US Patent 7,417,148: Scope, Claims, Expiration, and Bosutinib Patent Landscape

US Patent 7,417,148 covers a class of substituted quinoline-3-carbonitrile kinase inhibitors for treating or inhibiting chronic myelogenous leukemia (CML). The patent’s commercial center is bosutinib, marketed by Pfizer as Bosulif. Claim 7 specifically covers bosutinib, while the broader claims cover related quinoline compounds, pharmaceutically acceptable salts, CML treatment methods, kinase activity, and combinations with imatinib.

The patent was issued on August 26, 2008. Its principal Orange Book-listed patent term runs to December 27, 2026, subject to applicable pediatric exclusivity and any legally recognized term adjustments. The patent is a method-of-treatment patent rather than a simple composition-of-matter claim, which affects infringement analysis and generic launch strategy.

What does US Patent 7,417,148 cover?

US 7,417,148 covers methods of treating or inhibiting CML by administering specified quinoline compounds. The patent claims compounds that inhibit Src and Abl kinases, two kinase targets relevant to BCR-ABL-driven CML.

The core claim architecture is:

Claim group	Subject matter	Commercial relevance
Claim 1	Broad CML treatment method using a defined quinoline compound genus	Establishes the principal method scope
Claim 2	Narrower structural genus with n of 2 or 3	Reduces structural breadth
Claim 3	Specific substitution pattern with methyl groups	Covers a narrower compound subset
Claims 4-6	Restrictions on R2 and X	Narrow claim construction
Claim 7	Specific bosutinib compound	Most important claim for Bosulif
Claims 8-9	Enumerated bosutinib analogs and related compounds	Protects selected backup compounds
Claim 10	Compound is both a Src and Abl kinase inhibitor	Functional limitation
Claims 11-12	Combination therapy with other CML agents, including imatinib	Covers combination treatment methods

Claim 7 identifies bosutinib as:

4-[(2,4-dichloro-5-methoxyphenyl)amino]-6-methoxy-7-[3-(4-methyl-1-piperazinyl)propoxy]-3-quinolinecarbonitrile.

Bosutinib is also known as SKI-606. It is an orally administered tyrosine kinase inhibitor that inhibits BCR-ABL and Src-family kinases.

What is the scope of independent claim 1?

Claim 1 requires four principal elements:

A method of treating or inhibiting CML.
Administration to a patient in need of treatment.
A therapeutically effective amount.
Administration of a compound within the claimed quinoline genus or a pharmaceutically acceptable salt.

The structural limitations include:

A quinoline-type core containing a nitrile group.
A variable heteroatom or carbon position represented by X.
A linker of one to three carbon atoms, represented by n.
An alkyl substituent R containing one to three carbon atoms.
An aryl substituent R1 selected from specified chloro-, methoxy-, ethoxy-, and methyl-substituted phenyl groups.
An alkyl substituent R2 containing one or two carbon atoms.
Pharmaceutically acceptable salts.

Claim 1 is not limited to bosutinib. It covers a defined genus of related compounds, provided the administered compound satisfies every structural limitation.

The claim also requires CML treatment. Administration of a covered compound for a non-CML indication would not, by itself, satisfy the express method-of-use limitation. An infringement theory would therefore generally require evidence that the accused product is marketed, prescribed, or used for CML treatment, or that the labeling induces that use.

Does claim 7 cover bosutinib specifically?

Yes. Claim 7 expressly recites bosutinib by chemical name. It is the narrowest and commercially most important claim for the marketed product.

A generic bosutinib product would likely meet the chemical limitation of claim 7 if it contains bosutinib or a pharmaceutically acceptable salt of bosutinib. The remaining issue is whether the product’s use, labeling, or distribution satisfies the CML treatment method limitation.

For an ANDA applicant, the central legal question is usually not whether the generic contains bosutinib. That fact is generally established. The principal questions are:

Whether the patent is listed for the relevant reference product.
Whether the proposed label includes a patented CML use.
Whether the applicant files a Paragraph IV certification.
Whether the patent is valid and enforceable.
Whether the proposed generic label can lawfully omit the patented indication through a section viii statement.

Because Bosulif is approved for Philadelphia chromosome-positive CML, a label that retains that indication creates a direct method-of-use risk.

What compounds are covered by claims 8 and 9?

Claims 8 and 9 enumerate specific analogs. These claims expand protection beyond bosutinib itself and create a secondary layer around related substitution patterns.

Claim 8 compounds

Claim 8 covers analogs that retain the 2,4-dichloro-5-methoxyphenyl amino substituent and vary the solubilizing side chain or quinoline alkoxy group. The listed compounds include variations involving:

4-methylpiperazine;
4-ethylpiperazine;
4-propylpiperazine;
1-methylpiperidine;
1-ethylpiperidine;
Two-carbon and three-carbon ether linkers;
Methoxy and ethoxy groups at the quinoline position.

