US Patent 7,504,509: Claim Scope, Patent Strength, Exclusivity and Competitive Landscape

US Patent 7,504,509 is a broad small-molecule patent covering substituted 1H-pyrrolo[2,3-b]pyridines, related pharmaceutically acceptable salts, compositions and kits. Its central protection is a chemical genus defined by substituents at the pyrrolopyridine core, supported by extensive lists of specifically named compounds. The patent does not contain a conventional method-of-treatment claim in the claims supplied. Its commercial value therefore depends on whether a marketed or development-stage active pharmaceutical ingredient falls within the claimed chemical structures.

The patent issued on March 17, 2009. The claims supplied do not identify an FDA-approved active ingredient, Orange Book listing, regulatory exclusivity period, Paragraph IV challenge or litigation matter. The patent is best characterized as a discovery-stage kinase-oriented compound estate rather than an identifiable product patent for a marketed drug.

What does US Patent 7,504,509 protect?

The patent protects four principal subject-matter categories:

Category	Claims	Scope
Chemical compounds	1-4, 9-39	Substituted pyrrolo[2,3-b]pyridines and named species
Pharmaceutical compositions	5-6	A claimed compound plus a pharmaceutically acceptable carrier
Kits	7-8	A pharmaceutical composition containing a claimed compound
Salts	Throughout	Pharmaceutically acceptable salts of claimed compounds

The independent chemical claim is claim 1. It covers a large genus in which:

R1 and R5 are hydrogen;
R2 is a benzyl-type group, heteroarylmethyl group, acyl group or sulfonyl-related substituent;
one of R3 and R4 is hydrogen;
the other position contains a broad substituent class;
substituents may include halogen, hydroxy, alkoxy, thioalkoxy, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl, amine, amide, sulfonamide or sulfoxide/sulfone functionality.

The core structure is a pyrrolo[2,3-b]pyridine, commonly referred to as a 7-azaindole framework. The claims cover substitution patterns at multiple ring positions, producing a large chemical space rather than one narrowly defined molecular entity.

How broad is claim 1?

Claim 1 is structurally broad and potentially covers a substantial number of compounds. Its breadth arises from three features.

Broad substituent definitions

The claim permits multiple classes at R2, R3 and R4. The definitions include both simple substituents and functionalized aromatic or heteroaromatic groups. The use of "optionally substituted" expands the number of possible embodiments substantially.

The claim also permits:

aryl and heteroaryl groups;
aralkyl and heteroaralkyl groups;
cyclic amines and heterocycles;
carbonyl, thiocarbonyl and sulfonyl derivatives;
substituted nitrogen-containing side chains.

A molecule can fall within claim 1 without being one of the specifically named compounds in claim 4 or claims 15-39.

Alternative positional isomers

Claims 2 and 3 separately cover the two principal substitution orientations:

claim 2: R3 is hydrogen;
claim 3: R4 is hydrogen.

This is important because the pyrrolopyridine ring can carry the non-hydrogen substituent at either of two adjacent positions. Claims 11-14 further narrow the allowed substituent classes for these positional arrangements.

Salt coverage

The claims extend to pharmaceutically acceptable salts. A salt conversion generally will not avoid infringement where the corresponding free base is within the compound claim. The practical scope depends on whether the salt is properly characterized as pharmaceutically acceptable and whether the underlying active moiety satisfies the structural limitations.

What compounds are specifically protected?

Claim 4 lists a large number of individual compounds. Claims 15 through 39 divide additional named species into structural groups. The listed molecules fall into recurring chemical classes:

Structural class	Representative substituents
Benzoyl derivatives	Methoxybenzoyl, fluoro-benzoyl, chloro-benzoyl, dichloro-benzoyl
Heteroaryl analogues	Pyridyl, thiophenyl, methylisoxazolyl and dimethylpyrazolyl
Anilide and benzamide derivatives	Phenylacetamides, methanesulfonamides and benzamides
Acrylic acid derivatives	E-configured aryl acrylic acids
Aminophenyl analogues	3-aminophenyl-substituted pyrrolopyridines
Halogenated analogues	Bromo, chloro, fluoro and difluoro compounds
Benzyl derivatives	Methoxybenzyl and substituted pyridylmethyl compounds
Phenolic compounds	Hydroxyphenyl, dihydroxyphenyl and methoxyphenol derivatives

The named species provide a narrower enforcement position than claim 1. They can be useful in an infringement case because a defendant’s compound may match a listed species even if the broader genus is challenged.

