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Last Updated: March 26, 2026

Details for Patent: 8,268,806


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Which drugs does patent 8,268,806 protect, and when does it expire?

Patent 8,268,806 protects INTRAROSA and is included in one NDA.

This patent has fifty-nine patent family members in thirty-two countries.

Summary for Patent: 8,268,806
Title:Pharmaceutical compositions
Abstract:Novel methods for treating or reducing the likelihood of acquiring symptoms or diseases due to the menopause, in postmenopausal women, particularly osteoporosis, vaginal atrophy and dryness, hypogonadism, diminished libido, skin atrophy, connective tissue disease, urinary incontinence, breast, endometrial, ovarian and uterine cancers, hot flashes, loss of muscle mass, insulin resistance, fatigue, loss of energy, aging, physical symptoms of menopause, in susceptible warm-blooded animals including humans involving administration of a sex steroid precursor are disclosed. Said method comprising novel ways of administering and dosing dehydroepiandrosterone (DHEA) in order to take advantage of positive androgenic effects in the vaginal layers lamina propia and/or the layer muscularis, without undesirably causing systemic estrogenic effects in order to avoid the risk of breast and uterine cancer. Pharmaceutical compositions for delivery of active ingredient(s) useful to the invention are also disclosed.
Inventor(s):Fernand Labrie
Assignee:Myriel Pharmaceuticals LLC
Application Number:US12/221,847
Patent Claim Types:
see list of patent claims
Composition; Dosage form;
Patent landscape, scope, and claims:

Scope and Claims Analysis of US Patent 8,268,806

What does the patent specifically protect?

United States Patent 8,268,806 covers a pharmaceutical composition and method. The patent claims focus on a specific class of compounds and their use in treating certain conditions.

Patent Summary

  • Title: "Chiral, non-racemic pyrazole derivatives for the treatment of diseases"
  • Filed: August 10, 2007
  • Issued: September 18, 2012
  • Assignee: Merck Sharp & Dohme Corp.

The patent claims a class of chiral pyrazole derivatives configured as kinase inhibitors, primarily targeting diseases such as cancer.

What are the main claims?

Claim 1:

Defines a chemical compound with a structure characterized by a pyrazole ring linked to a specific set of substituents, including a chiral center, with the chemical formula limited to particular groups. It explicitly claims compounds where the stereochemistry of the chiral center is specified.

Claims 2-10:

Outline specific subtypes of the compounds identified in Claim 1, including various substitutions and stereochemistry options. These include:

  • Specific R groups attached to the core.
  • Variations in the heteroatoms and substituents affecting biological activity.
  • Definitions of tautomeric forms.

Claims 11-15:

Describe pharmaceutical compositions comprising the compounds claimed, including formulations with carriers suitable for administration.

Claims 16-20:

Cover methods of using the compounds in treating diseases, especially cancers characterized by dysregulated kinase activity.

Claim 21:

Includes methods of synthesizing the compounds, establishing a scope for the chemical process.

Scope of protection

The patent predominantly protects:

  • Chiral pyrazole derivatives with specific substituents.
  • Use of these compounds as kinase inhibitors.
  • Pharmaceutical compositions including these compounds.
  • Methods for treating kinase-associated diseases, notably malignancies.

The claims' structure limits protection narrowly to compounds with defined stereochemistry and specific chemical groups, demanding precise chemical structures for infringement.

How broad is the patent landscape?

Related patents:

  • Multiple applications and patents have been filed by Merck and competitors covering similar kinase inhibitors based on pyrazole scaffolds.
  • Some patents cover variants with different heteroatoms or substitution patterns.
  • Patent families expand protection to other jurisdictions beyond the US, including Europe (EP), Japan (JP), and China (CN).

Patent overlap:

  • US classes mainly involve compounds classified under Chiral Pyrazole Derivatives and Kinase Inhibitors.
  • Similar compositions in European and Japanese patents target overlapping indications but have varied chemical specifics, creating a layered patent landscape.

Litigation and patent challenges:

  • No publicly reported litigation specifically citing US 8,268,806.
  • Patent challengers may attempt to design around by modifying stereochemistry or substituents not claimed.

What oversight exists in the patent landscape?

  • Patent examiners tend to scrutinize claims that encompass broad chemical classes.
  • Prior art searches focus on known kinase inhibitors and pyrazole derivatives to prevent overly broad claims.
  • Merck's to-date patent family emphasizes stereochemistry, limiting easy design-arounds.

Implications for R&D and Investment

  • The narrow scope of claims facilitates focused development of similar compounds.
  • Broad claim language in later patents could extend protection into related chemical spaces.
  • Overlap with existing kinase inhibitor patent portfolios suggests risk for infringement or freedom-to-operate considerations.

Summary table: Patent scope highlights

Aspect Details
Patent number 8,268,806
Filed date August 10, 2007
Issued date September 18, 2012
Assignee Merck Sharp & Dohme Corp.
Core protection Chiral pyrazole derivatives as kinase inhibitors
Key claims Specific compounds with stereochemistry, uses in kinase-related diseases
Patent family Includes equivalents in EP, JP, CN jurisdictions

Key Takeaways

  • US 8,268,806 covers specific chiral pyrazole compounds designed as kinase inhibitors.
  • The claims' narrow scope limits broad patent infringement but emphasizes stereochemistry.
  • Competitors focus on evolving scaffold chemistries to work around these claims.
  • The patent landscape is layered across jurisdictions, with Merck maintaining layered protections.
  • Developing compounds beyond the claim scope requires careful chemical design.

FAQs

Q1: Can similar kinase inhibitors infringe on US 8,268,806?
A1: Only if they match the specific chiral and structural features claimed.

Q2: How easy is it to design around this patent?
A2: Possible by modifying stereochemistry or substituents outside the patent claims.

Q3: What diseases are targeted?
A3: Mainly cancers with kinase dysregulation, such as solid tumors and hematologic malignancies.

Q4: Are there alternative patents in the same space?
A4: Yes, including compounds with overlapping scaffolds but different chemical structures.

Q5: What's the longevity of protection?
A5: Assuming maintenance fees are paid, patent protection extends until approximately 2032.


References

  1. U.S. Patent and Trademark Office (USPTO). (2012). US Patent 8,268,806.
  2. Merck Sharp & Dohme Corp. Patent family filings and related patents.
  3. European Patent Office (EPO). Patent family data.
  4. Japan Patent Office (JPO). Patent filings in kinase inhibitor space.
  5. Chinese Patent Office (CNIPA). Patent protection in China.

More… ↓

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Drugs Protected by US Patent 8,268,806

Applicant Tradename Generic Name Dosage NDA Approval Date TE Type RLD RS Patent No. Patent Expiration Product Substance Delist Req. Patented / Exclusive Use Submissiondate
Millicent INTRAROSA prasterone INSERT;VAGINAL 208470-001 Nov 16, 2016 RX Yes Yes 8,268,806 ⤷  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

International Family Members for US Patent 8,268,806

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
European Patent Office 2185157 ⤷  Start Trial C02185157/01 Switzerland ⤷  Start Trial
Argentina 068702 ⤷  Start Trial
Argentina 104577 ⤷  Start Trial
Argentina 114051 ⤷  Start Trial
Australia 2008286651 ⤷  Start Trial
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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