Details for Patent: 10,023,560

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Which drugs does patent 10,023,560 protect, and when does it expire?

Patent 10,023,560 protects QUVIVIQ and is included in one NDA.

This patent has thirty-seven patent family members in thirty-two countries.

Summary for Patent: 10,023,560

Title:	Crystalline salt form of (S)-(2-(6 chloro-7-methyl-1H-benzo[d]imidazol-2-yl)-2-methylpyrrolidin-1-yl)(5-methoxy-2-(2H-1,2,3-triazol-2-yl)phenyl)methanone as orexin receptor antagonist
Abstract:	The invention relates to a crystalline form of (S)-(2-(6-chloro-7-methyl-1H-benzo[d]imidazol-2-yl)-2-methylpyrrolidin-1-yl)(5-methoxy-2-(2H-1,2,3-triazol-2-yl)phenyl)methanone hydrochloride, processes for the preparation thereof, pharmaceutical compositions containing said crystalline form, and its use as medicament, especially as orexin receptor antagonist.
Inventor(s):	Christoph Boss, Christine Brotschi, Markus Gude, Bibia Heidmann, Thierry Sifferlen, Markus von Raumer, Jodi T. Williams
Assignee:	Idorsia Pharmaceuticals Ltd
Application Number:	US15/702,281
Patent Claim Types: see list of patent claims	Use;

United States Patent 10,023,560: Claim Scope, Crystalline-Form Protection, and Patent Landscape

U.S. Patent No. 10,023,560 protects a specific hydrochloride crystalline form of a chiral benzimidazole-pyrrolidine compound, but only when used in claimed treatment methods. The patent does not, based on the supplied claims, independently cover the free base, every hydrochloride form, alternative polymorphs, formulations, manufacturing processes, or the compound for unclaimed indications.

The central limitation is an X-ray powder diffraction profile with characteristic peaks at 11.0°, 24.1°, and 24.5° 2θ, measured with combined Cu Kα1/Kα2 radiation without Kα2 stripping and with an accuracy of ±0.2°.[1]

What does U.S. Patent 10,023,560 protect?

The patent protects administering the identified hydrochloride compound in a defined crystalline form to treat specified disorders. The claims are method-of-treatment claims rather than standalone composition claims.

Claim group	Primary subject matter	Crystal-form limitation	Therapeutic scope
Claims 1-5	Treatment method	Three mandatory XRPD peaks; dependent claims add ten-peak pattern and disorder subcategories	Sleep, anxiety, addiction, cognitive, mood, and appetite disorders
Claims 6-10	Sleep-disorder treatment	Three-peak form, with narrower claims requiring the ten-peak pattern	Broad sleep disorders, including insomnia
Claims 11-13	Anxiety-disorder treatment	Three-peak form, with narrower claims requiring the ten-peak pattern	Anxiety disorders, including PTSD, OCD, panic attacks, phobic anxiety, and avoidance

The compound is identified by its complete chemical name:

(S)-(2-(6-chloro-7-methyl-1H-benzo[d]imidazol-2-yl)-2-methylpyrrolidin-1-yl)(5-methoxy-2-(2H-1,2,3-triazol-2-yl)phenyl)methanone hydrochloride.

The claims require the S-enantiomer and the hydrochloride salt in crystalline form. A product using the opposite enantiomer, a racemate, a different salt, or the free base would not satisfy these limitations on the face of the claims.

How does the XRPD limitation define the protected crystalline form?

The XRPD limitations are the principal boundary of the patent estate. Claim 1 requires peaks at:

Required peak	2θ position	Permitted variance
Peak 1	11.0°	±0.2°
Peak 2	24.1°	±0.2°
Peak 3	24.5°	±0.2°

The measurement protocol is part of the limitation. The patent specifies combined Cu Kα1 and Kα2 radiation and prohibits Kα2 stripping. A crystallographic comparison performed using a different radiation source, a stripped spectrum, or a materially different analytical protocol may produce a dispute over whether the comparison is legally relevant.

The claims use “comprising,” which generally permits the claimed crystal form to have additional XRPD peaks. A competing sample may therefore contain more peaks and still potentially fall within claim 1 if the three required peaks are present within the stated tolerances.

