Details for Patent: 9,815,827

Summary for Patent: 9,815,827

Title:	Agent for treatment of schizophrenia
Abstract:	The present invention provides a novel method for treatment of schizophrenia which can improve wide-ranging symptoms of schizophrenia, especially positive symptoms and negative symptoms without being accompanied by extrapyramidal symptoms, which comprises orally administering as an active compound (1R,2S,3R,4S)-N-[(1R,2R)-2-[4-(1,2-benzoisothiazol-3-yl)-1-piperazinylmethyl]-1-cyclohexylmethyl]-2,3-bicyclo[2.2.1]heptanedicarboxyimide or a pharmaceutically acceptable salt thereof (e.g., hydrochloride) at a daily dose of 5 mg to 120 mg once a day to a patient with schizophrenia, and a therapeutic agent to be used in said method.
Inventor(s):	Mitsutaka Nakamura, Masaaki Ogasa, Shunsuke Sami
Assignee:	Sumitomo Pharma Co Ltd
Application Number:	US14/471,919
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 9,815,827
Patent Claim Types: see list of patent claims	Use; Composition; Dosage form;

Scope, Claim Strategy, and US Patent Landscape for US 9,815,827

US 9,815,827 is a method-of-treatment patent built around a single stereochemically defined antipsychotic active: (1R,2S,3R,4S)-N-[(1R,2R)-2-[4-(1,2-benzoisothiazol-3-yl)-1-piperazinylmethyl]-1-cyclohexylmethyl]-2,3-bicyclo[2.2.1]heptanedicarboximide (and pharmaceutically acceptable salts, with the key salt repeatedly specified as the hydrochloride). The core commercial differentiation is not the drug itself but the clinical use condition: oral dosing at 20 to 120 mg/day such that the treated patient does not experience clinically significant weight gain, with multiple claim variants anchoring a 6-week assessment window and, in several dependent claims, no concurrent antipsychotic.

This creates a landscape in which the enforceable scope is concentrated on method and dosing conditions rather than composition structure. Competitive work that uses the same active or salt must then navigate whether it still meets the defined weight-gain outcome, time window, and concomitant-therapy restrictions.

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What exactly is claimed?

What treatment modalities does the patent cover?

The claims cover oral administration methods for antipsychotic treatment, with functional endpoints tied to weight gain (and, in some claims, disease-state severity and symptom reduction metrics).

Three overlapping claim groupings recur:

1. Schizophrenia treatment with “no clinically significant weight gain”

   • Independent method claim is oriented to schizophrenia (Claim 1).
   • Dependent claims add salt specificity, time window, and concomitant-therapy restrictions.

2. Manic depressive psychosis treatment with “no clinically significant weight gain”

   • Independent method claim mirrors the schizophrenia structure but targets manic depressive psychosis (Claim 8).
   • Dependent claims again specify salt, time window, and no concurrent antipsychotic.

3. Broad antipsychotic treatment framed as “without a clinically significant weight gain,” plus composition-including formats

   • Independent claim treats “a patient with an antipsychotic without clinically significant weight gain,” describing once-daily oral administration of the active as a “sole active ingredient” in a 20 to 120 mg range (Claim 25).
   • Another independent claim focuses on oral dosing using a “pharmaceutical composition” (Claims 40 and 56), also with “sole active ingredient” and tablet embodiment language.

Disease targets inside the “broad antipsychotic” bucket still explicitly include:

• schizophrenia (Claims 29, 45, 61)
• manic depressive psychosis (Claims 30, 46, 62)

What active ingredient is locked in?

Across the claim set, the active is fixed to the stereochemical compound:

• (1R,2S,3R,4S)-N-[(1R,2R)-2-[4-(1,2-benzoisothiazol-3-yl)-1-cyclohexylmethyl]-2,3-bicyclo[2.2.1]heptanedicarboximide
• and pharmaceutically acceptable salts, with hydrochloride repeatedly singled out as a preferred embodiment (Claims 2, 9, 41, 26, 43-44 depending on claim family; and multiple dose variants specify the hydrochloride).

What dosing regimen is required?

