United States Patent 6,162,802: Claim Scope, Expiration, Orange Book Status, and Patent Landscape for Lotrel

US Patent 6,162,802 covers fixed-dose and co-administered combinations of benazepril and amlodipine, including the marketed Lotrel combination. Its core limitations are the therapeutic pairing, dose ranges, benazepril-to-amlodipine ratio, and physical separation of the two active ingredients in certain dosage forms. The patent issued on December 19, 2000, from a priority chain beginning April 30, 1996, and its ordinary patent term ended in 2017. It is no longer an enforceable barrier to generic entry.

What does US Patent 6,162,802 protect?

The patent protects two related subject-matter groups:

Methods of treating specified cardiovascular, renal, vascular, and neurological conditions by administering benazepril and amlodipine.
Pharmaceutical compositions containing the two agents in physically separated form.

The protected combination is based on:

Element	Claimed requirement
ACE inhibitor	Benazepril, free form or pharmaceutically acceptable salt
Calcium-channel blocker	Amlodipine, free form or pharmaceutically acceptable salt
Benazepril dose	2 to 80 mg, expressed as benazepril hydrochloride
Amlodipine dose	1 to 20 mg, expressed as amlodipine free base
Weight ratio	1:1 to 8:1 benazepril hydrochloride to amlodipine free base
Covered conditions	Hypertension, congestive heart failure, angina, myocardial infarction, atherosclerosis, diabetic nephropathy, diabetic cardiac myopathy, renal insufficiency, peripheral vascular disease, left ventricular hypertrophy, cognitive dysfunction, stroke, and headache
Physical separation	Required by composition claim 19 and related claims
Preferred salts	Benazepril hydrochloride and amlodipine besylate
Preferred doses	5 to 20 mg benazepril hydrochloride and 2.5 to 5 mg amlodipine free base
Exemplary commercial strength	20 mg benazepril hydrochloride plus amlodipine corresponding to 5 mg free base
Dosage-form embodiment	Capsule containing a coated compressed benazepril tablet and amlodipine powder

The claims do not cover benazepril or amlodipine individually. They cover their use or combination within the specified quantitative parameters.

How are the claims organized?

Method claims 1-18

Claim 1 is the principal method claim. It requires:

Treatment of a listed condition in a human;
Administration of benazepril and amlodipine;
Daily doses within the stated ranges; and
A 1:1 to 8:1 weight ratio based on benazepril hydrochloride and amlodipine free base.

Dependent method claims narrow the scope by specifying:

A single dosage form;
Physical separation of the active ingredients;
Benazepril hydrochloride;
Amlodipine besylate;
Ratios of 1:1, 2:1, 4:1, or 8:1;
The 20 mg/5 mg strength;
Separate formulations administered within approximately one hour.

Claim 17 is commercially significant because it reaches separate benazepril and amlodipine formulations. A product does not necessarily avoid the method claims merely because the active ingredients are supplied in separate tablets. If the two products are administered as a regimen within the claimed dosing and timing parameters, claims 1 and 17-18 may be implicated, subject to ordinary infringement requirements.

Composition claims 19-33

Claim 19 is the principal composition claim. It requires:

A daily dose containing both active ingredients;
The same broad dose ranges and ratio range as claim 1; and
Physical separation of benazepril and amlodipine.

The dependent composition claims narrow the invention to:

Benazepril hydrochloride;
Amlodipine besylate;
Specific ratios;
Preferred dose ranges;
A capsule containing a coated benazepril tablet and amlodipine powder;
The 20 mg/5 mg commercial strength.

These claims are directed to the product architecture rather than the administration method. A product containing the two agents in separate internal compartments, layers, pellets, tablets, or powders could fall within the physical-separation limitations if the remaining dose and ratio requirements are met.

What is the scope of the ratio limitation?

The ratio is calculated using:

Benazepril hydrochloride mass; and
Amlodipine free-base equivalent mass.

The claimed ratio range is 1:1 to 8:1. The expressly identified ratios are:

Benazepril hydrochloride	Amlodipine free-base equivalent	Ratio
2 mg	2 mg	1:1
5 mg	2.5 mg	2:1
10 mg	2.5 mg	4:1
20 mg	5 mg	4:1
20 mg	2.5 mg	8:1
20 mg	20 mg	1:1

The marketed 20 mg/5 mg combination is within the 4:1 ratio. A formulation using amlodipine besylate must be converted to its amlodipine free-base equivalent for claim analysis. The claim does not measure the mass of the besylate salt as if it were entirely active amlodipine.

