US Patent 7,176,211: Claim Scope, Relugolix Coverage and Patent Landscape

US Patent 7,176,211 is an expired Takeda patent directed to methods of treating hormone-dependent diseases with pyrimidine-2,4-dione compounds that act as gonadotropin-releasing hormone, or GnRH, antagonists. The claims cover a broad chemical genus and specifically enumerate compounds that include relugolix. The patent’s nominal US term ended on May 31, 2022, subject to any applicable patent-term adjustment. It no longer provides an operative US exclusivity barrier for relugolix or other compounds within the claimed scope.

The patent remains commercially important because it is an originating compound patent for the relugolix program, but current US market protection for Orgovyx depends on later patents, FDA regulatory exclusivity, and any pending ANDA litigation rather than US 7,176,211.

What drug and therapeutic class does US 7,176,211 cover?

US 7,176,211 covers nonpeptide GnRH antagonists. GnRH antagonists suppress pituitary secretion of luteinizing hormone and follicle-stimulating hormone, reducing downstream sex-hormone production.

The claimed indications are:

Claimed condition	Therapeutic relevance
Prostate cancer	Androgen-deprivation treatment
Benign prostatic hypertrophy	Reduction of androgen-driven prostate stimulation
Breast cancer	Hormone-sensitive disease
Endometriosis	Suppression of ovarian hormone production

The patent is associated with the relugolix chemical program. Relugolix is marketed in the United States as Orgovyx for the treatment of adults with advanced prostate cancer. The FDA approved Orgovyx on December 18, 2020. The product is administered orally and is a small-molecule GnRH receptor antagonist, not a biologic.[1]

The claims also cover numerous relugolix analogs. The patent therefore has two distinct commercial dimensions:

A broad genus covering structurally related pyrimidinedione compounds.
Specific compound claims that identify named analogs, including relugolix.

What is the scope of independent claim 1?

Claim 1 is a method-of-treatment claim. It requires all of the following elements:

Treatment of prostate cancer, benign prostatic hypertrophy, breast cancer, or endometriosis.
A subject in need of treatment.
Administration of a pharmaceutically effective amount.
A compound having the claimed pyrimidinedione scaffold.
A compound satisfying the specified substituent definitions.
A stereoisomer or pharmaceutically acceptable salt of the compound.

The claim is not limited to relugolix. It covers a large Markush genus defined by variable substituents R1a through R6 and X.

Chemical limitations in claim 1

Variable	Claimed scope
R1a, R1b, R1c	Hydrogen, halogen, C1-4 alkyl, hydroxy or alkoxy; selected pairs may form methylenedioxy or ethylenedioxy rings
R2a, R2b	Hydrogen, halogen, trifluoromethyl, cyano or methylsulfonyl
R3	Hydrogen or methyl
R4	Phenyl or C3-7 alkyl
R5	Hydrogen or C1-4 alkyl
R6	Carboxylic acid or an acid isostere
X	C1-6 alkanediyl, optionally substituted with up to three C1-6 alkyl groups

The claim reaches compounds with:

A substituted aromatic ring;
A second aromatic or alkyl substituent;
A benzyl-type N-substituent;
A chiral aminoalkyl side chain;
A carboxylic acid or bioisosteric replacement;
Optional stereoisomeric and salt forms.

The use of “acid isostere” materially expands the claim beyond compounds containing a literal carboxylic acid. Depending on the specification’s disclosure and the prosecution history, that language may include tetrazoles and other acidic bioisosteres. The named relugolix compound contains a tetrazole-containing side chain and a methylsulfonyl-substituted benzyl group.

How do claims 2 through 10 narrow claim 1?

Claims 2 through 10 progressively narrow the genus and treatment indications.

Claim	Limitation
2	X is straight-chain C1-6 alkanediyl
3	R6 is carboxylic acid
4	R4 is phenyl
5	R1a is halogen and R1b is alkoxy
6	R3 is methyl
7	Treatment of endometriosis
8	Treatment of benign prostatic hypertrophy
9	Treatment of prostate cancer
10	Treatment of breast cancer

Claims 7 through 10 are not independent composition claims. They remain method claims and inherit every limitation of claim 1, together with the limitations of the claims from which they depend.

This structure creates a hierarchy of protection:

Claim 1 provides the broadest method genus.
Claims 2 through 6 narrow the chemistry.
Claims 7 through 10 narrow the clinical indication.
A potential infringer must practice every limitation of the asserted claim to be liable for literal infringement.

What compounds are specifically listed in claims 11 and 16?

Claims 11 and 16 identify specific chemical entities rather than relying solely on the Markush definitions.

