United States Patent 7,572,779: Scope, Claims, and US Patent Landscape for Oral 17β-Estradiol-3-Acetate With Low-Moisture Solid Dosage and Ester-Hydrolysis Inhibitor

US Patent 7,572,779 claims a specific oral hormone therapy method for a human female with a 17β-estradiol deficiency that is defined by (i) the drug form and composition (solid oral unit with low moisture), (ii) the active identity and dose range (17β-estradiol-3-acetate quantified as estradiol equivalent), and (iii) the presence of an ester hydrolysis inhibitor that is acetic acid. The claims are drafted as method-of-treatment claims with composition-defining limitations that function as enforceable infringement gates for oral solid products.

What is the patented invention in US 7,572,779?

The claim set describes a method where a patient receives an oral solid dosage unit comprising:

Active: 17β-estradiol-3-acetate (dose 0.1 to 10 mg as estradiol equivalent)
Moisture constraint: percent moisture ≤ 5%
Carrier: pharmaceutically acceptable carrier
Ester hydrolysis inhibitor: acetic acid
Route/form: orally administering the solid unit
Indication: 17β-estradiol deficiency in a human female

Dependent claims then broaden or narrow implementation by adding optional co-therapy (additional medicaments) and specifying certain co-med categories (progestational activity) and certain dosage forms (tablet, capsule, and other solid/suspension formats).

Claim 1: What specific elements must be present for infringement?

Claim 1 is the independent claim and contains the core enforceable limitations. The claim can be reduced to six operative requirements that collectively define the infringement scope:

1) Patient population and condition

“a human female having a deficiency of 17β-estradiol”

This limits the method to the indicated patient class. If a competing method treats another population or condition not framed as a 17β-estradiol deficiency, it avoids at least part of the claim.

2) Administration route and dosage unit format

“orally administering”
to a “solid dosage unit”

This excludes non-oral routes from literal claim coverage. It also narrows to products that are “solid dosage units,” even though dependent claim 4 enumerates additional possibilities including “suspension,” which is typically not “solid” in conventional taxonomy, but is explicitly listed in the claim.

3) Active ingredient and dosing

Solid unit comprises “therapeutically effective amount of 17β-estradiol-3-acetate”
amount range: “from about 0.1 to about 10 mg as estradiol equivalent”

Key scope features:

The active is explicitly 17β-estradiol-3-acetate.
The range is specified as estradiol equivalent, which controls how dose is computed and labeled.

4) Low moisture requirement

“percent moisture of said dosage unit is ≤ 5%”

This is a composition property limitation. It is not merely a manufacturing goal; it is a claim constraint that ties infringement to the moisture content of the administered unit (or, in practice, what is established for the product).

5) Ester hydrolysis inhibitor identity

Solid unit includes “a pharmaceutically acceptable inhibitor of ester hydrolysis that is acetic acid”

This is a strong identity limitation: the inhibitor must be acetic acid (not a different ester hydrolysis inhibitor).

6) Formulation components

“pharmaceutically acceptable carrier”

Carrier language is broad, so most standard oral excipient systems will satisfy it, leaving the moisture and inhibitor identity as the likely differentiators.

Claim 1 summary (hard gate list):
Oral method treating 17β-estradiol deficiency in a human female using a solid oral dosage containing: 1) 17β-estradiol-3-acetate in the 0.1 to 10 mg estradiol equivalent range
2) moisture ≤ 5%
3) acetic acid as the ester hydrolysis inhibitor
4) pharmaceutically acceptable carrier
5) administered orally

Claim 2: How does the scope expand with additional medicaments?

Claim 2 depends from claim 1 and adds:

The dosage unit “further comprises one or more additional medicaments”

This expands coverage to combination products so long as the claim-1 core elements remain present (active, moisture ≤ 5%, acetic acid inhibitor, oral solid unit, and the method’s patient indication).

Claim 3: What happens if an added medicament has progestational activity?

Claim 3 depends from claim 2 and specifies:

“at least one additional medicament has progestational activity”

This aligns the formulation to common hormone replacement therapy patterns where a progestin is co-administered. It can matter for product differentiation: a combination that includes a progestational agent is within claim 3 if claim 1 and claim 2 are also met.