The ratio limitation is potentially important for design-around analysis. A product outside the 1:1 to 8:1 range would not literally satisfy the ratio limitation, although equivalence arguments could have been relevant while the patent was enforceable. Because the patent has expired, those historical infringement issues have no current exclusionary effect.

What formulations are protected by US 6,162,802?

The claims cover more than a conventional blended tablet.

Physically separated combination products

Claim 19 requires the benazepril and amlodipine to be physically separated. Claim 29 identifies a specific embodiment:

A capsule;
A coated compressed tablet containing benazepril; and
Amlodipine powder inside the same capsule.

The physical-separation limitation may cover:

A tablet-in-capsule product;
Separate mini-tablets in a capsule;
A bilayer tablet;
Distinct coated particles;
A benazepril tablet and amlodipine powder in one capsule;
Other internally separated dosage forms meeting the claim language.

The patent does not require a particular coating material, release profile, excipient system, manufacturing sequence, or dissolution specification in the claims provided.

Separate formulations administered together

Claims 17 and 18 extend method coverage to a regimen in which:

Benazepril is supplied in a formulation free of amlodipine;
Amlodipine is supplied in a formulation free of benazepril; and
The two formulations are administered within about one hour.

This creates a broader method layer than the physically separated composition claims. A generic manufacturer supplying two separate products would need to assess not only the composition claims but also the prescribing, labeling, and induced-infringement implications of any still-enforceable method claim. That concern is historical for this patent because the patent term has ended.

Is claim 3 internally defective?

The claim text supplied contains a dependency inconsistency. Claim 3 states that it depends on claim 7, while claim 7 depends on claim 6 and ultimately on claim 1. That creates an apparent circular or procedurally improper dependency because claim 3 is positioned as an earlier claim but refers to claim 7.

The issued patent and its prosecution history should control the legally operative claim text. A claim reproduced from a database, OCR source, or amended document may contain a typographical or transcription error. The apparent dependency problem does not change the central scope of the patent, which is defined principally by claims 1 and 19 and their valid dependent claims.

When did US Patent 6,162,802 expire?

Event	Date
Earliest identified priority date	April 30, 1996
US patent filing chain	1997
Issue date	December 19, 2000
Expected 20-year term endpoint	April 30, 2017
Potential pediatric extension	Requires confirmation from the FDA patent listing and regulatory record
Current enforceability	Expired

The patent’s ordinary term was tied to the 1996 priority and 1997 US/PCT filing chain. A patent-term calculation should distinguish between:

Expiration under the 20-year patent term;
Patent-term adjustment for USPTO delay;
Patent-term extension under 35 U.S.C. § 156; and
Pediatric exclusivity under the FD&C Act.

The patent was associated with the Lotrel product and was historically relevant to generic approval strategy. Any pediatric extension, if applicable, would have extended regulatory exclusivity rather than created a new ordinary patent term. The patent is no longer a current patent barrier.

What is the Orange Book status of Lotrel and US 6,162,802?

Lotrel is the branded combination of amlodipine besylate and benazepril hydrochloride. Novartis marketed Lotrel in multiple strengths, including combinations corresponding to:

2.5 mg amlodipine/10 mg benazepril;
5 mg amlodipine/10 mg benazepril;
5 mg amlodipine/20 mg benazepril;
5 mg amlodipine/40 mg benazepril;
10 mg amlodipine/20 mg benazepril;
10 mg amlodipine/40 mg benazepril.

The commercial strength most directly reflected in the claims supplied is 5 mg amlodipine with 20 mg benazepril, corresponding to a 4:1 ratio.

The FDA Orange Book historically listed patents associated with Lotrel and its combination product. Orange Book listings are regulatory certifications used in abbreviated new drug applications, not conclusive determinations of patent validity or infringement. Because US 6,162,802 expired in 2017, it does not presently create a live Paragraph IV barrier.

What Paragraph IV challenges affected Lotrel?

Generic applicants seeking approval before expiration of listed Lotrel patents could file Paragraph IV certifications alleging that listed patents were invalid, unenforceable, or not infringed. The commercial dispute around Lotrel involved the usual combination-product issues:

Whether a generic product fell within the listed composition claims;
Whether separate tablets implicated method claims;
Whether the listed claims were valid over earlier combination therapy disclosures;
Whether the claims were obvious in view of benazepril and amlodipine monotherapy data;
Whether formulation and physical-separation limitations were independently patentable;
Whether an ANDA filing triggered the 30-month stay under 21 U.S.C. § 355(j)(5)(B)(iii).

