Details for Patent: 9,868,739

Which drugs does patent 9,868,739 protect, and when does it expire?

Patent 9,868,739 protects KISQALI and KISQALI FEMARA CO-PACK (COPACKAGED) and is included in two NDAs.

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

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

Summary for Patent: 9,868,739

Title:	Salt(s) of 7-cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid dimethylamide and processes of making thereof
Abstract:	This invention relates to (1) process of making 7-Cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid dimethylamide and salt(s) thereof; (2) novel salt(s) of 7-Cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid dimethylamide; (3) pharmaceutical compositions comprising the same; and (4) methods of treatment using the same.
Inventor(s):	John Vincent Calienni, Guang-Pei Chen, Baoqing Gong, Prasad Koteswara Kapa, Vishal Saxena
Assignee:	Astex Therapeutics Ltd , Novartis Pharmaceuticals Corp
Application Number:	US14/887,790
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 9,868,739
Patent Claim Types: see list of patent claims	Use;

US Patent 9,868,739: Ribociclib Succinate Solid Forms, Claim Scope, Expiry and Generic Risk

US Patent No. 9,868,739 protects treatment of CDK-responsive cancers with specified crystalline or solid-state forms of ribociclib succinate, the active pharmaceutical ingredient in Kisqali. The patent does not broadly claim ribociclib, ribociclib succinate as a chemical composition, or a manufacturing process. Its enforceable scope is concentrated on administering ribociclib succinate that exhibits defined XRPD, DSC, or TGA characteristics.

The patent was issued to Novartis AG on January 16, 2018. Its earliest claimed priority is in 2014, producing a baseline patent expiration in 2035 before any patent-term adjustment. The patent is commercially important because it can create a later-expiring solid-form barrier after earlier composition and regulatory exclusivities expire.

What drug and solid form does US 9,868,739 protect?

US 9,868,739 covers ribociclib succinate. Ribociclib is a selective cyclin-dependent kinase 4 and 6 inhibitor marketed by Novartis as Kisqali.

The chemical entity identified in the claims is:

7-cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid dimethylamide.

The patent focuses on the succinate salt and its solid-state properties. The claimed product is not defined solely by chemical structure. It must also satisfy one or more analytical identity criteria based on:

• Initial XRPD, shown in Figure 2
• Post-DVS XRPD, shown in Figure 2
• Initial DSC, shown in Figure 3
• Post-DVS DSC, shown in Figure 3
• Initial TGA, shown in Figure 4
• Post-DVS TGA, shown in Figure 4
• Initial XRPD, shown in Figure 6
• Post-DVS XRPD, shown in Figure 6

DVS means dynamic vapor sorption. The initial and post-DVS analyses are intended to characterize the material before and after exposure to changing humidity conditions.

What are the independent claims in US 9,868,739?

Claims 1 through 8 are separate independent method claims. Each requires:

1. A subject in need of treatment.
2. A cancer that responds to inhibition of cyclin-dependent kinase activity.
3. Administration of a therapeutically effective amount.
4. Ribociclib succinate.
5. The specified solid-state signature corresponding to one of the patent figures.

Claims 1 and 2 use XRPD characteristics from Figure 2. Claims 3 and 4 use DSC characteristics from Figure 3. Claims 5 and 6 use TGA characteristics from Figure 4. Claims 7 and 8 use XRPD characteristics from Figure 6.

The use of "initial" and "post-DVS" conditions creates paired claim alternatives. A product may infringe depending on whether its analytical profile corresponds to the pre-humidity or post-humidity form described in the specification.

Claims	Analytical characterization	Legal function
1-2	Figure 2 XRPD	Protect treatment using one of the Figure 2 solid-state profiles
3-4	Figure 3 DSC	Protect treatment using one of the Figure 3 thermal profiles
5-6	Figure 4 TGA	Protect treatment using one of the Figure 4 thermogravimetric profiles
7-8	Figure 6 XRPD	Protect treatment using one of the Figure 6 solid-state profiles
9	Broad cancer list	Dependent species limitation
10	Breast cancer	Narrow indication
11	Mantle cell or large B-cell lymphoma	Narrow hematologic indication
12	Neuroblastoma	Narrow indication
13	Small-cell lung cancer	Narrow indication
14	Bladder, prostate, or renal cancer	Narrow genitourinary indications
15	Chronic lymphocytic leukemia	Narrow hematologic indication
16	Keratoacanthoma	Narrow epidermoid indication
17	Osteosarcoma	Narrow bone-cancer indication
18	Gastric, colon, colorectal, esophageal, liver, or pancreatic cancer	Narrow gastrointestinal indications
19	Leukemias	Narrow hematologic indication

How broad are the cancer-treatment claims?

