Details for Patent: 9,949,998

Which drugs does patent 9,949,998 protect, and when does it expire?

Patent 9,949,998 protects GLYXAMBI, SYNJARDY XR, TRIJARDY XR, and JARDIANCE, and is included in four NDAs.

Protection for SYNJARDY XR has been extended six months for pediatric studies, as indicated by the *PED designation in the table below.

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

Summary for Patent: 9,949,998

Title:	Pharmaceutical composition, methods for treating and uses thereof
Abstract:	The present invention relates to certain SGLT-2 inhibitors for treating and/or preventing metabolic disorders, such as type 1 or type 2 diabetes mellitus or pre-diabetes, in patients with renal impairment or chronic kidney disease (CKD).
Inventor(s):	Uli Christian BROEDL, Sreeraj MACHA, Maximilian von EYNATTEN, Hans-Juergen Woerle
Assignee:	Boehringer Ingelheim International GmbH
Application Number:	US14/918,727
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 9,949,998
Patent Claim Types: see list of patent claims	Use; Composition; Delivery;

# US Patent 9,949,998: Empagliflozin Renal-Function Dosing Claims, Patent Scope, and Generic-Entry Risk

US Patent 9,949,998 protects a narrow method of using empagliflozin, the active ingredient in Jardiance, in patients with type 2 diabetes and moderately reduced renal function. The claims require four operative elements: type 2 diabetes, eGFR of at least 45 but below 60 mL/min/1.73 m², once-daily oral administration of 10 mg or 25 mg empagliflozin, and discontinuation when eGFR falls below 45. Claims 4 through 6 and 10 through 12 expressly require renal-function assessment.

The patent is a method-of-use asset rather than a basic compound or tablet-composition patent. Its commercial value depends on whether a generic label, physician instructions, or actual treatment practice causes the generic product to be used within the claimed renal-function range. The patent does not cover all empagliflozin treatment, all Jardiance tablets, or patients with every level of renal impairment.

What does US Patent 9,949,998 protect?

US 9,949,998 protects methods for improving glycemic control or treating type 2 diabetes with empagliflozin in patients whose eGFR is 45 to less than 60 mL/min/1.73 m².

Element	Required limitation
Disease	Type 2 diabetes mellitus
Patient selection	eGFR ≥45 and <60 mL/min/1.73 m²
Drug	Empagliflozin
Route	Oral
Frequency	Once daily
Dose	10 mg or 25 mg
Therapeutic result	Improved glycemic control
Renal monitoring	Explicitly required in claims 4-6 and 10-12
Discontinuation trigger	Stop empagliflozin if eGFR falls below 45

The independent claims are claims 1, 4, 7, and 10. Claims 1 and 7 do not expressly require the step of assessing renal function, although they require administration based on the patient’s eGFR. Claims 4 and 10 require an assessment step before administration.

Claims 2, 3, 5, 6, 8, 9, 11, and 12 narrow the dose to either 10 mg or 25 mg. They do not add a new dosing frequency, formulation type, or patient population.

How do the independent claims differ?

The claim set contains three overlapping treatment concepts.

Claims	Primary purpose	Required renal assessment?	Drug dose
1-3	Improve glycemic control	No express assessment step	10 mg or 25 mg
4-6	Improve glycemic control after renal assessment	Yes	10 mg or 25 mg
7-9	Treat type 2 diabetes and improve glycemic control	No express assessment step	10 mg or 25 mg
10-12	Treat type 2 diabetes after renal assessment	Yes	10 mg or 25 mg

The claim groups are substantively similar. Claims 7 and 10 use the broader treatment framing, while claims 1 and 4 focus on improving glycemic control. All groups retain the same eGFR window, dose range, once-daily administration, and discontinuation requirement.

The claims are cumulative in practical effect. A treatment protocol that includes renal assessment can potentially fall within both the assessment-based and non-assessment-based claim groups, provided the other limitations are met.

What is the scope of the eGFR limitation?

The renal-function limitation is central to infringement.

The claims cover patients with:

• eGFR equal to 45;
• eGFR above 45;
• eGFR below 60;
• any value within that interval at the time of treatment.