Claim 4: What dosage forms are within the claim set?

Claim 4 depends from claim 1 and enumerates dosage forms:

“tablet, capsule, powder, lozenge, troche or suspension”

This is a practical implementation breadth. Any accused product must fall into one of these enumerated categories to satisfy this dependent-claim structure. Since claim 4 depends on claim 1, the core limitations still apply.

Claim 5: Tablet or capsule narrowing

Claim 5 depends from claim 4 and limits:

dosage unit is “a tablet or capsule”

This is the narrowest dosage-form dependent claim provided in the text you provided. In litigation, this kind of dependent claim can capture a commercial product type even when there are disputes about other dosage-form classifications.

How would these claims likely be construed in practice?

Moisture ≤ 5% is a key product attribute

Because the claims define “percent moisture” of the dosage unit, enforcement can target products where stability or storage conditions do not keep moisture at or below the claimed threshold. In a patent landscape sense, this moisture limit creates a design-around axis:

Change moisture profile above 5% to avoid literal “≤ 5%” coverage (if a competent argument supports that product does not meet the moisture constraint).
Or position the product’s moisture content as meeting the limit. Either way, competitors must align with measured moisture at relevant conditions.

Ester hydrolysis inhibitor must be acetic acid

The claim requires an inhibitor “that is acetic acid.” This is a sharp specificity lever:

A different ester hydrolysis inhibitor is outside the literal scope.
Even if the inhibitor functionally performs similarly, literal scope still turns on identity unless doctrine of equivalents is argued in court.

Dosage range controlled “as estradiol equivalent”

The active is 17β-estradiol-3-acetate but the numeric limit is given as “estradiol equivalent.” That suggests conversion factors are used to express amount. For competitors, this controls whether their dose falls inside the 0.1 to 10 mg window after conversion.

Route restriction

Because claim 1 is an oral administration method, non-oral delivery (transdermal, injection, vaginal, etc.) falls outside the claimed method pathway.

Patent landscape: where US 7,572,779 sits relative to likely adjacent US filings

This section is structured for business planning: (i) key scope-specific design-around points that will drive freedom-to-operate analysis, and (ii) the types of competitors’ filings most likely to cluster around these claims.

Landscape anchors implied by the claim scope

US 7,572,779 is likely to sit within an oral estrogen formulation and prodrug/stabilization space built around:

1) 17β-estradiol prodrug/ester chemistry

Active is specifically 17β-estradiol-3-acetate. 2) Oral solid formulation stabilization
“percent moisture ≤ 5%” signals sensitivity to moisture-driven degradation or hydrolysis. 3) Ester hydrolysis inhibition by a simple acid
Explicit identity of acetic acid suggests that the formulation chemistry uses acid environment to suppress hydrolysis.

In the US patent landscape, this combination of (a) a particular estradiol ester and (b) a particular inhibitor identity and (c) a measurable moisture threshold typically results in a dense cluster of continuation applications and formulation patents around those same “gates.”

Likely adjacent protection themes (design-around map)

Competitors seeking to avoid infringement would typically shift one or more claim gates:

Gate A: Ester identity and dose

Replace 17β-estradiol-3-acetate with a different estradiol ester (or different prodrug).
Or keep identity but place dose outside 0.1 to 10 mg estradiol equivalent.

Gate B: Ester hydrolysis inhibitor identity

Replace acetic acid with a different hydrolysis inhibitor.
If acetic acid is removed, claim 1 literal coverage is harder to sustain.

Gate C: Moisture threshold

Move formulation moisture above 5% (if feasible while maintaining therapeutic performance).
Or argue product meets the threshold; either direction requires moisture testing and stability evidence.

Gate D: Dosage route and form

Use non-oral delivery.
Or move outside the enumerated dosage forms relevant to dependent claims (tablet/capsule/powder/lozenge/troche/suspension). Claim 1 still requires a “solid dosage unit,” so “not solid” is another axis.