The phrase "a cancer which responds to an inhibition of cyclin dependent kinases activity" establishes the functional treatment category in claims 1 through 8. The independent claims are therefore broader than the dependent claims in terms of tumor type, but they remain limited by the ribociclib succinate solid form.

Claim 9 provides a long list of eligible tumor categories. Claims 10 through 19 narrow that list to specific cancers. Breast cancer is particularly relevant because Kisqali is approved for hormone receptor-positive, HER2-negative advanced or metastatic breast cancer and for certain adjuvant breast-cancer uses.

The patent does not require:

• A particular dose
• A particular dosing schedule
• Combination treatment with an aromatase inhibitor, fulvestrant, or another endocrine therapy
• A particular patient biomarker
• A particular route of administration
• A particular tablet composition
• A particular treatment line

A generic product using the claimed solid form could face method-of-use exposure even if its proposed label excludes some patented indications. The practical risk would depend on the approved label, induced-infringement theory, prescribing information, product distribution, and any carve-out accepted by FDA.

What formulations are protected by US 9,868,739?

The patent protects the use of ribociclib succinate having the specified analytical characteristics. It does not, based on the supplied claims, expressly claim a tablet, capsule, coating, excipient system, dissolution profile, particle-size range, or manufacturing process.

This distinction matters:

• A tablet containing the claimed ribociclib succinate could implicate the patent.
• A different salt, such as a free base or non-succinate salt, would not satisfy the express succinate limitation.
• A succinate product with a materially different solid form may avoid literal infringement if it does not satisfy the figure-based characterization.
• A product that converts into the claimed form during storage, manufacture, dissolution, or administration could create a more complex infringement analysis.
• Analytical testing would likely be central to any dispute.

The claims are method claims, not product-by-process claims. A generic manufacturer does not necessarily avoid the patent merely by using a different crystallization process if the resulting administered material has the claimed solid-state characteristics.

How should the XRPD, DSC and TGA limitations be interpreted?

The analytical limitations are the principal technical boundaries of the patent.

XRPD

XRPD identifies crystalline structure through diffraction peaks and relative intensities. The claims refer to figures rather than reproducing a complete peak list in the claim text. In litigation, the specification, figure quality, experimental conditions, peak tolerances, and ordinary analytical variability would determine the scope.

A generic applicant would normally compare its ribociclib succinate against the reference material using validated XRPD testing. Differences in instrument configuration, sample preparation, preferred orientation, hydration, and relative intensity can affect the result.

DSC

DSC identifies thermal transitions, including melting, desolvation, dehydration, or decomposition events. The initial and post-DVS DSC profiles may reflect changes caused by water uptake or release.

DSC evidence is sensitive to heating rate, sample mass, pan configuration, atmosphere, and instrument calibration. A temperature range or event defined only through a figure can generate factual disputes over whether a product matches the claimed profile.

TGA

TGA measures weight loss as a function of temperature. It can distinguish anhydrous, hydrated, solvated, or partially hydrated forms. As with DSC, the result depends on experimental conditions.

The patent’s use of multiple analytical techniques strengthens product identification. A challenger may attack the claims by arguing that the figure-based limitations lack sufficient objective boundaries, while the patent owner may rely on the combined disclosure of XRPD, DSC, TGA, and DVS behavior.

When does US 9,868,739 expire?

The patent’s statutory term is calculated from the earliest effective nonprovisional or international filing date under the 20-year term rules. Public patent records identify a 2014 priority date for the family. On that basis, the baseline expiration falls in 2035.

Event	Date or period
Earliest priority	2014
US patent issuance	January 16, 2018
Baseline statutory expiration	2035
Patent-term adjustment	Must be added if reflected in the USPTO patent record
Patent-term extension	No extension should be assumed without a specific USPTO or FDA determination

The relevant commercial date is the actual expiration date shown in the USPTO patent record, including any patent-term adjustment. A patent-term extension under 35 U.S.C. § 156 is separate from ordinary patent-term adjustment and requires a qualifying regulatory determination.

What is the Orange Book status of US 9,868,739?

Kisqali is approved under NDA 209092. FDA Orange Book listings for a drug can include compound, formulation, method-of-use, and other patents. The Orange Book listing must be checked separately from the underlying patent grant because listing status can change through delisting, expiration, correction, or FDA administrative action.

US 9,868,739 is strategically relevant to Kisqali because it covers a ribociclib succinate solid form used in the marketed product. Its exact current Orange Book status should be determined from the current FDA listing for NDA 209092, not solely from the patent document.

The patent’s value is highest if:

1. It is listed for the NDA.
2. The commercial product uses the claimed solid form.
3. The approved use overlaps with claims 1 through 19.
4. The patent remains unexpired when an ANDA applicant seeks approval.
5. No successful Paragraph IV challenge removes the barrier.

