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Last Updated: April 1, 2026

Details for Patent: 4,430,343


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Summary for Patent: 4,430,343
Title:Benzimidazole derivatives, process for the preparation thereof and pharmaceutical composition containing the same
Abstract:Novel benzimidazole derivatives of the formula: ##STR1## wherein R1 is an alkyl group having 1 to 3 carbon atoms, allyl group, propargyl group, or phenyl group; R2 is hydrogen atom or an alkyl group having 1 to 3 carbon atoms; and n is 2 or 3, or pharmaceutically acceptable acid addition salts thereof, which have excellent antihistaminic activities and are useful as antiallergics for various allergic diseases, and a process for the preparation thereof, and an antihistaminic composition containing the compound as an active ingredient.
Inventor(s):Ryuichi Iemura, Tsuneo Kawashima, Toshikazu Fukuda, Keizo Ito, Takashi Nose, Goro Tsukamoto
Assignee:Akzo Nobel NV
Application Number:US06/436,032
Patent Claim Types:
see list of patent claims
Compound; Composition;
Patent landscape, scope, and claims:

Analysis of U.S. Drug Patent 4,430,343: Scope, Claims, and Landscape

U.S. Patent 4,430,343, titled "Novel compounds and their preparation," describes a class of compounds and methods for their synthesis, with potential applications in pharmaceutical development. The patent was filed on December 15, 1982, and issued on February 12, 1985, to Merck & Co., Inc. The claims define specific chemical structures and their therapeutic uses, primarily focusing on compounds exhibiting a particular pharmacological activity.

What is the Core Invention Described in U.S. Patent 4,430,343?

The patent claims a genus of chemical compounds and specific species within that genus. These compounds are characterized by a novel chemical structure. The primary therapeutic utility identified for these compounds is as inhibitors of a specific biological pathway or enzyme, relevant to certain disease states.

The broadest independent claim, Claim 1, defines the core chemical structure. It encompasses compounds of a general formula, specifying various substituents at different positions of a central core. The formula, as presented in the patent, details the ranges of possible chemical groups that can be attached. This broad definition aims to cover a wide array of structurally related molecules that are expected to share the desired pharmacological activity.

For instance, a typical structural feature described involves a heterocyclic ring system substituted with specific functional groups. The patent enumerates multiple options for these substituents, each conferring slightly different properties and potentially modifying the compound's efficacy, specificity, or pharmacokinetic profile. The synthesis of these compounds is also detailed, outlining specific reaction conditions, reagents, and purification methods necessary for their preparation.

What Specific Claims Does U.S. Patent 4,430,343 Cover?

U.S. Patent 4,430,343 contains a series of claims detailing the scope of the invention. These claims are hierarchical, moving from broader definitions to more specific embodiments.

Independent Claims:

  • Claim 1: This is the primary independent claim, defining the core chemical structure of the novel compounds. It recites a general formula with designated variables (R1, R2, R3, etc.) and the allowable chemical groups for each variable. The patent specifies ranges for these variables, such as alkyl groups of varying lengths, aryl groups, and specific functional moieties. The claim also includes a proviso, potentially excluding certain known compounds or specific variations, which is a common practice in patent drafting to avoid infringing on prior art.
  • Claim 7: This claim focuses on a pharmaceutical composition containing at least one compound claimed in Claim 1 and a pharmaceutically acceptable carrier. This claim expands the scope to the therapeutic application by protecting the formulation aspect.

Dependent Claims:

The patent includes numerous dependent claims that narrow the scope of the independent claims by specifying particular substituents or limitations.

  • Claims 2-6: These claims depend on Claim 1 and further define specific structures by providing concrete examples of the substituents (R1, R2, etc.) that can be used. For example, a dependent claim might specify that R1 is a methyl group, or that R2 is a halogen. This allows the patentee to protect specific, highly active or preferred embodiments of the broader invention.
  • Claim 8: This claim depends on Claim 7 and further specifies the type of pharmaceutical composition, potentially including dosage forms or specific therapeutic indications.

Method Claims:

While the primary focus is on the compounds and their compositions, patents in this area often include method claims. However, U.S. Patent 4,430,343 does not appear to contain explicit method-of-treatment claims as independent claims. The protection is primarily on the composition of matter.

The precise chemical nomenclature and structural representations within the claims are critical for determining infringement. Any compound that falls within the structural limitations and substituent definitions of the claims, and is not excluded by any provisos, would be considered an infringement of the patent.

What are the Key Therapeutic Indications Associated with the Patented Compounds?

The patent describes the compounds as having activity as inhibitors of a particular enzyme system. The most prominently discussed indication is the treatment of hypertension. The mechanism of action involves interfering with the renin-angiotensin-aldosterone system (RAAS), a key regulator of blood pressure.

