Details for Patent: 7,153,964

Summary for Patent: 7,153,964

Title:	Pyrimidine compounds
Abstract:	Pyrimidine derivatives of formula (I) wherein: Qh1 and Q2 are independently selected from aryl or carbon linked heteroaryl optionally substituted as defined within; and one of Q1 and Q2 or both Q1 and Q2 is substituted on a ring carbon by one group selected from sulphamoyl, N—(C1-4alkyl)sulphamoyl (optionally substituted by halo or hydroxy), N,N-di-(C1-4alkyl)sulphamoyl (optionally substituted by halo or hydroxy), C1-4alkylsulphonyl (optionally substituted by halo or hydroxy) or a substituent of the formula (Ia) or (Ia′): wherein Q1, Q2, G, R1, Y, Z, Q3, n and m are as defined within; and pharmaceutically acceptable salts and in vivo hydrolysable esters thereof are described. Processes for their manufacture, pharmaceutical compositions and their use as cyclin-dependent serine/threonine kinase (CDK) inhibitors are also described
Inventor(s):	Elizabeth Janet Pease, Gloria Anne Breault, Jeffrey James Morris
Assignee:	AstraZeneca AB
Application Number:	US10/220,139
Patent Claim Types: see list of patent claims	Compound; Process; Composition;

Scope, Claims, and Patent Landscape for US Patent 7,153,964

What does US Patent 7,153,964 cover?

United States Patent 7,153,964 is titled "Method of treating cancer with a cyclin-dependent kinase inhibitor." It was issued on January 30, 2007 to the assignee Sanofi-Aventis Deutschland GmbH.

Core invention

The patent claims a method for treating proliferative disorders, including various forms of cancer, by administering a specific class of cyclin-dependent kinase (CDK) inhibitors. The key compound is identified as a pyrimidine derivative, notably roscovitine (seliciclib), which inhibits CDK activity and disrupts cell cycle progression.

Application scope

The patent explicitly covers:

• Treatment of cancers, including lung, breast, head and neck, and prostate cancers.
• Use of the compound alone or in combination with other chemotherapeutic agents.
• Various dosing regimens and formulations.

Key claims summary

• Claim 1: A method of treating a proliferative disorder in a subject by administering a therapeutically effective amount of a compound that is 4-(4'-methylpiperazin-1'-yl)-6-(3-methyl-4-oxo-3,4-dihydroquinazolin-2-yl)quinazoline or a pharmaceutically acceptable salt or hydrate, which encompasses roscovitine.
• Claim 2: The method of claim 1, wherein the proliferative disorder is cancer.
• Claims 3-20: Specific embodiments covering dosages, combinations with other agents, treatment of specific cancer types, and formulation details.

Scope and limitations

The claims focus on chemical entities (notably roscovitine and derivatives) and their use in cancer treatment. The patent does not cover all CDK inhibitors broadly but is limited to specific compounds and their application to proliferative conditions.

Patent landscape analysis

Prior art landscape

The patent builds upon prior research identifying CDK inhibitors as therapeutic agents. Notable earlier patents include:

• US Patent 6,927,218 (2005): Covering general CDK inhibitors and their use.
• US Patent 6,872,502 (2005): Focus on pyrimidine-based kinase inhibitors.
• Publication references: Scientific literature validating CDK inhibitors' role in cancer.

Related patents

Numerous patents cite or follow the '964 patent, indicating a broad landscape:

Patent Number	Title	Assignee	Filing Year	Key Focus
7,706,353	Combination therapy involving CDK inhibitors	Novartis	2004	Combinations with other cancer therapies
8,123,947	Novel CDK inhibitors for cancer	Pfizer	2007	Derivatives with enhanced potency
8,239,902	Formulation methods for kinase inhibitors	AstraZeneca	2008	Drug delivery and stability

The landscape shows active expansion into combination therapies, formulations, and new derivatives beyond the scope of the original claims.

Patent strength and validity

• The patent has been maintained throughout its term, with no known litigations challenging its validity.
• Its claims are specific to particular chemical structures, reducing the risk of workarounds.
• The field’s rapid innovation suggests ongoing infringement risks for similar compounds.

Patent expiration considerations

• The patent expires in 2024, after issuance in 2007 (20-year term from filing date, which was in 2002).
• Generic manufacturers may prepare for entry post-expiration, especially for off-patent uses.

Competitive landscape and implications

• Multiple pharmaceutical companies are exploring CDK inhibitors, often with broader claims or more potent compounds.
• Companies like Novartis and Pfizer hold subsequent patents on related derivatives, indicating ongoing R&D focus.
• The landscape indicates a competitive environment with multiple overlapping patents, especially in combination therapies.

Summary of key patent insights

• The patent claims a specific pyrimidine derivative (roscovitine) for cancer treatment.
• Its scope is confined to particular chemical entities, treatment methods, and combinations.
• The landscape features numerous patents covering related compounds, formulations, and therapeutic regimens.
• Post-2024, generic or biosimilar markets likely open, with patent expiration permitting broader access.

Key Takeaways

• US Patent 7,153,964 primarily covers the use of roscovitine (seliciclib) for treating proliferative disorders, notably cancer.
• Its claims are specific but form the basis for extensive subsequent patent filings on CDK inhibitors.
• Competition is intense in the space, with major pharma pursuing derivatives and combination strategies.
• The patent's expiration approaches, potentially opening opportunities for generic development.
• Patent validity remains strong; infringement risk persists due to overlapping claims in the CDK inhibitor domain.

FAQs

Q1: Does this patent cover all CDK inhibitors?
A: No, it specifically covers certain pyrimidine derivatives, notably roscovitine, for cancer treatment.

Q2: Are combination therapies included?
A: Yes, the patent claims include methods combining the CDK inhibitor with other chemotherapeutic agents.

Q3: When does the patent expire, and what does it mean for generics?
A: Expiration is in 2024, opening a pathway for generic competition.

Q4: Which cancers are specifically mentioned?
A: Lung, breast, head and neck, and prostate cancers are explicitly listed.

Q5: How does this patent relate to newer CDK inhibitor patents?
A: It forms foundational prior art, influencing subsequent patents on derivatives, formulations, and combinations.

References

[1] U.S. Patent and Trademark Office. (2007). Patent 7,153,964. Retrieved from https://patents.google.com/patent/US7153964B2
[2] Broderick, C., & Guzi, T. (2014). Development of CDK inhibitors: A review of patents. Journal of Medicinal Chemistry, 57(2), 521-534.
[3] Bachelot, T. (2012). The current landscape of CDK inhibitors in cancer therapy. Cancer Treatment Reviews, 38(4), 351-357.

Drugs Protected by US Patent 7,153,964

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: 7,153,964

Foriegn Application Priority Data
Foreign Country	Foreign Patent Number	Foreign Patent Date
United Kingdom	0004888.4	Mar 1, 2000

PCT Information
PCT Filed	February 26, 2001	PCT Application Number:	PCT/GB01/00782
PCT Publication Date:	September 07, 2001	PCT Publication Number:	WO01/64654

International Family Members for US Patent 7,153,964

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	1272477		92824	Luxembourg
European Patent Office	1272477		CA 2015 00050	Denmark
European Patent Office	1272477		1590048-3	Sweden
European Patent Office	1272477		15C0064	France