Details for Patent: 4,695,590

Summary for Patent: 4,695,590

Title:	Method for retarding aging
Abstract:	Methods and compositions are provided for retarding aging, i.e., inhibiting damage to human cells caused by toxic byproducts of oxygen metabolism. The anti-aging active ingredient is a compound or mixture of compounds represented by the following structural formula: (1) wherein m is 0, 1 or 2; n is 0 or 1; R1 is hydrogen, halogen or hydroxy; and R2 and R3 each independently represent hydrogen or methyl provided that when m is 0, n is 0 and when m is 1 or 2, n is 1 and R1 is hydroxy or halogen and that when m is 2, each R2 can be the same or different and each R3 can be the same or different or a pharmaceutically acceptable alkali or alkaline earth metal salt thereof.
Inventor(s):	Richard D. Lippman
Assignee:	UCB Inc
Application Number:	US06/859,464
Patent Claim Types: see list of patent claims	Use; Composition; Delivery; Dosage form;

Scope and Claim Coverage of US Patent 4,695,590 (Method and Compositions for Retarding Aging)
US 4,695,590 is a composition-and-method-of-use patent that claims daily-dosage ranges and specific embodiment molecules defined by a tight structural genus (m, n, R1, R2, R3 constraints) for “retarding aging in humans,” including oral/parental delivery, and topical skin formulations. The independent claims lock the pharmacological activity to an anti-aging/anti-aging retardation effect, and they lock the chemical scope to compounds within the defined structural formula plus pharmaceutically acceptable salts. Downstream risk for generic or alternative-product entrants is highest if they fall inside the claimed genus and dosage/concentration windows and if they target the claimed route-to-result pairing (systemic dosing for aging retardation or topical-only active ingredient for skin aging retardation).

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What is US Patent 4,695,590 and what does it claim?

Featured snippet answer: US 4,695,590 claims (i) a human anti-aging method using a defined chemical genus at a specified daily mg/kg range, (ii) solid systemic dosage compositions containing a specified 20–100 mg of active per solid composition, and (iii) topical skin compositions where the only active ingredient is the defined chemical genus (with sub-range concentrations, including 0.5%–20% w/w for NDGA embodiments).

Claim-set structure: method, systemic composition, and topical composition

From the provided claims text, the patent’s scope is split across three claim families:

1. Method claim (Claim 1)

   • Purpose/indication: “retarding aging in humans”
   • Patient administration: “to a human”
   • Dosing window: daily dosage “from about 0.5 mg per kilogram of body weight to less than about 2 mg per kilogram”
   • Chemical scope: pharmaceutically acceptable composition comprising a compound (or mixture) represented by the structural formula meeting constraints on m, n, R1, R2, R3, plus salts.

2. Dependent method embodiment claims (Claims 2–5)

   • Specific actives:
     • Claim 2: nordihydroguairetic acid (as written in your excerpt; commonly NDGA in industry shorthand)
     • Claim 3: bis(p-hydroxyphenyl)methane
   • Route:
     • Claim 4: oral
     • Claim 5: parenteral/skin-contact via “intravenously, subcutaneously, intramuscularly and intracutaneously”

3. Systemic composition claims (Claims 6–8)

   • Dosage form: “solid dosage form”
   • Active: essentially the defined compound(s) as the active ingredient
   • Dose per solid: “from about 20 mg to 100 mg of said active ingredient is present in the composition”
   • Dependent embodiments: Claim 7 (NDGA) and Claim 8 (bis(p-hydroxyphenyl)methane).

4. Topical skin composition claims (Claims 9–16)

   • Topical carrier: “topical pharmaceutically acceptable carrier”
   • Active ingredient requirement: “the only active ingredient” in Claim 9
   • Concentration constraint: Claims 12, 13, 16 include “about 0.5% to about 20% by weight” for NDGA or the genus.
   • Dependent embodiments: Claim 10 (NDGA) and Claim 11 (bis(p-hydroxyphenyl)methane).

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What is the chemical genus covered by US 4,695,590 (structural formula scope)?

Featured snippet answer: The active ingredient scope is a structural genus defined by parameters m (0–2), n (0–1), R1 (H/halogen/hydroxy), and R2/R3 (H/methyl) with conditional restrictions that sharply define the allowed combinations. The claim covers the compound(s) meeting those structural conditions and also pharmaceutically acceptable alkali/alkaline earth salts.

Parameter constraints (as provided) and how they narrow coverage

Claims define the genus with these rules:

• m is 0, 1, or 2
• n is 0 or 1
• R1 is hydrogen, halogen, or hydroxy
• R2 and R3 each independently is hydrogen or methyl
• Conditional restrictions:
  1. If m = 0, then n = 0
  2. If m = 1 or 2, then n = 1, and R1 is hydroxy or halogen
  3. If m = 2, then each R2 can be the same or different and each R3 can be the same or different (still restricted to H or methyl).