Claim 9 compounds

Claim 9 covers compounds with changes to the aniline ring, including:

2,4-dichlorophenyl;
3,4,5-trimethoxyphenyl;
2-chloro-5-methoxyphenyl;
5-methoxy-2-methylphenyl;
2,4-dimethylphenyl;
5-methoxy-2,4-dimethylphenyl;
2,4-dichloro-5-ethoxyphenyl.

These dependent claims may have limited direct relevance to bosutinib supply, but they matter for follow-on discovery, freedom-to-operate analysis, and any attempt to commercialize closely related compounds.

How does claim 10 affect the scope?

Claim 10 requires that the claimed compound be both a Src inhibitor and an Abl kinase inhibitor.

This is a functional limitation. It may narrow the claim if a compound satisfies the structural limitations but does not inhibit both kinase families. The practical effect depends on claim construction and proof of biological activity.

For bosutinib, the limitation is commercially relevant because bosutinib is characterized as a dual Src/Abl inhibitor. FDA labeling identifies bosutinib as a kinase inhibitor and describes activity against BCR-ABL and Src-family kinases (FDA, 2023).

A claimant would generally need to establish:

The identity of the accused compound;
Its inhibition of Abl or BCR-ABL;
Its inhibition of Src-family kinases;
The relationship between those activities and the claimed compound.

The claim is less useful against structurally unrelated kinase inhibitors, even if they treat CML.

What does claim 12 cover with respect to imatinib?

Claim 12 depends on claim 11 and covers administration of the patented compound in combination with imatinib.

It does not claim imatinib alone. The claim requires:

A compound within claim 1;
Use in treating or inhibiting CML;
Combination administration with imatinib.

This claim could be relevant to combination-treatment studies, clinical protocols, or labeling that recommends bosutinib with imatinib. It is unlikely to materially expand the ordinary Bosulif monotherapy risk unless combination use is promoted or included in an approved indication.

What is the FDA and Orange Book status of US 7,417,148?

Bosutinib received FDA approval on September 4, 2012, under the brand name Bosulif for adults with Philadelphia chromosome-positive CML in specified treatment settings. The product is approved as an oral tablet and is available in multiple strengths (FDA, 2023).

Key FDA milestones

Event	Date
US Patent 7,417,148 issued	August 26, 2008
Bosutinib FDA approval	September 4, 2012
New chemical entity exclusivity	Ended in 2017
Seven-year orphan-drug exclusivity period	Generally ended in 2019
Listed patent expiration	December 27, 2026
Potential pediatric exclusivity extension	Six additional months, if applicable

The Orange Book identifies US 7,417,148 as a patent associated with Bosulif. The listing supports a Paragraph IV certification and creates the statutory framework for patent litigation after an ANDA applicant provides notice to the patent holder (FDA, 2024).

Orange Book listing does not establish validity. It identifies the patent information submitted by the reference-product sponsor and permits the Hatch-Waxman certification process.

When does bosutinib lose exclusivity?

Bosutinib lost regulatory exclusivity before the principal patent expires.

The relevant distinction is:

Protection	Status
New chemical entity exclusivity	Expired
Orphan-drug exclusivity	Expired
Patent-based protection under US 7,417,148	Runs to December 27, 2026
Pediatric exclusivity	May add six months to otherwise applicable exclusivity or patent term

The practical generic-entry date depends on several factors:

The patent expiration date;
Any pediatric extension;
The timing of ANDA approval;
Paragraph IV litigation;
A 30-month stay;
Settlement terms;
Whether additional Orange Book patents remain enforceable;
Whether the generic applicant uses a label carve-out.

A patent expiry in December 2026 does not necessarily mean that a generic can launch on that date if other listed patents remain in force or if a settlement imposes a later launch date.

What other patents protect Bosulif?

Bosutinib’s patent estate is broader than US 7,417,148. Commercial protection can include several patent categories:

Patent category	Typical subject matter
Core compound patents	Bosutinib and related quinoline compounds
Method-of-use patents	CML treatment and kinase inhibition
Salt and solid-state patents	Pharmaceutical salts, polymorphs, and crystalline forms
Formulation patents	Tablet composition, dissolution, stability, or dosage forms
Manufacturing patents	Synthetic intermediates, reaction sequences, purification, and crystallization
Combination patents	Bosutinib with other CML therapies
Regulatory exclusivity	NCE, orphan, pediatric, or other FDA exclusivity

US 7,417,148 is principally a method patent with compound-specific dependent claims. It should not be assumed to capture every formulation, polymorph, manufacturing process, or dosage-form patent associated with Bosulif.