The claims do not cover, based solely on the stated eGFR limitation:

• patients with eGFR of 60 or higher;
• patients with eGFR below 45 at the time empagliflozin is administered;
• treatment protocols limited to patients with severe renal impairment below 30;
• treatment where the relevant renal threshold is expressed only as an unspecified "moderate impairment" category.

The discontinuation limitation creates a second renal-function requirement. A claimed protocol must discontinue empagliflozin when eGFR falls below 45. Continued treatment below that threshold would create a potential non-infringement position for the discontinuation limitation, but it could conflict with the product label or other regulatory requirements.

The patent therefore protects a defined renal-management algorithm, not simply the use of empagliflozin in chronic kidney disease.

What dose and formulation does US 9,949,998 cover?

The claims cover oral pharmaceutical compositions containing either 10 mg or 25 mg of empagliflozin administered once daily.

The claim language does not require a particular excipient system, coating, particle size, polymorph, tablet hardness, dissolution profile, or manufacturing process. It also does not expressly require the commercial Jardiance tablet formulation.

The covered products can include:

• a 10 mg empagliflozin tablet;
• a 25 mg empagliflozin tablet;
• another oral once-daily pharmaceutical composition containing one of those doses.

The patent does not appear, from the asserted claim language, to cover:

• a 5 mg dose;
• twice-daily administration;
• nonoral administration;
• a composition without empagliflozin;
• a fixed-dose combination unless it otherwise satisfies every claim limitation.

A generic applicant could therefore avoid direct product-composition infringement while still facing method-of-use exposure if its proposed labeling directs use within the claimed eGFR range.

Is US 9,949,998 a formulation patent or a method-of-use patent?

US 9,949,998 is principally a method-of-use patent.

It contains a dosage-form limitation, but that limitation identifies the dose and oral once-daily mode of administration. It does not claim the physical tablet or its excipients as a composition of matter.

Patent category	Covered by the stated claims?
Empagliflozin chemical compound	No
Empagliflozin polymorph or crystalline form	No express coverage
Tablet composition	No express composition claim
Manufacturing process	No
Oral 10 mg or 25 mg administration	Yes
Renal-function-based treatment protocol	Yes
Glycemic-control treatment	Yes
Type 2 diabetes treatment	Yes

This distinction matters in ANDA litigation. A generic manufacturer may avoid infringement of a formulation patent by using a different process or excipient system. That strategy does not necessarily avoid a method-of-use claim if the proposed labeling still instructs the same renal-function-based administration.

When does US Patent 9,949,998 lose exclusivity?

US 9,949,998 was issued on April 17, 2018. Public patent records generally identify an expiration date in August 2030 for the patent family, subject to the controlling USPTO term calculation and any applicable terminal-disclaimer or patent-term-adjustment information. The relevant patent-term event should be confirmed against the USPTO patent record and the current FDA Orange Book before a launch decision.

Event	Date or status
Patent	US 9,949,998
Patent type	Utility patent, B2 grant
Grant date	April 17, 2018
Product association	Empagliflozin, marketed as Jardiance
Expected listed expiration	August 2030
Regulatory exclusivity	Separate from patent term
Pediatric extension	Must be checked against the current Orange Book record

Patent expiration does not automatically mean generic launch on the same day. Launch timing can be affected by:

• other Orange Book-listed Jardiance patents;
• 30-month stays from Paragraph IV litigation;
• settlement agreements;
• pediatric exclusivity;
• regulatory review of an ANDA;
• separate patents covering crystalline forms, combinations, or formulations.

US 9,949,998 is therefore one part of the Jardiance exclusivity structure rather than the entire patent barrier.

What is the Orange Book status of US 9,949,998?

The patent has been associated with the empagliflozin product and is relevant to Jardiance ANDA certification analysis. The precise Orange Book listing, use code, expiration date, and status should be read from the current FDA publication because listings and administrative information can change.

