Details for Patent: 5,854,259

Summary for Patent: 5,854,259

Title:	Quinoline type mevalonolactones
Abstract:	Described herein are mevalonolactone derivatives having a quinoline ring of formula (I) (I) wherein the R1, R2, R3, R4, R5, Y and Z variables are described therein.
Inventor(s):	Yoshihiro Fujikawa, Mikio Suzuki, Hiroshi Iwasaki, Mitsuaki Sakashita, Masaki Kitahara
Assignee:	Nissan Chemical Corp
Application Number:	US07/978,884
Patent Claim Types: see list of patent claims	Use; Composition; Compound;

US Patent 5,854,259 Scope, Claims, and US Patent Landscape for Calcium Salt Pharmaceutical Compositions Targeting Hyperlipidemia, Hyperlipoproteinemia, and Atherosclerosis

US 5,854,259 is a formulation-type composition patent that claims pharmaceutical compositions containing a specific stereochemically defined active agent: “a compound of the formula” with Z set to –CH(OH)–CH2–CH(OH)–CH2–COO and defined as “1/2 Ca” in a pharmaceutically effective amount, combined with a pharmacologically acceptable carrier. Claim coverage is anchored to (i) the chemical identity of the active agent (by formula and Ca stoichiometry) and (ii) the therapeutic purpose labeling (hyperlipidemia/hyperlipoproteinemia/atherosclerosis) rather than to a specific route of administration or excipient system.

Core conclusion: The enforceable scope is limited to compositions that include the claimed calcium salt active agent defined by the formula element Z and “1/2 Ca,” for lipid disorders and/or atherosclerosis, in a conventional pharmaceutical carrier. Design-around risk is driven primarily by whether a competitor’s active agent is a non-infringing variant of the claimed compound, and secondarily by whether the competitor’s product is “pharmaceutically effective” for the claimed indications.

---

What does US 5,854,259 claim and what is its active agent definition?

Featured snippet answer: US 5,854,259 claims pharmaceutical compositions comprising a calcium salt active agent defined by a specific formula element Z = –CH(OH)–CH2–CH(OH)–CH2–COO with “1/2 Ca,” plus a pharmaceutically acceptable carrier, for treatment or control of hyperlipidemia, hyperlipoproteinemia, and atherosclerosis.

Claim 1: composition, active agent identity, and therapeutic purpose

Claim 1 is the only independent claim described in the prompt. It has three essential limitations:

1. Pharmaceutical composition
   “A pharmaceutical composition for the control or treatment of” one or more of:

   • hyperlipidemia
   • hyperlipoproteinemia
   • atherosclerosis

2. Active agent with formula constraint
   “comprising an active agent which consists of a compound of the formula,” with:

   • Z = –CH(OH)–CH2–CH(OH)–CH2–COO
   • “1/2 Ca” in a pharmaceutically effective amount

3. Pharmacologically acceptable carrier The active agent is administered with “a pharmacologically acceptable carrier.”

Interpretation-level scope points that matter for infringement

• “active agent which consists of” tends to be interpreted as excluding additional active agents in the same composition claim, absent allowance under doctrine of equivalents (jurisdiction dependent). If a competitor uses the claimed calcium salt plus another lipid-active drug in the same dosage form, infringement analysis turns on whether the added component is considered part of the “active agent” and whether it changes the “consists of” boundary.
• The formula restriction is the main technical gate. If the competitor’s chemistry changes any structural element required by the formula (or the calcium stoichiometry effect implied by “1/2 Ca”), non-infringement arguments are strongest.
• The therapeutic purpose is likely treated as a functional limitation. If a product is not actually intended and effectively used for those conditions, the “for treatment or control” language can become a factual issue in US litigation.

Claims 2–4: narrowing by indication only

Claims 2–4 are dependent claims that do not add new chemistry or new formulation features; they just specify the therapeutic framing:

• Claim 2: “agent is an anti-hyperlipidemia agent”
• Claim 3: “agent is an anti-hyperlipoproteinemia agent”
• Claim 4: “agent is an anti-atherosclerosis agent”

These dependent claims mainly support the same core chemical infringement theory but help with enforcement by aligning product marketing and medical use with one of the asserted indications.

---

How broad is the formulation coverage versus the chemical coverage?

Featured snippet answer: US 5,854,259 is broad on “pharmaceutical composition” and carrier use, but narrow on the chemical identity of the active agent because the claims require a specifically defined calcium-containing compound with Z = –CH(OH)–CH2–CH(OH)–CH2–COO and “1/2 Ca.”

What is broad in practice

• The claims do not specify excipient types, dosage forms (tablets, capsules, powders, solutions), or routes (oral vs injectable). That means a wide range of standard formulation vehicles can fall within the carrier language if the active agent is the same claimed calcium salt.
• The claims do not specify a particular manufacturing method.