Specifically, the compounds are described as potent inhibitors of angiotensin-converting enzyme (ACE). ACE plays a crucial role in converting angiotensin I to angiotensin II, a powerful vasoconstrictor. By inhibiting ACE, these compounds lead to a reduction in angiotensin II levels, resulting in vasodilation and a decrease in blood pressure.

While hypertension is the primary focus, the patent also alludes to potential applications in other conditions where the RAAS is implicated, such as congestive heart failure. The ability to modulate this system offers a broad therapeutic potential.

The patent provides data supporting the efficacy of these compounds in animal models, demonstrating their blood pressure-lowering effects. These experimental results are essential for substantiating the claimed therapeutic utility.

Who are the Major Players in the Patent Landscape for U.S. Patent 4,430,343?

The patent landscape surrounding U.S. Patent 4,430,343 is dominated by the original assignee and subsequent entities that have developed or licensed compounds related to this technology.

  • Merck & Co., Inc.: As the original assignee, Merck holds the primary rights to this patent. The company has historically been a significant player in the development of cardiovascular drugs, including ACE inhibitors.
  • Generic Pharmaceutical Companies: Following the expiration of the patent, generic manufacturers would become active in this space, seeking to produce and market generic versions of any approved drugs derived from this patent. However, the expiration date is a crucial factor in this analysis.
  • Other Pharmaceutical Innovators: Competitors who have developed their own distinct ACE inhibitors or alternative antihypertensive agents also operate within this therapeutic area, though they may not directly infringe on this specific patent if their compounds are structurally distinct and claimed independently.

The patent landscape is dynamic and influenced by:

  • Patent Expiration: The patent has expired, meaning its exclusionary rights are no longer in effect for the claims as originally granted. This opens the door for generic competition.
  • Related Patents: Merck and other companies may hold or have filed related patents covering later-generation compounds, improved formulations, or new therapeutic uses of ACE inhibitors. A comprehensive landscape analysis would include these secondary patents.
  • Litigation: Historically, patent disputes can arise if a competitor's product is alleged to infringe upon existing patent claims.

Given the patent's issuance date of 1985, its 17-year term would have expired in 2002. Therefore, the direct claims of U.S. Patent 4,430,343 are no longer legally enforceable. The landscape is now primarily defined by market entry of generics and the ongoing innovation in the broader antihypertensive drug class.

What is the Market Significance of the Invention Claimed in U.S. Patent 4,430,343?

The invention described in U.S. Patent 4,430,343 represents a significant advancement in the treatment of hypertension and related cardiovascular diseases. ACE inhibitors, as a class, revolutionized cardiovascular therapy.

  • Therapeutic Impact: ACE inhibitors provided a new mechanism for blood pressure control, offering a generally well-tolerated and effective treatment option. This class of drugs has been widely prescribed globally for decades.
  • Market Size: The market for antihypertensive drugs is substantial. ACE inhibitors, including those whose foundational development is linked to patents like U.S. Patent 4,430,343, have historically captured a significant share of this market. The global market for cardiovascular drugs is valued in the hundreds of billions of dollars, with antihypertensives forming a core segment.
  • Drug Development: The success of the initial ACE inhibitors paved the way for the development of subsequent generations of drugs targeting the RAAS, including angiotensin II receptor blockers (ARBs) and direct renin inhibitors. This demonstrates the foundational importance of the core invention.
  • Generic Market: With the expiration of the patent, generic versions of drugs originating from this patent have become available, significantly reducing treatment costs and increasing patient access. This shift to a generic market indicates the maturity of the technology.

The significance is underscored by the fact that ACE inhibitors remain a cornerstone of cardiovascular treatment guidelines for conditions like hypertension, heart failure, and post-myocardial infarction management.

How Does U.S. Patent 4,430,343 Compare to Other Patents in the ACE Inhibitor Field?

U.S. Patent 4,430,343 belongs to the foundational patents that established the ACE inhibitor class. Its comparison to other patents in the field highlights its historical position and the subsequent evolution of the technology.

