Share This Page
Details for Patent: 4,430,343
✉ Email this page to a colleague
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 LandscapeU.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:
Dependent Claims: The patent includes numerous dependent claims that narrow the scope of the independent claims by specifying particular substituents or limitations.
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.
The patent landscape is dynamic and influenced by:
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.
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.
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:
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
FAQs
Citations[1] Merck & Co., Inc. (1985). U.S. Patent 4,430,343: Novel compounds and their preparation. United States Patent Office. More… ↓ |
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 |
| Japan | 56-178804 | Nov 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 |
