Details for Patent: 9,561,236

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Which drugs does patent 9,561,236 protect, and when does it expire?

Patent 9,561,236 protects BYFAVO and is included in one NDA.

This patent has twenty-one patent family members in sixteen countries.

Summary for Patent: 9,561,236

Title:	Dosing regimen for sedation with CNS 7056 (Remimazolam)
Abstract:	The invention relates to a dosing regimen for sedation with the fast-acting benzodiazepine CNS 7056 in combination with an opioid, in particular fentanyl, whereas CNS 7056 is given in a dose of 2 to 20 mg, preferably between 4 and 9 mg and most preferably between 5 and 8 mg.
Inventor(s):	Karin Wilhelm-Ogunbiyi, Keith Borkett, Gary Stuart Tilbrook, Hugh Wiltshire
Assignee:	Paion UK Ltd
Application Number:	US13/883,935
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 9,561,236
Patent Claim Types: see list of patent claims	Use; Delivery;

United States Patent 9,561,236 (CNS 7056 besylate) Coverage Map: Method-of-Sedation Claims with Fixed Dosing + Opioid Co-Administration (Fentanyl-Focused)

US Patent 9,561,236 claims methods for sedating a subject using CNS 7056 as its besylate salt in combination with an opioid, with the core technical/legal boundary being fixed, body-weight-independent dosing of the CNS 7056 besylate and specific co-dosing logic for fentanyl and other opioids (including timing windows and titration limits). Claim scope is concentrated around IV administration, perioperative/conscious sedation use cases, and structured fentanyl dosing schedules (including “lead-in” fentanyl given before CNS 7056).

Below is a scope-and-landscape analysis organized to support freedom-to-operate (FTO), generics/label design, and potential Paragraph IV risk mapping.

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What does US Patent 9,561,236 claim for sedation using CNS 7056 besylate + opioids?

Answer (claim essence): The patent is a method-of-use patent that covers administering CNS 7056 besylate at fixed dose levels that do not depend on body weight, in combination with an opioid (with fentanyl singled out through dependent claims), for sedation in procedural settings, using defined timing and dosing schedules.

Core active ingredient boundary

The claimed CNS 7056 is specified as the besylate salt of:

3-[(4S)-8-bromo-1-methyl-6-(2-pyridinyl)-4H-imidazo[1,2-a][1,4]benzodiazepin-4-yl]-propionic methyl ester (CNS 7056)

The claims repeatedly anchor to “besylate salt” and formula (I), meaning non-besylate salt forms or non-specified stereochemical/structural variants are outside the literal metes-and-bounds of these claims.

Core co-therapy boundary

Claim 1 requires opioid co-administration. Claim 7 defines opioid selection broadly; subsequent claims narrow to fentanyl and related analogs.

Core dosing boundary

The critical technical and legal feature is fixed-dose ranges:

• Initial dose fixed at ~2 mg to ~10 mg, irrespective of body weight
• Subsequent doses (dependent claims) fixed at defined ranges (e.g., ~1 mg to ~4 mg, ~1.5 mg to ~3.5 mg, ~2 mg to ~3 mg), also irrespective of body weight

This makes the patent’s infringement theory strongly tied to label-like regimen selection rather than to free-form individualized titration.

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How broad are claim 1 and the dosing ranges for CNS 7056 besylate irrespective of body weight?

Answer: Claim 1 is broad on the opioid side but narrow on the CNS 7056 dosing structure: it requires fixed initial dosing independent of body weight combined with an opioid.

Independent claim 1 (scope drivers)

Claim 1 covers:

• Method of sedating a subject
• Administering initial dose of CNS 7056 besylate (formula I)
• Initial dose is fixed dose between ~2 mg and ~10 mg
• Dose is irrespective of body weight
• In combination with one or more doses of an opioid

Implications for FTO and label design:

• A regimen that varies CNS 7056 dosing by weight is less likely to fit literal “irrespective of body weight.”
• A regimen that uses a different salt form (non-besylate) is less likely to fit literal salt identity.
• A regimen without opioid co-administration is outside literal scope.

Claim 2 (narrower fixed initial dose selection)

Claim 2 restricts initial fixed dose choices to subsets:

• ~3–10 mg
• ~3–9 mg
• ~5–8 mg

This tightens the “initial dose” boundary to selected ranges.

Claim 3-6 (subsequent fixed dosing + count limitation)

• Subsequent doses are fixed doses independent of body weight, selected from:
  • ~1–4 mg
  • ~1.5–3.5 mg
  • ~2–3 mg
• Claim 5: subsequent doses not earlier than 2 minutes from initial dose
• Claim 6: not more than six subsequent fixed doses

The patent thus creates a dosing “grid”: fixed dose level + timing minimums + maximum number of subsequent administrations.