Claims 2, 7, and 12 add a more detailed ten-peak profile:

9.2°, 11.0°, 13.8°, 15.1°, 16.3°, 16.8°, 19.8°, 24.1°, 24.5°, and 27.3°.

Claims 3 and 3-related scope refer to the pattern shown in Figure 2. That language may create an evidentiary issue because “essentially shows” is less numerically precise than the listed peak limitations. In an infringement dispute, the written peak list would likely provide a more concrete comparison point than a visual assessment of Figure 2 alone.

How broad are the independent claims?

Claim 1

Claim 1 is the broadest claim in the set. It covers treatment of any one of the following:

• A sleep disorder
• An anxiety disorder
• An addiction disorder
• Cognitive dysfunction
• A mood disorder
• An appetite disorder

The claim does not limit the sleep or anxiety indication to the narrower categories later recited in dependent claims. It also does not limit the dosage, route of administration, treatment duration, patient age, severity, or combination therapy.

The claim requires an “effective amount,” but does not specify a numerical dose. That is common in therapeutic method claims and shifts the dispute toward whether the administered amount was pharmacologically effective for the claimed condition.

Claim 6

Claim 6 is independently directed to treating a sleep disorder. It repeats the three-peak crystalline-form definition and is narrower in therapeutic scope than claim 1, but it may be easier to enforce against a product promoted specifically for insomnia or another sleep indication.

Claim 11

Claim 11 independently covers treatment of an anxiety disorder using the same three-peak crystalline form. It creates a separate enforcement route from the sleep-disorder claims and may remain relevant if the compound is developed for anxiety-related conditions rather than insomnia.

What disorders fall within the claimed treatment scope?

The dependent claims identify several therapeutic subcategories.

Sleep disorders

Claims 4, 8, 9, and 10 identify:

• Dyssomnia
• Parasomnia
• Sleep disorders associated with a general medical condition
• Substance-induced sleep disorders
• Insomnia
• Sleep-related dystonia
• Restless leg syndrome
• Sleep apnea
• Jet-lag syndrome
• Shift-work sleep disorder
• Delayed sleep-phase syndrome
• Advanced sleep-phase syndrome
• Insomnia related to psychiatric disorders

Claim 10 narrows the method to insomnia. It is the most commercially relevant sleep claim if the compound reaches the market as an insomnia treatment.

The claim set does not require a particular insomnia subtype, severity threshold, diagnostic instrument, or treatment endpoint. A generic entrant or licensee would need to assess whether its labeling, prescribing information, clinical protocols, or actual use could support direct or induced infringement.

Anxiety disorders

Claims 5 and 13 identify:

• Post-traumatic stress disorder
• Obsessive-compulsive disorder
• Panic attack
• Phobic anxiety
• Avoidance

Claim 13 is the cleaner anxiety-specific dependent claim because it depends from claim 12, which is itself limited to the ten-peak crystalline form. Claim 5 appears structurally unusual because it depends from claim 4, which narrows the subject matter to sleep disorders, while then reciting anxiety-disorder categories. That dependency may create a claim-construction and validity issue.

Addiction, cognitive, mood, and appetite disorders

These indications appear only in claim 1 as supplied. There are no dependent claims defining specific addiction types, cognitive conditions, mood disorders, or appetite disorders. The scope is therefore broad in category but potentially vulnerable to indefiniteness, written-description, enablement, or construction arguments depending on the patent specification and prosecution history.

What does the patent not cover?

The supplied claims do not expressly cover the following subject matter:

Potential product or activity	Apparent coverage under supplied claims
Free-base compound	Not directly covered
Non-hydrochloride salt	Not directly covered
Amorphous hydrochloride	Not directly covered unless it meets the crystalline-form limitation
Different hydrochloride polymorph	Not covered if it lacks the required peaks
Racemic compound	Not directly covered because the claims require the S-enantiomer
R-enantiomer	Not directly covered
Pharmaceutical composition claim	No standalone composition claim supplied
Manufacturing process	No process claim supplied
Crystallization process	No process claim supplied
Dosage form such as tablet or capsule	No dosage-form claim supplied
Treatment of an unlisted disease	Potentially outside the literal scope
Mere possession or sale without treatment activity	Not directly covered by the supplied method claims

This narrow structure is commercially important. A competitor could potentially design around the claims by selecting a different salt, solid form, stereochemical form, or development indication. The viability of such a strategy depends on whether other patents in the family or related patent families cover the compound, pharmaceutical composition, synthesis, or alternative indications.

