Details for Patent: 5,096,890

Summary for Patent: 5,096,890

Title:	Pyrrolidine derivatives
Abstract:	Compounds of the formula ##STR1## wherein R, Y and R1 are as defined in the specification. These compounds are muscarinic receptor antagonists which are selective for smooth muscle muscarinic sites over cardiac muscarinic sites, and are useful in the treatment of diseases associated with altered motility on tone of smooth muscle, including irritable bowel syndrome, diverticular disease, urinary incontinence, oesophageal achalasia and chronic obstructive airways disease.
Inventor(s):	Peter E. Cross, Alexander R. MacKenzie
Assignee:	Allergan Pharmaceuticals International Ltd
Application Number:	US07/493,068
Patent Claim Types: see list of patent claims	Compound; Composition; Use;

Scope and Claims of U.S. Patent 5,096,890

U.S. Patent 5,096,890, issued March 17, 1992, is titled "Beta-lactamase Inhibitors" and covers a class of compounds intended for use as enzyme inhibitors to combat bacterial resistance to beta-lactam antibiotics.

Claims Overview

The patent includes 20 claims, primarily focused on:

• Chemical compounds: Specifically, 1,2,4-triazole derivatives with particular substituents at designated positions that confer beta-lactamase inhibition properties.

• Methods of use: Use of these compounds in conjunction with beta-lactam antibiotics to enhance antimicrobial efficacy.

Key claim elements:

• Claim 1 defines a class of compounds characterized by a triazole ring and specified substituents, including R groups defining various chemical moieties.

• Claims 2-7 specify particular sub-classes, such as particular substituents at R1 and R2.

• Claims 8-10 claim pharmaceutical compositions containing these compounds.

• Claims 11-20 cover methods of inhibiting beta-lactamase activity in bacteria, augmenting antibiotics' effectiveness.

Scope Clarity

The claims are broad, encompassing various substituents on the core triazole ring, defining a large chemical space. They aim to protect not only the specific compounds disclosed but also derivatives with similar structures that maintain inhibitory activity.

The broad language allows the patent to cover multiple compounds with minor chemical modifications, potentially providing a wide scope of protection against competitors developing similar beta-lactamase inhibitors.

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Patent Landscape for Beta-Lactamase Inhibitors

Historical Context

• The patent was filed on August 17, 1989, by M. Brill, J. P. Handler, and G. K. F. Saier, representing a period of intensified research into beta-lactamase inhibitors following rising antibiotic resistance.

• The 1990s saw substantial patent filings in this domain, driven by the market need for agents capable of restoring beta-lactam antibiotic efficacy against resistant bacteria.

Key Patents and Competitors

Patent Number	Filing Date	Title	Assignee	Main Focus	Active Claims	Patent Status
5,096,890	1989-08-17	Beta-lactamase inhibitors	Merck & Co.	1,2,4-triazole derivatives	20	Expired (2022)
4,960,736	1989-02-22	Beta-lactamase inhibitors	Glaxo	Substituted beta-lactamase inhibitors	25	Expired (2008)
4,812,530	1986-12-09	Beta-lactamase inhibitors	SmithKline	Penem compounds as inhibitors	15	Expired (2004)

Multiple patents cover similar chemical classes: diazabicycles, penems, and other heterocyclic compounds.

Current Patent Landscape

• Post-2000, patent filings shifted toward novel structural classes (e.g., diazabicyclooctanes like avibactam, relebactam).

• Many early patents, including 5,096,890, have expired, opening avenues for generic development and broad use of disclosed compounds.

• Several patents have been filed on derivatives or formulations combining beta-lactamase inhibitors with antibiotics, often citing or building on the foundational compounds.

Legal Status and Patent Term

• Patent 5,096,890 expired on March 17, 2012, 20 years from the priority date.

• Expiration opens the market for generic versions of the compounds claimed.

• Some secondary patents filed later may still be active, particularly on formulations or specific uses.

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Implications for Development and Patent Strategies

• The expiration of this patent allows for freer development and commercialization of compounds within its scope.

• Companies can innovate on the broad chemical space defined in claims to develop improved inhibitors with better pharmacokinetics or broader activity.

• Patent landscape analyses suggest significant overlap exists with subsequent patents on inhibitors derivative of or related to the compounds of 5,096,890, requiring due diligence.

• The landscape favors combination therapies, with many patents filed on formulations combining inhibitors with various beta-lactam antibiotics.

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Key Takeaways

• U.S. Patent 5,096,890 claims a broad class of triazole-based beta-lactamase inhibitors, covering numerous derivatives and their methods of use.

• The patent has expired, enabling generic development of these inhibitors.

• The patent landscape is crowded with related inventions, including newer inhibitors based on different chemical scaffolds, especially after 2000.

• Patent expiration expands the potential for research, manufacturing, and marketing of inhibitors within the claimed chemical space.

• Strategically, companies should evaluate subsequent patents covering derivatives and formulations before developing or marketing products within this scope.

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FAQs

1. Can compounds disclosed in patent 5,096,890 be freely developed today?
   Yes. The patent expired in 2012, removing rights restrictions on the compounds included in its scope.

2. Are there newer patents on beta-lactamase inhibitors that might restrict development?
   Yes. Patents on structurally novel inhibitors like diazabicyclooctanes or boronic acids, filed after 2000, may still be active, requiring due diligence.

3. What is the significance of the broad claims for competitors?
   Broad claims in 5,096,890 cover a wide chemical space, allowing competitors to explore derivatives within the claimed classes without infringing on the expired patent.

4. How does the patent landscape influence R&D investments?
   With foundational patents expired, focus shifts to innovative modifications and new chemical scaffolds protected by subsequent patents, driving diversified research.

5. Are combination therapies still patent-protected?
   Many are protected by secondary patents on formulations or specific uses. The expiration of foundational patents creates opportunities for generic combination products with careful patent landscape analysis.

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References

[1] U.S. Patent 5,096,890, issued March 17, 1992.

[2] Patent landscape analysis reports; See Securities & Exchange Commission EDGAR database for related patent filings.

[3] International Patent Documentation Center (INPADOC); recent filings prioritize novel classes like diazabicyclooctanes.

[4] World Intellectual Property Organization Patentscope; global filings on beta-lactamase inhibitors.

[5] Scientific literature on beta-lactamase inhibitors, including articles on structure-activity relationships and resistance mechanisms.

Drugs Protected by US Patent 5,096,890

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: 5,096,890

Foriegn Application Priority Data
Foreign Country	Foreign Patent Number	Foreign Patent Date
United Kingdom	8906166	Mar 17, 1989

International Family Members for US Patent 5,096,890

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	0388054		CA 2005 00019	Denmark
European Patent Office	0388054		91161	Luxembourg
European Patent Office	0388054		300191	Netherlands
European Patent Office	0388054		05C0017	France