Practical impact: While the language is generically written, the conditional relationships eliminate large portions of theoretical substitution. Infringement for “other” bisphenyl/methane-like scaffolds depends on mapping them into the same structural pattern and substitution constraints.

Salt coverage

The claims explicitly include:

• “pharmaceutically acceptable alkali or alkaline earth metal salt thereof” (for the genus conditions when the structural template is met).
  This matters because many NDGA analogs are sold as salts or can be formulated as salts to alter solubility.

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Which compounds specifically fall within the independent claim genus?

Featured snippet answer: Claim 2 and Claim 3 identify two specific embodiments inside the broader structural template: nordihydroguairetic acid and bis(p-hydroxyphenyl)methane. Claims 7–8 and 10–11 repeat those embodiments in systemic and topical compositions.

Enumerated embodiments in dependent claims

• Nordihydroguairetic acid
  • Appears in Claims 2, 7, 10, 14, and in topical concentration-dependent Claims 12 and 16.
• Bis(p-hydroxyphenyl)methane
  • Appears in Claims 3, 8, 11, and 15.

What this implies for “design-around”

Because the patent explicitly names at least two embodiments, litigation risk concentrates not only on strict chemical-genus mapping but also on whether competitors choose structural variants that still satisfy the genus constraints. If a product uses either named embodiment, the remaining design-around path is mainly:

• avoid the genus constraints entirely (structural non-inclusion), and/or
• avoid the claimed dosing/concentration/range, and/or
• avoid the claimed route-to-purpose combination.

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What dosage and administration limits define infringement risk for systemic use?

Featured snippet answer: For the method claim, the defining boundary is daily 0.5 mg/kg (about) to less than 2 mg/kg (about) for human anti-aging retardation, and the method must involve the genus compound(s). For systemic solid dosage compositions, the defining boundary is 20–100 mg active per solid dosage form.

Method claim dosage window (Claim 1)

• Daily dosage range: from about 0.5 mg/kg to less than about 2 mg/kg
• Route is not limited in Claim 1, only in dependent claims (oral and several injection routes).

Infringement trigger mechanics: If a competitor’s clinical dosing is inside that mg/kg window and uses the claimed genus, the route may still matter for infringement depending on the claim pursued (Claim 1 is route-agnostic; dependent claims constrain route).

Solid dosage form limit (Claim 6)

• “solid dosage form for retarding aging in humans”
• active “essentially” the genus compounds
• 20 mg to 100 mg active present in the composition

Implication: A competitor can avoid Claim 6 by formulating below 20 mg or above 100 mg per unit, but that can create clinical translation challenges (dose practicality and mg/kg alignment).

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What topical requirements narrow the composition scope for skin products?

Featured snippet answer: The patent’s topical claims include a strict “only active ingredient” limitation (Claim 9) plus explicit concentration windows for at least the NDGA embodiment (0.5% to 20% w/w, Claims 12 and 16) and for the genus in general (Claim 13).

“Only active ingredient” requirement (Claim 9)

Claim 9 recites a topical composition where the genus compound(s) is:

• “the only active ingredient in a topical pharmaceutically acceptable carrier”

Design-around pathway: A topical product that includes the genus compound plus other actives (even if clinically adjacent) may fall outside the “only active ingredient” limitation, depending on how “only” is interpreted in claim construction and whether the additional ingredient is considered an active versus an excipient.

Concentration window (Claims 12, 13, 16)

• Claim 12 (NDGA): 0.5% to 20% by weight
• Claim 13 (genus): same concentration window, using the structural formula as active ingredient
• Claim 16 (NDGA topical): 0.5% to 20% by weight

Implication: Concentration outside the window is a primary commercial and formulation steering lever for topical competitors, though it can conflict with target performance.

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How broad are “essentially,” “comprising,” and the “mixture of compounds” language?

Featured snippet answer: “Comprising” in Claim 1 and “consisting essentially of” in Claim 6 and “consisting essentially of” in the topical composition claims jointly broaden infringement for mixtures but narrow it for systemic and topical compositions by excluding certain non-essential components.

Claim-text effect (high-level, for enforcement posture)

• Claim 1 uses “pharmaceutically acceptable composition comprising”
  This signals open-ended inclusion of additional formulation components, as long as the claimed active genus is present at the claimed dose window.
• Claim 6 uses “consisting essentially of”
  This usually allows non-essential components (carriers/excipients) but can reduce arguments that a materially different active is present.
• Topical Claim 9 uses “consisting essentially of” with “only active ingredient”
  The “only active ingredient” requirement is the sharper boundary.