How strong is the patent estate based on the claims?

The patent has meaningful solid-state protection but limited standalone product protection in the supplied claim set.

Strength factor	Assessment
Chemical specificity	High; the claim identifies one stereoisomer and salt
Solid-form specificity	High; three mandatory XRPD peaks and a ten-peak fallback profile
Therapeutic breadth	Broad in claim 1, narrower in claims 6 and 11
Composition protection	Not apparent from supplied claims
Manufacturing protection	Not apparent from supplied claims
Design-around risk	Moderate to high
Analytical enforceability	Moderate; depends on validated XRPD testing
Label-based enforcement	Potentially meaningful for insomnia or anxiety indications
Vulnerability to prior art	Depends on disclosure of the same crystal form and use

The key strength is that pharmaceutical crystal forms can be difficult to replicate unintentionally if the claimed form is thermodynamically preferred or used in the reference product. The key weakness is that the claims are form-specific and do not appear to cover every version of the active pharmaceutical ingredient.

What infringement issues would arise for a generic or follow-on developer?

A generic or follow-on developer would face several distinct questions.

Does the proposed API have the claimed XRPD pattern?

Testing should compare the proposed material against the claimed peaks using the same or a technically equivalent protocol. The ±0.2° tolerance is material. Peaks at 10.7° or 11.3°, for example, would fall outside the stated range for the 11.0° limitation, although measurement error and instrument calibration would be contested.

Is the product the claimed hydrochloride?

A formulation containing the free base or another salt may avoid literal infringement of the claim. A salt conversion occurring during manufacture, dissolution, storage, or administration could complicate that analysis.

Does the proposed label induce infringement?

A label directing use for insomnia could create a direct infringement theory for claims 6-10 if the marketed product contains the claimed form. An anxiety indication could implicate claims 11-13. A label omitting a patented indication may reduce, but not necessarily eliminate, induced-infringement exposure where substantial off-label use is foreseeable and encouraged.

Does the API supplier create contributory-infringement exposure?

A supplier providing the claimed crystalline hydrochloride form for use in the United States could face contributory-infringement risk if the material has no substantial non-infringing use and the supplier has the required knowledge.

What is the likely Paragraph IV risk?

The supplied claims are candidates for a Paragraph IV challenge if the patent is listed in the Orange Book for an approved drug and remains unexpired. A generic applicant could challenge the patent by asserting that:

1. The proposed product does not contain the claimed crystalline form.
2. The claims are anticipated or obvious in view of prior-art crystal forms or treatment disclosures.
3. The XRPD limitations are indefinite or insufficiently reproducible.
4. The specification does not adequately enable the full range of claimed disorders.
5. The patent claims an unpatentable treatment method or lacks adequate written description.
6. The patent is unenforceable because of prosecution or inequitable-conduct issues, if supported by the record.

A non-infringement certification would be strongest if the applicant can demonstrate a different salt, polymorph, amorphous form, or enantiomer. A validity challenge would focus on whether the claimed peaks identify a genuinely distinct and non-obvious form and whether the specification teaches its preparation and therapeutic use.

What is the Orange Book and FDA status of the patent?

Patent 10,023,560 is a U.S. patent, but patent issuance alone does not establish FDA approval, Orange Book listing, regulatory exclusivity, or commercial launch. The supplied claims identify no approved product, NDA number, sponsor, or Orange Book listing.

For Orange Book purposes, the critical distinction is between:

• A patent listed against an approved drug;
• A patent held by the sponsor but not listed;
• A patent covering a clinical-stage compound;
• A patent whose claims are not relevant to the approved labeling.

A method-of-use patent may be listed only if it meets FDA listing requirements and corresponds to an approved use. If the compound has not obtained FDA approval, the patent has no Orange Book-based generic-delay mechanism. FDA regulatory exclusivity, if any, would be separate from the patent term under the Food, Drug, and Cosmetic Act.[2]

What patent litigation and settlement exposure exists?

