement

The NDA holder would need to show that the proposed generic product, labeling, or intended use satisfies every limitation of an asserted claim. For claim 1, the central issues would be whether the label or induced use covers Parkinson's disease psychosis and whether the product contains pimavanserin or a covered salt.

For claims 2 through 11, the analysis would also address dose, salt, composition, and frequency.

Induced infringement

A generic company may face induced-infringement allegations if its labeling encourages physicians to use the product for Parkinson's disease psychosis. A label carve-out can reduce risk, but it does not automatically eliminate liability if evidence shows the product is intended for the patented use.

Validity

Potential validity theories could involve:

• Anticipation;
• Obviousness;
• Lack of written description;
• Lack of enablement;
• Indefiniteness;
• Improper claim construction;
• Double patenting;
• Patent-term or terminal-disclaimer issues.

The supplied claims are narrow in disease indication but broad in compound identity and therapeutic purpose. Their validity would depend heavily on the prior art and prosecution record available when the application was examined.

Orange Book listing

A listed use patent can impose a practical ANDA barrier even when the patent does not cover the molecule or every possible use. The applicant must address the listing and the NDA holder may sue following a Paragraph IV notice.

Does US 7,659,285 cover all pimavanserin products?

No. The patent does not appear to cover every pimavanserin product irrespective of use.

The claims require a treatment method involving Parkinson's disease psychosis. A pimavanserin product marketed solely for a non-Parkinson's indication may fall outside the literal scope of these claims, although other patents could apply.

The patent also does not expressly require:

• Nuplazid branding;
• A specific manufacturer;
• A specific tablet or capsule design;
• A particular excipient;
• A particular manufacturing process;
• A particular release profile;
• A specific commercial package.

Its principal coverage is use-based. The commercial risk is highest when the generic label reproduces the approved Parkinson's disease psychosis indication and the product uses pimavanserin tartrate in a covered dose.

Is there biosimilar risk for Nuplazid?

No. Pimavanserin is a small-molecule drug, not a biologic. A competing product would generally be submitted as an ANDA generic or potentially a 505(b)(2) application, not as a biosimilar under the Public Health Service Act.

The relevant competitive risks are:

• Paragraph IV generic entry;
• 505(b)(2) approval for a modified formulation or indication;
• Off-label use after generic launch;
• Authorized generic competition;
• Product-label carve-outs;
• Patent settlement timing.

How strong is the patent estate for pimavanserin?

US 7,659,285 provides meaningful use protection but is narrower than a valid, unexpired composition-of-matter patent. Its practical strength depends on four factors:

1. Whether the patent remains in force after term adjustment or extension;
2. Whether the Orange Book listing remains active;
3. Whether a generic label includes Parkinson's disease psychosis;
4. Whether later patents cover the selected salt, formulation, or dosing regimen.

The patent is strongest against a generic that:

• Uses pimavanserin tartrate;
• Copies the Parkinson's disease psychosis indication;
• Uses a once-daily regimen;
• Supplies a dose within the claimed range;
• Relies on labeling that encourages the patented use.

It is weaker against a generic that uses a legally distinct indication carve-out, a different dosing design, or a product and label outside the asserted claims. Those strategies must still be evaluated against the full patent estate and induced-infringement facts.

Key Takeaways

• US 7,659,285 is a method-of-treatment patent for pimavanserin in Parkinson's disease psychosis.
• Claims 1 and 2 are the principal claims; claim 1 is the broadest because it does not require a specific dose.
• Claims 3 through 7 cover specified doses, dose ranges, and once-daily administration.
• Claims 8 and 9 directly cover pimavanserin tartrate, the active salt used in Nuplazid.
• Claims 10 and 11 cover the hydrochloride salt.
• The patent does not broadly claim the pimavanserin molecule, every formulation, or every indication.
• FDA Orange Book listings and Paragraph IV certifications are central to generic-launch analysis.
• Nuplazid is a small-molecule product, so biosimilar rules do not apply.
• A generic entrant faces the greatest risk when its label includes Parkinson's disease psychosis and once-daily pimavanserin tartrate dosing.
• Later formulation, salt, dosing, and method patents must be reviewed before assessing a practical launch date.

FAQs About US Patent 7,659,285 and Nuplazid

Does US 7,659,285 cover pimavanserin tartrate specifically?

Yes. Claims 8 and 9 expressly recite the tartrate salt of pimavanserin.

Can a generic company sell pimavanserin for schizophrenia without infringing this patent?

Potentially, because the asserted claims require Parkinson's disease psychosis. Other pimavanserin patents, regulatory restrictions, or induced-use evidence could still affect the analysis.

Does the patent cover the 34 mg Nuplazid capsule?

The answer depends on whether the claimed amount is measured as pimavanserin free-base equivalent or salt weight. The marketed dose is generally expressed as 34 mg pimavanserin tartrate equivalent to 20 mg pimavanserin. Dose construction must be performed against the patent specification and product labeling.

Is US 7,659,285 a formulation patent?

No. The supplied claims are method claims. They do not require a particular excipient, dosage form, release profile, or manufacturing process.

What is the likely legal route for a Nuplazid generic?

The principal route is an ANDA supported by a Paragraph III or Paragraph IV patent certification. A 505(b)(2) application may be relevant for a modified product, indication, or formulation, but it would not eliminate the need to address applicable patents and regulatory exclusivity.

References

1. U.S. Food and Drug Administration. (2016). Nuplazid (pimavanserin tartrate) prescribing information. FDA.

2. U.S. Food and Drug Administration. (n.d.). Approved drug products with therapeutic equivalence evaluations: Orange Book. FDA.

3. U.S. Patent and Trademark Office. (n.d.). US Patent No. 7,659,285, methods of treating psychosis. USPTO.

4. U.S. Code, 35 U.S.C. §§ 156, 271(e), 282.

5. U.S. Code, 21 U.S.C. §§ 355(j), 360cc.

Drugs Protected by US Patent 7,659,285

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Acadia Pharms Inc	NUPLAZID	pimavanserin tartrate	CAPSULE;ORAL	210793-001	Jun 28, 2018		RX	Yes	Yes	7,659,285					TREATMENT OF PARKINSON'S DISEASE PSYCHOSIS
Acadia Pharms Inc	NUPLAZID	pimavanserin tartrate	TABLET;ORAL	207318-002	Jun 28, 2018		RX	Yes	Yes	7,659,285					TREATMENT OF PARKINSON'S DISEASE PSYCHOSIS
Acadia Pharms Inc	NUPLAZID	pimavanserin tartrate	TABLET;ORAL	207318-001	Apr 29, 2016		DISCN	Yes	No	7,659,285					TREATMENT OF PARKINSON'S DISEASE PSYCHOSIS

International Family Members for US Patent 7,659,285

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Austria	407117
Austria	512136
Australia	2004206886
Brazil	PI0406591
Canada	2512639
China	101780080