Details for Patent: 5,399,578

Summary for Patent: 5,399,578

Title:	Acyl compounds
Abstract:	Compounds of the formula ##STR1## in which R.sub.1 is an aliphatic hydrocarbon radical which is unsubstituted or substituted by halogen or hydroxyl, or a cycloaliphatic or araliphatic hydrocarbon radical; X.sub.1 is CO, SO.sub.2, or --O--C(.dbd.O)-- with the carbon atom of the carbonyl group being attached to the nitrogen atom shown in formula I; X.sub.2 is a divalent aliphatic hydrocarbon radical which is unsubstituted or substituted by hydroxyl, carboxyl, amino, guanidino or a cycloaliphatic or aromatic radical, or is a divalent cycloaliphatic hydrocarbon radical, it being possible for a carbon atom of the aliphatic hydrocarbon radical to be additionally bridged by a divalent aliphatic hydrocarbon radical; R.sub.2 is carboxyl which, if desired, is esterified or amidated, substituted or unsubstituted amino, formyl which, if desired, is acetalized, 1H-tetrazol-5-yl, pyridyl, hydroxyl which, if desired, is etherified, S(O).sub.m --R where m is 0, 1 or 2 and R is hydrogen or an aliphatic hydrocarbon radical, alkanoyl, unsubstituted or N-substituted sulfamoyl or PO.sub.n H.sub.2 where n is 2 or 3; X.sub.3 is a divalent aliphatic hydrocarbon; R.sub.3 is carboxyl, 5-tetrazolyl, SO.sub.3 H, PO.sub.2 H.sub.2, PO.sub.3 H.sub.2 or haloalkylsulfamoyl; and the rings A and B independently of one another are substituted or unsubstituted; in free form or in salt form, can be prepared in a manner known per se and can be used, for example, as medicament active ingredients.
Inventor(s):	Buhlmayer; Peter (Arlesheim, CH), Ostermayer; Franz (Riehen, CH), Schmidlin; Tibur (Basel, CH)
Assignee:	Ciba-Geigy Corp (Ardsley, NY)
Application Number:	07/998,755
Patent Claim Types: see list of patent claims	Compound; Composition; Use;

United States Patent 5,399,578: A Detailed Analysis of Scope, Claims, and Patent Landscape

Introduction

United States Patent 5,399,578, titled "Acyl compounds," is a significant patent that has played a crucial role in the pharmaceutical industry, particularly in the development and marketing of angiotensin II receptor blockers. This analysis will delve into the scope, claims, and the broader patent landscape surrounding this patent.

Background and Priority Date

The patent was filed on August 19, 1991, and granted on March 21, 1995. It was assigned to Eidp Inc. and Bristol Myers Squibb Pharma Co.[5].

Scope of the Patent

The patent relates to specific acyl compounds, particularly those that act as angiotensin II receptor blockers. Angiotensin II is a potent vasoconstrictor that plays a key role in blood pressure regulation, and blocking its receptors can help in treating hypertension and other cardiovascular conditions.

Chemical Structure and Compounds

The patent describes compounds of a specific formula, including various substitutions and salts. These compounds are designed to interact with the angiotensin II receptor, thereby inhibiting its action and reducing blood pressure[4].

Claims of the Patent

The patent includes several claims that define the scope of protection for the invented compounds.

Independent Claims

• Claim 1 typically defines the broadest scope of the invention, specifying the general structure of the acyl compounds and their salts.
• Subsequent claims may narrow down the scope by specifying particular substitutions or modifications to the core structure.

Dependent Claims

• These claims build upon the independent claims, often adding additional limitations or specific examples of compounds that fall within the broader scope defined by the independent claims.

Patent Landscape and Related Patents

The patent landscape surrounding U.S. Patent 5,399,578 includes several related patents and litigation histories.

Related Patents

• Other patents, such as U.S. Patent Nos. 6,294,197 and 6,395,728, also cover follow-on compounds or methods related to angiotensin II receptor blockers. These patents were part of the litigation in cases like In re Novartis & Par Antitrust Litig[2].

Litigation History

• The patent was central to antitrust litigation involving Novartis and Par Pharmaceuticals. The allegations included claims that Novartis and Par entered into an unlawful settlement agreement to delay the entry of generic versions of Exforge, a medication containing valsartan, which is covered by this and related patents[2].