The patent requires:

• Oral administration
• Once daily in multiple independent frameworks:
  • Claim 25: “once daily”
  • Claim 40: “sole active ingredient” composition administered to produce no clinically significant weight gain (also “once daily” in its preamble)
  • Claim 56: “orally administering once daily”
  • Dose window in all core method claims: 20 to 120 mg/day
• Dose specification dependent variants:
  • 20 mg once daily (e.g., Claims 13, 19, 34, 51, 57, 67)
  • 40 mg once daily (e.g., Claims 14, 20, 35, 52, 68)
  • 60 mg once daily (e.g., Claims 15, 21, 36, 53, 70, 71)
  • 80 mg once daily (e.g., Claims 16, 22, 37, 54, 72, 73)
  • 120 mg once daily (e.g., Claims 17, 23, 38, 55, 74, 75)

What clinical outcome drives infringement risk?

The patent uses “clinically significant weight gain” as the differentiator. Several claims add timing and monitoring.

Key outcome elements:

• The method is performed “such that the patient does not experience a clinically significant weight gain.” (Claims 1, 8, 25, 40, 56)
• A 6-week window appears as a key dependent limitation:
  • “does not experience a clinically significant weight gain after six weeks of administration” (Claims 3, 10, 27, 43, 59)
• Monitoring:
  • “further comprising: detecting a weight gain after six weeks of administration” (Claims 5, 11, 28, 44, 60)

What concomitant-therapy restriction is written?

Several dependents impose:

• “without concurrently administering another antipsychotic medication.” (Claims 4, 12, 32, 33, 47, 48, 63, 64, plus disease-specific dependents)

This matters because it frames a clear boundary around polypharmacy regimens. If a physician uses the active while concurrently administering another antipsychotic, the patent may not read cleanly on that use (at least for those dependent claim paths).

What psych symptom endpoints appear?

Only one claim family includes a disease severity inclusion and symptom response metric:

• Claim 6: patient has BPRS score at least 42, and the BPRS score is significantly reduced from baseline.

This implies the inventors may have used structured endpoints in the exemplars supporting the weight-gain differentiation, but only that claim explicitly imports BPRS criteria.

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How the claim set is built: scope and leverage

What is the breadth of the independent claims?

There are multiple independent method claims with different preambles, creating layered coverage.

1. Schizophrenia method with weight-gain outcome and dose range

   • Claim 1: schizophrenia + oral administration + 20 to 120 mg/day + “no clinically significant weight gain”
   • Dependent variants: salt specificity (Claim 2), 6-week condition (Claim 3), no concurrent antipsychotic (Claim 4), monitoring for weight gain after six weeks (Claim 5), plus BPRS/BPRS-response limitation (Claim 6).

2. Manic depressive psychosis method with weight-gain outcome and dose range

   • Claim 8: manic depressive psychosis + oral administration + 20 to 120 mg/day + “no clinically significant weight gain”
   • Dependent variants: hydrochloride (Claim 9), 6-week condition (Claim 10), monitoring (Claim 11), no concurrent antipsychotic (Claim 12).

3. Broad “antipsychotic without clinically significant weight gain” framed around once-daily dosing and composition language

   • Claim 25: treats “a patient with an antipsychotic” + oral once daily + 20 to 120 mg/day + “no clinically significant weight gain” + active locked in + “once daily” framing.
   • Dependent variants tie to hydrochloride (Claim 26), 6-week condition (Claim 27), monitoring (Claim 28), and disease-specific versions (Claims 29-30).

4. Composition-including method versions

   • Claim 40: includes a “pharmaceutical composition” administered once daily including 20 to 120 mg of the active or a salt, as the “sole active ingredient,” producing “no clinically significant weight gain.”
   • Claim 56: parallel “antipsychotic without weight gain” method using a pharmaceutical composition administered once daily with 20 to 120 mg of the active or salt as “sole active ingredient.”

These composition-framed method claims can matter because they can be harder to design around using “same drug but different formulation” arguments. Still, the claims fix the active to a precise stereochemical identity and usually specify tablet embodiment (Claims 42 and 58).

Where is the claim boundary tightest?

