United States Patent 10,342,800: Claim Scope, Exclusivity, and Remimazolam Patent Landscape

U.S. Patent No. 10,342,800 protects weight-independent administration of remimazolam, particularly when combined with an analgesic or opioid, for general anesthesia, loss of consciousness, and short procedural sedation. The strongest commercial claims are claims 19-28, which cover intravenous, fixed-dose procedural sedation in adults with supplemental dosing at specified intervals. The patent does not broadly protect remimazolam as a molecule, all remimazolam formulations, or every clinical use.

The patent is a method-of-treatment patent directed to remimazolam, the active ingredient in Byfavo. It is commercially relevant because its claims track the FDA-approved procedural-sedation dosing paradigm, including an initial intravenous dose, supplemental doses, short administration intervals, and optional opioid pretreatment [1, 2].

What drug and clinical use does U.S. Patent 10,342,800 protect?

The protected compound is:

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

This compound is remimazolam, also known as CNS 7056. The commercial product is Byfavo, remimazolam besylate, marketed in the United States by Acacia Pharma following FDA approval in 2020 [2].

The claims cover four principal use categories:

Claim group	Protected use	Key limitations
Claims 1-9	Induction and maintenance of general anesthesia	Remimazolam plus an analgesic; dose does not depend on body weight
Claims 10-18	Induction and maintenance of loss of consciousness	Remimazolam plus an analgesic; dose does not depend on body weight
Claims 19-28	Induction and maintenance of procedural sedation	Intravenous fixed-dose administration; adult patients; supplemental doses and timing
Claims 5-9 and 14-18	Opioid combinations	Opioid is required; remifentanil is a specific dependent embodiment

The claims are directed to clinical administration rather than chemical composition. They therefore operate differently from a compound patent or formulation patent. A competitor that makes remimazolam may not infringe merely by manufacturing or selling the active ingredient. Infringement risk arises when the accused party induces or performs a claimed treatment regimen.

How broad are the independent claims in Patent 10,342,800?

Claims 1, 10, and 19 are the independent claims.

Claim 1: general anesthesia

Claim 1 requires all of the following:

A subject.
Administration of remimazolam or a pharmaceutically acceptable salt.
An amount sufficient to induce general anesthesia.
Administration of an analgesic drug.
A remimazolam dose that does not depend on body weight.

The claim is broad as to the analgesic because claim 1 does not limit the analgesic to an opioid. Claims 5-9 narrow the scope to opioids and identify remifentanil as a specific embodiment.

The claim is narrower than a general remimazolam anesthesia claim because it requires a non-weight-based dose and coadministration of an analgesic. A weight-based dosing protocol, or remimazolam administered without an analgesic, would present a noninfringement position against claim 1, subject to the construction of "does not depend on the body weight."

Claim 10: loss of consciousness

Claim 10 mirrors claim 1 but substitutes "induce loss of consciousness" for "induce general anesthesia." This language creates a potentially broader clinical category. Loss of consciousness may occur during procedural sedation without meeting the full clinical definition of general anesthesia.

Claims 10-18 preserve the same principal limitations:

remimazolam or a pharmaceutically acceptable salt;
an analgesic drug;
a non-weight-based remimazolam dose;
optional maintenance dosing;
optional airway maintenance or positive-pressure ventilation;
optional opioid use.

The distinction between general anesthesia and loss of consciousness may become important in litigation involving deep sedation protocols. The clinical record, drug administration records, monitoring requirements, and stated indication would likely be relevant to whether the treatment falls within the claim language.

Claim 19: procedural sedation

Claim 19 is the most commercially aligned independent claim. It requires:

intravenous administration;
induction and maintenance of procedural sedation;
an initial remimazolam dose of about 2 mg to about 10 mg;
administration over one minute;
a dose that does not depend on body weight.

Unlike claims 1 and 10, claim 19 does not require an analgesic. It also does not require an opioid, airway maintenance, positive-pressure ventilation, or general anesthesia.

The use of "about" creates range flexibility but does not eliminate the need to remain within a clinically and legally reasonable interpretation of the 2 mg to 10 mg range. The claim does not expressly require that the product be Byfavo, remimazolam besylate, or any particular vial strength.

What do claims 20-28 add to the procedural-sedation protection?

The dependent claims create a dosing-protocol layer around claim 19.