What is narrow in practice

• The active agent must “consist of” the claimed compound. The “consists of” language limits the ability to add other actives within the same composition.
• The chemical formula element Z and calcium stoichiometry “1/2 Ca” are exacting. Competitors using:
  • a different counterion (Na, K, Mg, etc.)
  • a different calcium salt stoichiometry (e.g., 1 Ca vs 1/2 Ca)
  • a modified carbon skeleton or stereochemistry affecting the two hydroxyl-bearing carbons and the carboxylate chain could avoid infringement.

---

What kinds of non-infringement and design-around strategies follow from the claim language?

Featured snippet answer: The most direct design-around path is to change the claimed active agent identity by altering the calcium salt form or the chemical structure tied to Z = –CH(OH)–CH2–CH(OH)–CH2–COO, while using a pharmaceutically acceptable carrier and keeping the therapeutic purpose distinct if needed.

1) Active agent substitution: calcium form and stoichiometry

Because the claim expressly uses “1/2 Ca,” a competitor can focus on salt form:

• different calcium stoichiometry
• polymorphs are less useful unless polymorph affects chemical identity
• different hydration state is only relevant if it changes the stoichiometry recognized as “1/2 Ca” under claim construction

2) Chemical structure modifications around Z

The claim locks in a functional group pattern:

• two alcohol-bearing carbons separated by a methylene chain structure
• terminal carboxylate Any modification that removes or relocates the required hydroxyl-bearing carbon atoms or changes the chain arrangement offers a strong non-infringement basis.

3) Composition “consists of” boundary

If a competitor includes additional lipid-lowering agents in the same dosage form:

• infringement arguments turn on whether the formulation includes additional “active agent” components and whether “consists of” is treated strictly.
• even if a product has a primary claimed agent, the presence of a second active component can be leveraged for a “consists of” non-infringement argument.

4) Therapeutic purpose and labeling

Even if chemical identity matches, a challenger can contest “for control or treatment” if the product is:

• not marketed for the claimed indications
• not prescribed or used for those conditions This is fact-specific but can be decisive in some cases, especially with “for treatment” language.

---

What patents likely surround US 5,854,259 in the US landscape?

Featured snippet answer: The patent landscape around a composition claim tied to a specific calcium salt active agent typically includes (i) upstream patents covering synthesis/intermediates of the calcium salt compound, (ii) formulation patents on carriers/dosage forms, and (iii) downstream patents on methods of treatment for lipid disorders/atherosclerosis using the same active.

This prompt does not include the patent title, inventor/assignee, earliest priority date, or the identity name of the active compound behind the Z and “1/2 Ca” language. Without that, a complete, enumerated “how many US patents” map cannot be produced.

How to structure the likely patent estate (what to search in practice)

• Compound patents: claims to the core compound (the moiety defined by Z) and related salts (including calcium).
• Salt form patents: polymorphs, hydrates, and stoichiometry-specific calcium salts.
• Pharmaceutical composition patents: carrier systems, dosage forms, and oral bioavailability formulations.
• Medical use patents: method-of-treatment claims for hyperlipidemia, hyperlipoproteinemia, or atherosclerosis, including specific dosing regimens.
• Combination patents: if any exist, they would conflict with the “consists of” limitation, but they can still be present as separate claims on different “active agent” definitions.

Key litigation and leverage points

For a composition patent, litigation often turns on:

• chemical identity of accused product (salt form and structure)
• whether the accused composition contains additional actives under “consists of”
• whether labeling and intended use align with claimed indications

---

When does exclusivity end and what generic or biosimilar risks exist?

Featured snippet answer: Determining exclusivity end dates requires the patent’s filing date, priority, statutory term, any PTA, and whether continuation family members exist. This information is not provided, so precise launch risk timing cannot be stated from the supplied claim text.

What can be inferred from the claim type

• Because the claims are composition claims (not biologics), the competitor risk is “small-molecule generic” style: a generic that contains the same calcium salt active agent and same carrier conceptually risks infringement.
• If the active agent is specific and tightly defined, generic risk depends on whether the generic can lawfully practice the same compound identity (including salt stoichiometry) without infringing.

Patent-expiration timing analysis cannot be completed here

No filing/priority dates, continuation history, maintenance status, or Orange Book listing data is included in the prompt, so a calendar of expiry and exclusivity cannot be produced.

---

What is the Orange Book status of US 5,854,259 and what certifications matter?

Featured snippet answer: Orange Book status and associated FDA certifications require the specific reference listed drug (RLD) and the exact FDA NDC/RLD pairing. The prompt does not provide drug name, RLD, or any Orange Book listing identifiers, so an Orange Book status map cannot be generated.

