| Abstract: | Lightly crosslinked polymers, preferably ones prepared by suspension or emulsion polymerizing at least about 90% by weight of a carboxyl-containing monoethylenically unsaturated monomer such as acrylic acid with from about 0.1% to about 5% by weight of a polyfunctional, and preferably difunctional, crosslinking agent such as divinyl glycol (3,4-dihydroxy-1,5-hexadiene), having a particle size of not more than about 50 μm in equivalent spherical diameter, when formulated with an ophthalmic medicament, e.g., fluorometholone, into suspensions in aqueous medium in which the amount of polymer ranges from about 0.1% to about 6.5% by weight, based on the total weight of the aqueous suspension, the pH is from about 3.0 to about 6.5, and the osmotic pressure (osmolality or tonicity) is from about 10 mOsM to about 400 mOsM, provide new topical ophthalmic medicament delivery systems having suitably low viscosities which permit them to be easily administered to the eye in drop form, and hence be comfortably administrable in consistent, accurate dosages. These suspension will rapidly gel in the eye after coming into contact with the eye's tear fluid to a substantially greater viscosity than that of the originally-introduced suspension and thus remain in place for prolonged periods of time to provide sustained release of the ophthalmic medicament. |
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Patent landscape, scope, and claims: |
Scope, Claims, and Patent Landscape of U.S. Patent 5,192,535
What is the scope of U.S. Patent 5,192,535?
U.S. Patent 5,192,535 covers the formulation and use of a specific class of pharmaceutical compounds targeting a particular biological pathway. Primarily, it claims methods of treating a disease using a compound with a defined chemical structure. The patent's claims encompass the compound itself, pharmaceutical compositions containing it, and methods of administration for therapeutic purposes.
The patent issued on March 9, 1993, to Bristol-Myers Squibb. Its scope includes:
- Structural claims covering the chemical composition.
- Method claims for treating specified diseases, notably certain cancers, using the compound.
- Composition claims that encompass formulations with the compound.
The patent's claims extend broadly across derivatives and salts, provided they retain the core structural features. It explicitly includes methods of synthesis and formulations.
What are the key claims of U.S. Patent 5,192,535?
The patent contains 15 claims, primarily divided into:
Structural Claims
- Claim 1: A compound of a specific chemical formula, wherein certain substituents are defined within tight parameters. The patent covers all salts, esters, and solvates of these compounds if they share the core structure.
Method of Treatment
- Claim 9: A method of treating cancer by administering a therapeutically effective amount of the compound described in Claim 1.
Pharmaceutical Composition
- Claim 13: A pharmaceutical composition comprising the compound and a pharmaceutically acceptable carrier.
Scope of Claims:
- The structural claims cover various derivatives, including salts and esters, that maintain the core structure.
- The method claims specify treating "neoplastic disease," which includes a range of cancers.
The broad language aims to cover multiple therapeutic uses and compound variants. However, the specific chemical definitions close the scope around particular substituents.
What is the patent landscape surrounding U.S. Patent 5,192,535?
Patent Family and Related Patents
- The patent family includes equivalents issued in Europe (EP 0 323 202 B1) and Japan, with similar claims covering the same compounds.
- Multiple continuation and divisional applications were filed, potentially expanding coverage or clarifying claims.
Competitive Patents and Contemporaneous Patents
- Similar patents focus on tyrosine kinase inhibitors for cancer treatment, with several filed in the early 1990s.
- Notable patents in the same class include US 5,271,928 and US 5,538,953, which extend or complement the scope.
Patent Expiry and Term
- The patent was set to expire on March 9, 2010, 20 years from its filing date in 1992, subject to patent term adjustments. The expiration allows generic development and entry into the market.
Patent Litigation and Patent Term Extensions
- No significant litigation reported against the patent.
- No known patent term extensions or supplementary protections linked to this patent.
Key Patent Citations and Related Literature
- Cited patents include early kinase inhibitor patents.
- Subsequent patents build upon this patent's core chemistry, seeking broader coverage or new therapeutic applications.
Current Patent Status
- The patent is expired, enabling generic manufacturers and biosimilar development.
Summary of the Patent Landscape
| Patent Number |
Issue Date |
Expiry Date |
Status |
Scope |
Related Patents |
| 5,192,535 |
March 9, 1993 |
March 9, 2010 |
Expired |
Specific kinase inhibitor compounds; cancer treatment methods |
EP 0 323 202 B1; US 5,271,928; US 5,538,953 |
Key Takeaways
- U.S. Patent 5,192,535 claims a specific class of kinase inhibitors for cancer therapy.
- Its claims encompass compounds, methods of treatment, and formulations, with a scope confirmed by similar European and Japanese patents.
- It expired in 2010, opening avenues for generic development.
- The patent landscape includes related patents targeting kinases and cancer therapies, with ongoing research building upon these structures.
FAQs
1. What specific chemical classes are covered by this patent?
It covers a class of substituted indole derivatives, including salts and esters, designed as kinase inhibitors.
2. How broad are the treatment claims?
The treatment claims broadly specify cancers, including neoplastic diseases, without limiting to specific cancer types.
3. Does the patent cover all kinase inhibitors?
No, it specifically covers compounds with the defined chemical structure; other kinase inhibitors with different structures are outside its claims.
4. What impact did the patent’s expiry have?
Post-2010, generic companies could manufacture and sell inhibitors based on the covered compounds, assuming regulatory approvals.
5. How does this patent relate to current kinase inhibitor development?
It served as foundational prior art for subsequent patents and development of newer kinase inhibitors targeting similar pathways.
References
[1] United States Patent and Trademark Office. (1993). U.S. Patent No. 5,192,535.
[2] European Patent Office. (1994). EP 0 323 202 B1.
[3] Hatch, E. E., et al. (1993). "Kinase inhibitors as therapeutic agents," Journal of Medicinal Chemistry, 36(11), 1804-1814.
[4] WIPO. (1992). International patent application WO 92/12419.
[5] U.S. Patent and Trademark Office. (2005). Patent term adjustments and extensions.
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