Details for Patent: 10,195,205

Which drugs does patent 10,195,205 protect, and when does it expire?

Patent 10,195,205 protects LYNKUET and is included in one NDA.

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

Summary for Patent: 10,195,205

Title:	Uses of dual NK1/NK3 receptor antagonists for treating sex-hormone diseases
Abstract:	This invention relates to new use of dual NK-1/NK-3 receptor antagonists or a pharmaceutically acceptable salt thereof in the treatment of sex-hormone dependent diseases.
Inventor(s):	Mike Trower
Assignee:	Kandy Therapeutics Ltd
Application Number:	US15/157,430
Patent Claim Types: see list of patent claims	Use;

US Patent 10,195,205 scope and claims for dual NK-1/NK-3 antagonist in hot flush treatment: what the claims cover, what’s excluded, and where generic risk sits

Executive summary: U.S. Patent 10,195,205 is a method-of-treatment patent that asserts hot flush therapeutic use for a specific dual NK-1/NK-3 receptor antagonist defined by a formula (A) chemical name (and pharmaceutically acceptable salts). The claim set is tightly focused on (i) treatment of hot flushes by administering the compound or salt, and (ii) oral administration that alleviates symptoms. A dependent scope carve-in requires crystalline anhydrate Form 1 when practicing claims 2 and 4. The patent landscape implications are that a generic/biosimilar risk depends primarily on whether a challenger can avoid practicing the claimed method (hot flushes) and, for the Form 1 dependent claims, avoid sourcing or using the specific Form 1 solid form (or use a formulation that does not infringe those dependent limitations).

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What does US Patent 10,195,205 claim for hot flushes using dual NK-1/NK-3 antagonists?

Core answer (claim scope): The patent covers methods of treatment of hot flushes in humans that are performed by administering a specific dual NK-1/NK-3 receptor antagonist of formula (A) or a pharmaceutically acceptable salt. It also covers oral administration effective to alleviate hot flush symptoms. Two dependent claims restrict the compound to crystalline anhydrate Form 1.

Claim 1: “method of treatment” for hot flushes

Claim type: method of treatment (medical use)

Preamble/setting: “A method of treatment of hot flushes comprising administering to a human in need thereof an effective amount …”

Active ingredient limitation:

• “dual NK-1/NK-3 receptor antagonist”
• chemical identity fixed as the full named compound of formula (A):
  2-[3,5-Bis(trifluoromethyl)phenyl]-N-{4-(4-fluoro-2-methylphenyl)-6-[(7S,9aS)-7-(hydroxymethyl)hexahydropyrazino[2,1-c][1,4]oxazin-8(1H)-yl]-3-pyridinyl}-N,2-dimethylpropanamide
• or pharmaceutically acceptable salt of that compound

Functional boundary: “administering … an effective amount”

• This is a typical efficacy trigger; it does not expressly define dose mg ranges, titration, or regimen length.
• It is still a strict claim requirement because infringement hinges on whether the administered amount is “effective” for treating hot flushes.

Practice boundary (where infringement concentrates):

• infringement is most likely tied to clinician prescribing and patient administration for hot flushes, not just supply of API.

Claim 2: Form 1 crystalline anhydrate limitation

Claim type: dependent

Additional limitation:

• The dual NK-1/NK-3 receptor antagonist is the compound of formula (A) as crystalline anhydrate Form 1.

Scope consequence:

• Claim 2 is narrower than claim 1 because it requires the specific solid-state form “crystalline anhydrate Form 1.”
• In infringement analysis, solid-form evidence becomes central: polymorph/salt/hydrate/isomeric form characterization, supplier documentation, and formulation manufacturing records.

Claim 3: oral administration effective to alleviate symptoms

Claim type: dependent

Additional structural/route limitation:

• “orally administering … an effective amount …”
• “wherein said orally administering is effective to alleviate symptoms of hot flushes.”

Scope consequence:

• Claim 3 is narrower than claim 1 by adding route of administration (oral) and symptom-alleviation language tied to hot flushes.

Claim 4: oral + Form 1

Claim type: dependent on claim 3

Additional solid-form limitation:

• The compound must be crystalline anhydrate Form 1.

Scope consequence:

• Claim 4 is the narrowest claim in the set.

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How broad is the chemical and salt coverage in US 10,195,205?

Core answer: The chemical coverage is broad in one key respect (salts), but narrow in another (a single named compound of formula (A), including pharmaceutically acceptable salts only).

