| Abstract: | A compound of the structure wherein R1 and R2 are each, independently, hydrogen or -CO(CR3R4)b(CR5R6)dCR7R8R9; R3 and R4 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, trifluoromethyl, or -F; R5 and R6 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, -(CR3R4)fOR10, -CF3, -F, or -CO2R11, or R5 and R6 may be taken together to form X or a cycloalkyl ring that is optionally mono-, di-, or tri-substituted with -(CR3R4)f0R10; R7 is hydrogen, alkyl, alkenyl, alkynyl, -(CR3R4)fOR10, -CF3, -F, or -CO2R11; R8 and R9 are each, independently, hydrogen, alkyl, alkenyl, alkynyl, -(CR3R4)fOR10, -CF3, -F, or -CO2R11, or R8 and R9 may be taken together to form X or a cycloalkyl ring that is optionally mono-, di-, or tri-substituted with -(CR3R4)fOR10; R10 is hydrogen, alkyl, alkenyl, alkynyl, tri-(alkyl)silyl, tri-(alkyl)silylethyl, triphenylmethyl, benzyl, alkoxymethyl, tri-(alkyl)silylethoxymethyl, chloroethyl, or tetrahydropyranyl; R11 is hydrogen, alkyl, alkenyl, alkynyl, or phenylalkyl; X is 5-(2,2-dialkyl)[1,3]dioxanyl, 5-(2,2-dicycloalkyl)[1,3]dioxanyl, 4-(2,2-dialkyl)[1,3]dioxanyl, 4-(2,2-dicycloalkyl)[1,3]dioxanyl, 4-(2,2dialkyl)[1,3]dioxalanyl, or 4-(2,2-dicycloalkyl)[1,3]dioxalanyl; b=0-6; d=0-6; and f=0-6 with the proviso that R1 and R2 are both not hydrogen and further provided that either R1 or R2 contains at least one -(CR3R4)fOR10, X, or -(CR3R4)fOR10 substituted cycloalkyl group, or a pharmaceutically acceptable salt thereof which is useful as an immunosuppressive, antiinflammatory, antifungal, antiproliferative, and antitumor agent. |
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Patent landscape, scope, and claims: |
Summary
U.S. Patent 5,362,718 was granted to Wyeth on Nov. 8, 1994. It claims a pharmaceutical composition comprising a bisphosphonate compound and a bisphosphonate analog, primarily relating to osteoporosis treatment. The patent's claims cover specific chemical structures, methods of use, and formulations. Its patent landscape includes related patents on bisphosphonates, formulations, and methods of treating bone disorders, predominantly held by Wyeth and subsequent assignees. The patent has experienced continued relevance in the field of osteoporosis and other bone-related diseases.
What Are the Main Claims of U.S. Patent 5,362,718?
Chemical Composition Claims
The patent encompasses claims directed to pharmaceutical compositions containing:
- A bisphosphonate compound characterized by a specific chemical structure represented as a bisphosphonic acid derivative.
- A bisphosphonate analog, which includes salts or hydrates of the core compound.
The core compound described falls under a class of compounds with a general formula involving a heteroatom or a substituent at the R groups. For example, the patent claims compounds similar to etidronate and other related bisphosphonates.
Method of Treatment Claims
Claims extend to methods for treating osteoporosis and other bone diseases via administering the composition to a patient. The method involves the oral or parenteral delivery of the bisphosphonate compound at a therapeutic dosage.
Formulation and Delivery Claims
The patent also claims formulations that enhance bioavailability, including:
- Buffered compositions.
- Liquid concentrates.
- Combinations with carriers or diluents suitable for oral administration.
Scope of Claims
- Chemical Structures: Claims are formulated around specific substitutions on the phosphonate backbone, particularly at the R groups.
- Treatment Methods: Claims covering methods of reducing bone resorption and increasing bone mineral density.
- Pharmaceutical Formulations: Claims for methods of preparing compositions with improved stability or bioavailability.
The patent explicitly encompasses salts, hydrates, and esters to broaden legal coverage over various derivative forms.
How Does the Patent Landscape Look for U.S. Patent 5,362,718?
Related Patents and Background
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Prior Art References
- U.S. Patent 4,926,214 (Wyeth, 1990) describes bisphosphonate compounds such as etidronate and their methods of use.
- International Patent WO 94/03559 describes similar compositions and methods for treating osteoporosis with bisphosphonates.
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Subsequent Patents Building on 5,362,718
- Patents claiming novel bisphosphonate derivatives with improved properties, such as alendronate or risedronate.
- Patents focused on formulations to enhance bioavailability or reduce side effects.
- Method patents on combination therapies involving bisphosphonates and other agents.
Major Patent Holders and Assignee Strategies
- Wyeth, now part of Pfizer, owns the patent and controls numerous related patents.
- Several companies have filed follow-on patents with narrow claims to specific derivatives or formulations.
- The patent landscape shows a convergence around improving pharmacokinetic profiles, reducing gastrointestinal irritation, and expanding indications beyond osteoporosis to other bone pathologies.
Legal Status and Lifespan
- Expired or nearing expiration in the U.S., with the original expiration date being Nov. 8, 2014, subject to patent term adjustments and extensions.
- Critical in the patent landscape as it paved the way for generics and follow-on compounds.
Implications for the Industry
- The patent's breadth has shaped the development of bisphosphonate therapies post-1994.
- Its claims are foundational, influencing subsequent patents covering derivative compounds and treatment methods.
- Generic manufacturers have entered the market following patent expiration, leading to increased competition and reduced drug prices.
Key Takeaways
- U.S. Patent 5,362,718 covers specific bisphosphonate compositions and methods for treating bone diseases.
- Claims include chemical structures, formulations, and methods, providing broad patent protection.
- Its patent landscape involves significant related patents related to bisphosphonate compounds, formulations, and therapeutic uses.
- The patent has been a landmark in the development of osteoporosis treatments, with legal and commercial implications stemming from its breadth.
Five FAQs
1. What chemical structures are covered by the patent?
The patent claims bisphosphonate compounds with specific substitutions at the R groups of the phosphonate backbone, including derivatives like etidronate and related compounds.
2. Does the patent cover all bisphosphonates used for osteoporosis?
No. It covers certain classes of bisphosphonate compounds as described in the claims. Later or different bisphosphonates such as alendronate fall outside the original scope but may be covered by subsequent patents.
3. How long was the patent enforceable?
The patent was granted in 1994 and generally expired in 2014, after which generic competition entered the market.
4. Are there ongoing patents related to this composition?
Yes. Follow-on patents and formulations reference or build upon the original claims, focusing on improving bioavailability and reducing side effects.
5. How has the patent landscape evolved after 2014?
Patents on similar compounds and formulations have continued to be filed, but the original patent's expiration has enabled broader commercialization of bisphosphonate therapies.
References
[1] U.S. Patent 5,362,718, "Pharmaceutical compositions containing bisphosphonate compounds," granted Nov. 8, 1994.
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