Details for Patent: 8,012,976

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Which drugs does patent 8,012,976 protect, and when does it expire?

Patent 8,012,976 protects TALZENNA and is included in two NDAs.

This patent has fifty-six patent family members in thirty-two countries.

Summary for Patent: 8,012,976

Title:	Dihydropyridophthalazinone inhibitors of poly(ADP-ribose)polymerase (PARP)
Abstract:	A compound having the structure set forth in Formula (I) and Formula (II): wherein the substituents Y, Z, A, B, R1, R2, R3, R4 and R5 are as defined herein. Provided herein are inhibitors of poly(ADP-ribose)polymerase activity. Also described herein are pharmaceutical compositions that include at least one compound described herein and the use of a compound or pharmaceutical composition described herein to treat diseases, disorders and conditions that are ameliorated by the inhibition of PARP activity.
Inventor(s):	Bing Wang, Daniel Chu
Assignee:	Medivation Technologies LLC
Application Number:	US12/510,096
Patent Claim Types: see list of patent claims	Composition; Compound;

Patent 8,012,976 Scope and Claims: What the US8213976 Estate Covers, What It Excludes, and How It Shapes Generic and Reformulation Risk

Executive summary

US 8,012,976 is a small-molecule US patent centered on a single chemical entity defined by a pyrido[4,3,2-de]phthalazin-3(7H)-one scaffold with specific substituents (5-fluoro, 8-(4-fluorophenyl), 9-(1-methyl-1H-1,2,4-triazol-5-yl)) plus stereochemical dependent coverage for two enantiomeric configurations. The claim set also expands to (i) a composition claim pairing that entity (or salts) with pharmaceutically acceptable carriers and (ii) narrower enantiomer claims that can support separate infringement theories for racemate versus isolated stereoisomers. The practical scope is “compound first” with composition coverage that is broad on carriers but narrow on the API identity.

What patents protect US 8,012,976’s specific compound formula and stereochemistry?

Direct answer: The protection is driven by the compound claims (including salts) and then split by enantiomer for (8R,9S) and (8S,9R). That creates three infringement-relevant API buckets: (1) the generic “compound of formula” as claimed, (2) the racemate or non-enantiopure material that still falls within the claimed compound definition, and (3) the two stereospecific embodiments.

How claim 2 operationalizes the chemical identity

Claim 2 defines a single structure:

• Core: 8,9-dihydro-2H-pyrido[4,3,2-de]phthalazin-3(7H)-one
• Substituents:
  • 5-fluoro
  • 8-(4-fluorophenyl)
  • 9-(1-methyl-1H-1,2,4-triazol-5-yl)

If a competitor’s API does not match this substitution pattern, it is not captured by claim 2. If the structure matches but uses a different stereochemical configuration, it may still fall under the “compound of formula” claim if that claim is not limited by stereochemistry, depending on how the “formula” is written in the patent specification and whether the formula includes absolute stereochemical assignment.

What do the enantiomer claims add (claims 4 and 5)?

Claims 4 and 5 are stereochemically constrained:

• Claim 4: (8R,9S)-configured species
• Claim 5: (8S,9R)-configured species

Business implication: A defendant that designs around by switching the stereochemical composition can reduce risk for one enantiomer claim, but not for the other. If the patent estate relies only on these enantiomer claims plus an undirected compound claim, enforcement strategy can still capture stereochemical variants if the compound claim is broad enough.

What is covered by “pharmaceutically acceptable salts”?

All compound claims include “or a pharmaceutically acceptable salt thereof.” That expands infringement coverage to:

• salts of the claimed base compound (or salts of the compound as formulated in the patent)
• common salt forms used for formulation and solid-state processing

Scope effect: Even if a generic developer uses a different counterion, infringement risk remains if the salt is pharmaceutically acceptable and falls within the salt definition in the claim. Salt design-around is typically a limited strategy unless the competitor can credibly avoid “pharmaceutically acceptable salt” as construed under the patent’s intrinsic record.

Does US 8,012,976 cover only the API or also formulations?

Direct answer: It covers a pharmaceutical composition containing the claimed compound (or salt) plus pharmaceutically acceptable excipients.

Claim 3: composition claim breadth and its limits

Claim 3: “A pharmaceutical composition comprising a compound of the formula… and a pharmaceutically acceptable diluent, excipient or carrier.”

Breadth drivers:

• Carrier/excipient language is open-ended.
• No method-of-manufacture requirements in the claim.

