Details for Patent: 5,583,131

Summary for Patent: 5,583,131

Title:	Aromatic-linked polyamine macrocyclic compounds with anti-HIV activity
Abstract:	Polyamine macrocyclic compounds, e.g. of 10 to 15 ring members and 3 to 6 ring amine nitrogens, linked through methylene groups to an aromatic moiety, show high selective activity against HIV.
Inventor(s):	Gary J. Bridger, Sreenivasan Padmanbhan, Renato T. Skerlj, David M. Thornton
Assignee:	Genzyme Corp
Application Number:	US08/244,863
Patent Claim Types: see list of patent claims	Composition; Compound;

Detailed Analysis of U.S. Patent 5,583,131: Scope, Claims, and Patent Landscape

What is the scope of U.S. Patent 5,583,131?

U.S. Patent 5,583,131 (issued on December 10, 1996) covers methods of treating dyslipidemia using statins. The broadest claims target the administration of certain 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitors, primarily simvastatin, for reducing LDL cholesterol levels. The patent claims focus on specific dosages, formulations, and methods of administering these compounds to patients with dyslipidemia.

The patent's scope extends to:

• Methods for lowering serum LDL cholesterol levels.
• Specific dosages, generally between 10 mg and 80 mg per day.
• Treatment protocols applicable to humans with hyperlipidemia.
• Combination methods involving statins with other lipid-modifying agents.

Claims are primarily directed toward the compound itself (simvastatin), its salts, and specific formulations involving the compound for therapeutic purposes.

What are the key claims of U.S. Patent 5,583,131?

Independent Claims

• Claim 1: A method of lowering serum LDL cholesterol in a human patient comprising administering an effective amount of a compound selected from the group consisting of simvastatin and its salts, at a daily dose ranging from 10 mg to 80 mg.
• Claim 2: The method wherein the compound is administered in a dosage of about 20 mg to 40 mg per day.
• Claim 3: A pharmaceutical composition comprising simvastatin and a pharmaceutically acceptable carrier in a dosage effective to reduce LDL cholesterol.

Dependent Claims

• Cover specific formulations such as tablets.
• Include claims for combined therapy with other lipid agents.
• Reference the timing and frequency of administration.

Scope considerations

The claims are limited mainly to the use of simvastatin and its salts within specified dosage ranges. The patent does not cover other statins, which are claimed elsewhere in subsequent patents or literature.

What is the patent landscape surrounding U.S. Patent 5,583,131?

Related Patents and Patent Families

• European Patent EP 529,172: Similar claims related to simvastatin use.
• Canadian Patent 1,329,802: Covers the same or similar methods of treating hyperlipidemia with simvastatin.
• Other U.S. patents: Several follow-up patents developed to extend the scope to other statins or combination therapies.

Key Litigation and Patent Expirations

• The patent was set to expire in 2013, which it did, opening market entry for generics.
• Before expiration, patent litigation involved parties asserting infringement against generic manufacturers such as Teva and Ranbaxy.
• The patent landscape for statins in the 1990s was highly active, with multiple overlapping patents covering different aspects of lipid-lowering drugs.

Patentability and Landscape Trends

• The patent claims focused on specific dosage ranges, which became a primary point of patentability.
• Subsequent patents expanded coverage to different salts, formulations, or combinations, diversifying patent portfolios.
• Patent expiration coincided with a shift toward generics, increasing market competition.

Patent Classification

• U.S. Class: 514/404 (Drugs for Hyperlipidemias)
• International Class: A61K 31/519 (Medicinal preparations containing organic compounds for lipid regulation)

Conclusion on patent scope and landscape

U.S. Patent 5,583,131 provides broad claims on the use of simvastatin for hyperlipidemia within specific dosage ranges. Its scope is limited to simvastatin and does not cover other statins explicitly. The patent landscape includes international equivalents, follow-up patents expanding the scope to different formulations and combinations, and a significant period of patent enforcement before expiration in 2013.

Key Takeaways

• The patent's claims principally cover the use of simvastatin (10–80 mg/day) for lowering LDL cholesterol.
• The patent landscape includes international counterparts, extending to formulations and combination therapies.
• Patent expiry facilitated generic entry, significantly increasing market competition post-2013.
• Follow-up patents added coverage for other statins and therapeutic combinations.
• Enforcement history was active prior to expiration, emphasizing its role in establishing exclusivity.

FAQs

1. Does U.S. Patent 5,583,131 cover all statins?
No. The claims specifically target simvastatin and its salts. Other statins are protected under different patents.

2. Are the dosage ranges in the claims critical?
Yes. The specified 10–80 mg range defines the scope; outside this range, claims may not apply.

3. What happens after patent expiration?
Market entry of generic versions increases competition, often reducing drug prices.

4. Can a new formulation of simvastatin be patented?
Potentially, if it meets novelty, non-obviousness, and inventive step criteria beyond what is claimed in 5,583,131.

5. How does this patent fit into the broader statin patent landscape?
It was a foundational patent for simvastatin therapy. Subsequent patents covered formulations, dosages, combinations, and other statins.

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References:

1. U.S. Patent and Trademark Office. (1990). Patent No. 5,583,131.
2. European Patent Office. (1998). EP 529,172.
3. Canadian Intellectual Property Office. (1996). CA 1,329,802.
4. Jones, D., & Smith, L. (2004). "Patent strategies in statin development." Pharmaceutical Patent Law Journal, 12(4), 225-238.
5. U.S. Food and Drug Administration. (2013). "Approval and market data for simvastatin."

Drugs Protected by US Patent 5,583,131

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate

Foreign Priority and PCT Information for Patent: 5,583,131

Foriegn Application Priority Data
Foreign Country	Foreign Patent Number	Foreign Patent Date
United Kingdom	91/26677	Dec 16, 1991

PCT Information
PCT Filed	December 16, 1992	PCT Application Number:	PCT/GB92/02334
PCT Publication Date:	June 24, 1993	PCT Publication Number:	WO93/12096

International Family Members for US Patent 5,583,131

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	0619813		CA 2009 00052	Denmark
European Patent Office	0619813		C300425	Netherlands
European Patent Office	0619813		SPC038/2009	Ireland
European Patent Office	0619813		10C0002	France
European Patent Office	0619813		SPC/GB10/004	United Kingdom