Practical implication for freedom-to-operate strategy

For oral estradiol ester products, US 7,572,779’s claim architecture means most freedom-to-operate disputes will focus on:

Is the administered unit’s moisture ≤ 5%?
Is the ester hydrolysis inhibitor acetic acid?
Is the active 17β-estradiol-3-acetate at the claimed estradiol-equivalent amount?

This is a formulation-centric landscape rather than a purely pharmaceutical-method landscape.

How much coverage does the claim set provide?

Independent claim coverage breadth

Claim 1 is relatively broad in:

dosage forms (it says “solid dosage unit,” then dependent claim 4 enumerates types)
carrier selection (broad “pharmaceutically acceptable carrier”)
“therapeutically effective amount” coupled to a numeric range for the estradiol-equivalent active content

But it is relatively narrow in two decisive dimensions:

inhibitor must be acetic acid
moisture must be ≤ 5%

Dependent claims expand combinations

Claim 2 and 3 add additional medicaments and progestational activity, covering combination products without creating a new chemistry gate. They mostly extend coverage to HRT-type regimens.

Dependent claim 4 and 5 focus on dosage form used in the market

Claim 4 includes tablet, capsule, powder, lozenge, troche, suspension. Claim 5 narrows to tablet or capsule. This provides multiple potential claim targets for different product lines.

Competitive mapping: what products are most at risk?

A product is high-risk if it is an oral, solid formulation for 17β-estradiol deficiency featuring:

17β-estradiol-3-acetate
acetic acid as the ester hydrolysis inhibitor
moisture ≤ 5%
dose within 0.1 to 10 mg estradiol equivalent
delivered in tablet/capsule/powder/lozenge/troche/suspension forms (as applicable)

If the product differs from US 7,572,779 in only one gate, risk is still meaningful because the claims are structured to preserve coverage on all other dimensions. But the most decisive displacing design-around variables are acetic acid identity and moisture threshold.

Key Takeaways

US 7,572,779 is a method-of-treatment patent that is enforceable through composition-defined gates: oral dosing of a solid unit for 17β-estradiol deficiency in a human female using 17β-estradiol-3-acetate (0.1 to 10 mg as estradiol equivalent), with moisture ≤ 5% and acetic acid as the ester hydrolysis inhibitor.
Acetic acid identity and moisture ≤ 5% are the two most structurally limiting requirements and the primary design-around levers.
Dependent claims expand into combination formulations (additional medicaments including progestational activity) and cover multiple oral dosage form types, with tablet/capsule captured in the narrowest dependent claim provided.
The infringement analysis for any accused product will likely be formulation- and testing-driven: inhibitor identity, moisture testing, and dose conversion to estradiol-equivalent.

FAQs

1) Does the patent cover non-oral delivery routes?
No. Claim 1 requires “orally administering” a solid dosage unit.

2) Can a product be outside the claim if it uses a different hydrolysis inhibitor but the same active and moisture profile?
Yes for literal coverage, because claim 1 requires the inhibitor be “acetic acid.”

3) Does claim coverage depend on the exact dosage form?
Claim 1 requires a “solid dosage unit.” Dependent claim 4 adds explicit categories (tablet, capsule, powder, lozenge, troche, suspension), and claim 5 narrows to tablet or capsule.

4) What is the active-dose constraint?
17β-estradiol-3-acetate must be present at “about 0.1 to about 10 mg as estradiol equivalent.”

5) Does the patent cover combination HRT with a progestin?
Yes if the combination meets claim 1 and the additional medicament has “progestational activity” as required by claim 3.

References

US Patent 7,572,779. Claims provided in prompt text.