Business consequence: Competitors must evaluate not only chemical identity and concentration/dose, but also whether additional actives could be characterized as “active” and whether the composition could be argued as materially different from the “consisting essentially of” limitation.

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What is the likely scope of the method claim versus product claims?

Featured snippet answer: Even if a competitor avoids the solid dosage unit strength window (Claim 6) or topical concentration window (Claims 9/13), they may still trigger infringement exposure under the method claim (Claim 1) if their administered daily mg/kg dose and the administered compound fit the genus and purpose (“retarding aging in humans”).

Claim pathway mapping for enforcement

• Systemic therapy:
  • Method exposure: Claim 1 (mg/kg window; genus; humans; “retarding aging”)
  • Composition exposure: Claim 6 (solid unit strength 20–100 mg; essentially genus active)
• Topical therapy:
  • Composition exposure: Claim 9 and 13 (only active + concentration window; genus; topical carrier)

Route-limited dependent claims

If a competitor pursues a route different from the dependent claim routes, Claim 1 may still apply if route-agnostic. If the dispute centers on dependent claims, route becomes material.

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What patent landscape questions does US 4,695,590 raise for generics, follow-on molecules, and formulation entrants?

Featured snippet answer: The enforceability posture hinges on whether competitors can (i) exit the genus structural template, (ii) exit the systemic mg/kg window or solid unit strength window, (iii) exit topical “only active ingredient” and w/w range, and (iv) avoid the claimed anti-aging purpose framing in labeling and marketing.

Because this patent is built on a “method for retarding aging,” enforcement is likely tied to how products are prescribed and represented, not just chemical presence.

Generic entry risks for structurally identical actives

If a generic includes NDGA (as defined) or bis(p-hydroxyphenyl)methane and:

• uses dosing within 0.5–<2 mg/kg daily for anti-aging indication, and
• uses a solid unit with 20–100 mg active per dose form (if Claim 6 is asserted), then the risk of direct infringement exposure is elevated.

Formulation and delivery system risk

• Solid dosage forms with unit strengths in the 20–100 mg range increase Claim 6 exposure.
• Topical formulations at 0.5%–20% w/w that use the genus compound as the only active increase Claim 9/13 exposure.

“Next-gen” chemical modifications

To reduce genus inclusion risk, follow-on molecules must fall outside the structural parameter constraints (m, n, R1, R2/R3 conditional rules). Minor substitution may still fall inside the genus if the substituted scaffold matches the allowed parameter ranges.

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What do the claims suggest about litigation targets and settlement leverage?

Featured snippet answer: The tight numeric windows (mg/kg daily range, 20–100 mg per solid dosage form, 0.5%–20% w/w topical) create relatively clean infringement “in or out” positions for accused products, and the “only active ingredient” topical limitation creates a strong negotiating lever around combination products and labeling.

Likely contested elements

Across cases, disputes usually converge on:

• structural identity mapping to the genus formula
• dosing calculations (mg/kg and “about” interpretation)
• unit dose strength (for solid dosage)
• topical concentration and percent-by-weight determination
• whether other actives are present (topical “only active ingredient”)

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Key Takeaways

• US 4,695,590 claims anti-aging retardation methods and compositions built around a defined structural genus plus salts, with numeric systemic daily mg/kg limits, solid unit strength limits (20–100 mg), and topical concentration limits (0.5%–20% w/w).
• The patent contains explicit dependent embodiments for nordihydroguairetic acid and bis(p-hydroxyphenyl)methane, concentrating infringement risk for products using these actives within the specified dosing/formulation constraints.
• Topical scope is constrained by a strict “only active ingredient” requirement, making combination formulations a core design-around strategy.
• For systemic therapies, the method claim can remain a threat even if composition unit strengths are changed, because Claim 1 is defined around the administered daily mg/kg range.

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FAQs

1) Does US 4,695,590 require a specific route for systemic aging retardation?
Claim 1 is not limited by route; dependent claims add route limits (oral and certain injection routes).

2) What dosing range is claimed for retarding aging in humans under Claim 1?
About 0.5 mg/kg/day up to less than about 2 mg/kg/day.

3) What solid dosage unit strength is claimed for the systemic composition?
About 20 mg to 100 mg active per solid dosage form.

4) Can a topical product with additional actives avoid the topical claims?
Claim 9 requires the genus compound(s) as “the only active ingredient,” so adding other active ingredients risks falling outside the claim.

5) Are salts of the claimed genus covered?
Yes, the claims include pharmaceutically acceptable alkali or alkaline earth metal salts of the genus.

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References

1. United States Patent 4,695,590 (claims excerpt provided by user).

Drugs Protected by US Patent 4,695,590

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

International Family Members for US Patent 4,695,590

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Austria	87473
Australia	645771
Australia	6930591