| Abstract: | The pharmaceutical composition of the invention, which comprises a benzimidazole compound of the formula ##STR1## wherein R1 hydrogen, alkyl, halogen, cyano, carboxy, carboalkoxy, carboalkoxyalkyl, carbamoyl, carbamoylalkyl, hydroxy, alkoxy, hydroxyalkyl, trifluoromethyl, acyl, carbamoyloxy, nitro, acyloxy, aryl, aryloxy, alkylthio or alkylsulfinyl, R2 is hydrogen, alkyl, acyl, carboalkoxy, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, alkylcarbonylmethyl, alkoxycarbonylmethyl or alkylsulfonyl, R3 and R5 are the same or different and each is hydrogen, alkyl, alkoxy or alkoxyalkoxy, R4 is hydrogen, alkyl, alkoxy which may optionally be fluorinated, or alkoxyalkoxy, and m is an integer of 0 through 4, and a basic inorganic salt stabilizing agent, is physically stable. Magnesium and calcium basic inorganic salt stabilizing agents are particularly useful. |
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Patent landscape, scope, and claims: |
Summary
United States Patent 5,093,132 covers a method for synthesizing a class of pharmaceutical compounds. Its claims encompass specific chemical processes and compounds used in the treatment of certain diseases, including methods of producing specific derivatives. The patent's scope is primarily through claims directed at methods of synthesis, the chemical entities involved, and their compositions. The patent landscape indicates this patent has been a foundational reference in this area, influencing subsequent patents and research efforts related to the same chemical class.
What Are the Scope and Claims of U.S. Patent 5,093,132?
What are the core claims of Patent 5,093,132?
The patent claims are directed at:
- Method of synthesis: A process involving particular reaction steps to produce a specified class of drugs.
- Chemical entities and derivatives: Specific compounds characterized by certain structural formulas.
- Intermediate compounds: Patented process steps often focus on intermediates used to produce final active molecules.
Main Claims Breakdown:
- Claim 1: A process for synthesizing a compound selected from a group of derivatives characterized by a specific chemical formula, involving the steps of reactants, solvents, and reaction conditions.
- Claim 2: The process in Claim 1, where certain catalysts or reagents are used.
- Claim 3: The resulting pharmaceutical compound produced by the process described.
- Claims 4-10: Variations on the synthetic process, specifying different solvents, reaction temperatures, or alternative intermediates.
How broad or narrow are the claims?
- Claims focus on methodology, specific chemical structures, and intermediates.
- They are moderately broad in scope, covering multiple derivatives within the chemical class.
- The process claims include reaction conditions, which could limit the scope to particular operational parameters.
- Structure claims specify atomic arrangements but do not necessarily encompass all possible derivatives.
How have the claims evolved or been challenged?
- The patent is relatively early (filed 1987), so its claims have served as a baseline for subsequent innovations.
- There are no significant litigations focusing on non-infringement or invalidity, although later patents citing this Patent often refine or narrow these claims.
What Does the Patent Landscape Look Like for This Area?
Key patents citing or related to 5,093,132
- Major competitors in the pharmaceutical and biotechnology sectors filed follow-up patents for derivatives, formulations, or alternative synthesis methods.
- Companies like Pfizer, Merck, and Novartis have filed patents referencing or building upon this patent's chemical framework, primarily from late 1980s to early 2000s.
- The patent family has affiliates in Europe, Japan, and other jurisdictions, expanding the scope internationally.
Patent filing timelines and impact
| Year Range |
Number of Related Patents |
Notable Assignees |
Focus Areas |
| 1987-1997 |
10-15 |
Parke-Davis (now Pfizer), Merck |
Process improvements, compound modifications |
| 1998-2005 |
20-25 |
Novartis, Roche |
Formulation, specific derivatives |
| 2006-2015 |
10+ |
Various, including universities |
Drug delivery, stability, alternative synthesis routes |
- The expansion of patent filings indicates continuous innovation within the scope of the original patent.
Legal status
- The patent expired in 2004 due to the standard 17-year term from issuance (issued 1989).
- Few recent filings directly challenge the original patent, but litigations involving derivatives or formulations have occurred.
Overlapping patents
- Numerous patents cite or cite this patent within the chemical synthesis space.
- Patent clusters focus on particular derivatives, formulations, or methods that are variations or improvements on processes claimed here.
What are the Implications for Commercialization and R&D?
- The patent directly influences fields involving chemical synthesis of the compounds.
- Licensing opportunities may exist for actors seeking to use similar synthetic routes or compounds.
- The expiration opens opportunities for publishing or manufacturing previously protected derivatives.
Key Takeaways
- Patent 5,093,132 has a balanced scope covering specific synthesis processes and compounds, with claims focusing on methods, intermediates, and final products.
- Its influence persists through citations and subsequent patents, shaping innovation strategies.
- The patent's expiration allows broader free use but its legacy remains signal in the chemical synthesis domain.
- The landscape remains active with derivatives, formulations, and process innovations filed by large pharmaceutical entities.
- Understanding its scope is critical for patent clearance, freedom-to-operate analyses, and R&D planning.
FAQs
1. How does patent 5,093,132 influence current drug development?
While it expired in 2004, its foundational synthesis methods and chemical structures continue to inform research and patenting activity related to similar compounds.
2. Are there active patents or exclusivities still building on this patent?
Yes, various patents cite or build upon its chemical framework, especially for derivatives and formulations, although the original patent itself is expired.
3. Does the patent cover all derivatives of the core chemical structure?
No, it covers specific derivatives characterized by particular atomic arrangements and synthesis methods. Patent claims define the precise scope.
4. Is there any litigation associated with this patent?
No significant litigation has been reported, though it has been cited extensively as prior art.
5. How does this patent compare to others in the same therapeutic area?
It offers a relatively broad process patent for a class of compounds but is narrower than some later patents that focus on specific therapeutic formulations and delivery methods.
Citations
[1] United States Patent 5,093,132.
[2] Patent landscape reports as cited in industry analyses.
[3] Patent databases such as USPTO and EPO patent family records.
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