Claim	Added limitation
20	Subject is at least 18 years old
21	Supplemental remimazolam doses of about 2 mg to about 10 mg over 15 seconds
22	Supplemental dosing no less than four minutes after the initial or prior supplemental dose
23	Supplemental dosing no less than three minutes after the initial or prior supplemental dose
24	Supplemental dosing no less than two minutes after the initial or prior supplemental dose
25	Opioid administered before the initial remimazolam dose
26	Opioid is fentanyl
27	Supplemental dose adjusted according to sedation level
28	Dose adjusted to maintain mild to moderate sedation

Claims 22-24 require careful construction. Claim 22 recites a four-minute minimum, while claims 23 and 24 recite three-minute and two-minute minimums, respectively. Because each depends on claim 22, the literal claim structure creates a drafting issue: the four-minute limitation remains inherited unless a court treats the later timing language as modifying or superseding the earlier limitation. A two-minute dosing interval is commercially important, but claim 24 should not automatically be read as eliminating claim 22's four-minute limitation.

The FDA-approved Byfavo label describes a 5 mg initial dose administered over one minute and 2.5 mg supplemental doses administered over 15 seconds, with supplemental doses administered at least two minutes apart when clinically indicated [2]. That regimen maps closely to the numerical and timing limitations in claims 19, 21, 24, 27, and 28.

When does U.S. Patent 10,342,800 lose exclusivity?

The patent issued July 9, 2019. Its effective patent-term expiration depends on the applicable earliest effective U.S. filing or international filing date, patent-term adjustment, and any terminal disclaimer. The nominal term should be assessed from the patent's recorded priority and filing data rather than the issue date.

The patent is expected to provide protection into the mid-2030s, subject to the official USPTO term calculation. The practical exclusivity date for Byfavo cannot be determined from the claims alone. It must be read with the patent's front-page term data, any patent-term adjustment, and the FDA Orange Book listing.

Exclusivity timeline

Event	Date or status
U.S. Patent 10,342,800 issued	July 9, 2019
FDA approval of Byfavo	July 2, 2020
Approved indication	Intravenous induction and maintenance of procedural sedation in adults
Patent category	Method-of-treatment patent
Small-molecule regulatory exclusivity	Not biologic exclusivity; standard drug exclusivity framework
Expected patent horizon	Mid-2030s, subject to USPTO term calculation
Pediatric exclusivity	Must be confirmed from FDA records; not established by the supplied claims

FDA approval does not convert the patent into a composition-of-matter patent. It confirms that the claimed clinical use overlaps with the approved product's labeling and dosing instructions.

What is the Orange Book status of Patent 10,342,800?

A patent is Orange Book-relevant only if it is listed for an approved drug and satisfies FDA listing standards for the drug substance, drug product, or method of use. Method-of-use patents are generally listed with a use code describing the protected indication.

For Byfavo, the relevant Orange Book analysis should separate:

compound or drug-substance patents;
formulation or drug-product patents;
method-of-use patents;
patents covering specific dosing regimens;
any listed patents that have expired, been delisted, or been replaced.

Patent 10,342,800 is principally a method-of-use patent. Its likely relevance to an abbreviated new drug application depends on whether FDA lists it for Byfavo and whether the applicant must make a Paragraph IV certification against it. A generic applicant could instead file a section viii statement and carve out the patented use, but that strategy would be difficult if the label's remaining uncarved language still directs use in the claimed procedural-sedation regimen [3, 4].

How does a Paragraph IV challenge affect Patent 10,342,800?

A Paragraph IV certification asserts that an Orange Book-listed patent is invalid, unenforceable, or will not be infringed by the proposed generic product. For a method patent, the principal litigation issues would include:

Claim construction. The meaning of "does not depend on the body weight" would be central.
Indefiniteness. The phrase may be challenged if the patent does not provide an objective boundary for fixed versus weight-adjusted dosing.
Written description and enablement. A challenger could test whether the disclosure supports the breadth of all analgesics, opioids, salts, doses, and anesthesia settings recited in the claims.
Anticipation. Prior clinical or patent publications describing remimazolam with opioids, fixed dosing, or procedural sedation could be asserted.
Obviousness. The combination of a short-acting benzodiazepine, opioid analgesia, fixed dosing, and procedural sedation may be challenged as an obvious clinical protocol.
Infringement. A generic label, distributor instructions, or institutional use protocol would be examined for induced infringement.