What is included

• the exact dual NK-1/NK-3 receptor antagonist defined in formula (A)
• pharmaceutically acceptable salts of that antagonist

What is not captured by claim text

• no explicit coverage for analogs, prodrugs, other NK-1/NK-3 antagonists, or different stereoisomers (the name indicates (7S,9aS) stereochemistry, locking identity through the full chemical definition)
• no explicit coverage for metabolites or active intermediates unless they meet the definition of formula (A) or salts

Salt strategy

Because claim 1 includes “pharmaceutically acceptable salt,” a challenger cannot easily avoid infringement by switching between salts unless the alternate salt is argued not to be “pharmaceutically acceptable” or not within the defined compound(s) and their salts.

Practically, this means salt selection may not be a clean design-around if the salt is standard and recognized.

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Where does infringement turn: method-of-use vs product manufacture?

Core answer: The claims are “method of treatment” claims, so the infringement fact pattern is linked to using the compound for hot flush treatment in the claimed manner.

Claim 1 infringement levers

• is the patient a human “in need” of treatment for hot flushes?
• is the administered compound the formula (A) dual NK-1/NK-3 antagonist or a pharmaceutically acceptable salt?
• was the administered amount “effective” to treat hot flushes?

Claim 3 infringement levers

• same as claim 1 plus:
• route: oral administration
• effectiveness: “effective to alleviate symptoms”

Claim 2/4 infringement levers

• same as claim 1/3 plus:
• the solid form is crystalline anhydrate Form 1

Bottom line:

• A product-only sale with no “hot flush” usage may be a weaker infringement pathway depending on factual and jurisdictional enforcement posture.
• Product labels, clinical indications, physician prescribing patterns, REMS/OTC posture, and FDA labeling all influence whether the claimed “method” is actually practiced.

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What patents or patent categories usually surround this kind of method claim? (Landscape mapping by claim dependency)

Core answer: Method claims like these typically sit in a broader estate that includes chemical composition, solid form, and formulation, plus earlier pharmacology and clinical claims.

Because the provided prompt contains only the claim text, the landscape below is structured as category-level risk for any portfolio built around a crystalline Form 1 NK-1/NK-3 antagonist for hot flushes.

Likely adjacent patent buckets

1. Active ingredient / composition of matter

   • coverage for formula (A) (and possibly salt forms)
   • may be a “base” composition patent earlier in time than the method patent

2. Solid-state / polymorph patents

   • specifically crystalline anhydrate Form 1
   • commonly includes preparation, characterization, and use in pharmaceutical compositions

3. Formulation patents

   • oral dosage forms that deliver the drug (tablets/capsules) and may be designed to maintain Form 1 stability

4. Method-of-use patents

   • hot flushes (what this patent covers)
   • related menopausal symptoms or other NK-1/NK-3-responsive indications (often broader or narrower variants)

5. Manufacturing / process patents

   • processes to produce Form 1, prevent conversion to other polymorphs, or control crystallization conditions

6. Biomarkers / endpoints / dosing regimens

   • sometimes adds separate claims with measurable hot flush endpoints or dosing schedules

Why the “Form 1” dependent claims matter

Form 1 is a strong hinge point because it can be used for:

• claim differentiation (claim 2 and 4 narrow relative to claim 1 and 3)
• enforcement against specific manufacturing/solid form sourcing
• design-around: developing an alternative solid form or a formulation that avoids infringement of the “Form 1” limitation

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What is the likely claim-construction focus for “crystalline anhydrate Form 1”?

Core answer: Claim scope for Form 1 turns on whether the administered drug in practice is the crystalline anhydrate Form 1 as defined in the patent record.

Key evidentiary targets in infringement

• solid-state characterization (typical methods include XRD patterns, DSC, TGA, IR, Raman)
• stability and polymorphic conversion behavior in formulation and storage
• whether the supplier consistently delivers Form 1 or a mixture (Form 1 plus other forms)

Design-around vectors

• develop a different solid form (hydrate, other anhydrate polymorph)
• use a formulation that transforms the administered solid state such that it is no longer Form 1 at time of administration (fact-dependent)
• use a salt different in crystal lattice such that the claimed “compound as crystalline anhydrate Form 1” limitation is not met (again depends on solid form definitions)

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When does US 10,195,205 lose exclusivity: how to reason from claim type

Core answer: For method-of-treatment patents like this, regulatory exclusivity (Hatch-Waxman) is separate from patent expiration. Patent expiration timing drives enforceability, not FDA exclusivity alone.

Because the actual patent record details (filing date, priority, and expiry) are not included in the prompt, a numeric exclusivity timeline cannot be produced from the provided data without risking inaccuracy.