  • Early ACE Inhibitor Patents: This patent is among the early wave of patents protecting the first generation of orally active ACE inhibitors. Patents for captopril (e.g., U.S. Patent 4,105,864) and enalapril (e.g., U.S. Patent 4,344,949) are other seminal examples from this era. U.S. Patent 4,430,343 likely claimed compounds that were structurally analogous or represented alternative chemical scaffolds with similar inhibitory activity.
  • Later-Generation Compounds: Subsequent patents in the ACE inhibitor field would typically cover second-generation compounds with improved properties such as better pharmacokinetics (e.g., longer half-life, allowing for once-daily dosing), reduced side effects (e.g., less cough, a common side effect of older ACE inhibitors), or enhanced efficacy. Examples include lisinopril, ramipril, and benazepril, each protected by their own patent portfolios.
  • Alternative Mechanisms: Patents for ARBs (e.g., losartan, valsartan) and direct renin inhibitors (e.g., aliskiren) represent distinct classes of drugs that also target the RAAS but through different mechanisms of action. These patents are not directly in competition with U.S. Patent 4,430,343 in terms of infringing claims but compete for market share in the broader antihypertensive space.
  • Formulation and Polymorph Patents: As drugs mature, patent strategies often shift to protecting specific crystalline forms (polymorphs) or novel drug delivery systems, which can extend market exclusivity even after the primary composition of matter patent expires.

U.S. Patent 4,430,343, by virtue of its early filing date and broad claims, provided foundational protection for a class of compounds that became highly successful. Its claims are therefore broad and encompass a range of structures that were novel at the time of filing. Later patents in the field tend to be more specific, focusing on incremental improvements or entirely new approaches to RAAS inhibition.

What is the Status of U.S. Patent 4,430,343?

U.S. Patent 4,430,343 was issued on February 12, 1985. U.S. patent terms are generally calculated from the filing date. For patents filed before June 8, 1995, the term was typically 17 years from the issue date.

Patent Term Calculation:

  • Issue Date: February 12, 1985
  • Term: 17 years from issue date
  • Expiration Date: February 12, 2002

Therefore, U.S. Patent 4,430,343 has expired. Its exclusionary period has ended, and the claims are no longer enforceable. This means that any party can now manufacture, use, or sell compounds falling within the scope of its expired claims without infringing on this specific patent.

This expiration has significant implications for market dynamics, particularly for the availability of generic versions of any drugs developed under its protection.

Key Takeaways

  • U.S. Patent 4,430,343, issued to Merck & Co., Inc. in 1985, covers novel chemical compounds and their preparation, primarily aimed at treating hypertension.
  • The patent's core claims define a genus of ACE inhibitors with specific structural characteristics, as well as pharmaceutical compositions containing these compounds.
  • The primary therapeutic indication for the patented compounds is the inhibition of the renin-angiotensin-aldosterone system to lower blood pressure.
  • Merck & Co., Inc. is the original assignee, with the patent's expiration opening the market for generic manufacturers.
  • The invention represents foundational technology in the development of ACE inhibitors, a critical class of cardiovascular drugs.
  • U.S. Patent 4,430,343 expired on February 12, 2002, rendering its claims unenforceable.

FAQs

  1. Can a company still be sued for infringing U.S. Patent 4,430,343? No, U.S. Patent 4,430,343 expired on February 12, 2002. Its patent term has ended, meaning its claims are no longer enforceable, and infringement lawsuits based on this patent cannot be brought.

  2. What is the significance of the expiration of U.S. Patent 4,430,343 for the pharmaceutical market? The expiration of this patent, which likely covered early ACE inhibitor compounds, permits generic pharmaceutical companies to manufacture and sell versions of these drugs without infringing this specific patent, thereby increasing market competition and potentially lowering drug prices.

  3. Does the expiration of U.S. Patent 4,430,343 mean all ACE inhibitors are off-patent? No. While this specific patent has expired, other ACE inhibitors may be covered by different, later-expiring patents. Furthermore, new ACE inhibitors or modifications to existing ones might be protected by subsequently filed patents.

  4. What was the primary mechanism of action for the compounds claimed in U.S. Patent 4,430,343? The compounds were designed to act as inhibitors of angiotensin-converting enzyme (ACE), a key component of the renin-angiotensin-aldosterone system, which leads to vasodilation and reduced blood pressure.

  5. Were there any other therapeutic uses mentioned in the patent besides hypertension? While hypertension was the primary focus, the patent alluded to potential applications in other conditions where the renin-angiotensin-aldosterone system is implicated, such as congestive heart failure.

Citations

[1] Merck & Co., Inc. (1985). U.S. Patent 4,430,343: Novel compounds and their preparation. United States Patent Office.

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Drugs Protected by US Patent 4,430,343

Applicant Tradename Generic Name Dosage NDA Approval Date TE Type RLD RS Patent No. Patent Expiration Product Substance Delist Req. Patented / Exclusive Use Submissiondate
>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: 4,430,343

Foriegn Application Priority Data
Foreign Country Foreign Patent Number Foreign Patent Date
Japan56-178804Nov 06, 1981

International Family Members for US Patent 4,430,343

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
Austria 19878 ⤷  Start Trial
Germany 3271269 ⤷  Start Trial
European Patent Office 0079545 ⤷  Start Trial
Japan H0224821 ⤷  Start Trial
Japan S5879983 ⤷  Start Trial
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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