The FDA's approval of a generic application does not itself decide patent validity or infringement. A 30-month stay may apply if the patent owner files suit within the statutory period after receiving a Paragraph IV notice [3].

What formulations are protected by Patent 10,342,800?

Patent 10,342,800 does not principally claim a formulation. It covers administration of remimazolam or a pharmaceutically acceptable salt. The claims do not expressly require:

a particular excipient;
a lyophilized powder;
a vial configuration;
a reconstitution solvent;
a specific concentration;
a pH range;
a preservative;
a particular infusion device;
a ready-to-use solution.

This limits its value against formulation-only competitors. A separate formulation patent could protect stability, reconstitution, concentration, packaging, or administration-device features. Conversely, a competitor could avoid a formulation claim while still infringing a method claim if it uses remimazolam according to the claimed regimen.

How strong is the patent estate for remimazolam?

The estate should be assessed by patent category rather than by the number of patents alone.

Patent category	Commercial purpose	Relevance of Patent 10,342,800
Composition of matter	Blocks manufacture and use of the molecule	Low; the patent is not principally a compound patent
Salt or solid form	Protects remimazolam besylate or another solid form	Limited
Formulation	Protects vial, concentration, stability, or reconstitution	Limited
Manufacturing process	Raises production barriers	None apparent from the supplied claims
General anesthesia method	Protects remimazolam plus analgesic dosing	High
Procedural sedation method	Protects fixed-dose IV protocols	High
FDA-approved labeling	Defines commercial use and generic carve-out options	High

The method estate is strongest where the commercial label directly practices the limitations: adult procedural sedation, intravenous delivery, a five-milligram initial dose, supplemental dosing, short administration intervals, and sedation-level titration [1, 2].

The estate is weaker against:

nonclinical research use;
manufacturing-only activity;
a product sold without instructions for the patented use;
a dosing protocol expressly based on body weight;
a formulation that cannot reasonably be administered under the claimed protocol;
a use outside procedural sedation, general anesthesia, or loss of consciousness.

Which companies are challenging remimazolam exclusivity?

Remimazolam is a small molecule, so biosimilar competition is not the relevant pathway. The principal future challenge would come from an ANDA applicant seeking approval for a generic remimazolam product.

Potential challengers would need to address:

the listed drug's active ingredient and salt;
injectable formulation requirements;
clinical labeling;
method-of-use patents;
Paragraph IV or section viii certifications;
controlled-substance and hospital-use distribution requirements, if applicable.

No biosimilar pathway applies to Byfavo. A 505(b)(2) applicant could be more relevant than a conventional ANDA applicant if it proposes a different formulation, route, dosing regimen, or clinical use requiring reliance on the reference product's safety and efficacy data.

What patent litigation and settlements affect Patent 10,342,800?

The supplied information does not establish a specific Paragraph IV complaint, judgment, settlement, license, or covenant not to sue involving Patent 10,342,800. The patent record and FDA litigation documents must be read separately from the issued claims.

No licensing right can be inferred from patent ownership alone. Commercial rights for remimazolam have involved corporate transactions and regional commercialization arrangements, but a license or settlement affecting this specific patent requires documentary confirmation from the agreement, court docket, SEC filing, or patent assignment record.

What generic launch scenarios exist for Byfavo?

Scenario 1: launch after all relevant patents expire

This is the lowest litigation-risk path. The applicant avoids a Paragraph IV dispute but accepts delayed market entry.

Scenario 2: Paragraph IV challenge

The applicant challenges Patent 10,342,800 and any other listed patents. The key defenses would likely target obviousness, indefiniteness, enablement, and the scope of the dosing language.

Scenario 3: section viii carve-out

The applicant removes the patented use from its label. This may be viable if the remaining label does not instruct procedural sedation using the claimed fixed-dose protocol. It is less attractive when the patented regimen is the principal or only commercial use of the reference product.

Scenario 4: 505(b)(2) product

A reformulated or differently dosed remimazolam product could pursue a 505(b)(2) application. It would still face listed-patent certifications and possible infringement litigation.

How does remimazolam compare with midazolam and propofol patent risk?

