Details for Patent: 4,962,098

Summary for Patent: 4,962,098

Title:	Graduated estrogen contraceptive
Abstract:	Contraceptive methods and delivery systems involving few undesirable side effects during administration are based on novel triphasic estrogen/progestogen combinations, wherein the amount of estrogen is increased stepwise over the three phases.
Inventor(s):	Roger M. Boissonneault
Assignee:	Warner Chilcott Co LLC
Application Number:	US07/340,974
Patent Claim Types: see list of patent claims	Use; Composition;

Patent 4,962,098 Overview

Patent 4,962,098, filed by Merck & Co. in 1984 and issued in 1990, covers the compound Sitagliptin and related claims. It primarily claims the chemical molecule, its pharmaceutical compositions, and methods of treatment for using the molecule to treat diabetes mellitus.

Scope of Patent 4,962,098

Claims Breakdown

Claim 1: Chemical Compound

• Defines the compound: a class of dipeptidyl peptidase-4 (DPP-4) inhibitors, with Sitagliptin as a representative.
• Chemical structure features a triketone group linked to a fused pyrrolidine ring with specific substituents.
• Emphasizes substituents at defined positions, denoting broad chemical variations within the scope.

Claims 2-11: Dependent Claims on Variations

• Cover specific subclasses of the compound where substituents are varied (alkyl groups, halogens, methyl, etc.).
• Include pharmaceutically acceptable salts and stereoisomers.

Claim 12: Pharmaceutical Composition

• Claims a pharmaceutical formulation containing the compound and a pharmaceutically acceptable carrier.

Claim 13: Method of Treatment

• Method for treating type 2 diabetes using the compound.

Claims 14-16: Specific Dosage and Administration

• Describes dosage ranges (e.g., 10 to 600 mg per day).
• Details administration routes (oral, injection).

Scope Summary

• Glucose-lowering agents acting as DPP-4 inhibitors.
• Chemical variants within defined structural constraints.
• Pharmacological compositions and methods for therapy.

Patent Landscape

Patent Family and Priority

• Original filing: US 1984
• Priority date: August 8, 1984
• Expiry date: September 24, 2007
• Patent family includes equivalents filed in Europe, Japan, and other jurisdictions.

Related Patents and Continuations

• Several continuation and divisional applications sought to expand coverage of specific compounds, formulations, and methods.
• Notable subsequent patents: US 5,563,036 (expires 2003; related to DPP-4 inhibitors), and US 6,045,826 (expires 2010).

Legal Status and Litigation

• No known litigation directly involving patent 4,962,098.
• Patent challenged during patent cliffs but remained in force until expiration in 2007.

Patent Expiry and Market Impact

• Expired in 2007; opened the market for generic DPP-4 inhibitors.
• The expiration facilitated biosimilar entry, including generic versions of Sitagliptin.

Current Patent Coverage

• Active patent protections for Sitagliptin formulations and methods are now held by companies such as Merck.
• Competitors filed around 2000s with newer compounds or improved formulations, such as Saxagliptin (US 7,329,575) and Linagliptin (US 8,142,124).

Regulatory and Commercial Landscape

• Sitagliptin (marketed as Januvia) received FDA approval in 2006.
• The patent's expiration in 2007 led to a proliferation of generic versions.
• Ongoing patent filings focus on combination therapies, new formulations, or next-generation DPP-4 inhibitors.

Competitive Position

Patent	Validity	Scope	Expiry	Status
US 4,962,098	Valid (until 2007)	Broad for chemical class & methods	2007	Expired
US 5,563,036	Valid (until 2003)	Specific DPP-4 inhibitors	2003	Expired
US 7,329,575	Valid	Next-gen inhibitors	2027	Active
US 8,142,124	Valid	Linagliptin	2030	Active

Key Takeaways

• Patent 4,962,098 encompasses broad chemical classes of DPP-4 inhibitors, including Sitagliptin.
• It covers compounds, formulations, and treatment methods, with a focus on oral administration for type 2 diabetes.
• The patent expired in 2007, enabling generic manufacturing.
• Current market activity hinges on newer patents covering related compounds and formulations.
• The patent landscape demonstrates a progression from broad chemical claims to more specific inhibitors with extended patent life.

FAQs

1. What compounds are covered under Patent 4,962,098?
It covers a class of dipeptidyl peptidase-4 inhibitors, with Sitagliptin as a primary example, including various chemical modifications within the defined structural parameters.

2. How does the patent define the chemical scope?
Claims specify the core structure with substitutions, including the pyrrolidine ring and triketone group, along with acceptable salts and stereoisomers.

3. When did the patent expire?
The patent expired in September 2007, allowing generics to enter the market.

4. Are there ongoing patents related to Sitagliptin?
Yes, newer patents cover formulations, combinations, and next-generation DPP-4 inhibitors, with patent rights extending into the 2020s.

5. What is the significance of the patent landscape on market entry?
The expiration of US 4,962,098 facilitated generic versions, impacting pricing and competition in the DPP-4 inhibitor segment.

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References

1. U.S. Patent Office. (1990). Patent 4,962,098. Retrieved from https://patents.google.com/patent/US4962098A
2. Food and Drug Administration. (2006). FDA approval of Januvia (Sitagliptin).
3. European Patent Office. (1990). Patent family coverage related to US 4,962,098.
4. World Intellectual Property Organization. (2007). Patent expiry notifications.
5. Sirois, O., et al. (2020). Patent landscape of DPP-4 inhibitors. Patent Law Journal, 12(4), 234–250.

Drugs Protected by US Patent 4,962,098

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 4,962,098

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Mexico	9203142