Claim 11 lists four compounds. They share several structural characteristics:

A pyrimidine-2,4-dione core;
A chiral aminoethyl substituent;
A carboxylic acid or tetrazole-containing side chain;
A substituted benzyl group;
A substituted aryl or cyclohexyl group;
In several examples, a 6-methyl substitution on the pyrimidinedione ring.

The fourth compound in claim 11 is the relugolix compound:

3-[2(R)-{2-[1-(5-tetrazolyl)propyl]amino}-2-phenylethyl]-5-(2-fluoro-3-methoxyphenyl)-1-[2-fluoro-6-(methylsulfonyl)benzyl]-6-methylpyrimidine-2,4(1H,3H)-dione.

Claims 12 through 15 limit the claim 11 compounds to endometriosis, benign prostatic hypertrophy, prostate cancer and breast cancer, respectively.

Claim 16 lists six additional compounds. These include analogs with:

2-chlorophenyl and 2-fluoro-3-methoxyphenyl groups;
Methylsulfonyl or trifluoromethyl benzyl substituents;
Phenyl, isobutyl or other side-chain groups;
Carboxylic acid-containing aminoalkyl substituents.

Claims 17 through 20 apply the four disease indications to the compounds of claim 16.

Is US 7,176,211 a composition patent or a method-of-use patent?

US 7,176,211 is principally a method-of-treatment patent.

The asserted claims require administration to treat a specified condition. They do not independently claim:

A pharmaceutical composition;
A tablet formulation;
A dosage regimen;
A sustained-release delivery system;
A manufacturing process;
A crystalline polymorph;
A particular salt or solid form as a composition;
A package or combination product.

The claims include pharmaceutically acceptable salts and stereoisomers, but that inclusion occurs within a treatment method. It does not convert the patent into a standalone composition claim.

This distinction matters in generic litigation. A generic manufacturer may avoid direct infringement of a method claim if its labeling omits or carves out the patented indication, provided the remaining label and marketing conduct do not induce infringement. That strategy is less effective when the patented indication is the principal FDA-approved use or when the label encourages the claimed use.

What is the expiration date of US 7,176,211?

The patent’s ordinary US patent term ran from the relevant international filing date and reached its nominal end on May 31, 2022. The patent was issued on February 13, 2007, as US Patent 7,176,211 B2.[2]

Event	Date
Earliest stated priority	June 1, 2001
International filing	May 31, 2002
US patent grant	February 13, 2007
Nominal US patent expiration	May 31, 2022
Current status	Expired by ordinary term

The patent is therefore not a current blocking patent in the United States. Any patent-term adjustment would need to be confirmed from the USPTO patent record. No patent-term extension under 35 U.S.C. § 156 should be assumed for this patent merely because relugolix received FDA approval.[3]

What is the Orange Book status of US 7,176,211?

The relevant FDA-listed product is Orgovyx, containing relugolix. FDA Orange Book treatment of a patent depends on the patent’s listed claims and the sponsor’s certification of the patent’s relevance to the approved drug.[4]

US 7,176,211 does not provide current Orange Book exclusivity because its patent term has ended. If it was previously listed for relugolix, the listing cannot preserve market exclusivity after expiration.

The practical distinction is:

Protection type	Position for US 7,176,211
Active compound patent	Expired
Active formulation patent	No formulation claim in the supplied claims
Active method-of-use patent	Expired
FDA NCE exclusivity	Separate regulatory protection
Generic substitution barrier	No longer supplied by this patent
Biosimilar exclusivity	Not applicable

Relugolix is a small molecule. Generic applicants use the ANDA pathway, not the biosimilar pathway under the Public Health Service Act.

When did Orgovyx lose or gain regulatory exclusivity?

FDA approved Orgovyx on December 18, 2020. As a new chemical entity, relugolix was eligible for five years of FDA data exclusivity, subject to the statutory treatment of the product and any applicable exceptions. The five-year period would ordinarily run through December 18, 2025.[1][5]

Regulatory exclusivity and patent exclusivity operate independently:

US 7,176,211 expired in 2022.
FDA NCE exclusivity extended beyond the patent expiration.
Later patents may extend commercial protection beyond the NCE period.
FDA exclusivity does not extend the patent term.

An ANDA applicant could therefore face a regulatory filing restriction even after the core compound patent expired.

What formulation patents and later patents may protect Orgovyx?

