Details for Patent: 8,809,336

Which drugs does patent 8,809,336 protect, and when does it expire?

Patent 8,809,336 protects TRUQAP and is included in one NDA.

This patent has twenty-two patent family members in seventeen countries.

Summary for Patent: 8,809,336

Title:	Ortho-condensed pyridine and pyrimidine derivatives (e.g., purines) as protein kinases inhibitors
Abstract:	The invention provides a compound for use as a protein kinase B inhibitor, the compound being a compound of the formula (I) or salts, solvates, tautomers or N-oxides thereof, wherein T is N or CR; J-Jis N═C(R), (R)C═N, (R)N—C(O), (R)C—C(O), N═N or (R)C═C(R); E is a monocyclic carbocyclic or heterocyclic group of 5 or 6 ring members, the heterocyclic group containing up to 3 heteroatoms selected from O, N and S; Qis a bond or a saturated Chydrocarbon linker group, one of the carbon atoms in the linker group being optionally be replaced by an oxygen or nitrogen atom, or an adjacent pair of carbon atoms may be replaced by CONRor NRCO where Ris hydrogen or methyl, or Ris a Calkylene chain linked to Ror a carbon atom of Qto form a cyclic moiety; and wherein the carbon atoms of the linker group Qmay optionally bear one or more substituents selected from fluorine and hydroxy; Qis a bond or a saturated hydrocarbon linker group containing from 1 to 3 carbon atoms, wherein one of the carbon atoms in the linker group may optionally be replaced by an oxygen or nitrogen atom; and wherein the carbon atoms of the linker group may optionally bear one or more substituents selected from fluorine and hydroxy, provided that the hydroxy group when present is not located at a carbon atom a with respect to the G group; and provided that when E is aryl or heteroaryl, then Qis other than a bond; G is hydrogen, NRR, OH or SH provided that when E is aryl or heteroaryl and Qis a bond, then G is hydrogen; Ris hydrogen or an aryl or heteroaryl group, with the proviso that when Ris hydrogen and G is NRR, then Qis a bond; and R, R, R, Rand Rare as defined in the claims.
Inventor(s):	Berdini Valerio, Boyle Robert George, Saxty Gordon, Walker David Winter, Woodhead Steven John, Wyatt Paul Graham, Donald Alastair, Caldwell John, Collins Ian, Da Fonseca Tatiana Faria
Assignee:
Application Number:	US14017814
Patent Claim Types: see list of patent claims

United States Patent 8,809,336: A Detailed Analysis of Scope, Claims, and Patent Landscape

Introduction

United States Patent 8,809,336, titled "Ortho-condensed pyridine and pyrimidine derivatives (e.g., purines) as protein kinases inhibitors," is a significant patent in the field of pharmaceuticals, particularly in the area of protein kinase inhibitors. This patent, issued on August 19, 2014, is assigned to AstraZeneca AB and involves a novel group of compounds designed to inhibit or modulate the activity of protein kinase B (PKB).

Background

Protein kinases are enzymes that play crucial roles in cellular signaling pathways, and their dysregulation is often associated with various diseases, including cancer and metabolic disorders. The development of specific inhibitors for these enzymes is a key area of research in pharmaceuticals.

Scope of the Patent

The patent 8,809,336 focuses on ortho-condensed pyridine and pyrimidine derivatives, which include purine, purinone, and deazapurine compounds. These compounds are designed to inhibit or modulate the activity of protein kinase B (PKB), also known as AKT, which is a critical enzyme in the PI3K/AKT signaling pathway involved in cell survival, growth, and metabolism.

Chemical Structure and Synthesis

The patent describes the chemical structure of these compounds, including their synthesis methods. The compounds are characterized by specific formulae and structural features that confer their inhibitory activity on protein kinases. The synthesis involves various chemical reactions and purification steps to obtain the desired compounds[4].

Claims of the Patent

The patent includes several claims that define the scope of the invention:

Compound Claims

• The patent claims specific chemical compounds that fall under the category of ortho-condensed pyridine and pyrimidine derivatives.
• These claims are detailed and specify the structural features of the compounds, including the presence of particular functional groups and ring systems[4].

Method of Use Claims

• The patent also claims methods of using these compounds for inhibiting or modulating protein kinase activity.
• These claims include the therapeutic use of the compounds for treating diseases associated with abnormal protein kinase activity, such as cancer and metabolic disorders[4].

Pharmaceutical Composition Claims

• The patent claims pharmaceutical compositions that include the described compounds, along with suitable carriers and excipients.
• These compositions are intended for various routes of administration, including oral, intravenous, and topical[4].

Patent Landscape

The patent landscape surrounding 8,809,336 is complex and involves several related patents and technologies.

Related Patents

• Other patents by AstraZeneca AB, such as 10,059,714 and 10,654,855, also relate to protein kinase inhibitors and share similar inventors and assignees. These patents expire on October 10, 2028, and March 10, 2030, respectively[2].
• There are also patents related to different classes of protein kinase inhibitors, such as the substituted pyrrolo[2,3-d]pyrimidine compounds described in patent 8,101,623[2].