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How would a Paragraph IV challenge typically attack US 10,195,205?

Core answer: A Paragraph IV theory against a method-of-use patent commonly focuses on one or more of: (i) non-infringement (no “hot flush” use or no effective administration for that purpose), (ii) invalidity (anticipation/obviousness of NK-1/NK-3 hot flush therapy or Form 1), and (iii) failure to meet solid-form limitations for dependent claims.

Non-infringement routes

• no oral label or no indication for hot flushes
• different compound (not formula (A))
• different salt
• different solid form (not crystalline anhydrate Form 1)

Invalidity routes

• earlier prior art teaching hot flush treatment with the same compound or a compound falling within the claim definition
• prior publications or patents describing Form 1 and its use
• obviousness combinations of known NK-1/NK-3 antagonists for hot flushes
• lack of enablement or indefiniteness tied to Form 1 definition (if claim relies on characterization without clear criteria)

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Which product features increase risk of infringement under this patent?

Core answer: Risk rises with (i) hot flush labeled use, (ii) oral route, and (iii) formulation that uses or converts to crystalline anhydrate Form 1.

High-risk fact pattern

• oral dosage form of formula (A) delivered as crystalline anhydrate Form 1
• intended and indicated for treating hot flushes in humans
• prescribing and administration consistent with “effective amount” for symptom relief

Lower-risk fact pattern

• non-oral administration
• non-Form-1 solid form
• non-formula (A) active ingredient
• use not directed to hot flush treatment (fact-dependent on how “method” infringement is pursued)

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What commercial exposure exists from this claim set?

Core answer: The commercial exposure is concentrated around the marketed drug that:

• contains the formula (A) dual NK-1/NK-3 antagonist
• is used for hot flushes (likely menopausal vasomotor symptoms, though the claim text is “hot flushes”)
• is administered orally for symptom relief
• supplies or maintains crystalline anhydrate Form 1

Where the same molecule is sold for other indications or delivered via non-oral route, the method claim’s practical exposure drops.

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Key Takeaways

• US 10,195,205 is a method-of-treatment patent covering hot flush therapy by administering a specific dual NK-1/NK-3 receptor antagonist (formula (A)) or pharmaceutically acceptable salts.
• Claim 1 covers treatment by administration of formula (A) (or salt) without specifying route.
• Claim 3 narrows to oral administration effective to alleviate hot flush symptoms.
• Claims 2 and 4 further narrow to the compound as crystalline anhydrate Form 1, making solid-state identity a central enforcement and design-around axis.
• Generic and biosimilar design-around strategies, in practice, focus on avoiding (i) the claimed compound identity, (ii) the claimed method context (hot flush treatment and “effective” administration), and (iii) for the narrowest claims, Form 1 solid-state delivery.

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FAQs

1) Does US 10,195,205 cover any NK-1/NK-3 antagonist for hot flushes?
No. It is limited to the specific dual NK-1/NK-3 receptor antagonist defined by formula (A) (or its pharmaceutically acceptable salts) and, for dependent claims, crystalline anhydrate Form 1.

2) Is oral dosing required to infringe?
Not for claim 1, but it is required for claims 3 and 4 (“orally administering”).

3) Can switching salts avoid infringement of claim 1?
Claim 1 already includes pharmaceutically acceptable salts, so routine salt switching is unlikely to avoid coverage unless an alternate salt is argued not to qualify under the claim or the active ingredient no longer matches the claimed chemical.

4) How important is the “crystalline anhydrate Form 1” limitation?
It is decisive for claims 2 and 4; infringement hinges on whether the administered compound is the claimed Form 1 solid form.

5) What is the primary attack surface in challenging this patent?
Non-infringement based on compound identity, route, intended hot-flush method use, and solid form; and invalidity based on prior art relating to hot flush treatment and/or Form 1.

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References (APA)

1. U.S. Patent 10,195,205.

Drugs Protected by US Patent 10,195,205

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Bayer Hlthcare	LYNKUET	elinzanetant	CAPSULE;ORAL	219469-001	Oct 24, 2025		RX	Yes	Yes	10,195,205					TREATMENT OF MODERATE TO SEVERE VASOMOTOR SYMPTOMS DUE TO MENOPAUSE

International Family Members for US Patent 10,195,205

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	3297631		PA2026506	Lithuania
European Patent Office	3297631		C20260003	Finland
European Patent Office	3297631		CR 2026 00007	Denmark
European Patent Office	3297631		LUC50035	Luxembourg