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Which specific CNS 7056 besylate dose combinations are expressly claimed (8 mg + 3 mg, 7 mg + 2 mg, 5 mg + 3 mg)?

Answer: The patent expressly claims paired initial/subsequent dosing regimens that are “ready-to-design” for protocolized procedural sedation.

Claim 4 states that the initial and subsequent fixed doses can be selected from:

• (a) ~8 mg initial + ~3 mg subsequent
• (b) ~7 mg initial + ~2 mg subsequent
• (c) ~5 mg initial + ~3 mg subsequent

These pairings likely map to clinical titration protocols where the clinician administers a structured starting dose and then gives standardized rescue/maintenance increments.

Operational consequences

If a sedation protocol uses:

• CNS 7056 besylate at ~5 mg or ~7 mg or ~8 mg as an initial fixed dose, and
• subsequent doses at ~2 mg or ~3 mg with the claimed timing constraints, then the regimen is within a heavily scaffolded claim set even if other elements vary.

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What opioid co-administration is covered, and how does fentanyl-specific coverage change infringement risk?

Answer: Claim 7 makes opioid coverage broad, but multiple dependent claims focus on fentanyl and specific fentanyl dosing timing, which increases practical risk because fentanyl is common in procedural anesthesia and sedation.

Broad opioid class (claim 7)

Claim 7 lists an opioid set including (non-exhaustive due to length): morphine-related agents, hydromorphone, hydrocodone, oxycodone/oxymorphone, methadone, tramadol, buprenorphine, fentanyl and numerous fentanyl analogs.

Fentanyl center of gravity (claims 8-10, 11-16)

• Claim 8: opioid is fentanyl (or salt)
• Claim 10 repeats fentanyl selection
• Claim 11: fentanyl dose ~50 mcg to ~200 mcg
• Claim 12: fentanyl administered before the initial CNS 7056 dose
• Claim 13: fentanyl timing within at least 1/2/5/10 minutes prior
• Claim 14: first fentanyl dose between ~50–200 mcg, second dose between ~10–50 mcg
• Claim 15: second dose no earlier than 5 minutes after first
• Claim 16: second dose not exceeding 200 mcg

Why the fentanyl lead-in matters

If a protocol gives CNS 7056 first and then fentanyl later, it may avoid the dependent claim structures requiring fentanyl administered before the initial CNS 7056 dose. Claim 1 alone still requires “one or more doses of an opioid,” but the fentanyl-specific dependent logic tightens the regimen.

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What timing constraints for subsequent CNS 7056 doses appear in the claim set?

Answer: The patent imposes a minimum inter-dose time for CNS 7056 subsequent fixed doses and several fentanyl timing windows.

CNS 7056 subsequent-dose minimum (claim 5)

• Subsequent CNS 7056 fixed dose: not earlier than 2 minutes after initial dose.

CNS 7056 titration cap (claim 6)

• No more than six subsequent fixed doses.

Fentanyl lead-in windows (claims 12-13, 23-27, 29-31)

• Claim 13: within at least 1/2/5/10 minutes prior to initial CNS 7056
• Claim 23 and 29 include explicit lead-in timing “no earlier than 10 minutes before” or “within about 5 minutes prior,” depending on the regimen version.
• Claim 27 includes CNS 7056 subsequent timing “no earlier than 2 minutes” from initial or previous subsequent dose.

This makes timing a central infringement design variable for competitors: a regimen that substitutes different spacing could reduce fit to dependent claims, though Claim 1’s broad language may still capture some configurations.

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What sedation use-cases are covered: preoperative, perioperative amnestic, diagnostic, endoscopic, mild-to-deep sedation?

Answer: The patent frames sedation broadly but explicitly includes procedural contexts and sedation depth scoring.

Procedural scope (claims 17-18, 21)

• Claim 17: preoperative sedation; perioperative amnestic use; conscious sedation during diagnostic/operative/endoscopic procedures
• Claim 18: operative or endoscopic procedures
• Claim 21: operative/endoscopic procedures includes endoscopy or colonoscopy

Sedation depth / measurement (claim 20)

Claim 20 ties sedation to MOAA/S score:

• MOAA/S ≤4 or within ranges:
  • 1 to 4
  • 2 to 4
  • 3 to 4

This provides a measurable endpoint that can matter in clinical protocol labeling and method-of-use enforcement.

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How does the patent treat route of administration, and does it narrow to intravenous dosing?

Answer: Claim 22 specifies intravenous administration.

• Claim 22: CNS 7056 besylate administered intravenously.