The practical regulatory question is whether the listed use code corresponds to the renal-function-based method described in the claims. If the patent is listed for a method of using empagliflozin in patients with reduced renal function, an ANDA applicant must address it through one of the following routes:

1. Paragraph I certification, if the patent information is inaccurate or no longer relevant;
2. Paragraph II certification, if the patent has expired;
3. Paragraph III certification, accepting approval after patent expiration;
4. Paragraph IV certification, asserting that the patent is invalid, unenforceable, or not infringed;
5. a section viii statement, carving out the patented method from the proposed label.

The feasibility of a section viii carve-out depends on whether the unpatented label can omit the renal-function language without retaining instructions that practice the patented method. FDA labeling requirements and the scope of the use code determine the result. [1]

Which companies are challenging the Jardiance patent estate?

Empagliflozin is a small-molecule product, so the relevant competitive threat is generic ANDA litigation rather than biosimilar litigation. Potential challengers are ANDA applicants seeking approval for empagliflozin tablets or empagliflozin combination products.

A complete challenger-by-challenger assessment requires matching each ANDA notice letter and district-court complaint to specific patents. The key risk is not limited to US 9,949,998. Generic applicants typically address the entire Orange Book patent group, which may include:

• compound patents;
• crystalline-form patents;
• formulation patents;
• fixed-dose combination patents;
• method-of-use patents;
• patents covering empagliflozin with metformin or other agents.

A Paragraph IV challenge to US 9,949,998 would likely focus on:

• lack of written description or enablement for the eGFR-specific regimen;
• obviousness based on prior empagliflozin renal-impairment studies;
• indefiniteness of the "improved glycemic control" limitation;
• failure to prove that a proposed label necessarily directs all claimed steps;
• noninfringement based on a label that omits the 45-to-less-than-60 eGFR population;
• noninfringement based on the absence of a mandatory discontinuation instruction.

The patent holder would likely argue that clinical data established a clinically meaningful renal-function-specific treatment protocol and that the proposed generic label or physician instructions induce performance of the claimed method.

What Paragraph IV issues are most important?

The strongest generic defenses are likely to involve label-based infringement and obviousness.

Label-based noninfringement

A generic applicant may argue that its label does not require:

• use in patients with eGFR of 45 to less than 60;
• discontinuation below 45;
• renal assessment before treatment;
• a glycemic-control indication in the claimed population.

That defense is stronger if the generic label uses a broad renal warning without instructing treatment in the patented eGFR interval. It is weaker if the label reproduces the reference product’s renal dosing instructions.

Induced infringement

The patent does not require the manufacturer itself to administer empagliflozin. The potential theory is induced infringement based on instructions, labeling, promotional material, or other conduct encouraging physicians to perform the claimed method.

A generic product can create risk even when its tablets are chemically and physically identical to the reference product but its label includes the patented treatment protocol.

Obviousness

The eGFR thresholds, once-daily dosing, and 10 mg or 25 mg doses may be challenged as obvious if earlier clinical studies disclosed empagliflozin treatment in patients with renal impairment. The patent holder’s counterargument would focus on the specific threshold combination and the clinical result of improved glycemic control within the claimed population.

The strength of this defense depends on the prior art available before the relevant priority date, not on the later Jardiance prescribing information.

How does US 9,949,998 compare with other Jardiance patents?

Patent type	Typical subject matter	Generic-entry effect
Compound patent	Empagliflozin molecule or chemical class	Broadest historical protection
Crystalline-form patent	Solid-state form of empagliflozin	May require a design-around or validity challenge
Formulation patent	Tablet composition, excipients, release profile	Can be avoided through formulation changes
Combination patent	Empagliflozin plus metformin or another agent	Applies to combination products
Method-of-use patent	Renal dosing, cardiovascular use, or disease-specific treatment	Label and physician-use dependent
US 9,949,998	Renal-function-based glycemic-control method	Narrow but potentially difficult to carve out

US 9,949,998 may have less breadth than a compound patent but can remain commercially important after basic compound protection expires. Its value is highest when:

• the patented population is included in the FDA-approved label;
• the label cannot be cleanly carved out;
• the renal protocol is routinely followed in clinical practice;
• competing products rely on the same treatment instructions.

Its value is lower if generic labels omit the claimed eGFR population and physicians can use the product for noninfringing indications without relying on the patented protocol.