A Paragraph IV notice is not itself proof of invalidity. The litigation consequences depended on the patent’s Orange Book listing, the timing of the ANDA, the asserted claims, and any settlement or consent judgment.

The passage of the patent term eliminates the current litigation risk associated with US 6,162,802. Historical Paragraph IV disputes may remain relevant for market-entry chronology, settlement analysis, and damages exposure, but not for present-day exclusion.

Which companies challenged the Lotrel patent estate?

The Lotrel generic market included ANDA applicants and generic manufacturers seeking approval for amlodipine/benazepril products. Public records associated with the product may include companies such as:

Teva Pharmaceuticals;
Dr. Reddy’s Laboratories;
Mylan;
Sandoz;
Watson/Actavis;
Apotex; and
Other ANDA sponsors.

The precise party involved depends on the particular patent, strength, ANDA number, and litigation year. A complete defendant-by-defendant litigation history cannot be reliably attributed to US 6,162,802 from the claim text alone. The legally relevant point is that the patent was part of the Lotrel combination-product estate and was subject to the generic certification and litigation framework applicable before expiration.

How strong was the patent estate for Lotrel?

The estate had moderate historical strength because it used several overlapping claim categories:

Estate layer	Scope	Commercial relevance
Combination method	Benazepril plus amlodipine for listed diseases	Broad therapeutic coverage
Dose and ratio	2-80 mg/1-20 mg and 1:1-8:1	Captured marketed strengths
Salt forms	Benazepril hydrochloride and amlodipine besylate	Matched commercial ingredients
Physical separation	Separate internal components	Protected product architecture
Capsule embodiment	Coated benazepril tablet plus amlodipine powder	Narrower but product-specific
Separate administration	Two formulations within about one hour	Extended method coverage

The principal vulnerability was likely obviousness. Benazepril and amlodipine were each known antihypertensive agents, and combination therapy using an ACE inhibitor and a calcium-channel blocker was a predictable therapeutic strategy. The patentee’s strongest arguments would have centered on the selected dose ratios, tolerability, blood-pressure control, reduction of adverse effects, and the formulation architecture.

The narrow physical-separation claims were potentially stronger against a product that copied the same capsule construction, but they were also easier to design around through a conventional co-formulated tablet or separate marketed dosage forms.

What was the role of formulation and manufacturing IP?

US 6,162,802 is primarily a combination therapy and product-architecture patent. It does not, based on the supplied claims, require:

A particular excipient;
A specified dissolution profile;
A sustained-release system;
A particular coating polymer;
A defined particle-size distribution;
A manufacturing process;
A stability threshold; or
A specific impurity limit.

The claim requiring a coated compressed benazepril tablet inside a capsule creates a manufacturing constraint, but the claims do not appear to claim the coating process itself. A competing manufacturer could have pursued:

A conventional bilayer tablet;
A homogeneous blend;
Separate tablets packaged together;
Separate dosage forms administered under a different regimen;
A ratio outside the claimed range; or
A different salt or formulation architecture, subject to the remaining claim elements.

The broader method claims reduced the value of a simple physical design-around while the patent was in force.

How does US 6,162,802 compare with competing Lotrel patents?

The Lotrel estate should be analyzed as a portfolio rather than as a single patent.

Patent type	Typical protection	Relationship to US 6,162,802
Core combination patent	Benazepril plus amlodipine	Directly overlapping
Formulation patent	Tablet, capsule, separation, stability, or release design	May narrow or supplement US 6,162,802
Method-of-use patent	Cardiovascular or renal treatment	May overlap claim 1
Salt or solid-state patent	Amlodipine besylate or benazepril hydrochloride form	Ingredient-specific
Manufacturing patent	Production, coating, granulation, or encapsulation	Process-focused
Regulatory exclusivity	FDA exclusivity periods	Separate from patent validity

US 6,162,802 is most important as a foundational combination patent. It does not necessarily capture every later formulation, polymorph, manufacturing, or method-of-use patent associated with Lotrel.

What generic launch risks existed?

Before expiration, generic launch risk depended on the product design and certification strategy.

Product risk

A generic was exposed if it used:

Benazepril and amlodipine within the claimed doses;
A ratio between 1:1 and 8:1;
Benazepril hydrochloride and amlodipine besylate;
A physically separated capsule;
The 20 mg/5 mg strength; or
Separate formulations promoted for administration within about one hour.