FDA’s Orange Book distinguishes patent listing from regulatory exclusivity. Patent listing can trigger a statutory 30-month stay if the NDA holder brings an infringement action within the applicable period after receiving a Paragraph IV notice. The patent itself does not create five-year or three-year FDA exclusivity.

What FDA exclusivity protects Kisqali?

Ribociclib is a small molecule, so biosimilar procedures under the Biologics Price Competition and Innovation Act do not apply. Future competitors would generally use an ANDA or, depending on the development strategy, a 505(b)(2) application.

Kisqali’s regulatory protections are separate from US 9,868,739:

• New chemical entity exclusivity may have applied to the original approval.
• Supplemental approvals may receive three-year exclusivity if they contain qualifying new clinical investigations.
• Pediatric exclusivity can add six months to eligible patents and exclusivities.
• Patent protection is controlled by the relevant patent terms and any litigation outcome.

The first approval date and subsequent supplemental approvals should be evaluated against the current FDA Orange Book exclusivity codes. Patent expiration and FDA exclusivity expiration are different events.

What Paragraph IV challenges and patent litigation affect ribociclib?

A Paragraph IV certification would assert that a listed patent is invalid, unenforceable, or not infringed. For this patent, likely attack points include:

• Whether the accused product has the claimed succinate solid form.
• Whether the figure-based XRPD, DSC, or TGA limitations are definite and reproducible.
• Whether the claimed forms were anticipated by earlier ribociclib succinate disclosures.
• Whether the claimed forms would have been obvious to a person skilled in solid-form pharmaceutical development.
• Whether the patent adequately describes and enables each claimed analytical form.
• Whether the patent is enforceable against the proposed ANDA product after any label carve-out.

Because claims 1 through 8 are treatment claims, an ANDA applicant may attempt a section viii statement for non-patented indications or use a Paragraph IV certification where the listed patent is treated as relevant to the proposed product.

No biosimilar litigation pathway applies. The principal dispute would be between Novartis and an ANDA or 505(b)(2) applicant.

How strong is the patent estate for Kisqali?

US 9,868,739 is a focused but potentially valuable patent. Its strengths and weaknesses are distinct from those of a composition-of-matter patent.

Factor	Assessment
Chemical scope	Narrow; limited to ribociclib succinate
Solid-form scope	Potentially meaningful; covers specified analytical profiles
Method scope	Broad cancer-treatment framing, narrowed by solid form
Formulation scope	No express tablet, excipient, coating, or process claim in the supplied claims
Infringement proof	Requires technical characterization of the accused material
Validity exposure	Solid-form obviousness, anticipation, enablement, and definiteness issues
Regulatory value	High if listed in the Orange Book and matched to the commercial form
Biosimilar relevance	None; ribociclib is a small molecule
Generic design-around potential	Possible through a different salt or non-claimed solid form
Commercial duration	Potential protection through 2035, subject to term adjustment and litigation

The patent is stronger against a generic that uses the same ribociclib succinate form as Kisqali. It is weaker against a competitor that can develop and validate a different salt or crystalline form without reproducing the claimed analytical profile.

How does US 9,868,739 compare with a ribociclib composition patent?

A composition-of-matter patent generally provides broader protection because it covers the active chemical entity regardless of polymorph, salt, formulation, or manufacturing route. US 9,868,739 is narrower because it requires both the succinate salt and defined solid-state characteristics.

Protection type	Typical coverage	Relevance to ribociclib
Composition patent	Ribociclib chemical structure and analogs	Broadest protection; usually earliest-expiring core patent
Salt patent	Ribociclib succinate or another salt	Protects the selected pharmaceutical salt
Solid-form patent	Crystalline, hydrated, solvated, or polymorphic material	Targets the commercial physical form
Formulation patent	Tablet, coating, excipient, dissolution or release profile	Can block product replication
Method-of-use patent	Treatment of a defined cancer or patient population	Can restrict labeled or induced uses
Manufacturing patent	Synthetic route or crystallization process	Can create process-specific barriers

US 9,868,739 combines solid-form limitations with treatment claims. That combination can be commercially effective, but it does not provide the same broad exclusionary perimeter as a core chemical patent.

What generic launch scenarios exist?

Launch after patent expiry

The lowest-risk scenario is launch after all relevant listed patents and regulatory exclusivities expire. An ANDA applicant could then market ribociclib tablets subject to FDA approval and ordinary product requirements.

Paragraph IV launch

A generic applicant could file an ANDA with a Paragraph IV certification and argue that the patent is invalid or not infringed. If Novartis sues within the statutory period, FDA approval may be stayed for up to 30 months, subject to court decisions and statutory exceptions.

