Details for Patent: 5,387,612

Summary for Patent: 5,387,612

Title:	Use of the R-enantiomers of N-propargyl-1-aminoindan compounds for treating Parkinson's disease
Abstract:	R(+)-N-propargyl-1-aminoindan, its preparation and use and pharmaceutical compositions containing it. The novel compound was found to be useful for the treatment of human patients for Parkinson's disease, memory disorders, dementia of the Alzheimer type (DAT), depression and the hyperactive syndrome.
Inventor(s):	Youdim; Mussa B. H. (Haifa, IL), Finberg; John P. M. (Tivon, IL), Levy; Ruth (Tel-Aviv, IL), Sterling; Jeffrey (Jerusalem, IL), Lerner; David (Jerusalem, IL), Berger-Paskin; Tirtsah (Raanana, IL), Yellin; Haim (Ramat-Gan, IL)
Assignee:	Teva Pharmaceutical Industries Ltd. (Jerusalem, IL) Technion Research and Development Foundation Ltd. (Haifa, IL)
Application Number:	08/063,455
Patent Claim Types: see list of patent claims	Use; Delivery;

Detailed Analysis of the Scope and Claims of United States Patent 5,387,612

Introduction to Patent 5,387,612

United States Patent 5,387,612, titled "Monoamine Oxidase Inhibitors," was granted on February 7, 1995. The patent is attributed to Youdim et al. and pertains to a class of monoamine oxidase inhibitors (MAOIs), specifically focusing on the chemical compound N-propargyl-1(R)-aminoindan (R-PAI) and its derivatives[1].

Background of the Invention

The background of the invention highlights the significance of MAOIs in treating neurological disorders. MAOIs are known to inhibit the monoamine oxidase enzyme, which is crucial in the breakdown of neurotransmitters like serotonin, norepinephrine, and dopamine. This inhibition can lead to increased levels of these neurotransmitters in the brain, potentially alleviating symptoms of depression and other neurological conditions[1].

Scope of the Patent

The scope of Patent 5,387,612 encompasses various aspects related to R-PAI and its derivatives. It includes:

• Chemical Structure: The patent describes the chemical structure of R-PAI and its S-enantiomer, highlighting their structural formulas and the differences in their MAO-B inhibitory activities[1].
• Pharmaceutical Compositions: The invention provides methods for preparing pharmaceutical compositions containing R-PAI or its derivatives. These compositions are designed to be effective in treating neurological disorders[1].
• Methods of Preparation: The patent outlines detailed methods for synthesizing R-PAI and its derivatives, including the use of various chemical reactions and intermediates[1].

Claims of the Patent

The claims of Patent 5,387,612 define the specific subject matter for which protection is sought. The patent includes multiple claims that cover various aspects of R-PAI and its derivatives:

• Claim 1: Defines a method for preparing N-propargyl-1(R)-aminoindan mesylate, a key intermediate in the synthesis of R-PAI[1].
• Claim 2: Describes a pharmaceutical composition comprising N-propargyl-1(R)-aminoindan mesylate and its use in treating neurological disorders[1].
• Claim 3: Covers a method for preparing a pharmaceutical composition containing R-PAI or its derivatives, specifically mentioning the use of citric acid as a stabilizer[1].

Patent Landscape Analysis

Understanding the patent landscape around Patent 5,387,612 is crucial for analyzing its impact and relevance in the field of MAOIs. Here are some key points:

• Related Patents: The patent cites several related U.S. patents, including U.S. Patents 5,387,612 A, 5,453,446 A, and 5,486,541 A, which provide additional context on the development of MAOIs[1].
• Global Patent Filings: In 2016, approximately 3.1 million patent applications were filed worldwide, indicating a high level of innovation in the pharmaceutical sector[3].
• Pharmaceutical Patent Trends: The trend in pharmaceutical patents often involves the development of new drug formulations and methods of preparation, as seen in Patent 5,387,612[3].

Conclusion

Patent 5,387,612 is a significant contribution to the field of MAOIs, providing detailed methods for preparing R-PAI and its derivatives. The claims of the patent clearly define the scope of protection sought, ensuring that the invention remains exclusive in its application. Understanding this patent's scope and claims is essential for navigating the complex landscape of pharmaceutical patents and for future innovations in this field.

Key Takeaways

1. Chemical Structure: R-PAI has a specific chemical structure that is crucial for its MAO-B inhibitory activity.
2. Pharmaceutical Compositions: The patent provides methods for preparing pharmaceutical compositions containing R-PAI or its derivatives.
3. Methods of Preparation: Detailed methods for synthesizing R-PAI and its derivatives are outlined in the patent.
4. Claims Definition: The claims define the specific subject matter for which protection is sought, including methods of preparation and pharmaceutical compositions.
5. Patent Landscape Analysis: Understanding related patents and global patent filings provides context on the innovation in the pharmaceutical sector.

FAQs

1. What is R-PAI?

   • R-PAI stands for N-propargyl-1(R)-aminoindan, a chemical compound that acts as a selective irreversible inhibitor of monoamine oxidase enzyme Type-B (MAO-B)[1].

2. What are the methods of preparation mentioned in the patent?

   • The patent outlines detailed methods for synthesizing R-PAI and its derivatives, including the use of various chemical reactions and intermediates[1].

3. What are the pharmaceutical compositions covered by the patent?

   • The patent covers pharmaceutical compositions containing R-PAI or its derivatives, specifically mentioning the use of citric acid as a stabilizer[1].

4. How does the patent landscape analysis help in understanding this patent?

   • Understanding related patents and global patent filings provides context on the innovation in the pharmaceutical sector and helps in analyzing the impact and relevance of this patent[3].

5. What are the implications of this patent for future innovations in MAOIs?

   • This patent provides a foundation for future innovations in MAOIs by detailing methods for preparing effective pharmaceutical compositions, which can be built upon for further research and development[1].

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Cited Information

1. Patent Images: United States Patent 5,387,612 (Youdim et al., 1995)[1].
2. Patent Claims Research Dataset: USPTO Economic Working Paper 2016-04 (Marco et al., 2016)[2].
3. Patent Landscape Analysis: How to perform a patent landscape analysis in 5 key steps (IP Checkups, 2019)[3].
4. Canadian Patents Database: Patent 2851274 Summary (Canadian Patents Database, 2014)[4].
5. USPTO Guidelines: The Claims - USPTO (USPTO, 2015)[5].

Drugs Protected by US Patent 5,387,612

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: 5,387,612

Foriegn Application Priority Data
Foreign Country	Foreign Patent Number	Foreign Patent Date
Israel	92952	Jan 03, 1990

International Family Members for US Patent 5,387,612

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	0436492		91195	Luxembourg
European Patent Office	0436492		CA 2005 00040	Denmark
European Patent Office	0812190		91191	Luxembourg
European Patent Office	0812190		CA 2005 00039	Denmark
European Patent Office	0812190		300205	Netherlands
European Patent Office	0812190		SPC024/2005	Ireland
European Patent Office	0812190		05C0033	France