Title:	Oral pharmaceutical products containing 17β-estradiol-3-lower alkanoate, method of administering the same and process of preparation
Abstract:	A pharmaceutical dosage unit for oral administration to a human female comprising a therapeutically effective amount of 17β-estradiol-3-lower alkanoate, most preferably 17β-estradiol-3-acetate, and a pharmaceutically acceptable carrier is disclosed. Also disclosed is a method for treating a human female in need of 17β-estradiol and a contraceptive method by oral administration of the pharmaceutical dosage unit and a method of preparing a pharmaceutical composition that may be used to form the pharmaceutical dosage unit of the invention.
Inventor(s):	Oluwole T. Aloba, Tina M deVries
Assignee:	Allergan Therapeudics LLC
Application Number:	US10/833,997
Patent Claim Types: see list of patent claims	Use; Composition; Dosage form;
Patent landscape, scope, and claims:	United States Patent 7,572,779: Scope, Claims, and US Patent Landscape for Oral 17β-Estradiol-3-Acetate With Low-Moisture Solid Dosage and Ester-Hydrolysis Inhibitor US Patent 7,572,779 claims a specific oral hormone therapy method for a human female with a 17β-estradiol deficiency that is defined by (i) the drug form and composition (solid oral unit with low moisture), (ii) the active identity and dose range (17β-estradiol-3-acetate quantified as estradiol equivalent), and (iii) the presence of an ester hydrolysis inhibitor that is acetic acid. The claims are drafted as method-of-treatment claims with composition-defining limitations that function as enforceable infringement gates for oral solid products. What is the patented invention in US 7,572,779? The claim set describes a method where a patient receives an oral solid dosage unit comprising: Active: 17β-estradiol-3-acetate (dose 0.1 to 10 mg as estradiol equivalent) Moisture constraint: percent moisture ≤ 5% Carrier: pharmaceutically acceptable carrier Ester hydrolysis inhibitor: acetic acid Route/form: orally administering the solid unit Indication: 17β-estradiol deficiency in a human female Dependent claims then broaden or narrow implementation by adding optional co-therapy (additional medicaments) and specifying certain co-med categories (progestational activity) and certain dosage forms (tablet, capsule, and other solid/suspension formats). Claim 1: What specific elements must be present for infringement? Claim 1 is the independent claim and contains the core enforceable limitations. The claim can be reduced to six operative requirements that collectively define the infringement scope: 1) Patient population and condition “a human female having a deficiency of 17β-estradiol” This limits the method to the indicated patient class. If a competing method treats another population or condition not framed as a 17β-estradiol deficiency, it avoids at least part of the claim. 2) Administration route and dosage unit format “orally administering” to a “solid dosage unit” This excludes non-oral routes from literal claim coverage. It also narrows to products that are “solid dosage units,” even though dependent claim 4 enumerates additional possibilities including “suspension,” which is typically not “solid” in conventional taxonomy, but is explicitly listed in the claim. 3) Active ingredient and dosing Solid unit comprises “therapeutically effective amount of 17β-estradiol-3-acetate” amount range: “from about 0.1 to about 10 mg as estradiol equivalent” Key scope features: The active is explicitly 17β-estradiol-3-acetate. The range is specified as estradiol equivalent, which controls how dose is computed and labeled. 4) Low moisture requirement “percent moisture of said dosage unit is ≤ 5%” This is a composition property limitation. It is not merely a manufacturing goal; it is a claim constraint that ties infringement to the moisture content of the administered unit (or, in practice, what is established for the product). 5) Ester hydrolysis inhibitor identity Solid unit includes “a pharmaceutically acceptable inhibitor of ester hydrolysis that is acetic acid” This is a strong identity limitation: the inhibitor must be acetic acid (not a different ester hydrolysis inhibitor). 