The supplied claims do not protect Orgovyx’s tablet formulation. Commercial protection for Orgovyx may instead depend on later patents directed to:

Relugolix-containing pharmaceutical compositions;
Tablet formulations;
Drug-release and stability properties;
Manufacturing methods;
Specific dosing regimens;
Combination treatment with androgen-receptor pathway inhibitors;
Methods of treating prostate cancer;
Product-specific formulations or solid-state forms.

A complete freedom-to-operate review must separate the following patent categories:

Patent category	Risk to a relugolix generic
Core compound patent	High before expiry; low after expiry
Specific salt or polymorph	Can block a particular API or dosage form
Tablet formulation	Can require a noninfringing formulation
Method of use	Can create induced-infringement exposure
Dosing regimen	Relevant if the generic label recommends the same regimen
Manufacturing process	Relevant only if the accused process is used
Combination therapy	Relevant to combination products and labeling
Packaging or device	Usually narrower and design-aroundable

The original patent does not, by itself, establish protection for all later Orgovyx patents.

Which companies are challenging Orgovyx patents?

Generic competition for relugolix is expected to proceed through ANDA filings and Paragraph IV certifications against unexpired Orange Book patents. A Paragraph IV certification alleges that a listed patent is invalid, unenforceable or will not be infringed.

The expired status of US 7,176,211 makes it an unlikely target for a commercially meaningful current Paragraph IV dispute. Any active litigation would more likely involve later patents covering formulation, dosage, use or other product-specific subject matter.

The critical litigation questions are:

Which active patents were listed for Orgovyx when the ANDA was filed?
Which patents did the applicant challenge under Paragraph IV?
Did the sponsor file suit within 45 days?
Did the suit trigger a 30-month FDA approval stay?
Were the parties subject to a settlement or license?
Is the generic label carved out for patented indications?

These facts must be analyzed from the FDA Orange Book, ANDA litigation dockets and settlement filings. They cannot be inferred from US 7,176,211 alone.

How strong is the patent estate for relugolix?

The strength of US 7,176,211 was high during the compound patent term because claim 1 covered a broad genus and claim 11 specifically identified relugolix. Its current blocking strength is zero because the patent has expired.

The patent had several potential vulnerability points:

Written-description and enablement risk

Claim 1 covers a large number of substituent combinations, stereoisomers and acid isosteres. A challenger could argue that the specification did not adequately describe or enable the full genus, particularly if the patent disclosed a limited number of examples relative to the breadth of claim 1.

Indefiniteness risk

The phrase “acid isostere” can be litigated if the specification and prosecution history do not provide a sufficiently definite boundary. The issue would be less significant for claim 11, where the listed chemical structures are more specific.

Method-of-treatment limitations

The claims require treatment of a specific disease in a subject in need thereof. An accused product does not necessarily infringe merely because it contains a covered compound. Use, labeling, prescribing and marketing evidence matter.

Species and genus coverage

Claims 11 and 16 provide species-level protection. Species claims are generally easier to analyze for infringement than broad genus claims, but they remain method claims and require proof of the claimed therapeutic use.

What generic launch scenarios exist for relugolix?

Scenario 1: Immediate launch after regulatory clearance

A generic applicant launches after FDA approval if no enforceable patent or settlement restriction remains. This is the most favorable scenario for generic entry.

Scenario 2: Paragraph IV litigation

The applicant challenges later unexpired patents. FDA approval may be delayed by litigation or a statutory stay. The result depends on patent validity, infringement and settlement terms.

Scenario 3: Section viii carve-out

The generic applicant removes a patented indication from its label. This strategy is more viable when the product has multiple approved uses and the unpatented use is commercially meaningful.

Scenario 4: At-risk launch

A generic launches before final resolution of litigation. The applicant assumes potential damages and injunction risk. This scenario is less likely where the remaining patents cover the core commercial indication or a necessary formulation.

Scenario 5: Authorized generic or license

The originator or licensee may grant rights, launch an authorized generic or settle with a defined entry date. A settlement can materially change market timing without invalidating the patents.

How does the patent landscape compare with other GnRH antagonists?

Product	Active ingredient	Modality	US regulatory pathway	Key patent issue
Orgovyx	Relugolix	Oral GnRH antagonist	NDA	Core compound patent expired; later product patents may remain
Orilissa	Elagolix	Oral GnRH antagonist	NDA	Compound, formulation and use patents
Myfembree	Relugolix combination	Oral combination product	NDA	Relugolix plus estrogen/progestin formulation and use protection
Firmagon	Degarelix	Injectable peptide antagonist	NDA	Biologic-like peptide product, formulation and manufacturing protection
Lupron	Leuprolide	Injectable GnRH agonist	NDA	Longstanding formulation and depot-delivery patents

Relugolix has a differentiated commercial position because it is orally administered and does not require an initial injectable loading dose. That advantage increases the importance of tablet formulation, dosing and combination-product patents after expiration of the original compound patent.

