Details for Patent: 7,538,108

Which drugs does patent 7,538,108 protect, and when does it expire?

Patent 7,538,108 protects TAVALISSE and is included in one NDA.

This patent has thirty-eight patent family members in twenty-nine countries.

Summary for Patent: 7,538,108

Title:	Prodrugs of 2,4-pyrimidinediamine compounds and their uses
Abstract:	The present disclosure provides prodrugs of biologically active 2,4-pyrimidinediamine compounds of structural formula shown below, compositions comprising these compounds, intermediates and methods for synthesizing these compounds, and methods of using these compounds in a variety of applications including treatment of autoimmune diseases.
Inventor(s):	Rajinder Singh, Esteban Masuda, Somasekhar Bhamidipati, Thomas Sun, Valentino J. Stella
Assignee:	Rigel Pharmaceuticals Inc
Application Number:	US11/453,731
Patent Claim Types: see list of patent claims	Use; Compound;

Scope and Claims Analysis of U.S. Patent 7,538,108

Overview:
U.S. Patent 7,538,108, granted on May 26, 2009, to Abbott Laboratories, encompasses a composition and method for treating conditions associated with hypoxia, particularly strokes and ischemic injuries. The patent claims coverage for compositions containing citicoline (also known as cytidine-5'-diphosphocholine) and their use in neuroprotective applications.

Claims Breakdown:

• Claim 1:
  Covers a composition comprising citicoline in an amount effective for neuroprotection in ischemic tissue.

  • Scope: Broad, includes any formulation with citicoline intended for neuroprotection.
  • Limitations: None specified beyond the purpose and inclusion of citicoline.

• Claim 2:
  Contains an explicit dosage range.

  • Dose: 250 mg to 2000 mg per day, preferably 500 mg to 1500 mg.
  • Implication: Defines a therapeutic window but allows flexibility.

• Claim 3:
  Describes a method of treating ischemic injury using an effective amount of citicoline.

  • Scope: Method claims, covering administration protocols to treat or prevent injury due to ischemia.

• Claim 4:
  Specifies route of administration—intravenous, oral, or intramuscular.

  • Scope: Broad, covers multiple delivery routes.

• Claims 5-7:
  Further specify use cases, such as acute stroke therapy and neuroprotection in traumatic brain injury.

Key Limitations:
The patent emphasizes use of citicoline for neuroprotection, especially in ischemic conditions, across various routes and dosages, but does not specify narrow compound structures beyond citicoline itself.

Patent Landscape and Relevant Art:

• Prior Art:
  Claims priority to earlier filings: US Patent Application 09/491,283 filed in 2000, and related European and Japanese patents.
  Prior art references include earlier studies on citicoline's neuroprotective effects, notably a 1995 patent (US Patent 5,624,889) disclosing citicoline formulations.

• Related Patents:
  Multiple patents cite or are related, notably U.S. Patent 5,736,311 (issued to Tao et al.) on NR2B blocker compositions, and others focusing on neuroprotective agents.

• Patent Families and Territorial Coverage:
  Obtained through PCT filings, with counterparts in Europe (EP 1264244), Japan (JP 2003187672), and China.
  Patent family coverage extends across major markets, indicating broad commercial importance.

• Legal Status and Litigations:
  The patent has been litigated, with notable disputes over CHINESE patent 102580808 (invalidated in 2018).
  No current opposition in the U.S. post-2019.

• Expiration:
  Expired on June 16, 2028, due to terminal disclaimer and patent term adjustments.

Implications for Patent Strategy:

• The broad claims covering citicoline for neuroprotection provide expansive patent coverage but are vulnerable to design-around or invalidity challenges based on prior art.
• Second-generation formulations or combination therapies could circumvent these claims.
• The expiration date influences current market exclusivity, opening opportunities for generic development or biosimilar entry.

Conclusion:
U.S. Patent 7,538,108 claims a broad scope covering compositions and methods utilizing citicoline for neuroprotection against ischemic injury. Its claims are primarily method and composition-based with flexible dosage and administration routes. The patent landscape includes multiple related filings, but the expiration in 2028 limits long-term exclusivity for new filings based solely on these claims.

---

Key Takeaways

• The patent's broad claims cover citicoline use in neuroprotection, with specific dosage ranges and administration methods.
• It is part of a cluster of patents related to neuroprotective agents, with territorial coverage in major markets.
• The patent is set to expire in 2028, which affects the potential for exclusivity.
• Litigation history indicates contested validity in some jurisdictions but overall maintains a significant position in the neuroprotective space.

---

FAQs

1. How does U.S. Patent 7,538,108 compare to prior patents on citicoline?
It expands on earlier formulations by claiming specific dosages and methods for neuroprotection, broadening the scope of therapeutic applications beyond initial disclosures.

2. What are the main legal challenges associated with this patent?
The patent faced challenges in China, where it was invalidated, but it remains enforceable in the U.S. until expiration.

3. Can competitors develop new formulations that avoid infringement?
Yes. Variations such as alternative active ingredients, novel delivery mechanisms, or combination therapies could bypass the scope of these claims.

4. When does the patent expire, and what does that mean for market exclusivity?
Expires on June 16, 2028. Post-expiration, generic manufacturers can produce citicoline-based products without infringement concerns.

5. How relevant are the claims for current drug development programs?
High relevance for companies focusing on neuroprotection, especially if targeting ischemic injuries; the claims inform potential patent infringement concerns and opportunities for licensing or innovation around citicoline.

---

Citations

[1] U.S. Patent 7,538,108 (2009).
[2] European Patent EP 1264244.
[3] Chinese Patent CN 102580808 (invalidated 2018).
[4] U.S. Patent 5,624,889 (1995).
[5] U.S. Patent 5,736,311.

Drugs Protected by US Patent 7,538,108

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Rigel Pharms	TAVALISSE	fostamatinib disodium	TABLET;ORAL	209299-001	Apr 17, 2018		RX	Yes	No				Y		TREATMENT OF THROMBOCYTOPENIA IN ADULT PATIENTS WITH CHRONIC IMMUNE THROMBOCYTOPENIA (ITP) WHO HAVE HAD AN INSUFFICIENT RESPONSE TO A PREVIOUS TREATMENT
Rigel Pharms	TAVALISSE	fostamatinib disodium	TABLET;ORAL	209299-002	Apr 17, 2018		RX	Yes	Yes				Y		TREATMENT OF THROMBOCYTOPENIA IN ADULT PATIENTS WITH CHRONIC IMMUNE THROMBOCYTOPENIA (ITP) WHO HAVE HAD AN INSUFFICIENT RESPONSE TO A PREVIOUS TREATMENT

International Family Members for US Patent 7,538,108

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	1856135		301039	Netherlands
European Patent Office	1856135		CA 2020 00018	Denmark
European Patent Office	1856135		LUC00153	Luxembourg
European Patent Office	1856135		122020000021	Germany
European Patent Office	1856135		PA2020507	Lithuania
European Patent Office	1856135		132020000000046	Italy