For freedom-to-operate purposes, a complete assessment requires review of:

All Orange Book-listed Bosulif patents;
Continuation and divisional applications;
Patent-family members outside the United States;
Expired and abandoned applications;
FDA-approved labeling;
ANDA litigation records;
Any later-issued formulation or solid-state patents.

What generic entry risks exist for bosutinib?

The highest-risk generic scenario is a product that:

Contains bosutinib;
Uses the same oral tablet route;
Carries a label for Philadelphia chromosome-positive CML;
Includes the patented indication;
Enters before expiration of the listed patent estate.

That product would face a direct claim 7 method-of-use risk.

A lower-risk pathway may exist if the applicant can use a section viii statement to omit a patented indication. The viability of that strategy depends on whether the remaining label still encourages the patented CML use. A label carve-out does not protect a generic if its marketing, promotional materials, or distribution practices induce infringement.

The risk is higher for:

A full-label ANDA;
A Paragraph IV challenge to claim 7;
A product promoted for the same CML population;
A product using bosutinib in a combination covered by claim 12.

The risk is lower for:

A post-expiration launch;
A properly limited label;
A product directed to an unpatented indication;
A non-infringing manufacturing route where process patents are relevant.

Which companies are challenging Bosulif patents?

The relevant challengers are ANDA applicants seeking approval for generic bosutinib tablets. Public patent records and FDA Orange Book data should be reviewed for each applicant because the litigation landscape can change as new ANDAs are filed, withdrawn, settled, or approved.

A definitive current list of challengers and settlement dates cannot be established from the claim text and patent number alone. The patent number identifies the asserted patent, but not the full set of ANDA certifications, district-court complaints, settlements, covenants not to sue, or launch licenses.

The principal public sources for this analysis are FDA Orange Book patent data, USPTO Patent Center, PACER and district-court dockets, and SEC filings by Pfizer where material.

How strong is the patent estate for bosutinib?

Strengths

US 7,417,148 has several commercially meaningful strengths:

Claim 7 names bosutinib directly.
The patent covers the approved therapeutic disease, CML.
The claim is linked to the marketed active ingredient.
The method claim can be asserted against a generic label that includes CML treatment.
Claims 8 and 9 provide additional compound-specific coverage.
Claim 12 addresses combination use with imatinib.

Weaknesses

The patent also has limitations:

It is not a pure composition-of-matter claim in the form presented.
Infringement requires proof of the claimed method of use.
Functional limitations in claim 10 may create proof issues.
Earlier prior art concerning quinoline kinase inhibitors could support an obviousness challenge.
The broad genus in claim 1 may face written-description, enablement, or anticipation arguments depending on the prior-art record.
The patent’s commercial value depends on the scope of other listed patents and the approved Bosulif label.

Claim 7 is materially stronger for commercial enforcement than claim 1 because it identifies bosutinib specifically. Claim 1 has greater theoretical breadth but greater vulnerability to structural and validity challenges.

What patent litigation affects US 7,417,148?

The relevant litigation pattern is Hatch-Waxman litigation involving ANDA applicants and Pfizer or its affiliates. The statutory trigger is a Paragraph IV notice asserting that the patent is invalid, unenforceable, or not infringed.

A litigation review should separate:

Challenges to US 7,417,148;
Challenges to other Bosulif patents;
Declaratory-judgment actions;
ANDA suits dismissed after settlement;
Cases involving only manufacturing or formulation patents;
Regulatory approval dates and actual launch dates.

A settlement may allow an earlier launch than patent expiry, but the agreed date, authorized generic terms, and scope of any license are material. The existence of a settlement does not necessarily mean that the patent was found valid or infringed.

How does bosutinib compare with other CML kinase inhibitors?

Drug	Main target profile	Commercial sponsor	Patent risk profile
Imatinib	BCR-ABL, KIT, PDGFR	Novartis	Mature generic market
Dasatinib	BCR-ABL, Src family	Bristol Myers Squibb	Core product patents largely expired or near expiry
Nilotinib	BCR-ABL	Novartis	Composition, formulation, and method patents
Ponatinib	BCR-ABL, including resistant mutants	Takeda	Later-generation patents and formulation protection
Bosutinib	BCR-ABL and Src family	Pfizer	US 7,417,148 plus related Orange Book and commercial patents

Bosutinib competes clinically with imatinib, dasatinib, nilotinib, and ponatinib. Its patent position is more commercially relevant against generics than against competing branded kinase inhibitors because competitors do not generally practice claim 7 by selling bosutinib.

What manufacturing and geographic barriers remain?

The chemical structure of bosutinib is publicly disclosed, and the active ingredient is a small molecule rather than a biologic. There is no biosimilar pathway issue. A generic manufacturer can pursue an ANDA rather than a 351(k) application.

Remaining barriers can include:

Process patents;
Solid-state and salt patents;
Specifications for impurities and degradation products;
Bioequivalence requirements;
Stability data;
Commercial-scale purification;
Foreign patent rights;
Local regulatory exclusivity;
Patent term differences by country.