What licensing deals affect relugolix rights?

Takeda originated the relugolix program. Myovant Sciences obtained rights to develop and commercialize relugolix outside territories retained by Takeda. Myovant later entered into a commercial collaboration with Pfizer for Orgovyx in the United States and Canada. Sumitomo Pharma subsequently acquired Myovant, consolidating control of Myovant’s relugolix-related assets and commercial rights.[6]

The licensing structure is relevant to patent enforcement because the party selling the product may differ from:

The original patent owner;
The current patent assignee;
The Orange Book patent holder;
The NDA holder;
The party bringing infringement litigation.

Ownership, assignment and standing should be checked separately for each asserted patent.

Does US 7,176,211 create current biosimilar risk?

No. Relugolix is a chemically synthesized small molecule, so biosimilar standards do not apply. The relevant competitive threat is an ANDA generic.

The principal current risks are:

Generic entry after FDA regulatory exclusivity;
Challenges to later Orange Book patents;
Label carve-outs;
Authorized-generic arrangements;
Price erosion from multiple ANDA approvals;
Loss of premium pricing after product-specific patents expire.

Key Takeaways

US 7,176,211 is a method-of-treatment patent for GnRH antagonist pyrimidinedione compounds.
Claim 1 covers a broad Markush genus, including stereoisomers and pharmaceutically acceptable salts.
Claims 11 and 16 identify specific compounds, and claim 11 includes relugolix.
The patent covers prostate cancer, benign prostatic hypertrophy, breast cancer and endometriosis.
It contains no standalone tablet, formulation, manufacturing or dosage-form claim in the supplied claims.
The patent’s nominal US expiration date was May 31, 2022.
US 7,176,211 is not a current US blocking patent for Orgovyx.
Relugolix received FDA approval on December 18, 2020 and was eligible for five years of NCE exclusivity, ordinarily through December 18, 2025.
Current generic-entry risk depends on later relugolix patents, Orange Book listings, ANDA certifications, litigation and settlement terms.
Biosimilar analysis is inapplicable because relugolix is a small molecule.
The original patent’s claim breadth created historical genus coverage, but its present commercial enforcement value is exhausted.

FAQs About US Patent 7,176,211 and Relugolix

Does US 7,176,211 claim Orgovyx directly?

Yes. Claim 11 specifically identifies the relugolix chemical entity, although the claim remains a method-of-treatment claim rather than a standalone composition claim.

Can a generic manufacturer infringe an expired US 7,176,211 patent?

No enforceable infringement liability ordinarily remains after patent expiration. Conduct that occurred before expiration may raise separate issues, but post-expiration manufacture and sale are not blocked by this patent.

Does the patent cover endometriosis treatment with relugolix?

Yes. Claims 12 and 17 expressly apply the specifically listed compounds to endometriosis treatment.

Is a tetrazole an acid isostere under claim 1?

The claim language is broad enough to contemplate acid isosteres, and the specifically named relugolix compound contains a tetrazole group. The precise scope depends on the patent specification and prosecution history.

Will expiration of US 7,176,211 automatically permit generic Orgovyx substitution?

No. Generic substitution also depends on FDA approval, regulatory exclusivity, active Orange Book patents, Paragraph IV litigation, label restrictions and any settlement or license governing entry.

References

U.S. Food and Drug Administration. (2020). FDA approves relugolix for advanced prostate cancer.
United States Patent and Trademark Office. (2007). U.S. Patent No. 7,176,211, pyrimidine derivatives.
35 U.S.C. §§ 154, 156.
U.S. Food and Drug Administration. (n.d.). Approved drug products with therapeutic equivalence evaluations: Orange Book.
Federal Food, Drug, and Cosmetic Act, 21 U.S.C. § 355(j).
Sumitomo Pharma Co., Ltd. (2023). Corporate disclosures regarding the acquisition of Myovant Sciences and relugolix commercialization rights.

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Austria	407679	⤷ Start Trial
Australia	2004257639	⤷ Start Trial
Brazil	PI0412314	⤷ Start Trial
Canada	2531508	⤷ Start Trial
China	100424078	⤷ Start Trial
China	1819829	⤷ Start Trial
>Country	>Patent Number	>Estimated Expiration	>Supplementary Protection Certificate	>SPC Country	>SPC Expiration

Details for Patent: 7,176,211

Summary for Patent: 7,176,211