Does this patent create biosimilar risk?

No. Empagliflozin is a chemically synthesized small molecule, not a biologic. The relevant pathway is an abbreviated new drug application under section 505(j) of the Federal Food, Drug, and Cosmetic Act, not a biosimilar application under the Public Health Service Act.

The competitive threat comes from:

• generic empagliflozin tablets;
• generic empagliflozin-metformin products;
• potential authorized-generic strategies;
• combination-product suppliers.

The FDA may approve a generic with a carved-out indication if the remaining labeling is consistent with the statutory requirements. [1, 2]

What manufacturing or intellectual-property barriers remain?

US 9,949,998 does not create a direct manufacturing barrier. It does not claim a synthetic route, crystallization process, tablet compression process, or specific excipient combination in the provided claims.

Manufacturing barriers may still arise from other patents covering:

• empagliflozin polymorphs;
• particle-size distributions;
• pharmaceutical formulations;
• combination tablets;
• processes for producing empagliflozin;
• impurity-control methods;
• packaging or stability systems.

A generic manufacturer can potentially design around this patent by separating its development strategy from the patented method, but it must still evaluate whether the final label induces use in the claimed population.

What geographic coverage does US 9,949,998 provide?

The patent provides rights in the United States only. Its claims do not establish protection in Europe, Japan, Canada, China, or other markets.

The corresponding international family may contain foreign applications with different:

• claim scope;
• prosecution history;
• expiration dates;
• validity outcomes;
• renal-function thresholds;
• national-use limitations.

A US Paragraph IV strategy does not resolve foreign patent exposure. Launch planning must be conducted country by country, especially for markets where empagliflozin has separate supplementary protection certificates or national method-of-use claims.

How strong is the patent estate for this renal-use claim?

The patent is commercially meaningful but technically narrow.

Strength factor	Assessment
Patient specificity	Narrow
Dose specificity	Moderate
Administration specificity	Moderate
Result limitation	Potentially vulnerable to proof disputes
Label-based enforcement	Potentially significant
Design-around potential	Moderate to high
Manufacturing barrier	Low under the stated claims
Relevance to Jardiance prescribing	Potentially high
Relevance to all empagliflozin sales	Low
Biosimilar exposure	None

The strongest feature is the combination of the eGFR range and discontinuation threshold. The principal weakness is that the method applies only to a defined renal-function subgroup and requires proof that all claim elements are practiced.

For a generic launch, the decisive issue is likely the proposed label rather than tablet similarity. A label that omits the claimed renal-use instructions may materially reduce infringement risk. A label that preserves the reference product’s renal dosing protocol may expose the applicant to a stronger induced-infringement case.

What revenue exposure does US 9,949,998 create?

The patent protects only a subset of Jardiance use, so it should not be valued as a complete product-level barrier. Revenue exposure depends on the proportion of Jardiance prescriptions involving patients with eGFR from 45 to less than 60 and the extent to which clinicians follow the claimed discontinuation rule.

Potential exposure is higher where:

• diabetes care occurs in populations with substantial chronic kidney disease;
• renal function is routinely assessed;
• Jardiance is used for glycemic control rather than solely for cardiovascular or kidney indications;
• the approved label preserves the claimed threshold;
• a generic applicant uses the same renal instructions as the reference product.

Potential exposure is lower where:

• the generic label uses a section viii carve-out;
• treatment is directed to patients with eGFR above 60;
• empagliflozin is used for heart failure or chronic kidney disease under a different indication;
• the claimed discontinuation protocol is not included in the generic label;
• physicians prescribe outside the claimed eGFR interval.

The patent should therefore be modeled as a partial erosion barrier, with separate scenarios for full-label generic entry, carved-out entry, and litigation-delayed entry.

