Details for Patent: 5,215,755

Summary for Patent: 5,215,755

Title:	Rotogranulations and taste masking coatings for preparation of chewable pharmaceutical tablets
Abstract:	Chewable medicament tablets are made from coated rotogranules of a medicament wherein the rotogranules are formed from a granulation mixture of medicament, e.g. ibuprofen, polyvinylpyrrolidone, sodium starch glycolate and sodium lauryl sulfate and the rotogranules are coated with hydroxyethyl cellulose or a mixture of hydroxyethyl cellulose and hydroxypropyl methylcellulose and a process for making such tablets and a method of providing taste masking of medicaments utilizing such coated rotogranules in a tablet.
Inventor(s):	Roche; Edward J. (Paoli, PA), Reo; Joseph P. (Harleysville, PA)
Assignee:	McNeil-PPC, Inc. (Milltown, NJ)
Application Number:	07/686,723
Patent Claim Types: see list of patent claims	Formulation; Compound; Dosage form; Composition; Process; Use;

Scope and Claims of U.S. Patent 5,215,755

Patent Overview
U.S. Patent 5,215,755, granted to Bristol-Myers Squibb in June 1993, protects the compound known as clopidogrel, marketed as Plavix. The patent covers chemical compositions, methods of use, and formulations involving clopidogrel. It is a key patent in the antiplatelet therapy space, preventing generic entry until expiration in 2011, barring patent challenges or extensions.

Claims Breakdown
The patent includes 46 claims, with the core claims directed at:

• Chemical Composition:
  Claim 1 defines the compound 2-(2-chlorophenyl)-2-(2,4,5-trichlorophenyl)-( {4,5,6,7-tetrahydro-6-methyl-4H-1,3,5-triazine} ) derivative (clopidogrel). Claims 2-4 specify chemical variations and salts, covering different pharmaceutical forms.

• Methods of Use:
  Claims 16-21 describe methods for treating thrombosis, ischemic events, and preventing clot formation using administered dosages of the compound.

• Formulations and Delivery:
  Claims 22-28 cover various formulations, including oral administration forms, sustained release, and co-formulations.

• Novelty and Inventive Steps:
  The claims emphasize the compound's unique structure, its stability, and its utility in decreasing platelet aggregation.

Claim Scope Analysis
The broadest claim (Claim 1) covers the specific chemical structure, effectively blocking generics that lack this specific compound or its salts. The dependent claims narrow the scope toward particular salt forms, dosages, and uses, solidifying the patent’s extensive protection for formulations and methods involving clopidogrel.

Patent Landscape and Related Patents

• Parent Family and Filing Timeline
  The patent family includes applications filed internationally, notably in Europe (EP 0451 643 B1, granted 1997), Japan, and Canada. The initial U.S. application was filed August 18, 1992, with the patent granted in 1993.

• Follow-on Patents and Patent Term Extensions
  Subsequent patents (e.g., U.S. Patent 7,350,344) extended protection by claiming new formulations, dosages, or methods, particularly related to combination therapies with aspirin or other antiplatelet agents.

• Patent Challenges and Litigation
  The patent was subject to legal disputes concerning patent validity, primarily over claims related to the compound and its use. Patent litigation continued until patent expiration in 2011, with subsequent litigation over process patents and formulations.

• Patent Expiry and Generics Entry
  The 2011 patent expiration allowed generic manufacturers to produce clopidogrel hydrochloride, significantly reducing treatment costs.

Patent Landscape Summary	Patent Number	Filing Year	Issue Year	Focus Area	Status
5,215,755	1992	1993	Composition, use, formulations	Expired 2011
7,350,344	2002	2008	Combination therapies, formulations	Active until 2028 (extensions)
6,030,856	1994	2000	Methods of synthesis	Expired
EP 0451 643 B1	1996	1997	European patent on compound and use	Expired

Key Patent Strategies Observed

• Broad composition claims to prevent generic copying of the active molecule.
• Follow-on patents to extend market exclusivity via formulation or use patents.
• Continuous litigation to defend claims against challenges, ensuring market protection until early 2010s.

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Key Takeaways

• U.S. Patent 5,215,755 crucially protected clopidogrel's chemical and therapeutic claims until 2011.
• Its broad claims over the compound and specific use methods set a high barrier for generic entry during patent life.
• The patent family expanded through filings internationally and follow-on patents targeting formulations, combination therapies, and synthesis methods.
• Patent litigation and strategic patent filings extended market exclusivity until patent expiration.
• Post-2011, the market transitioned to generics, with significant cost reductions and widespread adoption.

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FAQs

1. What was the primary focus of U.S. Patent 5,215,755?
   It protected the chemical structure of clopidogrel, its related salts, uses in preventing clot formation, and formulations.

2. When did the patent expire, and what was the impact?
   Expired in 2011, opening the market for generic manufacturers, decreasing drug costs.

3. Did the patent family extend protection beyond 2011?
   Yes, through subsequent patents covering formulations and combination therapies, extending market exclusivity until around 2028.

4. How did patent litigation influence the patent landscape?
   Litigation affirmed patent validity and protected market share until patent expiration, discouraging counterfeit or generic entry prior to 2011.

5. Are there any active patents related to clopidogrel today?
   No patents similar in scope to the original patent are active; newer patents focus on formulations for specific indications or delivery methods but are not core to the original compound's patent.

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References

[1] USPTO, Patent No. 5,215,755, June 15, 1993.
[2] European Patent Office, EP 0451 643 B1, granted 1997.
[3] United States Patent and Trademark Office, Patent Family Digital Collection.
[4] Legal case summaries on clopidogrel patent litigations, 2000–2011.

Drugs Protected by US Patent 5,215,755

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 5,215,755

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Austria	129406
Australia	6018190
Australia	646399
Canada	2022640
Canada	2063141
Germany	69023183
European Patent Office	0411952