Regulatory risk

The ANDA sponsor faced:

Patent listing review;
Paragraph III or Paragraph IV certification;
Potential 30-month stay;
Labeling and induced-infringement analysis;
Strength-by-strength product review; and
Possible settlement restrictions.

Commercial risk

Lotrel genericization could affect:

Branded prescription volume;
Net sales and price realization;
Combination-product switching;
Separate-component substitution;
Pharmacy benefit-manager formulary placement; and
Revenue from higher-strength products.

Those risks were material before 2017. They are no longer attributable to US 6,162,802 because the patent has expired.

What patent litigation and settlements affect the patent today?

No current injunction, Paragraph IV stay, or enforceable settlement restriction can be based solely on an expired patent. Historical litigation and settlement agreements may have governed entry before expiration, but their commercial effect ended when the relevant patent and regulatory exclusivity periods ended.

A current competitor should focus on:

Unexpired continuation patents;
Later formulation patents;
Separate patents covering salts or solid forms;
FDA-approved labeling;
Trade secrets involving manufacturing;
Trademark and trade-dress issues; and
Any remaining regulatory exclusivity.

US 6,162,802 itself does not create a current patent litigation obstacle.

What is the geographic coverage of US 6,162,802?

The patent is a United States patent. Its enforceable rights were limited to the United States and its territories. Corresponding foreign applications may have produced rights in Europe, Canada, Japan, and other jurisdictions, but foreign family members require separate review for:

Grant status;
Claim scope;
National phase dates;
Patent-term calculations;
Supplementary protection certificates;
Opposition proceedings; and
Local litigation.

A US expiration date does not establish the expiration status of foreign counterparts.

What licensing deals are associated with the patent?

Lotrel was commercialized by Novartis, and the patent estate was associated with the branded combination product. The supplied information does not establish a specific license, assignment, co-development agreement, or settlement involving US 6,162,802. Patent ownership and licensing rights should be separated from product marketing rights because assignments may have occurred during prosecution or commercialization.

Key Takeaways

US 6,162,802 covers methods and compositions combining benazepril and amlodipine.
The central quantitative limitation is a 1:1 to 8:1 ratio of benazepril hydrochloride to amlodipine free base.
The claims capture the commercial 20 mg benazepril hydrochloride/5 mg amlodipine strength.
Composition claims require physical separation of the two active ingredients.
Method claims also reach separate benazepril and amlodipine formulations administered within about one hour.
Benazepril hydrochloride and amlodipine besylate are expressly identified embodiments.
The patent issued December 19, 2000, and its ordinary term ended in 2017.
The patent is expired and does not currently block generic or follow-on combination products.
Historical Paragraph IV litigation and settlement analysis remains relevant to market-entry history, not present enforcement.
Current diligence must focus on later patents, regulatory status, labeling, manufacturing IP, and foreign family members.

FAQs

Does US 6,162,802 cover generic Lotrel tablets?

It historically covered products meeting the claimed drug identities, doses, ratio, and physical-separation limitations. It no longer blocks generic Lotrel because the patent has expired.

Does the patent cover benazepril and amlodipine sold as separate tablets?

The composition claims generally require a single composition with physical separation, but method claims 17 and 18 reach separate formulations administered within about one hour under the claimed conditions.

Is amlodipine besylate measured by its total salt weight?

No. The claims express the amlodipine amount as the equivalent quantity of amlodipine free base. The benazepril comparator is expressed as benazepril hydrochloride.

Could a 20 mg/10 mg benazepril/amlodipine product fall within the ratio range?

Yes. A 20 mg benazepril hydrochloride dose and 10 mg amlodipine free-base equivalent dose produce a 2:1 ratio, which falls within the claimed 1:1 to 8:1 range, although the expired patent no longer creates current infringement exposure.

Does expiration of US 6,162,802 eliminate all IP risk for amlodipine/benazepril products?

No. It eliminates this patent as a current barrier. Other patents, trademarks, regulatory requirements, manufacturing rights, foreign patents, or later formulation patents may still require review.

References

United States Patent and Trademark Office. (2000). United States Patent No. 6,162,802: Pharmaceutical composition containing benazepril and amlodipine.
U.S. Food and Drug Administration. (2024). Approved drug products with therapeutic equivalence evaluations.
U.S. Food and Drug Administration. (2024). Orange Book: Approved drug products with therapeutic equivalence evaluations.
United States Code, 35 U.S.C. §§ 154, 156.
United States Code, 21 U.S.C. § 355(j).

Details for Patent: 6,162,802

Summary for Patent: 6,162,802