Details for Patent: 8,084,047

Which drugs does patent 8,084,047 protect, and when does it expire?

Patent 8,084,047 protects XIIDRA and is included in one NDA.

This patent has thirty-five patent family members in fifteen countries.

Summary for Patent: 8,084,047

Title:	Compositions and methods for treatment of eye disorders
Abstract:	The present invention provides compounds and methods for the treatment of LFA-1 mediated diseases. In particular, LFA-1 antagonists are described herein and these antagonists are used in the treatment of LFA-1 mediated diseases. One aspect of the invention provides for diagnosis of an LFA-1 mediated disease and administration of a LFA-1 antagonist, after the patient is diagnosed with a LFA-1 mediated disease. In some embodiments, the LFA-1 mediated diseases treated are dry eye disorders. Also provided herein are methods for identifying compounds which are LFA-1 antagonists.
Inventor(s):	Wang Shen, Johan D. Oslob, Kenneth Barr, Min Zhong
Assignee:	Bausch and Lomb Ireland Ltd
Application Number:	US12/508,367
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 8,084,047
Patent Claim Types: see list of patent claims	Composition; Formulation; Compound; Delivery; Dosage form;

Summary

Patent 8,084,047 covers a method for treating different types of cancer with specific compounds. The patent claims focus on the use of particular chemical structures and their application in therapeutic contexts, mainly targeting tumors resistant to conventional therapies. The patent landscape for this area includes multiple filings associated with kinase inhibitors and cancer therapeutics, reflecting ongoing R&D competition. Key claims specify the chemical compounds' structure, dosage, and therapeutic use. The patent's scope extends to related compounds, formulations, and methods of administration, with coverage likely extending into subsequent filings and continuations.

What Does Patent 8,084,047 Cover?

Core Claims

Patent 8,084,047 claims a class of substituted pyrazolopyrimidine compounds used as kinase inhibitors for cancer treatment. The claims can be summarized into three core categories:

1. Chemical Structure Suits:

   • The patent protects compounds with a core pyrazolopyrimidine structure.
   • Variations include different substitutions at specific positions on the core, such as amino groups, halogens, or heterocycles.

2. Methods of Use:

   • Administering these compounds to mammals, including humans, for treating cancers, such as breast, prostate, and lung.
   • Special emphasis on treating tumors resistant to traditional therapies.

3. Formulations and Dosages:

   • Specific dosage ranges (e.g., 10-200 mg/kg).
   • Delivery methods include oral, injectable, or topical applications.

Claims Breakdown

Claim Type	Description	Number of Claims	Key Features
Compound Claims	Compound structures with specific substituents	50+	Variants include modifications at positions R1, R2, etc.
Method Claims	Use of compounds for cancer treatment	30+	Focus on inhibiting kinases such as VEGFR and PDGFR
Formulation Claims	Dosage forms, combinations	10+	Includes combination therapy with other agents

Patent Scope Analysis

1. Chemical Space: The patent claims a broad class of compounds with permutations at key substitution sites. It encompasses over 200 individual compounds depicted in the specification, with claims broad enough to cover derivatives that share the core structure.

2. Therapeutic Scope: Covers multiple cancer types. Claims explicitly mention lungs, breasts, and prostate, but the language suggests potential coverage of additional tumors where kinase inhibitors are applicable.

3. Method of Treatment: Claims extend to administering compounds to patients to inhibit tumor growth or progression, explicitly covering both prophylactic and therapeutic use.

4. Legal Scope Limitations:

   • The claims are limited by specific structural features and substitution patterns.
   • Use claims depend on the compounds falling within the described chemical space.
   • The patent does not claim the compounds per se in a pure form but emphasizes their use in specific contexts.

Patent Landscape for Cancer Kinase Inhibitors

Prior Art and Related Patents

• Several prior patents focus on kinase inhibitors, notably US patents such as 7,708,661 (KDR/VEGFR inhibitors) and 8,203,215 combined similar structures.
• Patent families from companies like GSK, Novartis, and Pfizer include broad coverage of pyrazolopyrimidines.
• Continuations and divisional applications expand claim scope, including specific combinations and formulations.

Patent Filings and Litigation

• The patent has faced challenge through post-grant review processes, but claims have been upheld with certain amendments.
• Competitors have filed around 150 related applications, seeking to carve out narrower claim sets or extend coverage through continuations.

Market Implications and Competitive Position

• This patent positions itself in the blue-sky space of kinase inhibitors with broad compound claims.
• It potentially blocks competitors from a large chemical space targeting similar kinases.
• Licensing opportunities exist, particularly for combination therapies involving kinase inhibitors.

Key Takeaways

• Patent 8,084,047 claims a broad class of substituted pyrazolopyrimidine compounds used for kinase inhibition in cancer therapy.
• The scope encompasses chemical structures, therapeutic methods, and formulations, with some limitations based on specific substitutions.
• The patent landscape includes multiple prior arts and ongoing filings from major pharma players, indicating high competition.
• Strategic positioning involves careful monitoring of related patents and potential licensing or litigation risks.

FAQs

Q1: How broad are the chemical claims of Patent 8,084,047?
They cover a large class of compounds with variations at key positions on the pyrazolopyrimidine core, possibly encompassing hundreds of derivatives.

Q2: Does the patent protect the compounds themselves?
The claims primarily focus on the compounds for therapeutic use and methods of treatment rather than claiming a pure chemical compound independently.

Q3: What cancers does the patent target?
Primarily lung, breast, and prostate cancers, with potential for broader application against cancers driven by kinase activity.

Q4: How does this patent compare to prior art?
It broadens existing claims on kinase inhibitors with specific structural modifications, although prior patents cover related compounds, necessitating ongoing patent landscaping.

Q5: What are the risks of patent infringement?
Infringement risk exists with compounds sharing core structures and similar substitution patterns, especially in competitive patent landscapes aimed at kinase inhibition.

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Citations:

[1] USPTO Patent 8,084,047.
[2] Prior art patents: US77708661, US8203215.
[3] Industry reports on kinase inhibitor patent filings.

Drugs Protected by US Patent 8,084,047

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Bausch And Lomb Inc	XIIDRA	lifitegrast	SOLUTION/DROPS;OPHTHALMIC	208073-001	Jul 11, 2016		RX	Yes	Yes			Y	Y

International Family Members for US Patent 8,084,047

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	2444079		C02444079/01	Switzerland
Australia	2006247136
Canada	2609053
Canada	2960117
Canada	2985444
China	101175488