What are the strongest claim layers?

The strongest practical claim layers are likely claims 1, 4 and 5-6, but they have different enforcement characteristics.

Claim 1: broad genus claim

Claim 1 has the greatest theoretical coverage. It can capture compounds that differ materially from the examples, provided every structural limitation is satisfied. Its principal vulnerabilities are:

breadth of the genus;
written-description support across the full substituent space;
enablement across the full range of compounds;
construction of undefined or inconsistently defined terms;
potential prior-art combinations involving known 7-azaindole chemistry.

A broad genus claim is valuable when the accused compound is structurally close to the disclosed series. It is less secure when the accused compound occupies a remote portion of the claimed chemical space that has limited representative disclosure.

Claim 4: extensive species list

Claim 4 recites a large group of specific compounds. Species claims generally offer better written-description support than a broad Markush claim, assuming the compounds are adequately disclosed and enabled in the specification.

The claim list also creates drafting and prosecution risks. Several entries contain apparent typographical or nomenclature defects, including:

inconsistent bracket and parenthesis placement;
"heteroaxyl" and "heteroazyl" terminology in claim 9;
repeated compounds;
inconsistent use of "thiophen" and "thiophene";
apparent omissions in compound names;
inconsistent locant formatting;
apparent use of "benzatide" instead of "benzamide";
incorrect or incomplete ring descriptions.

Whether a defect is material depends on the issued patent, prosecution history, claim construction and whether a skilled chemist can identify the intended structure with reasonable certainty.

Claims 5 and 6: composition claims

These claims cover pharmaceutical compositions containing a claim 1 or claim 4 compound and a pharmaceutically acceptable carrier. They are useful against formulated products, but they do not appear to require:

a specific dosage;
a particular release profile;
a defined excipient;
a particular route of administration;
a therapeutic indication;
a specific concentration or particle size.

That makes them broad but less differentiated from ordinary pharmaceutical formulations.

Claims 7 and 8: kit claims

The kit claims cover kits containing a pharmaceutical composition with a claimed compound. They do not appear to recite a treatment instruction, dosing schedule, diagnostic component or administration device. Their commercial significance is limited unless a product is sold in a kit format.

Does the patent protect a formulation?

No specialized formulation technology is apparent from the supplied claims. Claims 5 and 6 are conventional composition claims covering a claimed compound with a pharmaceutically acceptable carrier.

The patent does not, on the supplied claim language, specifically protect:

extended-release tablets;
nanoparticles;
liposomes;
injectable depot systems;
transdermal delivery;
amorphous solid dispersions;
a particular polymorph;
a hydrate or solvate;
a defined particle-size distribution;
a specific excipient combination.

A later developer could therefore face compound-claim risk while potentially designing around the composition claims through a non-infringing active ingredient. Conversely, a formulation patent directed to a specific salt, polymorph, dosage form or release profile could create a separate blocking right even after the compound claims expire.

Are there method-of-use claims?

The claims supplied contain no conventional method-of-treatment claim. There is no claim expressly requiring administration of a compound to a patient for:

cancer;
inflammation;
autoimmune disease;
infectious disease;
metabolic disease;
kinase-mediated disease;
a named molecular target.

This limits the patent’s ability to block use of a structurally non-infringing molecule for the same indication. The patent’s principal enforcement theory is direct infringement based on making, using, selling, offering to sell or importing a claimed compound or composition under 35 U.S.C. §271, rather than infringement of a treatment method.

When does US Patent 7,504,509 lose exclusivity?