Key limitation:

• The composition must include the claimed compound (or salt).
  So excipient changes, tablet coating systems, or dose-form selection generally do not avoid infringement unless the API itself is changed outside the claim scope.

What claim 3 does not cover by itself

Claim 3 is not a “use” claim. It is not a method-of-treatment claim. It does not state a route of administration, dosing regimen, or specific formulation type (tablet, capsule, lyophilized powder, etc.). Those gaps can matter for enforcement if a competitor uses a different delivery form but the same API identity.

How strong is the patent estate for US 8,012,976 compound claims versus generic design-arounds?

Direct answer: Strength is concentrated in API identity. The strongest design-around lever is changing the chemical structure such that it falls outside the specified substituents and ring system. Switching stereochemistry may not eliminate risk if the base compound claim is not stereochemically limited.

Structural design-around risk checklist

A product must avoid at least one of the claim-defining features:

• Ring system: pyrido[4,3,2-de]phthalazin-3(7H)-one with 8,9-dihydro-2H specification
• Substituent placement and identities:
  • 5-fluoro
  • 8-(4-fluorophenyl) (including the fluorine position on the phenyl)
  • 9-(1-methyl-1H-1,2,4-triazol-5-yl) (including the methyl and ring linkage positions)

If any of those is different, claim 2 likely does not read on the product.

Salt-only design-around

If the API structure remains the same but salt form is changed, infringement risk stays high under the salt language, assuming the alternative salt is found “pharmaceutically acceptable” in claim construction.

Enantiomer-only design-around

If the competitor uses an enantiomeric mixture, or isolates one enantiomer, the enantiomer-specific claims (claims 4 and 5) can still be asserted depending on:

• whether the competitor’s product is primarily one configuration
• whether claim 1 (“compound of formula”) is interpreted to include that stereoisomer even if claims 4 and 5 exist

Practical take: Stereochemical strategy only works if the independent compound claim is interpreted to require stereochemical alignment with the enantiomeric depiction in the formula, not a racemate-inclusive genus.

What is the likely claim construction boundary for “compound of the formula” (claim 1)?

Direct answer: Claim 1 is a genus “compound of the formula,” with claim 2 spelling out a specific member. The scope boundary depends on how the formula encodes stereochemistry.

Two competing interpretive outcomes

1. If the drawn/defined formula in claim 1 does not specify stereochemistry, claim 1 may cover both enantiomers (and potentially racemate), making claims 4 and 5 additive but not exclusive.
2. If the formula includes stereochemical variables or a fixed 3D assignment, then claim 1 may be narrower and enantiomer claims 4/5 become the true “full coverage” for both stereoisomers.

Enforcement consequence: Courts often prioritize the explicit enantiomer claims as defining stereochemical scope. If claim 1 is truly generic over stereochemistry, then enantiomer claims mainly prevent partial coverage defenses.

What generic entry risks exist for products containing this API?

Direct answer: High for an ANDA that relies on carving out claim 3 and the specific compound claims. The main risk is that the generic’s ANDA will include the identical API (or a salt) and therefore fall within the compound and composition claims.

ANDA risk channels

• If the generic API matches the claimed compound identity: likely direct infringement exposure under claims 1/2.
• If generic API matches as a salt: likely still within “pharmaceutically acceptable salt” language.
• If generic is formulated with typical excipients: likely still within claim 3.

Potential workarounds

• A structurally different analog outside the claim-defined substituents.
• A stereochemical approach only if it escapes the “compound of formula” interpretation and avoids both enantiomer claims.
• Non-infringing composition by using a non-claimed API member, not merely formulation changes.

How does US 8,012,976 compare with typical small-molecule patent claim patterns?

Direct answer: It follows a “compound + composition + stereochemical embodiments” architecture, which tends to be enforceable against both API manufacturers and downstream formulation sellers.

What is distinctive here: enantiomer partitioning

Many patents stop at a genus compound claim. Here, the explicit (8R,9S) and (8S,9R) coverage signals that stereochemistry is not incidental. That reduces the odds that a competitor can avoid coverage simply by changing chirality.

What Orange Book status and FDA exclusivity issues determine practical enforcement?

Direct answer: This analysis cannot be completed without the FDA Orange Book listing, listed patents, and the associated drug product. No reliable mapping can be produced from US 8,012,976 claims alone.

What patent litigation affects US 8,012,976 enforcement?

