United States Patent 7,612,058 (US7612058): Scope, Claim Coverage, and U.S. Patent Landscape for Formula (II) Sterol/stanol-Linked Vascular, Diabetes, and Obesity Treatments

US7612058 is a U.S. method-of-use and formulation-anchored patent centered on administering a specific “compound of Formula (II)” in an excipient-defined solid dosage composition. The independent claim set is supported by multiple dependent claims tied to therapeutic indications (atherosclerosis, diabetes, obesity) and a biochemical endpoint (lowering plasma sterol concentration), with an additional “consisting essentially of” claim line that narrows permissible formulation substitutions.

What is the scope of US 7,612,058 (US7612058) and what do claims actually require?

Short answer

The patent claims require (i) a method (treating vascular condition associated with elevated sterol and/or stanol; treating diabetes; treating obesity; or lowering plasma sterol), (ii) administration to a mammal, and (iii) administration of a pharmaceutical composition with excipients in specified weight percentages and containing the specific “Compound of Formula (II)” at 10% by weight, formulated with lactose monohydrate, microcrystalline cellulose, povidone, croscarmellose sodium, sodium lauryl sulfate, and magnesium stearate.

Claim architecture

US7612058’s claim set as provided has two parallel tracks:

“Consisting of” composition track (Claims 1, 3, 4, 5)
- The composition must contain the listed ingredients at the exact weight-percent values.
- Any formulation deviation outside the listed set is outside claim scope.
“Consisting essentially of” composition track (Claims 6, 8, 9, 10)
- The composition must be essentially the same as the defined formulation.
- Under U.S. claim interpretation, “consisting essentially of” allows the formulation to include additional components that do not materially affect basic and novel properties, but the provided text still recites a fixed excipient percentage block including the “10% Compound of Formula (II)” and specified excipients.

Core compositional limitations

For both composition tracks, the following composition is explicitly recited:

Compound of Formula (II): 10 wt%
Lactose monohydrate: 55 wt%
Microcrystalline cellulose: 20 wt%
Povidone: 4 wt%
Croscarmellose sodium: 8 wt%
Sodium lauryl sulfate: 2 wt%
Magnesium stearate: 1 wt%
Total: 100 wt%

This is not a “use any acceptable carrier” claim. It is an excipient-matched, weight-percent-matched, solid formulation template.

Therapeutic/endpoint limitations

The methods then bind that formulation to specific disease or endpoint contexts:

Claim 1: Treat a vascular condition associated with elevated sterol and/or stanol levels.
Claim 2: Vascular condition is atherosclerosis.
Claim 3: Treat diabetes.
Claim 4: Treat obesity.
Claim 5: Lower plasma sterol concentration.
Claims 6-10: Same structure, but compositions are “consisting essentially of” and Claim 7 further specifies atherosclerosis.

Which parts of US7612058 claims create the biggest infringement and validity leverage?

1) The excipient-weight-percentage lock-in

The claims as written are hard-coupled to a fixed excipient blend. For generic or reformulation strategies, this creates a direct infringement design constraint:

A competitor formulation that uses the same “Compound of Formula (II)” but changes excipient types or weight percentages can fall outside the “consisting of” claims (1, 3, 4, 5).
It can still risk infringement of the “consisting essentially of” line (6, 8, 9, 10) if added/changed components are considered to materially affect basic and novel properties.

2) Indication binding

The patent does not appear to claim the compound per se in the provided claim text; it claims methods of use tied to therapeutic indications and biochemical outcomes.

If a product targets sterol lowering but is labeled for a different endpoint/indication, there can be weaker marketing-driven exposure unless courts/experts apply broader theories of use.
If a product is used off-label in the U.S. for those methods, method claims can be harder to enforce against a manufacturer but can still be asserted in appropriate circumstances (facts matter, but the claim text shows direct indication tying).

3) “Elevated sterol and/or stanol” linkage

Claim 1 frames vascular conditions as those “associated with elevated sterol and/or stanol levels.” That can matter for claim construction and medical evidence:

It narrows “vascular condition” beyond generic cardiovascular disease if construed narrowly.
Claim 2 (atherosclerosis) supplies a specific example within the “vascular condition” universe.

How do “consisting of” vs “consisting essentially of” change patent scope in US7612058?

Consisting of (Claims 1, 3, 4, 5)

Requires the pharmaceutical composition to be exactly the combination of ingredients listed, in the recited weight-percent ranges (as provided, fixed).
Inclusion of additional ingredients is outside the literal scope.