Exclusivity and Expiration Dates

• The patent 8,809,336 is currently active, but its legal status and expiration date are critical for understanding its impact on the market.
• The patent is set to expire on August 19, 2034, assuming no extensions or adjustments[4].

Competitive Landscape

• The competitive landscape in the field of protein kinase inhibitors is highly competitive, with multiple pharmaceutical companies developing similar compounds.
• Companies like AstraZeneca, Pfizer, and Novartis have significant portfolios of patents related to protein kinase inhibitors, each with their own expiration dates and exclusivity periods[5].

Impact on Pharmaceutical Development

The patent 8,809,336 has significant implications for pharmaceutical development, particularly in the areas of cancer and metabolic disease treatment.

Therapeutic Applications

• The compounds described in the patent have potential therapeutic applications in treating various cancers and metabolic disorders by inhibiting protein kinase B.
• Clinical trials and further research are necessary to fully realize the therapeutic potential of these compounds[4].

Research and Development

• The patent encourages further research and development in the field of protein kinase inhibitors.
• It provides a foundation for scientists to build upon, exploring new compounds and therapeutic applications[4].

Challenges and Considerations

The patent landscape and the development of these compounds come with several challenges and considerations.

Patent Litigation

• The complexity of patent litigation in the pharmaceutical industry can be significant, especially when dealing with overlapping patents and claims[3].

Regulatory Approval

• Obtaining regulatory approval for new pharmaceutical compounds is a lengthy and rigorous process.
• The compounds must undergo extensive clinical trials to demonstrate safety and efficacy before they can be approved for market use[4].

Generic Competition

• The expiration of patents can lead to generic competition, which can significantly impact the market share of the original patented compounds.
• Companies must strategize to maintain market dominance through innovation, brand loyalty, and other competitive strategies[2].

Key Takeaways

• Patent Scope: The patent 8,809,336 covers ortho-condensed pyridine and pyrimidine derivatives as protein kinase inhibitors.
• Claims: The patent includes claims for specific compounds, methods of use, and pharmaceutical compositions.
• Patent Landscape: The patent is part of a broader landscape involving related patents and competitive technologies.
• Impact: The patent has significant implications for the development of therapeutic agents targeting protein kinases.
• Challenges: The development and commercialization of these compounds face challenges including patent litigation, regulatory approval, and generic competition.

Frequently Asked Questions (FAQs)

What is the main focus of United States Patent 8,809,336?

The main focus of this patent is on ortho-condensed pyridine and pyrimidine derivatives that act as inhibitors of protein kinase B (PKB).

Who is the assignee of this patent?

The assignee of this patent is AstraZeneca AB.

When does the patent expire?

The patent is set to expire on August 19, 2034.

What are the potential therapeutic applications of the compounds described in this patent?

The compounds have potential therapeutic applications in treating various cancers and metabolic disorders by inhibiting protein kinase B.

How does this patent fit into the broader patent landscape?

This patent is part of a broader landscape involving related patents and competitive technologies in the field of protein kinase inhibitors.

Cited Sources

1. Google Patents: WO1988009336A1 - Saponin adjuvant.
2. Drugs.com: Generic Truqap Availability.
3. University of Pennsylvania Law Review: Understanding Patent-Quality Mechanisms.
4. Google Patents: US8809336B2 - Ortho-condensed pyridine and pyrimidine derivatives (e.g., purines) as protein kinases inhibitors.
5. Orange Book Companion: Company - Orange Book Companion.

Drugs Protected by US Patent 8,809,336

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Astrazeneca	TRUQAP	capivasertib	TABLET;ORAL	218197-001	Nov 16, 2023		RX	Yes	No						TREATMENT WITH FULVESTRANT OF HR-POS. HER2-NEG. LOCALLY ADVANCED OR METASTATIC BREAST CANCER WITH PIK3CA/AKT1/PTEN-ALTERATION(S) FOLLOWING PROGRESSION ON ENDOCRINE THERAPY IN THE METASTATIC SETTING OR RECURRENCE ON OR WITHIN 12 MONTHS OF ADJUVANT THERAPY
Astrazeneca	TRUQAP	capivasertib	TABLET;ORAL	218197-002	Nov 16, 2023		RX	Yes	Yes						TREATMENT WITH FULVESTRANT OF HR-POS. HER2-NEG. LOCALLY ADVANCED OR METASTATIC BREAST CANCER WITH PIK3CA/AKT1/PTEN-ALTERATION(S) FOLLOWING PROGRESSION ON ENDOCRINE THERAPY IN THE METASTATIC SETTING OR RECURRENCE ON OR WITHIN 12 MONTHS OF ADJUVANT THERAPY

International Family Members for US Patent 8,809,336

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Argentina	051342
Argentina	103370
Austria	E513549