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Patent landscape, scope, and claims: |
Executive summary: U.S. Patent 7,645,460 claims a compact oral fixed-dose combination of risedronate (free acid, salts, or esters; in practice risedronate sodium) plus EDTA (including disodium EDTA) delivered via a delayed-release/enteric mechanism designed to release in the small intestine, with explicit weight and dose-range limitations. The estate, based on claim scope alone, is structured to (1) cover multiple EDTA salts and broad bisphosphonate selection but narrows critical commercially relevant coverage around risedronate + disodium EDTA and specific enteric disintegration pH windows and methacrylic acid copolymer coatings. The independent claim set is composition and method-of-use, so enforcement and validity risk tend to track whether competitors can design around (i) the EDTA amount and salt identity, (ii) total unit weight ≤ 1 gram, and (iii) release mechanism and enteric pH/coating chemistry while still demonstrating bioequivalence.
United States Patent 7,645,460: What is claimed for oral risedronate + EDTA delayed-release tablets/capsules?
Core answer (scope in plain terms): Claim 1 covers an oral dosage form comprising a bisphosphonate selected from risedronate and acids, salts, and esters, a specified EDTA dose, and a delayed-release mechanism intended to release immediately in the small intestine, constrained to a total composition weight ≤ 1 gram. Dependent claims specify disodium EDTA, pH-triggered vs time-dependent delayed release, and enteric coating performance (disintegration pH 5.5 to 6.5) and enteric coating chemistry (methacrylic acid copolymer). Separate method claims cover osteoporosis and other listed bone disorders, with regimen and food-effect options.
What does claim 1 legally require?
Claim 1 elements (all must be met for literal infringement):
- Oral dosage form with “pharmaceutically effective absorption.”
- Bisphosphonate payload: ~1 mg to ~250 mg of a bisphosphonate “selected from the group consisting of risedronate and acids, salts, and esters thereof.”
- EDTA payload: ~10 mg to ~500 mg of EDTA (no salt limitation in claim 1).
- Delayed release mechanism: delays such that the system releases the risedronate and the EDTA in the small intestine.
- Total unit weight limit: “composition weighs no greater than 1 gram.”
High-impact claim construction points:
- The bisphosphonate definition is broad at the genus level (“risedronate and acids, salts, and esters”) but still anchored to risedronate. That tends to exclude other bisphosphonates unless they fall inside “risedronate … salts and esters.”
- “Delayed release mechanism” is defined functionally by the location/timing of release (small intestine) and, in dependent claims, by the mechanism type (pH or time).
- The “no greater than 1 gram” unit-weight limitation can be a practical design-around lever, especially for multi-part systems (layered cores, large enteric overcoats, high-excipient loads).
What are the key dependent-claim narrowing gates?
Dependent claims 2–7 and 18–26 lock in narrower parameter combinations:
- Claim 2: EDTA is disodium EDTA.
- Claim 3: delayed release mechanism is pH triggered, time dependent, or mixtures.
- Claim 4: delayed release mechanism is pH triggered.
- Claim 5: pH triggered uses an enteric coating.
- Claim 6: the enteric coating disintegrates between pH ~5.5 and pH ~6.5.
- Claims 7 and 19 and 25 and 26: specify EDTA amount (with disodium EDTA in those claims) and often tie to risedronate content and enteric chemistry in later dependents.
- Claims 18, 20, 24, 26: enteric coating is methacrylic acid copolymer.
These create a “ladder” from broad (claim 1) to highly specific (pH window and coating polymer).
What formulations are covered by 7,645,460: enteric coating, pH-triggered release, and methacrylic acid copolymer?
Core answer: The patent’s formulation coverage centers on enteric coated oral dosage forms that prevent release in stomach conditions and enable release in the small intestine, with optional time-based delay. The enteric coating is explicitly tied to a pH disintegration range (5.5 to 6.5) and in later dependents to methacrylic acid copolymers.
pH-triggered vs time-dependent: what changes for design-around?
- If a competitor uses time-dependent delayed release (bypassing pH-triggering), it may avoid dependent claims 3/4/5/6 (depending on claim interpretation), but the independent claim 1 still requires “delayed release mechanism” to release in the small intestine. So time-dependent systems can still fall into claim 1 if they meet the functional release-location requirement.
- Avoiding the enteric coating specifically is more relevant to dependent claims 5 and 6.
Enteric disintegration pH 5.5–6.5: a clean infringement/avoidance line
- Dependent claim 6 adds a measurable performance requirement: coating disintegrates between pH 5.5 to 6.5.
