Details for Patent: 4,734,416

Summary for Patent: 4,734,416

Title:	Pharmaceutically useful carbostyril derivatives
Abstract:	Carbostyril derivatives having antihistamic action and central nervous controlling action are useful as antihistamic agents or central nervous controlling agents. The derivatives are represented by the general formula, ##STR1## wherein R.sup.1 is a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, an alkenyl group having 2 to 4 carbon atoms, an alkynyl group having 2 to 4 carbon atoms or a phenylalkyl group having an alkylene group containing 1 to 4 carbon atoms; R.sup.2 is a hydrogen atom, an alkyl group having 1 to 4 carbon atoms or a phenyl group; R.sup.3 is a hydrogen atom, a hydroxy group, an alkyl group having 1 to 4 carbon atoms, an alkanolyoxy group having 1 to 4 carbon atoms or a 3,4,5-trimethoxybenzoyloxy group; R.sup.4 is a hydrogen atom or an alkyl group having 1 to 4 carbon atoms; R.sup.5 is a cycloalkyl group having 3 to 8 carbon atoms, a phenyl group (which may have 1 to 3 substituted groups selected from the group consisting of halogen atoms, alkyl groups having 1 to 4 carbon atoms and alkoxy groups having 1 to 4 carbon atoms), an alkyl group having 1 to 4 carbon atoms (having one substituted group such as a hydroxy group, a phenyl group or an alkanoyloxy group having 1 to 4 carbon atoms), an alkanoyl group having 1 to 4 carbon atoms or benzoyl group; X is a halogen atom; n is 0, or an integer of 1 or 2; Q is an integer of 2 or 3, l and m are respectively an integer of 0 or 1-6, but the sum of l and m should not exceed 6; the carbon-carbon bond at the 3- and 4-positions in the carbostyril skeleton is a single or double bond; and the substituted position of the side chain of ##STR2## is any one of the 4-, 5-, 6-, 7- or 8-positions.
Inventor(s):	Banno; Kazuo (Tokushima, JP), Fujioka; Takafuni (Tokushima, JP), Oshiro; Yasuo (Tokushima, JP), Nakagawa; Kazuyuki (Tokushima, JP)
Assignee:	Otsuka Pharmaceutical Co., Ltd. (JP)
Application Number:	06/024,602
Patent Claim Types: see list of patent claims	Compound; Composition; Use;

Detailed Analysis of the Scope and Claims of United States Patent 4,734,416

Introduction

United States Patent 4,734,416, titled "Pharmaceutically Useful Carbostyril Derivatives," is a significant patent in the pharmaceutical industry, particularly in the realm of central nervous system (CNS) controlling agents. Here, we will delve into the scope, claims, and patent landscape surrounding this patent.

Background and Inventors

The patent was issued on March 29, 1988, to Otsuka Pharmaceutical Co., Ltd., and it expired on March 29, 2005. The inventors, including Dr. Kazuyuki Nakagawa, contributed to the development of carbostyril derivatives with various pharmacological activities[1][4].

Scope of the Patent

The patent covers a broad genus of carbostyril derivatives that exhibit antihistaminic and central nervous controlling actions. These compounds are described as useful for various therapeutic applications, including:

• Central muscle relaxing agents
• Sleep-inducing agents
• Pre-operative drugs
• Antischizophrenia agents
• Sedatives
• Antianxiety drugs
• Antimanic depressive psychosis agents
• Antipyretic agents
• Analgetic agents
• Depressors[1][4].

Claims of the Patent

The patent includes several key claims that define the scope of protection:

• Claim 13: Specifically claims the "unsubstituted butoxy" compound using its chemical name. This compound has a phenyl ring that is unsubstituted and a butoxy linker connecting the 7-position of its carbostyril core to its piperazine ring[1].
• Claim 50: Describes a method of producing an antihistaminic effect in a mammal by administering a pharmaceutical composition containing a suitable amount of a carbostyril derivative with a general chemical formula[1].
• Claim 116: Claims a method similar to Claim 50 but specifies nine particular carbostyril derivatives, including the unsubstituted butoxy[1].

