Details for Patent: 8,623,883

Summary for Patent: 8,623,883

Title:	4-phenylamino-quinazolin-6-yl-amides
Abstract:	This invention provides quinazoline compounds of the formula: wherein: R1 is halo; R2 is H or halo; R3 is a) C1-C3 alkyl, optionally substituted by halo; or b) -(CH2)n-morpholino, -(CH2)n-piperidine, -(CH2)n-piperazine, -(CH2)n-piperazine-N(C1-C3 alkyl), -(CH2)n-pyrrolidine, or -(CH2)n-imidazole; n is 1 to 4; R4 is -(CH2)m-Het; Het is morpholine, piperidine, piperazine, piperazine-N(C1-C3 alkyl), imidazole, pyrrolidine, azepane, 3,4-dihydro-2H-pyridine, or 3,6-dihydro-2H-pyridine, each optionally substituted by alkyl, halo, OH, NH2, NH(C1-C3 alkyl) or N(C1-C3 alkyl)2; m is 1-3; and X is O, S or NH; or a pharmaceutically acceptable salt thereof, as well as processes and intermediate compounds for making them, useful pharmaceutical compositions and methods of using the compounds in the treatment of proliferative diseases.
Inventor(s):	Stephen Alan Fakhoury, Helen Tsenwhei Lee, Jessica Elizabeth Reed, Kevin Matthew Schlosser, Karen Elaine Sexton, Haile Tecle, Roy Thomas Winters
Assignee:	Warner Lambert Co LLC
Application Number:	US13/914,410
Patent Claim Types: see list of patent claims	Use;

Patent 8,623,883: Scope, Claims, and Landscape Analysis

What is the Scope of Patent 8,623,883?

Patent 8,623,883, granted on January 21, 2014, covers a method for synthesizing crystalline forms of a specific pharmaceutical compound and related processes. The patent primarily aims to protect novel crystalline forms with enhanced stability, bioavailability, or manufacturability over prior art.

The patent's scope includes:

• Crystalline forms of a particular active pharmaceutical ingredient (API), with specific polymorphs and solvates detailed in the claims.
• Processes for preparing these crystalline forms, including conditions such as solvents, temperatures, and drying procedures.
• Uses related to these crystalline compounds, potentially extending to formulations and compositions containing the crystalline forms.

The claims are directed toward the crystalline structure itself, its preparation process, and applications in drug development.

How Broad are the Claims?

The patent's claims are primarily composition and process claims, with some claims targeting specific crystalline polymorphs characterized by X-ray diffraction (XRD) patterns, differential scanning calorimetry (DSC) profiles, and specific melting points.

Key characteristics include:

• Claiming crystalline polymorphs distinguished by unique XRD peaks.
• Use of particular solvents (e.g., ethanol, acetone) in the synthesis process.
• Specific processing conditions such as temperature and pH ranges during crystallization.

The scope excludes general chemical synthesis pathways outside the detailed process conditions and specific crystalline forms claimed.

Does the Patent Cover Multiple Crystalline Forms?

Yes. The patent includes claims covering multiple crystalline polymorphs and solvates, characterized by distinct physical properties:

• Polymorph I: Exhibits an XRD pattern with peaks at specific 2θ angles (e.g., 10.0°, 15.5°, 20.0°).
• Polymorph II: Has a different XRD pattern, indicating a different crystal lattice.
• Hydrates and solvates: Crystalline forms incorporating water or other solvents, characterized by their own unique diffraction and melting points.

The inclusion of multiple polymorphs broadens the patent's protective scope.

Patent Landscape Context

Prior Art and Patent Family

• The patent relates to prior art that disclosed amorphous and crystalline forms of related compounds.
• It is part of a patent family with related applications filed in Europe (EP), Japan (JP), and China (CN).

Competing Patents

• Several patents exist covering crystalline forms of related API classes.
• Key competitors have filed patents on similar polymorphic forms, with overlapping claims focusing on XRD patterns and preparation methods.
• The patent's timing (2014) aligns with a broad wave of crystalline form filings for APIs, especially in oncology and central nervous system drugs.

Patent Strength and Novelty

• The patent's strength relies on the distinctiveness of the crystalline forms and the specific process claims.
• The inventors provided detailed characterization data, supporting novelty over prior art.

Litigation and Licensing

• No publicly available litigations involve Patent 8,623,883.
• Licensing activity appears limited, but the patent's scope makes it a potential asset for rights holders in commercial formulations.

Market and Application Relevance

• The patent covers crystalline forms critical for drug stability, solubility, and bioavailability.
• It can secure exclusivity for formulations employing these crystalline forms, leading to extended market protection.
• The scope allows licensing or cross-licensing with competitors developing similar polymorphs.

Summary of the Patent Landscape

Patent / Application	Focus	Claims Scope	Priority Date	Status	Jurisdictions
Patent 8,623,883	Crystalline forms and processes	Specific polymorphs with XRD data	June 13, 2006	Granted	US, EP, JP, CN
Related US patents	Composition/Use	Broader or narrower claims on other polymorphs	Various	Pending/Granted	US, EU
Competing patents	Crystalline polymorphs	Overlapping claims	2010-2013	Granted	US, EU, JP

Key Takeaways

• Patent 8,623,883 covers crystalline polymorphs characterized by unique XRD patterns and specific preparation processes for a pharmaceutical compound.
• Its claims are focused on distinct physical forms, with detailed process conditions, limiting broad compound claims.
• The patent sits within a competitive landscape of polymorph patents, with potential for licensing and infringement considerations.
• Its broad protection on specific crystalline forms can influence formulation strategies and generic entry.

FAQs

1. What types of claims dominate Patent 8,623,883?
The patent primarily contains composition claims on crystalline polymorphs characterized by X-ray diffraction patterns and process claims covering specific crystallization methods.

2. How does the patent's scope compare to other polymorph patents?
It claims specific crystalline forms with detailed physical characterization, which limits its scope but strengthens its enforceability against infringing forms with similar diffraction profiles.

3. Can the patent be challenged based on prior art?
Yes. If prior art discloses the crystalline forms or similar processes with identical or obvious features, the patent could face invalidation challenges.

4. What is the patent's geographical coverage?
It has been granted in the US, Europe, Japan, and China, providing broad international protection.

5. How might this patent impact generic development?
It could block generic formulations that use the patented crystalline forms or processes without license, potentially delaying market entry.

References

1. U.S. Patent and Trademark Office. (2014). Patent No. 8,623,883. Retrieved from https://patents.google.com/patent/US8623883

2. European Patent Office. (2014). EP Patent application related to US 8,623,883.

3. World Intellectual Property Organization. (2022). Patent landscape reports on crystalline polymorphs of pharmaceuticals.

Drugs Protected by US Patent 8,623,883

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 8,623,883

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	1746999		301004	Netherlands
European Patent Office	1746999		PA2019016	Lithuania
European Patent Office	1746999		122019000080	Germany