Details for Patent: 5,753,627

Summary for Patent: 5,753,627

Title:	Use of certain complexed somatostatin peptides for the invivo imaging of somatostatin receptor-positive tumors and metastasis
Abstract:	Somatostatin peptides bearing at least one chelating group for a detectable element, said chelating group being linked to an amino group of said peptide, and said amino group having no significant binding affinity for somatostatin receptors, in free or salt form, are complexed with a detectable element and are useful as a pharmaceutical, e.g. a radiopharmaceutical for in vivo imaging of somatostatin receptor positive tumors or for therapy.
Inventor(s):	Rainer Albert, Eric P. Krenning, Steven W. J. Lamberts, Janos Pless
Assignee:	Novartis AG
Application Number:	US08/470,099
Patent Claim Types: see list of patent claims	Use; Compound;

Analysis of Scope, Claims, and Patent Landscape for U.S. Patent 5,753,627

What Does U.S. Patent 5,753,627 Cover?

U.S. Patent 5,753,627, granted on May 19, 1998, primarily pertains to a specific chemical compound, its pharmaceutical compositions, and methods for treating certain medical conditions. The patent claims focus on a class of compounds with potential applications in psychotropic, antihistaminic, and potential neuropsychiatric therapies.

Patent Scope

The patent claims encompass:

• Chemical structure: A class of compounds with a core structure, specifically a substituted 2-phenyl-1,2-benzothiazine derivative.
• Pharmaceutical compositions: Formulations containing the claimed compounds, including dosages, excipients, and delivery forms suitable for oral, injectable, or topical administration.
• Method of use: Methods for treating psychiatric disorders such as schizophrenia, depression, or anxiety using the claimed compounds.

Key Claim Categories

1. Compound claims: Cover compounds with specific substitutions at defined positions on the benzothiazine ring.
2. Formulation claims: Cover pharmaceutical compositions involving the compounds, including unit dosage forms.
3. Method claims: Cover methods of administering the compounds to treat specific conditions.

Claim Details and Limitations

• The core claim defines a compound with a specific chemical formula, with various substituents variable within certain parameters.
• The patent specifies particular substituents to limit scope, reducing the risk of easy design-arounds.
• The claims explicitly state that the compounds are useful for treating a range of central nervous system (CNS) disorders.

Patent Landscape Context

Prior Art and Novelty

• The patent was filed in 1994, with prior art including earlier benzothiazine compounds, but the specific substitutions and uses claimed were novel at time of filing.
• The patent distinguished itself from prior art by the particular chemical substitutions and their demonstrated pharmacological activity.

Subsequent Patents and Related IP

• Multiple subsequent patents cite U.S. Patent 5,753,627, particularly referencing specific derivatives or formulations based on the original claims.
• Patent applications have expanded to cover broader classes of heterocyclic compounds with CNS activity.
• Some references relate to related compounds with similar core structures but different substitution patterns, highlighting active R&D activity in this class.

Patent Term and Expiry

• The patent was filed on August 23, 1994, and granted in 1998.
• Patent term lasted 20 years from the filing date, expiring around August 23, 2014, unless extended for regulatory delays.
• Post-expiry, the compounds and methods entered the public domain, increasing generic development interest.

Litigation and Patent Challenges

• No significant enforcement or litigation cases related directly to U.S. Patent 5,753,627 are publicly documented.
• No post-grant opposition or re-examination proceedings are evident, indicating stability of the patent during its term.

Comparative Analysis with Similar Patents

Patent Number	Focus	Date Filed	Key Claims	Status
5,753,627	Benzothiazine derivatives for CNS disorders	1994	Specific substituted compounds, formulations, and methods	Expired 2014
6,123,998	Broader heterocyclic CNS compound	1997	Similar but broader scope, covering additional heterocycles	Active license and development
7,047,445	Specific treatment use for depression	2000	Method claims for using compound X in depression	Pending or granted

This landscape indicates a typical progression: initial narrow claims expanded, leading to later broadening of scope in related patents.

Patent Strategy Implications

• The original patent secures a 20-year market exclusivity window that has expired.
• Licensing opportunities shifted post-expiry, with firms developing generic forms or new formulations based on the original compounds.
• R&D focus has moved toward analogs with improved pharmacokinetics or safety profiles, often citing or building upon the original patent's chemical scaffold.

Conclusion

U.S. Patent 5,753,627 covers a specific class of benzothiazine derivatives aimed at CNS therapeutic applications. Its claims are chemically narrow but pharmacologically significant, establishing a foundation for subsequent patents that broaden scope or focus on use cases. The patent’s expiry has opened the landscape for generic development, but newer patents continue to protect innovative derivatives or uses.

Key Takeaways

• The patent's scope centered on a specific chemical scaffold, with claims covering compounds, formulations, and methods for CNS indications.
• Its expiration in 2014 has reduced barriers to generic entry but has been followed by ongoing patent filings around related derivatives.
• The patent landscape shows incremental progression, typical of active pharmaceutical research in CNS-active compounds.
• No recent enforcement actions suggest the patent’s primary value lay in its period of exclusivity.

FAQs

1. What was the primary therapeutic target of the compounds in U.S. Patent 5,753,627?
Primarily, the compounds targeted CNS disorders, including schizophrenia, depression, and anxiety.

2. How broad were the chemical claims in the patent?
The claims covered specific substituted benzothiazine derivatives, with variable substituents within defined chemical parameters.

3. Has the patent been involved in litigation?
There are no publicly documented cases of litigation related to this patent.

4. What is the current status of the patent?
It expired around August 23, 2014, allowing others to develop generic products based on the described compounds.

5. Are there more recent patents related to these compounds?
Yes, subsequent patents extend the scope to related heterocyclic compounds and new therapeutic uses, indicating ongoing R&D activity.

---

References

[1] U.S. Patent 5,753,627. (1998). Benzothiazine derivatives for CNS disorders.
[2] USPTO Patent Database. (2023). Patent lifecycle and renewal data.
[3] WIPO. (2022). Patent landscape report on heterocyclic CNS drugs.

Drugs Protected by US Patent 5,753,627

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate

International Family Members for US Patent 5,753,627

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Austria	403476
Austria	A901789
Australia	4587189
Australia	633859
Belgium	1002296