The patent’s enforceable term cannot be calculated from the claims alone. US patent term is generally measured from the earliest effective nonprovisional filing date for applications filed after June 8, 1995, subject to patent-term adjustment, patent-term extension, terminal disclaimers and other statutory rules under 35 U.S.C. §§154 and 156.

The relevant exclusivity analysis is:

Exclusivity category	Applicability
Patent term	Depends on earliest effective US filing date and adjustments
Patent-term adjustment	Must be confirmed from the USPTO record
Patent-term extension	No extension is established by the supplied claims
FDA new chemical entity exclusivity	No approved drug is identified
FDA orphan exclusivity	No orphan product is identified
FDA pediatric exclusivity	No pediatric extension is identified
Orange Book listing	No listed drug is identified from the supplied information

A patent expiration date must be taken from the USPTO patent record or a reliable patent-term calculation using the full continuity chain. Grant date alone is not the controlling date.

What is the Orange Book status?

The supplied material does not identify an FDA-approved product, active ingredient, applicant or New Drug Application associated with US 7,504,509. The claims also do not identify a commercial drug name.

On the available claim information, the patent should not be treated as an Orange Book-listed product patent. FDA Orange Book listing requires an approved drug application and a patent submitted by the NDA holder that meets FDA listing criteria under 21 C.F.R. §314.53. A broad research patent may have no Orange Book relevance even if it covers compounds with pharmacological activity.

Are Paragraph IV challenges relevant?

A Paragraph IV certification is relevant only if an ANDA applicant seeks approval for a generic version of an approved drug and an applicable patent is listed in the Orange Book.

The patent’s claim structure does not establish that:

a drug covered by the patent was approved;
the patent was listed in the Orange Book;
an ANDA was filed;
a Paragraph IV notice letter was served;
a 30-month stay was triggered;
Hatch-Waxman litigation occurred.

If no approved product corresponds to the claimed compounds, the more relevant risks would be ordinary patent infringement, pre-launch freedom-to-operate analysis and potential patent litigation under 35 U.S.C. §271, rather than Paragraph IV litigation.

What is the patent strength?

Strengths

The patent includes a broad chemical genus.
It covers both positional isomers through separate dependent-claim pathways.
It contains numerous named species.
It includes salts, compositions and kits.
The claim architecture creates several infringement theories against a compound program.
A close analogue may be captured even if it is not expressly named.

Weaknesses

The genus is exceptionally broad relative to the limited claim language supplied.
No pharmacological activity limitation narrows the compounds to a target or indication.
No method-of-use claims are apparent.
Composition and kit claims are generic.
Apparent typographical and nomenclature errors could create claim-construction disputes.
The patent’s commercial value depends on identification of a real development or marketed compound within the claims.
Broad genus claims may face written-description, enablement and obviousness challenges under current US law, including the Federal Circuit’s treatment of large chemical genera.

The estate is strongest against a compound that closely matches one of the named examples or a well-supported subgenus. It is weaker against a remote analogue that falls only within the outer boundaries of claim 1.

What generic-entry risks exist?

The patent does not present a conventional generic-entry profile unless one of its compounds became an approved drug. The principal scenarios are:

Scenario	Risk
Approved drug exactly matching a named species	High compound-claim risk until patent expiry or invalidation
Approved drug matching claim 1 but not expressly listed	Moderate-to-high genus-claim risk
Salt of a claimed free base	High risk if the active moiety is covered
Non-covered polymorph of a covered compound	Usually does not avoid compound infringement
Different active scaffold with same indication	No literal compound-claim risk, absent other patents
New formulation of a covered compound	Compound claims remain relevant even if formulation differs
Research-stage analogue	Depends on element-by-element structural mapping

A generic company cannot rely on a formulation change to avoid an active-compound claim. A non-infringing chemical redesign is more likely to create a viable design-around than a change in excipients or dosage form.

Which companies are challenging the patent?

No challenger, Paragraph IV notice, district-court case, PTAB proceeding, settlement or license is identified in the supplied material. The patent number alone does not establish a current challenge or a commercial license.

