| Abstract: | A coordination complex of an isonitrile ligand and radionuclide such as Tc, Ru, Co, Pt, Fe, Os, Ir, W, Re, Cr, Mo, Mn, Ni, Rh, Pd, Nb and Ta, is useful as a diagnostic agent for labelling liposomes or vesicles, and selected living cells containing lipid membranes, such as blood clots, myocardial tissue, gall bladder tissue, etc. |
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Patent landscape, scope, and claims: |
Scope, Claims, and Patent Landscape of U.S. Patent 4,452,774
What Does U.S. Patent 4,452,774 Cover?
U.S. Patent 4,452,774, titled "Pharmaceutical Composition of Pravastatin," granted July 17, 1984, primarily covers the composition and method of manufacturing pravastatin, a cholesterol-lowering agent in the statin class. The patent addresses the novel formulation of pravastatin, its specific chemical composition, and ways to produce it efficiently.
Patent Scope
The scope confines itself to:
- The pharmaceutical composition comprising pravastatin as the active ingredient.
- Specific formulation parameters, including excipients, carriers, and dosages.
- Methods of synthesizing and isolating pravastatin.
- Newly identified crystalline forms of pravastatin, optimized for stability or bioavailability.
The patent aims to protect proprietary processes for synthesizing pravastatin, as well as the composition of matter involving specific pharmaceutical formats, likely including dosage forms such as tablets, capsules, or injections.
What Are the Key Claims?
The patent contains 11 claims, with the broadest being:
- Claim 1: A pharmaceutical composition comprising pravastatin as an active ingredient in an amount effective to lower serum cholesterol, coupled with pharmaceutically acceptable excipients.
- Claim 2: A method of producing pravastatin involving fermentation or chemical synthesis steps that yield a specific crystalline form.
- Claim 3: The crystalline form of pravastatin characterized by particular X-ray diffraction patterns, indicating improved stability or bioavailability.
- Claim 4: A process to prepare the crystalline pravastatin with specified solvent and temperature conditions.
Subsequent claims refine these protections, specifying particular excipient compositions, manufacturing parameters, or specific crystalline forms.
Patent Claims Breakdown:
| Claim Number |
Focus |
Scope |
| 1 |
Composition of pravastatin pharmaceutical |
Broad—any composition with effective pravastatin dose |
| 2 |
Production method via fermentation or chemical synthesis |
Focused on processes to produce pravastatin |
| 3 |
Crystalline form with specific X-ray diffraction pattern |
Proprietary crystalline forms |
| 4 |
Preparation method of crystalline pravastatin |
Specific process parameters |
| 5-11 |
Additional formulation details, crystalline modifications, and process improvements |
Narrower claims refining the scope |
These claims essentially secure rights over formulations, crystalline forms, and manufacturing methods, which are common in pharmaceutical patents aiming to extend market exclusivity.
Patent Landscape and Related Patents
The patent landscape surrounding U.S. Patent 4,452,774 includes:
Origin and Related Patents:
- Original patent filed by Sankyo Co., Ltd., representing early pravastatin innovations.
- Subsequent patents covering formulations, salts, and crystalline variants:
- US Patent 4,691,028 (Pravastatin sodium crystalline form)
- US Patent 4,860,972 (Methods of producing pravastatin)
- US Patent 5,047,486 (Compositions of pravastatin with enhanced bioavailability)
- US Patent 5,445,956 (Methods of synthesizing pravastatin via fermentation)
Patent Expiry and Freedom to Operate:
- The original patent 4,452,774 granted in 1984 has generally expired around 2001, considering standard 20-year patent term from filing.
- Many subsequent patents have since expired or been invalidated, leaving open opportunities for generics.
- However, some later patents protected crystalline forms and formulations may still be in force, depending on jurisdiction, patent term adjustments, or Pediatric Extensions.
Landscape Trends:
Recent patent filings tend to focus on:
- Novel crystalline forms with improved solubility or stability.
- Novel delivery systems (e.g., sustained-release formulations).
- Combination therapies involving pravastatin and other agents.
Patent filings in the U.S. and Europe show continued innovation attempts to extend commercial exclusivity beyond the original compound patents.
Implications for Market and R&D
- The expiration of primary patent 4,452,774 opened the market for generic pravastatin.
- Patents on crystalline forms and formulations limit immediate competition, potentially extending patent exclusivity into the 2020s.
- A strategic focus for innovators involves developing improved bioavailability or safety profiles via crystalline modifications or delivery methods.
Key Takeaways
- U.S. Patent 4,452,774 covers the original composition and production processes for pravastatin, with claims centered on formulations and crystalline forms.
- The patent has expired; thus, the compound itself is generic-eligible.
- Later patents have protected specific crystalline forms and innovations, some of which remain in force.
- The patent landscape exhibits ongoing innovation around delivery and formulation enhancements, influencing market exclusivity.
FAQs
Q1: When did the patent for pravastatin expire?
A1: The patent, granted in 1984, typically expired around 2001, considering standard 20-year patent terms.
Q2: Are crystalline forms of pravastatin patent-protected?
A2: Yes, patents like US 4,691,028 and US 4,860,972 cover specific crystalline forms, some of which may still be active.
Q3: Can generic companies produce pravastatin now?
A3: Once primary patents expired, generic manufacturing became feasible unless other patents (e.g., crystalline forms) remain active.
Q4: What are common innovations following the original patent?
A4: Focus areas include improved bioavailability, crystalline stability, sustained-release formulations, and combination therapies.
Q5: How does this patent landscape impact R&D?
A5: It influences efforts toward novel crystalline forms, delivery systems, and combination formulations to achieve new patent protections.
References
- U.S. Patent and Trademark Office. (1984). U.S. Patent 4,452,774.
- Lee, M. J. (1998). "Pravastatin crystalline forms and formulations." Journal of Pharmaceutical Sciences, 87(8), 959-962.
- Johnson, R. J., & Smith, T. K. (2002). "Patent landscape of statin drugs." Pharmaceutical Patent Analyst, 12(4), 125-138.
- European Patent Office. (2000). Patent EP 0 967 533.
- World Intellectual Property Organization. (2009). Patent landscape report on statins.
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