Consisting essentially of (Claims 6, 8, 9, 10)

Permits additional components if they do not materially affect basic and novel properties.
Practical exposure risk remains high because the claims still recite the same excipient set and percentages in the claim text provided, which implies the “essential” portion is already defined tightly.

Featured practice implication

From a clearance and design-around perspective, a formulation that deviates from the excipient weights is a more direct strategy against claim 1/3/4/5 than against claim 6/8/9/10, because “consisting essentially of” can tolerate some differences depending on how a tribunal characterizes basic and novel properties.

What patent landscape surrounds US7612058 for sterol/stanol-linked lipid/vascular, diabetes, and obesity therapies?

Landscape posture based on claim form

US7612058 is structured as a combination of a specific active (Formula II compound) plus a specific solid formulation plus methods of use.

That claim format typically sits in the middle layer of IP coverage for a drug program:

Upstream: chemical synthesis/patents covering the compound itself (often earlier filings).
Midstream: formulation patents and solid-dose excipient blends (often co-pending or continuation strategy).
Downstream: method-of-use patents (therapeutic indications and biomarkers/endpoints).

Because your prompt only supplies the US7612058 claim text and not:

the patent’s title, assignee, inventors,
the detailed definition of “Compound of Formula (II),”
the specification’s full description of the compound and dosage units,
the rest of the claim set (if any beyond the ten you pasted), this response cannot enumerate the full U.S. or global family members or map exact citation graphs without risking incorrect patent-number assignments.

What can be concluded from the provided claim text

The landscape relevance vectors are:

Method-of-use coverage breadth
- The same compound/formulation combination is asserted for cardiovascular/vascular (atherosclerosis), diabetes, obesity, and plasma sterol lowering.
- This suggests prior art and competitors likely include cholesterol/sterol lowering agents and sterol absorption/modulation compounds, but the claims are anchored to the specific Formula (II) compound and the excipient-defined solid form.
Formulation/IP barrier
- Competitors attempting a “same API, different excipients” strategy must consider that US7612058 will be asserted against the specific solid composition.
Regulatory strategy exposure
- If the product is developed as a sterol lowering therapeutic, the endpoint claim (Claim 5/10) can broaden assertion beyond indication labeling, depending on how evidence of “lowering plasma sterol concentration” is presented.

How strong is the patent estate likely to be for infringement and validity positions (based on claim drafting alone)?

Strength indicators from the claim language provided

Multiple indications from one formulation scaffold can increase enforceable “use” pathways.
Fixed excipient weights create a crisp infringement matrix for “consisting of” claims.
Method + composition dual tether increases litigation flexibility: plaintiffs can argue both (i) the correct formulation was administered and (ii) the administration aligned with the claimed therapeutic purpose/endpoint.

Likely validity pressure points (claim-type specific)

Even without the chemical identity of Formula (II), the following are predictable validity levers against this kind of claim drafting:

Prior art that teaches treating a vascular condition linked to elevated sterols/stanols, diabetes, obesity, and/or sterol lowering using the same compound class.
Prior art solid formulation disclosures that use the same excipient set and ratios, or obvious variations.
For “consisting essentially of,” arguments around whether substitution materially affects the basic and novel properties.

No further validity mapping is possible from the provided excerpt because claim scope depends on the exact structural and functional definition of “Compound of Formula (II)” in the patent specification.

Key claim-by-claim scope map for US7612058 (from the provided text)

Claim	Method objective	Condition/endpoint	Composition requirement
1	Treat vascular condition	Elevated sterol and/or stanol-associated vascular condition	Composition “consisting of” fixed wt% excipients; Compound of Formula (II) 10 wt%
2	Narrow Claim 1	Atherosclerosis	Inherits Claim 1 composition and administration framework
3	Treat diabetes	Mammal with diabetes	“Consisting of” fixed wt% composition with Formula (II) compound
4	Treat obesity	Mammal with obesity	“Consisting of” fixed wt% composition with Formula (II) compound
5	Lower sterols	Lower plasma sterol concentration	“Consisting of” fixed wt% composition with Formula (II) compound
6	Treat vascular condition	Elevated sterol and/or stanol-associated vascular condition	“Consisting essentially of” fixed wt% composition with Formula (II) compound
7	Narrow Claim 6	Atherosclerosis	Inherits Claim 6 “consisting essentially of” composition framework
8	Treat diabetes	Mammal with diabetes	“Consisting essentially of” fixed wt% composition with Formula (II) compound
9	Treat obesity	Mammal with obesity	“Consisting essentially of” fixed wt% composition with Formula (II) compound
10	Lower sterols	Lower plasma sterol concentration	“Consisting essentially of” fixed wt% composition with Formula (II) compound

What generic entry risks exist for US7612058?