Key Takeaways

• US 9,949,998 is a renal-function-based method-of-use patent for empagliflozin.
• The core population has eGFR of at least 45 and below 60 mL/min/1.73 m².
• The regimen requires oral once-daily 10 mg or 25 mg empagliflozin.
• The claimed protocol requires discontinuation when eGFR falls below 45.
• Claims 4-6 and 10-12 expressly require renal-function assessment.
• The patent does not claim the empagliflozin molecule, a specific tablet formulation, or a manufacturing process.
• The principal generic defense is a label carve-out or a showing that the proposed label does not induce the claimed method.
• The relevant competitive pathway is generic ANDA litigation, not biosimilar litigation.
• The expected patent expiration is in August 2030, subject to the controlling USPTO and Orange Book records.
• US 9,949,998 is a potentially important Jardiance barrier, but it does not independently block every generic empagliflozin product or every use of the drug.

FAQs About US Patent 9,949,998 and Empagliflozin Exclusivity

Can a generic manufacturer sell empagliflozin before US 9,949,998 expires?

Potentially. A generic may seek approval through a Paragraph IV challenge, a section viii carve-out, or a settlement that permits launch before the listed expiration date. Approval and commercial launch depend on the full Jardiance patent estate, not this patent alone.

Does US 9,949,998 cover Jardiance tablets themselves?

No. The stated claims cover methods of administering empagliflozin. They do not claim every Jardiance tablet as a composition or manufacturing product.

Does the patent cover empagliflozin use when eGFR is above 60?

No, not under the provided claims. The claimed eGFR range ends below 60 mL/min/1.73 m².

Does the patent cover continued treatment after eGFR falls below 45?

The claims require discontinuation when eGFR falls below 45. Continued treatment would not satisfy that particular discontinuation limitation, although other patent, labeling, or regulatory issues could apply.

Is empagliflozin subject to biosimilar substitution rules?

No. Empagliflozin is a small-molecule drug. Generic substitution is governed by the ANDA framework rather than the biosimilar pathway.

References

1. U.S. Food and Drug Administration. (n.d.). Approved drug products with therapeutic equivalence evaluations: Orange Book. https://www.accessdata.fda.gov/scripts/cder/ob/

2. U.S. Food and Drug Administration. (n.d.). Jardiance prescribing information. Boehringer Ingelheim Pharmaceuticals, Inc. https://www.accessdata.fda.gov/drugsatfda_docs/label/

3. United States Patent and Trademark Office. (2018). U.S. Patent No. 9,949,998, methods of treating diabetes mellitus with empagliflozin. https://patents.google.com/patent/US9949998B2

4. U.S. Food and Drug Administration. (2020). Approved drug products with therapeutic equivalence evaluations, guidance for industry. https://www.fda.gov/drugs/abbreviated-new-drug-application-anda/abbreviated-new-drug-application-anda-resources

Drugs Protected by US Patent 9,949,998

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Boehringer Ingelheim	GLYXAMBI	empagliflozin; linagliptin	TABLET;ORAL	206073-001	Jan 30, 2015		RX	Yes	No						METHOD OF TREATING TYPE 2 DIABETES MELLITUS IN A PATIENT WITH RENAL IMPAIRMENT (45 ML/MIN/1.73 M2
Boehringer Ingelheim	GLYXAMBI	empagliflozin; linagliptin	TABLET;ORAL	206073-002	Jan 30, 2015		RX	Yes	Yes						METHOD OF TREATING TYPE 2 DIABETES MELLITUS IN A PATIENT WITH RENAL IMPAIRMENT (45 ML/MIN/1.73 M2
Boehringer Ingelheim	SYNJARDY XR	empagliflozin; metformin hydrochloride	TABLET, EXTENDED RELEASE;ORAL	208658-001	Dec 9, 2016		RX	Yes	No					Y
Boehringer Ingelheim	SYNJARDY XR	empagliflozin; metformin hydrochloride	TABLET, EXTENDED RELEASE;ORAL	208658-002	Dec 9, 2016		RX	Yes	No					Y
Boehringer Ingelheim	SYNJARDY XR	empagliflozin; metformin hydrochloride	TABLET, EXTENDED RELEASE;ORAL	208658-003	Dec 9, 2016		RX	Yes	No					Y

International Family Members for US Patent 9,949,998

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Australia	2014247092
Canada	2812519
Canada	2908635
Canada	3121761
Chile	2015002940