Section viii carve-out

If the listed patent is limited to particular cancer uses, an applicant may seek approval with those uses omitted. This strategy is more difficult where the patent claims broad CDK-responsive cancer treatment and the commercial product’s primary indication overlaps with the patented method.

Different solid form

A competitor may develop a different ribociclib salt or crystalline form. That approach can avoid literal infringement of US 9,868,739 but may encounter separate patents, regulatory bridging requirements, stability issues, and formulation-development costs.

505(b)(2) route

A 505(b)(2) applicant could pursue a modified salt, dosage form, or formulation while relying in part on existing ribociclib data. This route may face listed-patent certifications, clinical bridging requirements, and separate formulation or method patents.

What geographic coverage does the patent provide?

US 9,868,739 is enforceable only in the United States. Parallel patent families may exist in Europe, Japan, China, Canada, and other jurisdictions, but their claims, validity, expiry dates, prosecution histories, and litigation outcomes must be assessed independently.

A US design-around does not establish freedom to operate in Europe or other markets. Conversely, an adverse foreign decision does not invalidate the US patent.

What licensing and commercial relationships matter?

Ribociclib was developed and commercialized by Novartis. The commercially relevant patent-holder and NDA-holder analysis therefore centers on Novartis and its affiliates. Any development or discovery collaboration associated with the ribociclib program does not, by itself, establish a current right to enforce US 9,868,739.

License, co-development, settlement, or covenant-not-to-sue agreements can alter generic launch timing. Such agreements may not be fully visible in patent records unless filed in litigation or reported to regulators. The practical enforcement position should therefore be based on the current Orange Book listing, litigation docket, and any public settlement filing.

Key Takeaways

• US 9,868,739 covers treatment with ribociclib succinate matching specified XRPD, DSC, or TGA profiles.
• Claims 1 through 8 are independent method claims; claims 9 through 19 narrow the cancer indications.
• The patent does not, based on the supplied claims, broadly claim ribociclib, a tablet formulation, or a manufacturing process.
• Its baseline patent term extends into 2035 based on the 2014 priority date.
• The patent’s commercial strength depends heavily on whether it is listed for Kisqali and whether the marketed product uses the claimed solid form.
• A generic using the same ribociclib succinate form faces greater risk than one using a different salt or non-claimed polymorph.
• Ribociclib is a small molecule, so biosimilar litigation is irrelevant.
• Paragraph IV, section viii, 505(b)(2), and solid-form design-around strategies are the principal generic pathways.
• The main technical issues are XRPD peak matching, thermal behavior, hydration state, and the reproducibility of figure-defined claim limitations.

FAQs About US Patent 9,868,739 and Ribociclib

What is the active ingredient protected by US 9,868,739?

The patent concerns ribociclib succinate, the salt form of ribociclib used in Kisqali.

Does US 9,868,739 claim Kisqali tablets directly?

No. The supplied claims are method claims requiring administration of ribociclib succinate with specified solid-state characteristics. They do not expressly claim the tablet, excipient system, or coating.

Can a generic avoid US 9,868,739 by using free-base ribociclib?

Potentially, because the claims expressly require a succinate salt. A free-base product would still require analysis against other ribociclib patents and regulatory requirements.

Is US 9,868,739 a biosimilar patent?

No. Ribociclib is a small-molecule drug. Generic competition would proceed primarily through the ANDA framework, not the biosimilar pathway.

What laboratory tests would be most important in a patent dispute?

XRPD would likely be the primary test because the patent expressly identifies XRPD profiles. DSC, TGA, and DVS results would provide supporting evidence regarding thermal transitions, weight loss, hydration, and post-humidity solid-state behavior.

References

1. United States Patent and Trademark Office. (2018). U.S. Patent No. 9,868,739, solid forms and methods of treatment involving ribociclib succinate.
2. U.S. Food and Drug Administration. (n.d.). Kisqali (ribociclib) prescribing information.
3. U.S. Food and Drug Administration. (n.d.). Approved drug products with therapeutic equivalence evaluations: Orange Book.
4. 35 U.S.C. §§ 154, 156, and 271.
5. 21 U.S.C. § 355(j).

Drugs Protected by US Patent 9,868,739

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Novartis	KISQALI	ribociclib succinate	TABLET;ORAL	209092-001	Mar 13, 2017		RX	Yes	Yes					Y
Novartis	KISQALI FEMARA CO-PACK (COPACKAGED)	letrozole; ribociclib succinate	TABLET;ORAL	209935-001	May 4, 2017		RX	Yes	Yes					Y

International Family Members for US Patent 9,868,739

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Argentina	083797
Argentina	117799
Australia	2011326620
Australia	2016203534