What matters for Paragraph IV strategy (general)

If the patent is listed to an RLD, the key decisions usually are:

• whether a challenger files a Paragraph IV certification to US 5,854,259
• what exclusivity blocking (if any) applies (market exclusivity vs patent)
• settlement likely depends on the strength of chemical-identity infringement arguments

---

How strong is the patent estate for infringement based on the claim structure?

Featured snippet answer: Strength is anchored to chemical identity. If the asserted active agent in the competitor product matches the claimed formula element Z and calcium stoichiometry “1/2 Ca,” the claims present a direct infringement pathway for any composition using that active with a pharmacologically acceptable carrier for the claimed indications.

Claim strength indicators from the language given

• Direct structural limitation: the formula and Z parameter provide clear boundaries for expert-driven comparison.
• “Consists of”: this can be a strong defense lever against fixed-dose combination products containing other actives.
• Indication-limiting dependent claims: help enforcement by aligning evidence with one or more therapeutic frames.

Weakness indicators from the language given

• If competitors can change either structural features tied to Z or the calcium stoichiometry such that the active agent is not the claimed compound, the composition claim may not cover their product.
• If the competitor contests “for control or treatment” intent/effect, the case can become a labeling and evidence dispute.

---

What patent litigation affects US 5,854,259?

Featured snippet answer: Litigation history cannot be produced from the provided information because no assignee/inventor names, patent title, related case captions, or docket identifiers are supplied.

Litigation questions typically relevant for this claim type

• Does the case turn on infringement of the calcium salt identity?
• Is there a dispute over whether the accused formulation contains additional active agents within the “consists of” boundary?
• Are validity defenses raised, such as anticipation or obviousness based on prior art calcium salts or related Z-structured compounds?

---

What commercial product exposure exists?

Featured snippet answer: Commercial exposure depends on the specific drug product and whether it uses the claimed “1/2 Ca” active agent with Z as given. The prompt does not provide the drug’s identity, dosage form, approval status, or market data. A quantified revenue-at-risk analysis cannot be completed.

---

Key takeaways

• US 5,854,259 is a composition patent covering pharmaceutical compositions for hyperlipidemia/hyperlipoproteinemia/atherosclerosis containing a specific calcium-containing compound defined by Z = –CH(OH)–CH2–CH(OH)–CH2–COO and “1/2 Ca,” plus a pharmacologically acceptable carrier.
• Claims 2–4 add indication framing only and do not appear to add additional formulation or chemical features beyond Claim 1.
• Scope is broad on carrier/formulation but narrow on active agent chemical identity and constrained by “active agent which consists of.”
• Design-around probability is driven by active agent differences: salt form/stoichiometry and structural changes around Z.
• Exclusivity end date, Orange Book status, and litigation history cannot be mapped from the claim text alone.

---

FAQs

1. Can a fixed-dose combination that includes the claimed calcium salt still infringe US 5,854,259?
   Infringement depends on how “active agent which consists of” is construed and whether additional lipid-active components are treated as part of the “active agent” limitation.

2. What specific chemical differences are most likely to avoid infringement?
   Changes to the Z structural element (the hydroxyl-bearing carbon arrangement and terminal carboxylate chain) or alterations to the calcium salt stoichiometry implied by “1/2 Ca.”

3. Does the patent cover any dosage form or only certain routes?
   The provided claims do not limit dosage form or route; coverage depends on whether the composition uses the claimed active agent with a pharmacologically acceptable carrier and is used for the claimed indications.

4. How do labeling and intended use affect enforcement?
   “For control or treatment” can create evidence issues around marketing, prescription practice, and demonstrated or intended therapeutic use for hyperlipidemia/hyperlipoproteinemia/atherosclerosis.

5. What is the main validity risk for a composition claim like this?
   Validity often turns on whether prior art discloses the same calcium salt compound defined by the claim’s formula element and whether formulation/carrier elements were routine.

---

References

(No sources are cited because the prompt provides only the claim text and does not include bibliographic data, title, assignee, priority dates, or any Orange Book or litigation identifiers.)

Drugs Protected by US Patent 5,854,259

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate

Foreign Priority and PCT Information for Patent: 5,854,259

Foriegn Application Priority Data
Foreign Country	Foreign Patent Number	Foreign Patent Date
Japan	62-207224	Aug 20, 1987
Japan	63-15585	Jan 26, 1988
Japan	63-193606	Aug 03, 1988

International Family Members for US Patent 5,854,259

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Austria	114645
Canada	1336714
Germany	3852243
European Patent Office	0304063
Greece	3015186