Risk vector A: “Same compound, same excipient ratios”

A generic or follow-on manufacturer that uses the same Formula (II) compound and replicates the excipient composition and ratios would have direct exposure to Claims 1/3/4/5 and potentially 6/8/9/10.

Risk vector B: “Same API, different excipients”

Changing excipient identity or weight percentages can be a design-around candidate:

It likely avoids literal infringement of “consisting of” claims.
It may still trigger “consisting essentially of” claims if differences are argued not to alter basic and novel properties.

Risk vector C: Indication and endpoint proof

Even with labeling constraints, evidence that the product was administered to lower plasma sterols or treat diabetes/obesity/atherosclerosis in a manner consistent with the claims can create enforcement exposure.

What is missing for a complete U.S. patent landscape map (and why the gap matters)?

A complete landscape requires, at minimum:

the assignee and publication history,
patent title and the full “Compound of Formula (II)” definition,
family member identifiers (continuations, divisionals, related filings),
prosecution history and cited references,
and any Orange Book/Aggregated FDA listing link for actual product association.

The provided text contains neither the compound definition nor bibliographic identifiers for US7612058, which prevents accurate mapping to:

direct chemical composition patents,
formulation patents with similar excipient ratios,
related method-of-use continuation families,
or listed FDA products that would enable Paragraph IV/Orange Book enforcement analysis.

Given the instruction to avoid incomplete or incorrect patent-number assertions, this landscape section is limited to what can be derived strictly from claim drafting provided.

Key Takeaways

US7612058 claims are tightly anchored to a specific Formula (II) compound at 10 wt% within a fixed solid excipient blend (lactose monohydrate, microcrystalline cellulose, povidone, croscarmellose sodium, sodium lauryl sulfate, magnesium stearate at recited weights).
Independent methods cover vascular conditions associated with elevated sterol/stanol levels with a dependent atherosclerosis specification, plus diabetes, obesity, and a biochemical endpoint: lowering plasma sterol concentration.
The “consisting of” claims create a more stringent infringement boundary than the “consisting essentially of” claims, but both tracks preserve the same excipient-anchored formulation core as provided.
For competitors, the largest actionable risk lever is replicating (or closely approximating) the excipient ratios and composition language, combined with administration for the claimed indications/endpoints.

FAQs

1) Does US7612058 claim the compound itself or only its administration in a formulation?

Based on the provided claims, US7612058 is directed to methods of treating or methods of lowering plasma sterol concentration through administration of a pharmaceutical composition containing the Compound of Formula (II).

2) What is the primary design-around point for US7612058?

Changing the formulation so it no longer meets the “consisting of” fixed excipient and weight-percent requirements is the most direct approach against Claims 1/3/4/5.

3) Can a formulation that “mostly matches” still infringe US7612058’s “consisting of” claims?

No, because “consisting of” requires the composition to adhere to the specified ingredient set and weights as recited; “mostly matches” typically does not satisfy that limitation.

4) How broad are the vascular-condition claims in US7612058?

The vascular claim is limited to vascular conditions associated with elevated sterol and/or stanol levels, and a dependent claim narrows further to atherosclerosis.

5) Does US7612058 cover sterol lowering independent of a disease diagnosis?

Yes. Claim 5 (and Claim 10 in the “consisting essentially of” track) claims a method of lowering plasma sterol concentration.

References

US Patent 7,612,058 (US7612058). Claims as provided in the prompt.

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Organon	ZETIA	ezetimibe	TABLET;ORAL	021445-001	Oct 25, 2002	AB	RX	Yes	Yes	7,612,058*PED	⤷ 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
Argentina	032403	⤷ Start Trial
Argentina	032643	⤷ Start Trial
Argentina	033855	⤷ Start Trial
Argentina	034204	⤷ Start Trial
Argentina	035611	⤷ Start Trial
Argentina	035739	⤷ Start Trial
>Country	>Patent Number	>Estimated Expiration	>Supplementary Protection Certificate	>SPC Country	>SPC Expiration

Details for Patent: 7,612,058

Which drugs does patent 7,612,058 protect, and when does it expire?

Summary for Patent: 7,612,058