6) Formulation components “pharmaceutically acceptable carrier” Carrier language is broad, so most standard oral excipient systems will satisfy it, leaving the moisture and inhibitor identity as the likely differentiators. Claim 1 summary (hard gate list): Oral method treating 17β-estradiol deficiency in a human female using a solid oral dosage containing: 1) 17β-estradiol-3-acetate in the 0.1 to 10 mg estradiol equivalent range 2) moisture ≤ 5% 3) acetic acid as the ester hydrolysis inhibitor 4) pharmaceutically acceptable carrier 5) administered orally Claim 2: How does the scope expand with additional medicaments? Claim 2 depends from claim 1 and adds: The dosage unit “further comprises one or more additional medicaments” This expands coverage to combination products so long as the claim-1 core elements remain present (active, moisture ≤ 5%, acetic acid inhibitor, oral solid unit, and the method’s patient indication). Claim 3: What happens if an added medicament has progestational activity? Claim 3 depends from claim 2 and specifies: “at least one additional medicament has progestational activity” This aligns the formulation to common hormone replacement therapy patterns where a progestin is co-administered. It can matter for product differentiation: a combination that includes a progestational agent is within claim 3 if claim 1 and claim 2 are also met. Claim 4: What dosage forms are within the claim set? Claim 4 depends from claim 1 and enumerates dosage forms: “tablet, capsule, powder, lozenge, troche or suspension” This is a practical implementation breadth. Any accused product must fall into one of these enumerated categories to satisfy this dependent-claim structure. Since claim 4 depends on claim 1, the core limitations still apply. Claim 5: Tablet or capsule narrowing Claim 5 depends from claim 4 and limits: dosage unit is “a tablet or capsule” This is the narrowest dosage-form dependent claim provided in the text you provided. In litigation, this kind of dependent claim can capture a commercial product type even when there are disputes about other dosage-form classifications. How would these claims likely be construed in practice? Moisture ≤ 5% is a key product attribute Because the claims define “percent moisture” of the dosage unit, enforcement can target products where stability or storage conditions do not keep moisture at or below the claimed threshold. In a patent landscape sense, this moisture limit creates a design-around axis: Change moisture profile above 5% to avoid literal “≤ 5%” coverage (if a competent argument supports that product does not meet the moisture constraint). Or position the product’s moisture content as meeting the limit. Either way, competitors must align with measured moisture at relevant conditions. Ester hydrolysis inhibitor must be acetic acid The claim requires an inhibitor “that is acetic acid.” This is a sharp specificity lever: A different ester hydrolysis inhibitor is outside the literal scope. Even if the inhibitor functionally performs similarly, literal scope still turns on identity unless doctrine of equivalents is argued in court. Dosage range controlled “as estradiol equivalent” The active is 17β-estradiol-3-acetate but the numeric limit is given as “estradiol equivalent.” That suggests conversion factors are used to express amount. For competitors, this controls whether their dose falls inside the 0.1 to 10 mg window after conversion. Route restriction Because claim 1 is an oral administration method, non-oral delivery (transdermal, injection, vaginal, etc.) falls outside the claimed method pathway. Patent landscape: where US 7,572,779 sits relative to likely adjacent US filings This section is structured for business planning: (i) key scope-specific design-around points that will drive freedom-to-operate analysis, and (ii) the types of competitors’ filings most likely to cluster around these claims. Landscape anchors implied by the claim scope US 7,572,779 is likely to sit within an oral estrogen formulation and prodrug/stabilization space built around: 1) 17β-estradiol prodrug/ester chemistry Active is specifically 17β-estradiol-3-acetate. 2) Oral solid formulation stabilization “percent moisture ≤ 5%” signals sensitivity to moisture-driven degradation or hydrolysis. 3) Ester hydrolysis inhibition by a simple acid Explicit identity of acetic acid suggests that the formulation chemistry uses acid environment to suppress hydrolysis. In the US patent landscape, this combination of (a) a particular estradiol ester and (b) a particular inhibitor identity and (c) a measurable moisture threshold typically results in a dense cluster of continuation applications and formulation patents around those same “gates.” Likely adjacent protection themes (design-around map) Competitors seeking to avoid infringement would typically shift one or more claim gates: Gate A: Ester identity and dose Replace 17β-estradiol-3-acetate with a different estradiol ester (or different prodrug). Or keep identity but place dose outside 0.1 to 10 mg estradiol equivalent. Gate B: Ester hydrolysis inhibitor identity Replace acetic acid with a different hydrolysis inhibitor. If acetic acid is removed, claim 1 literal coverage is harder to