Product	Active ingredient	Patent risk profile	Regulatory position
Byfavo	Remimazolam besylate	Method, formulation, and related product patents may delay generic entry	FDA-approved procedural sedation
Versed	Midazolam	Mature generic market; primary compound exclusivity has expired	Established generic benzodiazepine
Diprivan and generic propofol	Propofol	Mature product and formulation competition	Established injectable anesthetic
Remifentanil products	Remifentanil	Separate opioid product and method estates	Used as analgesic adjunct

Patent 10,342,800 differentiates remimazolam through dosing and clinical-use claims rather than by excluding all competing anesthetics. A midazolam or propofol manufacturer generally would not infringe a remimazolam method claim because the claim requires the specific remimazolam molecule. The competitive risk is therefore primarily generic remimazolam and alternative-sedative substitution, not direct patent infringement by established anesthetic products.

What are the principal claim vulnerabilities?

The most material vulnerabilities are:

Functional dosing language: "does not depend on the body weight" may be disputed as indefinite or difficult to apply to real-world titration.
Clinical endpoint ambiguity: "general anesthesia," "loss of consciousness," and "procedural sedation" can overlap clinically.
Analgesic breadth: claims 1 and 10 cover an analgesic drug broadly, while dependent claims narrow to opioids.
Obviousness risk: fixed-dose remimazolam and opioid coadministration may be challenged using clinical prior art.
Redundant timing claims: claims 22-24 create an internal hierarchy issue.
Method-of-treatment enforcement: infringement may depend on physician conduct, label instructions, institutional protocols, or induced-infringement evidence.
No direct formulation protection: a competing formulation may avoid this patent while remaining commercially substitutable.

Key Takeaways

Patent 10,342,800 is a remimazolam method-of-use patent, not a broad molecule patent.
Claims 1-18 cover remimazolam with an analgesic or opioid for general anesthesia and loss of consciousness.
Claims 19-28 cover fixed-dose intravenous procedural sedation, adult use, supplemental dosing, timing, opioid pretreatment, and sedation-level adjustment.
The patent closely tracks the FDA-approved Byfavo procedural-sedation regimen.
The principal legal issue is whether a competitor's label or clinical protocol practices the claimed fixed-dose and timing limitations.
Remimazolam is a small molecule; biosimilar competition does not apply.
The patent is expected to remain relevant into the mid-2030s, but the precise expiration date requires the official USPTO term calculation.
No litigation, settlement, or license affecting this specific patent is established by the supplied claim text.
Generic entry could occur through patent expiry, a Paragraph IV challenge, a section viii carve-out, or a 505(b)(2) pathway.

FAQs About U.S. Patent 10,342,800

Does Patent 10,342,800 cover remimazolam itself?

No. The claims require administration of remimazolam in specified clinical methods. They do not broadly claim the chemical compound as a standalone composition.

Can a generic avoid Patent 10,342,800 by using weight-based dosing?

A genuinely weight-based protocol may avoid the express "does not depend on body weight" limitation. The result would depend on the label, actual clinical instructions, and whether the dosing method is fixed in practice.

Does the patent cover remimazolam administered without fentanyl?

Claims 1 and 10 require an analgesic, but they do not limit the analgesic to fentanyl. Claim 19 does not require an analgesic. Fentanyl is a narrower dependent embodiment under claims 25 and 26.

Is Patent 10,342,800 relevant to pediatric Byfavo use?

The independent procedural-sedation claim is not limited to adults, but claim 20 expressly requires a subject who is at least 18 years old. The FDA-approved indication and labeling must be compared with the specific claim being asserted.

Can a formulation patent and Patent 10,342,800 be infringed at the same time?

Yes. A product could practice a protected formulation and also be administered according to the patented remimazolam dosing method. The two patents would create separate infringement theories.

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	⤷ Start Trial	⤷ Start Trial				USE OF REMIMAZOLAM FOR INDUCTION AND MAINTENANCE OF PROCEDURAL SEDATION IN ADULTS UNDERGOING PROCEDURES LASTING 30 MINUTES OR LESS	⤷ Start Trial
>Applicant	>Tradename	>Generic Name	>Dosage	>NDA	>Approval Date	>TE	>Type	>RLD	>RS	>Patent No.	>Patent Expiration	>Product	>Substance	>Delist Req.	>Patented / Exclusive Use	>Submissiondate

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

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Australia	2011328497	⤷ Start Trial
China	103347519	⤷ Start Trial
Denmark	2637662	⤷ Start Trial
>Country	>Patent Number	>Estimated Expiration	>Supplementary Protection Certificate	>SPC Country	>SPC Expiration

Details for Patent: 10,342,800

Which drugs does patent 10,342,800 protect, and when does it expire?

Summary for Patent: 10,342,800