Direct answer: This analysis cannot be completed without docket-level information identifying which parties litigated US 8,012,976 and what constructions/validity rulings apply. The claim text alone is insufficient to determine litigation effects.

What formulations are protected by US 8,012,976 claim 3?

Direct answer: Any formulation with the claimed compound (or salt) and pharmaceutically acceptable diluent/excipient/carrier, regardless of dosage form, as long as the API identity remains within the claim.

Dosage forms that typically fall in-range

• tablets (including film-coated tablets)
• capsules
• granules
• powders
• oral suspensions and solutions
• injectable formulations using pharmaceutically acceptable carriers

Only an API non-infringing change can remove coverage; formulation excipient swaps rarely do it for a claim drafted at this level of generality.

Key Takeaways

• US 8,012,976’s protection is centered on a single, precisely specified small-molecule structure defined by the pyrido[4,3,2-de]phthalazin-3(7H)-one scaffold with fixed substituents (5-fluoro, 8-(4-fluorophenyl), 9-(1-methyl-1H-1,2,4-triazol-5-yl)).
• The patent expands coverage to pharmaceutically acceptable salts of that structure.
• Claim 3 covers pharmaceutical compositions containing that API plus any pharmaceutically acceptable carrier, creating broad formulation infringement exposure for generic formulators.
• Claims 4 and 5 add stereochemical enforcement hooks for (8R,9S) and (8S,9R), limiting stereochemistry-based design-around.
• The most reliable non-infringing route is structural redesign of the API, not formulation or salt changes.

FAQs

1. Can a generic avoid US 8,012,976 infringement by using a different salt form of the same compound?
   If the alternative salt is “pharmaceutically acceptable” and the API matches the claimed compound identity, salt-only changes typically do not avoid infringement.

2. Does US 8,012,976 allow a design-around by switching from the (8R,9S) to the (8S,9R) enantiomer?
   Claim 4 and claim 5 separately cover the two enantiomers; switching may avoid only one if the independent “compound of formula” claim is stereochemically limited.

3. Are method-of-use or dosing regimens protected by US 8,012,976 based on the provided claims?
   No method-of-use or dosing elements are present in the listed claim set excerpted here.

4. Would changing excipients or converting to a different dosage form avoid claim 3 infringement?
   No, claim 3 broadly covers compositions with pharmaceutically acceptable excipients, so the API identity is the gating factor.

5. Is stereochemistry covered only through claims 4 and 5, or also in claim 1?
   It depends on how stereochemistry is encoded in the “formula” underlying claim 1; the presence of enantiomer-specific claims suggests stereochemistry is material, but the final scope is tied to the formula language.

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References

1. US Patent 8,012,976 (claim set as provided).

Drugs Protected by US Patent 8,012,976

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Pfizer	TALZENNA	talazoparib tosylate	CAPSULE;ORAL	211651-005	Jun 20, 2023		DISCN	Yes	No	8,012,976		Y	Y
Pfizer	TALZENNA	talazoparib tosylate	CAPSULE;ORAL	217439-001	Mar 7, 2024		RX	Yes	No	8,012,976		Y	Y
Pfizer	TALZENNA	talazoparib tosylate	CAPSULE;ORAL	211651-001	Oct 16, 2018		DISCN	Yes	No	8,012,976		Y	Y
Pfizer	TALZENNA	talazoparib tosylate	CAPSULE;ORAL	217439-002	Mar 7, 2024		RX	Yes	No	8,012,976		Y	Y
Pfizer	TALZENNA	talazoparib tosylate	CAPSULE;ORAL	211651-006	Jun 20, 2023		DISCN	Yes	No	8,012,976		Y	Y
Pfizer	TALZENNA	talazoparib tosylate	CAPSULE;ORAL	217439-003	Mar 7, 2024		RX	Yes	No	8,012,976		Y	Y
Pfizer	TALZENNA	talazoparib tosylate	CAPSULE;ORAL	211651-003	Sep 20, 2021		DISCN	Yes	No	8,012,976		Y	Y

International Family Members for US Patent 8,012,976

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	2767537		CA 2019 00055	Denmark
European Patent Office	2767537		301021	Netherlands
European Patent Office	2767537		PA2019522	Lithuania
European Patent Office	2767537		LUC00140	Luxembourg
European Patent Office	2767537		2019C/551	Belgium
European Patent Office	2767537		122019000108	Germany
European Patent Office	2767537		1990055-4	Sweden