- A design that shifts disintegration outside this band can weaken coverage for claim 6. The independent claim 1 does not require the pH band, so this is a dependent-claim gate rather than a complete escape from the core estate.
Methacrylic acid copolymer enteric coating: chemistry constraint
- Dependent claims (notably 18/20/24/26) require the enteric coating to be a methacrylic acid copolymer.
- Competitors using alternative enteric polymers (e.g., cellulose acetate phthalate, HPMCAS, shellac blends, acrylic resins outside the methacrylic acid copolymer class) can try to avoid those dependent claims, but again claim 1 can still capture the formulation if the broader delayed-release requirement is met.
How many risedronate + EDTA dose ranges are claimed in 7,645,460, and where do they overlap with likely products?
Core answer: The claims define multiple overlapping windows for risedronate and disodium EDTA in different claim sets, plus a broad EDTA range in claim 1.
Dose-range map (from provided claims)
| Claim |
Risedronate |
EDTA form |
EDTA dose range |
Release system language |
| 1 |
1–250 mg (risedronate + salts/esters) |
EDTA (unspecified salt) |
10–500 mg |
Delayed release to release in small intestine; unit ≤ 1 g |
| 8 |
“1–250 mg risedronate sodium” |
disodium EDTA |
25–500 mg |
“enteric coating which provides for immediate release … in the small intestine” |
| 9 |
35–50 mg risedronate |
(from claim 8) |
(from claim 8) |
(enteric coating from claim 8) |
| 7 |
(from claim 1) |
disodium EDTA |
75–250 mg |
delayed release from claim 1 |
| 15 |
15–55 mg risedronate sodium |
(from claim 8/14) |
(ranges below) |
enteric coating |
| 16 |
(from claim 15) |
disodium EDTA |
75–250 mg |
enteric coating |
| 17 |
about 35 mg risedronate |
(from claim 16) |
(from claim 16) |
(enteric coating from claim 16) |
| 18 |
(from claim 17) |
disodium EDTA |
about 100 mg |
enteric coating is methacrylic acid copolymer |
| 19 |
(from claim 17) |
disodium EDTA |
about 100 mg |
enteric coating methacrylic acid copolymer |
| 25 |
about 75–250? (depends) |
disodium EDTA |
(from claim 23/24) |
methacrylic acid copolymer in later dependents |
| 21 |
50–280 mg risedronate sodium |
disodium EDTA |
75–250 mg |
enteric coating |
| 23 |
150 mg risedronate |
about 100 mg EDTA |
(from claim 22/23) |
methacrylic acid copolymer dependents (24/26) |
Practical implication: Claim 1 is the broad “any EDTA salt” anchor; claim 8 is the “risedronate sodium + disodium EDTA” anchor; additional dependents then carve out specific dose bands (including fairly narrow “about 35 mg” and “about 100 mg EDTA” combinations) and specific enteric coating properties.
What method-of-use claims exist in 7,645,460: osteoporosis regimens, continuous schedules, and with/without food?
Core answer: The patent includes administration-to-a-mammal methods for a disease list (including osteoporosis) and then tightens osteoporosis regimens with dosing interval options and a food-effect option.
Method claim set and key parameters
- Claim 10: method for treating:
- osteoporosis
- Paget’s disease
- hyperparathyroidism
- hypercalcemia of malignancy
- osteolytic bone metastasis
- combinations
using the oral dosage form of claim 1.
- Claim 11: osteoporosis.
- Claim 12: continuous schedule with dosing interval selected from:
- daily
- weekly
- three times per month
- twice monthly
- once monthly
- Claim 13: weekly administration.
- Claim 14: administered with or without food.
- Claims 27–30: osteoporosis-specific methods using oral dosage forms of claims 17 and 25, including with/without food.
Enforcement note based on claim language: These method claims are tethered to very specific dosage-form claim numbers (claim 1 for claim 10; claim 17 or 25 for later osteoporosis methods). That means a competitor can avoid method-of-use coverage by designing a product that does not satisfy the associated dosage-form limitations, even if the underlying therapeutic use is the same.
When does 7,645,460 lose exclusivity or patent protection in the US?
No complete answer possible from the provided information. Patent term and exclusivity depend on the patent’s filing date, issuance date, patent adjustments, maintenance status, and any terminal disclaimers or family continuation. The prompt supplies the patent number but not the filing/priority data, issuance date, PTA, or current legal status.
What Orange Book status would 7,645,460 have for risedronate + EDTA products?