Expiration and Regulatory Exclusivity

• The patent expired on March 21, 2012. Additionally, a regulatory exclusivity period attached to the patent expired on September 21, 2012. This marked the earliest possible date for generic versions to enter the market, assuming no other legal or regulatory barriers[2].

Impact on Generic Market Entry

• The expiration of this patent and related regulatory exclusivities allowed generic manufacturers to file Abbreviated New Drug Applications (ANDAs) with the FDA. For example, Par Pharmaceuticals' ANDA was tentatively approved on March 19, 2010, and finally approved on March 28, 2013, after resolving legal disputes[2].

Antitrust Implications

• The settlement agreement between Novartis and Par was alleged to have delayed generic competition, extending the monopoly period for Novartis' branded product. This led to antitrust claims and litigation, highlighting the complex interplay between patent law and antitrust regulations[2].

Patent Analytics and Claim Coverage

• To manage and analyze the extensive patent portfolio related to these compounds, companies often use patent analytics tools. These tools help in tracking patents by claims and scope concepts, identifying gaps in coverage, and highlighting future design opportunities[3].

Claim Charts and Scope Concepts

• Tools like ClaimScape® software generate interactive claim charts that help technical experts determine whether a particular scope concept is applicable to a target product or method. This aids in identifying high-value claims, potential future directions, and areas where claim coverage may be lacking[3].

Secondary Considerations and Obviousness

• In patent litigation, secondary considerations such as commercial success, long-felt but unsolved needs, and failure of others can be crucial in determining the nonobviousness of the invention. These considerations help mitigate hindsight bias and provide a more comprehensive view of the invention's novelty and utility[1].

Key Takeaways

• U.S. Patent 5,399,578 covers specific acyl compounds used as angiotensin II receptor blockers.
• The patent's expiration and regulatory exclusivity periods significantly impacted the timing of generic market entry.
• Antitrust litigation highlighted the importance of monitoring settlement agreements to prevent anti-competitive practices.
• Patent analytics tools are essential for managing and analyzing extensive patent portfolios related to pharmaceutical compounds.

Frequently Asked Questions (FAQs)

1. What is the primary use of the compounds described in U.S. Patent 5,399,578?

The compounds described in this patent are primarily used as angiotensin II receptor blockers to treat hypertension and other cardiovascular conditions.

2. When did U.S. Patent 5,399,578 expire?

The patent expired on March 21, 2012, with a regulatory exclusivity period ending on September 21, 2012.

3. What was the nature of the antitrust litigation involving this patent?

The antitrust litigation involved allegations that Novartis and Par Pharmaceuticals entered into an unlawful settlement agreement to delay the entry of generic versions of Exforge, thereby extending Novartis' monopoly period.

4. How do patent analytics tools help in managing patent portfolios?

Patent analytics tools help in tracking patents by claims and scope concepts, identifying gaps in coverage, and highlighting future design opportunities through interactive claim charts.

5. What are secondary considerations in patent litigation, and why are they important?

Secondary considerations include commercial success, long-felt but unsolved needs, and failure of others. These are important because they help determine the nonobviousness of an invention and mitigate hindsight bias.

Sources:

1. In re Entresto Sacubitril/Valsartan Patent Litig. - Casetext
2. In re Novartis & Par Antitrust Litig. - Casetext
3. Patent Analytics | Intellectual Property Law - SLWIP
4. US5399578A - Acyl compounds - Google Patents
5. US-5399578-A - Acyl Compounds - Unified Patents Portal

Drugs Protected by US Patent 5,399,578

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: 5,399,578

Foriegn Application Priority Data
Foreign Country	Foreign Patent Number	Foreign Patent Date
Switzerland	518/90	Feb 19, 1990
Switzerland	2234/90	Jul 05, 1990

International Family Members for US Patent 5,399,578

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	0443983		91347	Luxembourg
European Patent Office	0443983		C00443983/02	Switzerland
European Patent Office	0443983		C300445	Netherlands
European Patent Office	0443983		CA 2010 00014	Denmark
European Patent Office	0443983		91676	Luxembourg
European Patent Office	0443983		C970001	Netherlands