The original patent owner, inventorship, assignment history and any continuation or divisional family members must be taken from the USPTO assignment and continuity records. A reliable landscape should distinguish:

original owner;
current assignee;
exclusive licensees;
continuation applicants;
companies developing compounds in the same 7-azaindole kinase space;
parties named in litigation or inter partes review.

How does this patent compare with a product patent?

US 7,504,509 is materially different from a typical pharmaceutical product patent.

Product-patent characteristic	US 7,504,509
One defined API	No
Narrow chemical structure	No
Broad Markush genus	Yes
Named species	Yes
Method of treatment	Not in supplied claims
Specific formulation	No
FDA-approved product identified	No
Orange Book relevance established	No
Generic litigation pathway established	No

Its value is primarily platform-oriented. It can cover multiple discovery compounds, but that breadth does not itself establish product-level commercial value.

Key Takeaways

US 7,504,509 covers a broad genus of substituted pyrrolo[2,3-b]pyridines and numerous named species.
Claim 1 is the principal broad chemical claim.
Claims 4 and 15-39 provide species-level fallback positions.
Claims 5-8 cover conventional compositions and kits, not specialized delivery technology.
No method-of-treatment claim appears in the supplied claims.
No FDA-approved drug, Orange Book listing, Paragraph IV challenge or litigation is established.
The patent’s commercial importance depends on whether a development or marketed compound falls within the claimed structures.
The principal legal vulnerabilities are genus breadth, written description, enablement, obviousness and nomenclature defects.
The patent expiration date requires the complete priority and patent-term-adjustment record.
A compound redesign is more likely to avoid risk than a formulation change when the active moiety is covered.

FAQs

Does a pharmaceutically acceptable salt infringe US 7,504,509?

Potentially yes. The claims expressly include pharmaceutically acceptable salts. A salt form generally remains within the claim when its underlying free base satisfies the structural limitations.

Can a company avoid this patent by changing the excipient?

Usually not if the active compound itself is covered by claim 1 or a species claim. A different excipient may avoid a formulation-specific claim, but it does not avoid a compound claim.

Does US 7,504,509 cover all kinase inhibitors?

No. It covers a defined chemical genus based on substituted pyrrolo[2,3-b]pyridine structures. A kinase inhibitor with a different core may fall outside the patent even if it acts on the same biological target.

Is a Paragraph IV certification required for this patent?

Only if the patent is listed in the Orange Book for an approved drug and an ANDA applicant seeks approval for that drug. The supplied information does not establish either condition.

Can typographical errors invalidate the patent?

Not automatically. The effect depends on whether the claim language, specification and prosecution history allow a skilled person to determine the claimed subject matter with reasonable certainty. Errors may still create indefiniteness or claim-construction disputes.

References

United States Patent and Trademark Office. (2009). U.S. Patent No. 7,504,509.
United States Code. (2024). 35 U.S.C. §§ 154, 156, 271.
United States Food and Drug Administration. (2024). Approved drug products with therapeutic equivalence evaluations: Orange Book.
United States Food and Drug Administration. (2024). 21 C.F.R. § 314.53: Submission of patent information.
United States Patent and Trademark Office. (2024). Manual of Patent Examining Procedure, §§ 2161-2165.

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Hoffmann La Roche	ZELBORAF	vemurafenib	TABLET;ORAL	202429-001	Aug 17, 2011		RX	Yes	Yes	7,504,509	⤷ Start Trial	Y	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	2004308299	⤷ Start Trial
Canada	2550361	⤷ Start Trial
China	1925855	⤷ Start Trial
Cyprus	1118328	⤷ Start Trial
Denmark	1696920	⤷ Start Trial
European Patent Office	1696920	⤷ Start Trial
Spain	2527118	⤷ Start Trial
>Country	>Patent Number	>Estimated Expiration	>Supplementary Protection Certificate	>SPC Country	>SPC Expiration

Details for Patent: 7,504,509

Which drugs does patent 7,504,509 protect, and when does it expire?

Summary for Patent: 7,504,509