This route limitation appears as a dependent claim, not the independent claim. It still signals that the core development and enforcement thesis is IV procedural sedation.

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What are the fentanyl + CNS 7056 regimen sub-claims (claims 23-32) and how do they structure dose sequencing?

Answer: These dependent claims define multi-dose fentanyl lead-ins and CNS 7056 fixed-dose administration schedules with explicit microgram-to-milligram relationships and strict timing offsets.

Claim 23 (structured fentanyl lead-in + CNS 7056 fixed dosing)

• Fentanyl co-administration with:
  • first fentanyl dose: ~50–200 mcg, administered no earlier than 10 minutes before initial CNS 7056
  • initial CNS 7056 dose: fixed ~5–8 mg, irrespective of body weight

Claims 24-25

• Claim 24: initial fixed CNS 7056 dose is 5 mg
• Claim 25: first fentanyl dose administered within 5 minutes prior to initial CNS 7056

Claim 26

• second fentanyl dose: ~10–75 mcg, administered no earlier than 5 minutes after first

Claims 27-28 (CNS 7056 subsequent fixed doses in regimen form)

• One or more subsequent CNS 7056 fixed doses at ~2–3 mg
• Subsequent dosing no earlier than 2 minutes after initial or previous CNS 7056 dose
• Subsequent doses are fixed and weight-independent
• Claim 28 provides pairings:
  • 8 mg initial + 3 mg subsequent
  • 7 mg initial + 2 mg subsequent
  • 5 mg initial + 3 mg subsequent

Claims 29-32 (alternative structured regimen with 1st fentanyl dose 75-150 mcg, CNS 7056 initial 5 mg, 1 to 3 subsequent CNS 7056 doses 2-3 mg)

Claim 29 specifies:

• first fentanyl IV: ~75–150 mcg within about 5 minutes prior
• initial CNS 7056 IV: ~5 mg
• one to three subsequent CNS 7056 fixed doses: ~2–3 mg, no earlier than 4 minutes from initial or previous subsequent
• all CNS 7056 doses fixed and weight-independent

Claim 30: first fentanyl dose ~100 mcg
Claim 31: second fentanyl IV dose ~10–75 mcg, no earlier than 5 minutes after first fentanyl dose
Claim 32: second fentanyl dose ~25 mcg

These claims read like clinical operating instructions. From an infringement-risk perspective, they are more specific than Claim 1 and therefore more sensitive to protocol deviations.

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How many distinct “claim families” exist within the patent as provided, and what do they cover?

Based on the claim text supplied, the patent’s internal structure can be treated as three overlapping layers:

1. Base method layer (Claim 1)

   • Sedation with CNS 7056 besylate initial fixed dose (2–10 mg) irrespective of body weight + opioid co-administration.

2. Dose-titration protocol layer (Claims 2-6, 4, 5-6)

   • Specific fixed dose ranges and paired dose regimens.
   • Timing minimum for subsequent doses (≥2 min) and cap on subsequent dose count (≤6).

3. Fentanyl scheduling/regimen layer (Claims 7-16, 23-32)

   • Fentanyl identification and microgram dose ranges.
   • Lead-in timing before initial CNS 7056.
   • Additional fentanyl dosing split (first and second fentanyl doses) and CNS 7056 subsequent fixed dosing windows.

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What would a generic or alternative manufacturer need to avoid to reduce literal infringement?

Answer: The safest design changes from a literal infringement standpoint are to break at least one structural element of the claim set:

1. Remove or change the opioid combination requirement
   Claim 1 requires opioid co-administration. A non-opioid sedation regimen avoids Claim 1 (but would need to be assessed against other patents).

2. Change salt identity
   Claims require besylate salt of the specified compound (formula I). Alternative salts are outside literal scope of these particular claims.

3. Avoid weight-independent fixed dosing
   The patent is anchored on “irrespective of body weight.” If dosing is titrated or adjusted by weight (or another covariate-based dosing logic that is not “irrespective of body weight”), it may fall outside.

4. Change CNS 7056 dosing ranges and/or timing and/or subsequent-dose counts
   Dependent claims use defined mg ranges, minimum 2-minute spacing, and a maximum number of subsequent doses. Adjusting these can reduce fit to dependents, though Claim 1 could still apply.

5. Change fentanyl lead-in sequencing
   Several dependents require fentanyl prior to initial CNS 7056, with explicit microgram doses and lead-in timing windows. Re-sequencing can reduce fit to dependents.

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What does the claim text imply about the patent’s commercial and litigation leverage?

Answer: The patent is leverage-heavy because it is:

• method-of-use (protocol-based, label-driven),
• dose- and timing-structured (easier to enforce against standardized clinical pathways),
• opioid-centric with fentanyl emphasized (high relevance to actual procedural sedation practice).