The tightest enforceable boundary tends to be:

• the defined active identity (stereochemical specification)
• the dose window (20 to 120 mg/day)
• the weight gain outcome (no clinically significant weight gain)
• the time checkpoint where present (6 weeks)
• the absence of concurrent antipsychotic where present
• in Claim 6, the BPRS threshold and response

Because the claims repeatedly use “such that the patient does not experience” the outcome, infringement will likely hinge on whether the real-world treated population achieves the clinically significant weight-gain threshold under the claimed regimen.

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Claim-by-claim highlights (what each cluster adds)

Core independent schizophrenia + weight gain (Claim 1)

• Independent scope: schizophrenia treatment, oral dosing 20-120 mg/day of the stereochemical active or salt, with “no clinically significant weight gain.”
• Dominant dependents:
  • hydrochloride specificity (Claim 2)
  • 6-week no-weight-gain condition (Claim 3)
  • no concurrent antipsychotic (Claim 4)
  • detecting weight gain after six weeks (Claim 5)
  • BPRS ≥ 42 and significant reduction (Claim 6)
  • dose range specifics once-daily (Claim 7)

Core independent manic depressive psychosis + weight gain (Claim 8)

• Independent scope: manic depressive psychosis treatment, oral dosing 20-120 mg/day, no clinically significant weight gain.
• Dominant dependents:
  • hydrochloride specificity (Claim 9)
  • 6-week no-weight-gain condition (Claim 10)
  • detecting weight gain after six weeks (Claim 11)
  • no concurrent antipsychotic (Claim 12)
  • multiple discrete dose embodiments (Claims 13-18)

Broad antipsychotic + weight gain outcome (Claims 25 and 40)

• Claim 25 is the “patient with an antipsychotic” master formulation that still locks the active and dose range.
• Claim 40 shifts into “pharmaceutical composition” administered once daily with 20-120 mg, and “sole active ingredient.”
• Dependent claims in this segment include:
  • hydrochloride (Claims 26, 41)
  • tablet embodiment (Claims 42, 58)
  • 6-week no-weight-gain and detection (Claims 27-28, 43-44)
  • disease mapping to schizophrenia and manic depressive psychosis (Claims 29-30, 45-46)
  • no concurrent antipsychotic (Claims 32-33, 47-48)
  • discrete dose variants including 20/40/60/80/120 mg for hydrochloride (Claims 50-55, 49, 65-75 depending on claim family)

Broad antipsychotic “without weight gain” via composition (Claims 56)

• Claim 56 includes “without a weight gain” language and a “sole active ingredient” composition.
• Dependent claims add:
  • hydrochloride sole active ingredient (Claims 57)
  • tablet embodiment (Claims 58)
  • 6-week no-weight-gain (Claims 59)
  • detecting weight gain after six weeks (Claims 60)
  • disease mapping (Claims 61-62)
  • no concurrent antipsychotic (Claims 63-64)
  • dose-specific hydrochloride compositions (Claims 65-74 and 75)

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Design-around map: where competitors can route around

What is the most straightforward infringement path?

A competitor is most exposed when it:

• uses the same stereochemically defined active (and especially the hydrochloride salt)
• uses oral dosing within 20 to 120 mg/day
• targets the same indications (schizophrenia or manic depressive psychosis) or falls within the broad antipsychotic method claims
• achieves the clinical endpoint of “no clinically significant weight gain,” including the 6-week endpoint if invoked
• avoids adding another antipsychotic concurrently when dependent claim paths require “without concurrently administering another antipsychotic medication”

Where does the patent give competitors room?

The claim language suggests three potential design-out levers, at least for certain dependent claim families:

1. Concomitant antipsychotic therapy

   • Dependent limitations require no concurrent antipsychotic. If a regimen includes another antipsychotic concurrently, those dependent claims may not be met.

2. Not meeting the “no clinically significant weight gain” endpoint

   • Because infringement is tied to whether the patient experiences clinically significant weight gain, regimens that predictably produce that outcome could fall outside the “such that” limitation. This is risky to rely on because clinical variability can still produce a “no weight gain” population.

