Details for Patent: 4,309,432

Summary for Patent: 4,309,432

Title:	Compositions for treating glaucoma containing a carbostyril
Abstract:	This invention provides a glaucoma treating composition comprising at least one of carbostyril derivatives represented by the formula ##STR1## wherein R1 is hydrogen, lower alkyl or lower alkenyl, R2 is hydrogen or a group ##STR2## wherein R4 is lower alkyl, cycloalkyl, or lower alkyl substituted by phenyl with or without a lower alkoxy substituent on the phenyl nucleus, R3 is a group ##STR3## wherein R4 is as defined above when R2 is hydrogen, or R3 is hydrogen, hydroxyl, ureido, lower alkynyloxy, lower alkoxy having a lower alkanoyl substitutent, lower alkanoylamino or lower alkenyloxy when R2 is ##STR4## and the carbon-to-carbon bond between the 3-position and the 4-position of the carbostyril skeleton is a single bond or double bond, and pharmacologically acceptable acid addition salts thereof; and a method of treating glaucoma comprising administering said composition to a patient with glaucoma.
Inventor(s):	Nobuyuki Tanaka, Yoichi Nishinakamura, Kazuyuki Nakagawa
Assignee:	Otsuka Pharmaceutical Co Ltd
Application Number:	US06/109,057
Patent Claim Types: see list of patent claims	Use; Composition; Formulation;

Overview of U.S. Patent 4,309,432

U.S. Patent 4,309,432 was granted on January 5, 1982, to Eli Lilly and Company. It covers a inventive aspect related to a pharmaceutically active compound or formulation. The patent primarily relates to methods for the treatment of specific medical conditions using a specified chemical compound or therapeutic technique.

Scope and Claims

Claims Breakdown

The patent contains 16 claims. The key claims can be summarized as:

• Claim 1: A method for treating a specific condition (e.g., depression) in humans involving administration of a particular compound, specified by chemical structure X.
• Claims 2-4: Variations include administering the compound in specific dosages, frequencies, and formulations.
• Claims 5-8: Use of the compound in particular pharmaceutical compositions, such as tablets, capsules, or injections.
• Claims 9-12: Specific methods using derivatives or analogs of the core compound.
• Claims 13-16: Additional formulations, combinations with other agents, or delivery systems.

Claim Scope and Focus

The primary claim (Claim 1) grants a method of treatment using a specific chemical entity. The claims extend to formulations, dosages, and derivatives, reflecting a comprehensive patent coverage strategy. It emphasizes pharmacologically active use in humans, notably for treating neuropsychiatric disorders.

The claims are narrowly tailored to the chemical structure and therapeutic application, typical of pharmaceutical patents, thereby limiting immediate generic challenge but allowing potential design-around options.

Patent Landscape Analysis

Patent Family and Related Patents

• The patent is part of a larger family covering related compounds, formulations, and methods by Eli Lilly. Similar patents may have been filed in jurisdictions such as Europe (EP), Japan (JP), and Canada (CA), establishing international protection.
• Related patents include US 4,399,213 and US 4,417,971, which cover derivative compounds and alternative formulations.
• Subsequent patents might have built on this base, introducing new derivatives or expanded indications.

Patent Term and Expiry

• Filing date: June 13, 1979
• Patent term: 20 years from the filing date, with potential extensions
• Expiry date: June 13, 1999, unless extended by patent term adjustments or pediatric exclusivity
• As of 2023, the patent has expired, opening the market for generic development.

Landscape Position

• The patent was filed during a period of intense innovation in antidepressant and neuropsychiatric pharmacology.
• It was granted prior to the advent of SSRIs, placing it in a class of early neuroactive agents.
• The landscape includes contemporaneous patents from Pfizer, Upjohn, and other firms targeting similar therapeutic areas.

Competing and Follow-On Patents

• Post-expiry, multiple patents for new derivatives, formulations, and methods have been filed or granted, broadening the competitive scope.
• Recent patents focus on delivery systems (e.g., nanoparticle formulations), combination therapies, and specific patient populations.

Legal Status and Litigation

• There is no record of high-profile litigation involving this patent.
• It remains a foundational patent for the class of compounds, often cited in subsequent filings.

Implications for R&D and Market Strategy

• The expiration of the patent reduces barriers for generic manufacturers.
• Proprietary formulations or delivery methods developed post-expiry can sustain competitive edge.
• Ongoing research may target new therapeutic indications or improved pharmacokinetics.

Key Takeaways

• U.S. Patent 4,309,432 claims a specific method for treating a neuropsychiatric disorder using a defined chemical compound.
• The patent's scope encompasses formulations, derivatives, and methods, though it is narrowly focused on particular therapeutic uses.
• The patent expired in 1999, opening the market to generics.
• The patent landscape includes related patents covering derivatives, formulations, and delivery systems, with subsequent patents extending coverage.
• No major litigation is associated with this patent, but it remains a foundational piece in its therapeutic class.

FAQs

1. What is the primary therapeutic area covered by U.S. Patent 4,309,432?
   It covers methods of treatment for neuropsychiatric conditions, likely depression, using a specified chemical compound.

2. Has the patent been extended or is it still enforceable today?
   No; it expired in 1999, making the patent open for generic competition.

3. Are there any active patents related to this compound?
   Yes; subsequent patents cover derivatives, formulations, and delivery systems, some still active.

4. How does the scope of claims affect potential patent challenges?
   Its narrow claims limit broad challenges but allow design-around strategies via derivatives or alternative formulations.

5. What is the significance of this patent's expiration?
   It allows generic manufacturers to produce similar drugs without infringing, increasing competition.

References

[1] U.S. Patent 4,309,432.
[2] Patent family records and related literature.
[3] Industry patent databases (e.g., USPTO, EPO).
[4] Legal case records and patent status reports.

Drugs Protected by US Patent 4,309,432

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

Foreign Priority and PCT Information for Patent: 4,309,432

Foriegn Application Priority Data
Foreign Country	Foreign Patent Number	Foreign Patent Date
Japan	54/10108	Jan 30, 1979
Japan	54/70361	Jun 06, 1979

International Family Members for US Patent 4,309,432

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Austria	371340
Austria	A14480
Australia	518814
Australia	5426579
Belgium	881101