US 7,417,148 does not automatically determine rights in Europe, Japan, China, Canada, or other markets. International protection depends on the relevant PCT national-phase filings and the separate patent-family members.

Key Takeaways

US 7,417,148 is a CML method-of-treatment patent covering substituted quinoline kinase inhibitors.
Claim 7 specifically covers bosutinib, the active ingredient in Bosulif.
Claim 1 is broader but requires compliance with a detailed chemical genus and CML treatment.
Claim 10 adds the requirement that the compound inhibit both Src and Abl kinases.
Claim 12 covers combination treatment with imatinib and does not cover imatinib alone.
Bosutinib’s NCE and orphan exclusivities have expired.
The principal listed patent term runs to December 27, 2026, with possible pediatric exclusivity implications.
A full-label bosutinib ANDA presents the highest infringement risk.
A section viii label carve-out may reduce risk but depends on the final label and marketing conduct.
The complete commercial landscape requires review of every Orange Book-listed Bosulif patent, related patent families, and ANDA litigation records.
Because the patent claims provided are method claims, the patent should not be treated as a complete substitute for a product-by-product freedom-to-operate analysis.

FAQs About US Patent 7,417,148 and Bosutinib

Is US 7,417,148 a composition-of-matter patent?

The provided claims are method-of-treatment claims. Claim 7 identifies bosutinib specifically, but the claim requires use of the compound to treat or inhibit CML.

Does US 7,417,148 cover all bosutinib uses?

No. The claims are directed principally to CML treatment and related kinase-inhibitor use. They do not automatically cover every disease, dosage, formulation, or manufacturing process involving bosutinib.

Can a generic bosutinib manufacturer avoid claim 7 by omitting CML from its label?

Potentially, but only if the resulting label and commercial conduct do not induce the patented CML use and no other listed patent blocks approval.

Is bosutinib a biologic subject to biosimilar litigation?

No. Bosutinib is a synthetic small-molecule drug. Generic approval proceeds through the ANDA pathway, not the biosimilar pathway.

Does claim 12 prevent use of imatinib by itself?

No. Claim 12 requires combination use of a covered quinoline compound with imatinib. It does not independently claim imatinib monotherapy.

References

Food and Drug Administration. (2023). Bosulif (bosutinib) prescribing information. U.S. Department of Health and Human Services.
Food and Drug Administration. (2024). Approved drug products with therapeutic equivalence evaluations: Orange Book. U.S. Department of Health and Human Services.
U.S. Patent and Trademark Office. (2008). U.S. Patent No. 7,417,148: Quinoline derivatives as kinase inhibitors. U.S. Department of Commerce.
U.S. Food and Drug Administration. (2017). Guidance for industry: Determining whether to submit an ANDA or a 505(b)(2) application. U.S. Department of Health and Human Services.
U.S. Congress. (1984). Drug Price Competition and Patent Term Restoration Act of 1984, Pub. L. No. 98-417, 98 Stat. 1585.

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Pf Prism Cv	BOSULIF	bosutinib monohydrate	CAPSULE;ORAL	217729-001	Sep 26, 2023		RX	Yes	No	⤷ Start Trial	⤷ Start Trial			Y		⤷ Start Trial
Pf Prism Cv	BOSULIF	bosutinib monohydrate	CAPSULE;ORAL	217729-002	Sep 26, 2023		RX	Yes	Yes	⤷ Start Trial	⤷ Start Trial			Y		⤷ Start Trial
Pf Prism Cv	BOSULIF	bosutinib monohydrate	TABLET;ORAL	203341-001	Sep 4, 2012	AB	RX	Yes	Yes	⤷ Start Trial	⤷ Start Trial			Y		⤷ Start Trial
Pf Prism Cv	BOSULIF	bosutinib monohydrate	TABLET;ORAL	203341-003	Oct 27, 2017	AB	RX	Yes	No	⤷ Start Trial	⤷ Start Trial			Y		⤷ Start Trial
Pf Prism Cv	BOSULIF	bosutinib monohydrate	TABLET;ORAL	203341-002	Sep 4, 2012	AB	RX	Yes	No	⤷ Start Trial	⤷ Start Trial			Y		⤷ 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

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Australia	2003291245	⤷ Start Trial
Australia	2004289243	⤷ Start Trial
Brazil	PI0416289	⤷ Start Trial
Canada	2543163	⤷ Start Trial
China	1874776	⤷ Start Trial
>Country	>Patent Number	>Estimated Expiration	>Supplementary Protection Certificate	>SPC Country	>SPC Expiration

Details for Patent: 7,417,148

Which drugs does patent 7,417,148 protect, and when does it expire?

Summary for Patent: 7,417,148