3. Dose selection and timing controls

   • The patent fixes the dose window at 20 to 120 mg/day. Dosing outside that range avoids the explicit claim window.
   • Claims with 6-week limitations require the specified weight-gain outcome after six weeks.

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US patent landscape implications (what this implies for freedom-to-operate)

Is this a “compound patent” or a “use/dosing outcome patent”?

It is fundamentally a method-of-use patent for a specified active with specified clinical outcome framing. That structure shifts the competitive risk from:

• chemical synthesis or formulation alone to
• the clinical regimen and patient outcomes under that regimen.

How does claim style affect challenges and validity strategies?

Key features that drive examination/validity and litigation posture:

• Functional clinical outcome language (“such that” the patient does not experience clinically significant weight gain)
• Time checkpoint (six weeks) and monitoring step (detecting after six weeks)
• Concomitant therapy exclusion (“without concurrently administering another antipsychotic”)
• Multiple dependent claims lock down the preferred embodiments, especially the hydrochloride salt and discrete once-daily doses (20/40/60/80/120 mg)

As a result, challengers often focus on:

• whether the specification supports the outcome across the entire dose range and patient population
• whether “clinically significant weight gain” is defined with enough clarity and objective support to satisfy written description and enablement

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Enforcement focus: where the value likely concentrates

What is the commercial “sweet spot” of the patent?

The patent aligns to real-world schizophrenia and bipolar-spectrum prescribing where:

• oral once-daily dosing is common
• weight gain is a key tolerability and adherence driver
• clinicians use weight monitoring over weeks after initiation or titration

The repeated use of “after six weeks” suggests a practical assessment interval that could match clinical protocols and pivotal trial designs.

What claim clusters likely matter most to litigation?

In practice, litigated paths usually choose the narrowest claims that still cover the accused regimen. Here that likely means:

• hydrochloride + dose + 6-week weight-gain endpoint + absence of concurrent antipsychotic (depending on accused practice)
• or hydrochloride + weight-gain endpoint without the concurrent-therapy exclusion if the accused regimen is monotherapy

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Key Takeaways

• US 9,815,827 is a method-of-treatment patent tied to a stereochemically defined antipsychotic (and typically the hydrochloride salt) with oral dosing from 20 to 120 mg/day.
• The differentiator is a clinical outcome constraint: treatment is performed “such that” the patient does not experience clinically significant weight gain.
• Several dependent claims lock in a 6-week assessment window and include weight-gain detection as an added step.
• Multiple dependent claims also require no concurrent antipsychotic medication, creating a polypharmacy boundary.
• Independent claims cover both schizophrenia and manic depressive psychosis, plus a broader antipsychotic without weight gain framework with composition and “sole active ingredient” language.

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FAQs

1) Does the patent claim the drug structure, or only its medical use?

It claims methods of treating patients using the specified active ingredient (and salts) at specified doses under conditions that avoid clinically significant weight gain. The provided claim set is method-focused.

2) What time period is explicitly used for the weight-gain outcome?

A repeated dependent limitation is after six weeks of administration, with some claims adding detecting weight gain after six weeks.

3) Does the patent require once-daily dosing in all independent claim frameworks?

The schizophrenia and manic depressive psychosis independent claims state oral administration at 20 to 120 mg/day; the “broad antipsychotic” and composition framed independent claims explicitly use once daily.

4) Is hydrochloride specifically required?

No independent claim requires hydrochloride, but many dependent claims specify the hydrochloride and many dose-specific embodiments are written for the hydrochloride.

5) How can a competitor reduce exposure based on claim language?

The main written levers are: avoid dosing within 20 to 120 mg/day, avoid regimens that meet the “no clinically significant weight gain” outcome, and use concomitant antipsychotic therapy where dependent claims require no concurrent antipsychotic.

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References

[1] United States Patent No. 9,815,827. Claims as provided in user prompt (claims 1-75).

Drugs Protected by US Patent 9,815,827

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate

International Family Members for US Patent 9,815,827

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Austria	431147
Australia	2003257589
Germany	60327634
European Patent Office	1535616
European Patent Office	1944030
European Patent Office	2295061
Spain	2326078