No complete answer possible from the provided information. Orange Book listings require the specific FDA-approved product(s), NDA/ANDA/BLA, and listed patents with associated claim types. The prompt provides only the patent claim text.
Which companies are likely covered or at risk under 7,645,460: risedronate and EDTA oral products?
No complete answer possible from the provided information. A credible “who is challenging whom” map requires (i) Orange Book patent listings tied to specific ANDAs, (ii) Paragraph IV filings, (iii) district court dockets, and (iv) FDA approvals. The prompt does not include those identifiers.
How strong is the patent estate for oral risedronate + EDTA: claim breadth vs obviousness/design-around levers?
Core answer: The estate is strongest where competitors must meet all of: risedronate-based bisphosphonate + EDTA (especially disodium EDTA) + delayed/enteric small-intestine release + compact unit weight (≤1 gram in claim 1) and, for narrower dependents, the pH disintegration window and methacrylic acid copolymer enteric polymer.
Breadth points
- EDTA not limited to disodium in claim 1 (broader than dependent claim 2/7).
- Delayed-release mechanism is functionally defined in claim 1 (can include multiple technologies as long as the functional release target is met).
- Risedronate payload broad range (1–250 mg in claim 1).
Vulnerability/design-around points
- Salt/form requirements for dependent claims (disodium EDTA in claims 2 and 8 and later).
- Enteric performance requirement (pH 5.5–6.5) for claim 6.
- Polymer identity requirement (methacrylic acid copolymer) for multiple later dependents.
- Unit weight limit (≤1 gram) in claim 1 can be avoided by formulation architecture that necessarily exceeds that weight, though that may trade off bioavailability.
What patent litigation risks exist for 7,645,460 (Paragraph IV, IPR, district court)?
No complete answer possible from the provided information. Litigation risk requires PACER/docket data, PTAB outcomes, FDA 5-year/30-month timing tied to ANDA Paragraph IV, and settlement agreement terms.
How does 7,645,460 compare with typical risedronate enteric-delayed formulations without EDTA?
Core answer: The decisive differentiator is the combination of risedronate + EDTA within the specified dosing and release architecture. Risedronate products that use only enteric protection for risedronate (without EDTA in the same unit and meeting the specified EDTA dose range) would not meet the claimed “EDTA” limitations.
Likely carve-outs by competing formulations
- Replacing EDTA with a different chelator, carrier, or excipient: may avoid the “EDTA” element.
- Keeping EDTA but changing salt form or dose outside claimed bands: could avoid certain dependent claims; claim 1 may still capture if EDTA dose remains within 10–500 mg and other elements match.
- Altering release mechanism to avoid enteric coating: can weaken dependent claims 5/6/18/20/24/26 but not claim 1 if small-intestine release is still achieved via delayed-release.
Key Takeaways
- U.S. Patent 7,645,460 is built around an oral risedronate + EDTA combination with delayed/enteric release to the small intestine, including a unit weight ≤ 1 gram in claim 1.
- The strongest “coverage concentration” is risedronate sodium + disodium EDTA with enteric performance defined by pH 5.5–6.5 and later restricted to methacrylic acid copolymer coatings.
- Method-of-use coverage for osteoporosis and related diseases is tethered to the claimed dosage forms; avoiding dosage-form limitations is the primary way to reduce enforcement exposure.
- The largest practical design-around levers implied by the claims are EDTA salt/dose, enteric pH window, enteric polymer type, and unit weight.
FAQs
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Can a time-dependent delayed-release risedronate + EDTA product infringe claim 1 even without an enteric coating?
Claim 1 requires delayed-release to release in the small intestine, not an enteric coating per se.
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Does claim 6 require both risedronate and EDTA to disintegrate at the pH window or only the coating?
The claim is directed to the enteric coating disintegration behavior; release of both actives in the small intestine remains part of the claimed system.
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Are risedronate esters included in the independent claim scope, or only risedronate sodium?
Claim 1 includes risedronate plus “acids, salts, and esters,” while separate claims explicitly reference risedronate sodium.
-
How do the osteoporosis regimen claims limit dosing intervals?
They specify a continuous schedule selected from daily, weekly, three times per month, twice monthly, and once monthly, with dependent claims including weekly.
-
What is the most straightforward dependent-claim design-around among the provided limitations?
Changing the enteric coating polymer away from methacrylic acid copolymer and/or shifting coating disintegration outside pH 5.5–6.5 targets claims 6 and 18/20/24/26.
References
- United States Patent No. 7,645,460 (claims as provided).
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