Even if a competitor uses different fentanyl dosing microgram amounts, the broader opioid combination and fixed-weight-independent CNS 7056 dosing in Claim 1 can still preserve enforcement pathways.

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What patent landscape items are likely around US 9,561,236 given its claim structure (formulation, polymorph, salt, device, and other method claims)?

No additional patents, assignees, or expiration dates are provided here, and no Orange Book listing data is included in the input. For the purpose of this analysis, the landscape can only be mapped at a functional level consistent with claim scope:

Likely neighboring IP categories (to check in public records when available)

• Salt selection patents (besylate formation, crystallization, polymorphs) covering CNS 7056 as a specific salt form.
• Formulation patents for IV ready-to-use solutions, lyophilized reconstitution, and excipient systems that stabilize a benzodiazepine-derived compound.
• Method-of-use patents for sedation depth outcomes (MOAA/S targets), perioperative indication sets, and endoscopic contexts.
• Device or administration method patents (syringe kits, dosing cartridges, infusion schedules) if the regimen is operationalized.

Landscape linkage

Because US 9,561,236 is a method claim, even if a competitor could practice the chemical (or formulation) IP-free, they still face risk from protocol-constrained method claims like this one.

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Is US 9,561,236 limited to IV CNS 7056 besylate, or does it cover other routes?

From the provided claims:

• IV is explicitly claimed in Claim 22.
• Claim 1 does not explicitly state the route.

So the legal interpretation is that Claim 22 is a route-specific dependent claim; Claim 1 could still cover non-IV routes if the rest of the dosing and opioid combination elements are satisfied. Practical enforcement will depend on how CNS 7056 is actually administered in the competing protocol.

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Key Takeaways

• US 9,561,236 is a protocol-driven method-of-sedation patent: CNS 7056 besylate at fixed, body-weight-independent initial dosing (Claim 1) plus opioid co-administration, with additional dependents that tightly define titration and timing.
• Dependent claims build “regimen fences”: specific mg pairs (8/3, 7/2, 5/3), subsequent dose timing (≥2 minutes), and a subsequent-dose cap (≤6).
• Fentanyl is the dominant enforcement vector: multiple dependents specify fentanyl identification, fentanyl microgram ranges, fentanyl lead-in timing, and multi-dose fentanyl sequencing tied to fixed CNS 7056 dosing.
• FTO risk is highest where competitors mirror clinical pathways that use standardized dosing without body-weight adjustment and include fentanyl in the defined lead-in schedules.

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FAQs

1) What elements most directly determine infringement of US 9,561,236?
Fixed-dose CNS 7056 besylate irrespective of body weight, opioid co-administration, and (in dependents) specified dose ranges, timing offsets, and fentanyl sequencing.

2) Can a competitor reduce risk by using a non-besylate salt of CNS 7056?
Not under these literal claims, which require “besylate salt” and formula (I) in the claim text.

3) How does timing affect claim coverage?
Dependent claims require minimum delays for subsequent CNS 7056 doses (≥2 minutes) and define fentanyl lead-in and second-dose spacing windows.

4) Does the patent cover endoscopy and colonoscopy specifically?
Yes, via a dependent claim referencing endoscopy or colonoscopy as procedural contexts.

5) Is intravenous administration required for all claim coverage?
No. IV is explicitly recited in a dependent claim, while the independent claim focus is on dosing and opioid combination.

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References

1. US Patent 9,561,236 (claims as provided in the prompt).

Drugs Protected by US Patent 9,561,236

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Acacia	BYFAVO	remimazolam besylate	POWDER;INTRAVENOUS	212295-001	Oct 6, 2020		RX	Yes	Yes	9,561,236					USE OF REMIMAZOLAM FOR INDUCTION AND MAINTENANCE OF PROCEDURAL SEDATION IN ADULTS UNDERGOING PROCEDURES LASTING 30 MINUTES OR LESS

Foreign Priority and PCT Information for Patent: 9,561,236

Foriegn Application Priority Data
Foreign Country	Foreign Patent Number	Foreign Patent Date
	10014366	Nov 8, 2010
	10014784	Nov 19, 2010
	10014819	Nov 22, 2010
	10014972	Nov 25, 2010

PCT Information
PCT Filed	November 07, 2011	PCT Application Number:	PCT/EP2011/005581
PCT Publication Date:	May 18, 2012	PCT Publication Number:	WO2012/062439

International Family Members for US Patent 9,561,236

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Australia	2011328497
China	103347519
Denmark	2637662
Eurasian Patent Organization	024926