sustain. Gate C: Moisture threshold Move formulation moisture above 5% (if feasible while maintaining therapeutic performance). Or argue product meets the threshold; either direction requires moisture testing and stability evidence. Gate D: Dosage route and form Use non-oral delivery. Or move outside the enumerated dosage forms relevant to dependent claims (tablet/capsule/powder/lozenge/troche/suspension). Claim 1 still requires a “solid dosage unit,” so “not solid” is another axis. Practical implication for freedom-to-operate strategy For oral estradiol ester products, US 7,572,779’s claim architecture means most freedom-to-operate disputes will focus on: Is the administered unit’s moisture ≤ 5%? Is the ester hydrolysis inhibitor acetic acid? Is the active 17β-estradiol-3-acetate at the claimed estradiol-equivalent amount? This is a formulation-centric landscape rather than a purely pharmaceutical-method landscape. How much coverage does the claim set provide? Independent claim coverage breadth Claim 1 is relatively broad in: dosage forms (it says “solid dosage unit,” then dependent claim 4 enumerates types) carrier selection (broad “pharmaceutically acceptable carrier”) “therapeutically effective amount” coupled to a numeric range for the estradiol-equivalent active content But it is relatively narrow in two decisive dimensions: inhibitor must be acetic acid moisture must be ≤ 5% Dependent claims expand combinations Claim 2 and 3 add additional medicaments and progestational activity, covering combination products without creating a new chemistry gate. They mostly extend coverage to HRT-type regimens. Dependent claim 4 and 5 focus on dosage form used in the market Claim 4 includes tablet, capsule, powder, lozenge, troche, suspension. Claim 5 narrows to tablet or capsule. This provides multiple potential claim targets for different product lines. Competitive mapping: what products are most at risk? A product is high-risk if it is an oral, solid formulation for 17β-estradiol deficiency featuring: 17β-estradiol-3-acetate acetic acid as the ester hydrolysis inhibitor moisture ≤ 5% dose within 0.1 to 10 mg estradiol equivalent delivered in tablet/capsule/powder/lozenge/troche/suspension forms (as applicable) If the product differs from US 7,572,779 in only one gate, risk is still meaningful because the claims are structured to preserve coverage on all other dimensions. But the most decisive displacing design-around variables are acetic acid identity and moisture threshold. Key Takeaways US 7,572,779 is a method-of-treatment patent that is enforceable through composition-defined gates: oral dosing of a solid unit for 17β-estradiol deficiency in a human female using 17β-estradiol-3-acetate (0.1 to 10 mg as estradiol equivalent), with moisture ≤ 5% and acetic acid as the ester hydrolysis inhibitor. Acetic acid identity and moisture ≤ 5% are the two most structurally limiting requirements and the primary design-around levers. Dependent claims expand into combination formulations (additional medicaments including progestational activity) and cover multiple oral dosage form types, with tablet/capsule captured in the narrowest dependent claim provided. The infringement analysis for any accused product will likely be formulation- and testing-driven: inhibitor identity, moisture testing, and dose conversion to estradiol-equivalent. FAQs 1) Does the patent cover non-oral delivery routes? No. Claim 1 requires “orally administering” a solid dosage unit. 2) Can a product be outside the claim if it uses a different hydrolysis inhibitor but the same active and moisture profile? Yes for literal coverage, because claim 1 requires the inhibitor be “acetic acid.” 3) Does claim coverage depend on the exact dosage form? Claim 1 requires a “solid dosage unit.” Dependent claim 4 adds explicit categories (tablet, capsule, powder, lozenge, troche, suspension), and claim 5 narrows to tablet or capsule. 4) What is the active-dose constraint? 17β-estradiol-3-acetate must be present at “about 0.1 to about 10 mg as estradiol equivalent.” 5) Does the patent cover combination HRT with a progestin? Yes if the combination meets claim 1 and the additional medicament has “progestational activity” as required by claim 3. References US Patent 7,572,779. Claims provided in prompt text. More… ↓ ⤷ Start Trial

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Australia	2002359758	⤷ Start Trial
Canada	2470703	⤷ Start Trial
China	1273141	⤷ Start Trial
China	1564689	⤷ Start Trial
European Patent Office	1461043	⤷ Start Trial
>Country	>Patent Number	>Estimated Expiration	>Supplementary Protection Certificate	>SPC Country	>SPC Expiration

Details for Patent: 7,572,779

Summary for Patent: 7,572,779