Prior Art and Disclosure

The patent discloses a vast array of compounds, estimated to be approximately nine trillion, under the broad genus of carbostyril derivatives. The unsubstituted butoxy compound is specifically disclosed and claimed in this patent, as well as in the earlier U.S. Patent 4,734,416. This disclosure includes test data comparing the antihistaminic activity and other pharmacological properties of these compounds[1].

Patent Landscape

Regulatory and Legal Context

The patent's validity and scope have been subject to legal challenges. For instance, in the case of Otsuka Pharm. Co. v. Sandoz, Inc., the court upheld the validity of related patent claims (U.S. Patent 5,006,528) against generic drug manufacturers. The defendants had argued that the claims were invalid due to obviousness and obviousness-type double patenting, but these arguments were rejected[1].

Patent Term Extension

Although the patent itself has expired, the concept of patent term extension under 35 U.S.C. § 156 is relevant for understanding how patents in the pharmaceutical sector can be extended. However, this specific patent did not receive such an extension as it had expired before any potential extension could be applied[2].

Patent Analytics and Claim Coverage

To fully understand the protection and gaps in the patent landscape, companies often use patent analytics tools. These tools help in categorizing patents by claims and scope concepts, making it easier to determine which patents and claims are actively protecting the intellectual property. For example, a Claim Coverage Matrix can show which patents and claims cover specific technologies and where opportunities or gaps exist[3].

Impact on Pharmaceutical Development

The patent has had a significant impact on the development of CNS controlling agents. The disclosure of the unsubstituted butoxy compound and other carbostyril derivatives has contributed to the understanding of potential antipsychotic activities. For instance, the mouse jumping test data provided by Dr. Nakagawa, although not directly mentioning schizophrenia, was found to be indicative of potential antipsychotic activity by the skilled artisan[1].

Key Takeaways

• Broad Genus of Compounds: The patent covers a vast array of carbostyril derivatives with various pharmacological activities.
• Specific Claims: Key claims include the unsubstituted butoxy compound and methods of producing antihistaminic effects.
• Legal and Regulatory Context: The patent's validity was upheld in legal challenges, and it did not receive a patent term extension.
• Impact on Development: The patent has contributed significantly to the development of CNS controlling agents, including potential antipsychotic drugs.

FAQs

What is the main subject of United States Patent 4,734,416?

The main subject of the patent is the disclosure and claims of pharmaceutically useful carbostyril derivatives, particularly those with antihistaminic and central nervous controlling actions.

What is the "unsubstituted butoxy" compound mentioned in the patent?

The "unsubstituted butoxy" compound is a specific carbostyril derivative with an unsubstituted phenyl ring and a butoxy linker connecting the 7-position of its carbostyril core to its piperazine ring.

How did the patent impact the development of CNS controlling agents?

The patent contributed to the understanding and development of CNS controlling agents by disclosing a broad genus of carbostyril derivatives, including those with potential antipsychotic activities.

Was the patent extended under 35 U.S.C. § 156?

No, the patent did not receive a patent term extension under 35 U.S.C. § 156 as it had expired before any potential extension could be applied.

What tools can be used to analyze the claim coverage of this patent?

Tools such as patent analytics software, Claim Coverage Matrices, and interactive claim charts can be used to analyze the claim coverage and identify gaps or opportunities in the patent landscape.

Sources

1. Otsuka Pharm. Co. v. Sandoz, Inc., 678 F.3d 1280.
2. USPTO, Eligibility Requirements for Patent Term Extension.
3. Schwegman, Patent Analytics.
4. Google Patents, US4734416A - Pharmaceutically useful carbostyril derivatives.

Drugs Protected by US Patent 4,734,416

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

Foreign Priority and PCT Information for Patent: 4,734,416

Foriegn Application Priority Data
Foreign Country	Foreign Patent Number	Foreign Patent Date
Japan	53-37783	Mar 30, 1978

International Family Members for US Patent 4,734,416

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Austria	376432
Austria	376433
Austria	376434