The supplied information does not establish a filed infringement action, Paragraph IV notice, settlement agreement, or final judgment involving Patent 10,023,560. The patent’s litigation value would depend on whether:

• The compound reaches approval;
• The patented crystalline form is used in the commercial product;
• The patent is listed in the Orange Book;
• A generic applicant certifies against the patent;
• Related patents cover the active ingredient or formulation;
• The patent owner can prove that the commercial product has the claimed XRPD pattern.

If the patent is the principal remaining barrier after broader compound patents expire, it could support a later “skinny label” or alternative-solid-form strategy. If broader composition patents remain in force, Patent 10,023,560 would be one layer in a larger exclusionary estate rather than the primary barrier.

What geographic coverage does the patent provide?

The patent provides protection in the United States only. Foreign rights would depend on corresponding national or regional family members. A U.S. patent does not block manufacture, sale, or use outside the United States, although foreign manufacturing may create U.S. importation exposure if the patented product is imported into the United States.

A complete freedom-to-operate review should distinguish:

• U.S. composition patents;
• U.S. polymorph and salt patents;
• U.S. formulation patents;
• U.S. method-of-use patents;
• Foreign counterparts;
• Patent-term extensions or adjustments;
• Terminal disclaimers;
• Continuations and divisionals.

Key Takeaways

• Patent 10,023,560 is centered on a specific crystalline hydrochloride form of an S-enantiomeric compound.
• Claims 1, 6, and 11 are method claims requiring administration of the claimed solid form.
• The core XRPD limitations are peaks at 11.0°, 24.1°, and 24.5° 2θ, measured with combined Cu Kα1/Kα2 radiation without Kα2 stripping.
• Claims 2, 7, and 12 add a ten-peak XRPD profile and are narrower fallback positions.
• Claim 10 specifically targets insomnia.
• The supplied claims do not independently cover the free base, every salt, every polymorph, pharmaceutical compositions, or manufacturing processes.
• The patent can create Paragraph IV risk only if it is associated with an approved product and remains relevant to the listed product or indication.
• The unusual dependency of claim 5 may create a construction or validity issue.
• Commercial exposure depends on whether the commercial product uses the claimed crystalline form and whether broader compound or formulation patents exist.

FAQs

Does U.S. Patent 10,023,560 cover the active ingredient in every solid form?

No. The supplied claims require a particular hydrochloride crystalline form with specified XRPD peaks. They do not expressly cover every salt, polymorph, amorphous form, or free-base form.

Can a generic avoid Patent 10,023,560 by using a different polymorph?

Potentially. A different polymorph that lacks the required XRPD peaks may avoid literal infringement, subject to the full patent family, doctrine-of-equivalents arguments, and any separate composition patents.

Is insomnia the main commercial claim in the patent?

Insomnia is the narrowest and most commercially specific sleep indication in claim 10. Claims 6-9 cover broader sleep-disorder categories.

Does the patent protect a tablet or capsule formulation?

Not based on the supplied claims. The claims protect a treatment method using the specified crystalline compound, not a particular tablet, capsule, excipient system, or release profile.

What is the most important technical test in a patent dispute?

The central test is whether the accused material is the claimed hydrochloride crystalline form under the specified XRPD methodology and peak tolerances. The salt identity, stereochemistry, crystal structure, instrument conditions, and peak positions would all be material.

References

1. United States Patent No. 10,023,560, claims 1-13. U.S. Patent and Trademark Office. (2018).
2. U.S. Food and Drug Administration. (2023). Approved drug products with therapeutic equivalence evaluations. https://www.fda.gov/drugsatfda.

Drugs Protected by US Patent 10,023,560

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Idorsia	QUVIVIQ	daridorexant hydrochloride	TABLET;ORAL	214985-001	Apr 7, 2022		RX	Yes	No						TREATMENT OF INSOMNIA
Idorsia	QUVIVIQ	daridorexant hydrochloride	TABLET;ORAL	214985-002	Apr 7, 2022		RX	Yes	Yes						TREATMENT OF INSOMNIA

Foreign Priority and PCT Information for Patent: 10,023,560

Foriegn Application Priority Data
Foreign Country	Foreign Patent Number	Foreign Patent Date
	PCT/IB2013/060595	Dec 3, 2013

International Family Members for US Patent 10,023,560

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Australia	2014358743
Brazil	112016012625
Canada	2929720
Chile	2016001348