Details for Patent: 9,416,136

Which drugs does patent 9,416,136 protect, and when does it expire?

Patent 9,416,136 protects KISQALI and KISQALI FEMARA CO-PACK (COPACKAGED) and is included in two NDAs.

This patent has sixty-one patent family members in forty-eight countries.

Summary for Patent: 9,416,136

Title:	Pyrrolopyrimidine compounds and their uses
Abstract:	The disclosed compounds relate to treatments and therapies for protein kinase-associated disorders. There is also a need for compounds useful in the treatment or prevention or amelioration of one or more symptoms of cancer, transplant rejections, and autoimmune diseases. Furthermore, there is a need for methods for modulating the activity of protein kinases, such as CDK1, CDK2, CDK4, CDK5, CDK6, CDK7, CDK8 and CDK9, using the compounds provided herein. ##STR00001##
Inventor(s):	Besong; Gilbert (Cambridge, GB), Brain; Christopher Thomas (Cambridge, MA), Brooks; Clinton A (Beaufort, NC), Congreve; Miles Stuart (Cambridge, GB), Dagostin; Claudio (Cambridge, GB), He; Guo (Cambridge, MA), Hou; Ying (Cambridge, MA), Howard; Steven (Cambridge, GB), Li; Yue (Shanghai, CN), Lu; Yipin (Emeryville, CA), Mortenson; Paul (Cambridge, GB), Smith; Troy (Cambridge, MA), Sung; Moo Je (Cambridge, MA), Woodhead; Steven (Cambridge, GB), Wrona; Wojciech (Waltham, MA), Lagu; Bharat (Cambridge, MA)
Assignee:	Novartis AG (Basel, CH) Astex Therapeutics, Ltd. (Cambridge, GB)
Application Number:	14/158,358
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 9,416,136
Patent Claim Types: see list of patent claims	Use;

Detailed Analysis of the Scope and Claims of United States Patent 9,416,136

Introduction

United States Patent 9,416,136, titled "Pyrrolopyrimidine compounds and their uses," is a patent that discloses compounds and methods related to the treatment of protein kinase-associated disorders. This analysis will delve into the scope, claims, and the broader patent landscape surrounding this patent.

Overview of the Patent

Invention Description

The patent describes a class of pyrrolopyrimidine compounds, which are designed to inhibit protein kinases. These compounds are intended for use in various therapeutic applications, including the treatment of cancer, inflammatory diseases, and other conditions associated with abnormal protein kinase activity[1].

Scope of the Patent

Therapeutic Applications

The scope of the patent includes the use of pyrrolopyrimidine compounds in treating a range of diseases. This encompasses cancer, particularly those involving aberrant kinase activity, as well as inflammatory and autoimmune diseases. The compounds are also explored for their potential in treating other kinase-related disorders[1].

Chemical Structure

The patent details the chemical structure of the pyrrolopyrimidine compounds, including various substituents and modifications that enhance their therapeutic efficacy and pharmacokinetic properties. The structural descriptions are critical for understanding the novelty and inventiveness of the compounds[1].

Claims of the Patent

Independent Claims

The patent includes several independent claims that define the scope of the invention. These claims typically cover the chemical structure of the compounds, methods of preparing them, and their use in therapeutic applications. For example, Claim 1 might describe a specific pyrrolopyrimidine compound, while Claim 10 might cover a method of treating cancer using one of these compounds[1].

Dependent Claims

Dependent claims further narrow down the scope by adding additional limitations to the independent claims. These could include specific substituents, dosages, or administration methods that are part of the invention. Dependent claims help to provide a clearer definition of what is protected under the patent[1].

Patent Landscape

Prior Art and Novelty

To understand the patent landscape, it is essential to consider the prior art in the field of protein kinase inhibitors. The patent must demonstrate novelty and non-obviousness over existing compounds and methods. The disclosure must show how the pyrrolopyrimidine compounds differ from and improve upon prior art[1].

Competing Patents

The patent landscape includes other patents related to protein kinase inhibitors. Companies and researchers in the pharmaceutical industry often file multiple patents covering different aspects of kinase inhibition. Analyzing these competing patents helps in identifying potential infringement risks and opportunities for differentiation[3].

Administrative and Judicial Challenges

PTAB and Inter Partes Review

Given the significance of patents in the pharmaceutical industry, challenges to patent validity are common. The Patent Trial and Appeal Board (PTAB) plays a crucial role in this context through inter partes review (IPR) and post-grant review (PGR) proceedings. These administrative challenges can be more streamlined and cost-effective compared to federal court litigation, but they also introduce uncertainties and controversies regarding patent rights[2].

Judicial Precedents

Court decisions, such as those from the Federal Circuit, can impact the interpretation and enforcement of patents like US 9,416,136. For instance, decisions on issues like obviousness, double patenting, and patent term adjustments can affect the validity and scope of the patent claims[4].

Patent Analytics and Claim Coverage

Claim Coverage Matrix

To manage and analyze the patent portfolio effectively, companies use tools like Claim Coverage Matrix and Claim Charts. These tools help in categorizing patents by claims and scope concepts, making it easier to identify which patents and claims are actively protecting the intellectual property and where gaps or opportunities exist[3].

Scope Concepts and Claim Charts

The scope concepts of the patent claims are crucial for determining their value and applicability. Interactive claim charts generated by software like ClaimScape® can help technical experts and management to review patent coverage, identify gaps, and highlight future design opportunities[3].

Regulatory and Commercial Implications

Premarket Approval and Regulatory Review

For pharmaceutical patents, regulatory approval is a critical step. Patents like US 9,416,136 must align with regulatory requirements, such as those set by the FDA. The approval process can extend the patent term through mechanisms like patent term extension (PTE) due to regulatory review periods[5].

Market Impact and Competition

The commercial success of a patent depends on its ability to protect a unique and valuable invention. In the competitive landscape of pharmaceuticals, patents like US 9,416,136 must be strategically managed to ensure market exclusivity and to deter competitors from infringing on the protected claims.

Key Takeaways

• Therapeutic Applications: The patent covers the use of pyrrolopyrimidine compounds in treating various diseases, including cancer and inflammatory disorders.
• Chemical Structure: The patent details the specific chemical structure of the compounds, which is crucial for their therapeutic efficacy.
• Claims: The patent includes independent and dependent claims that define the scope of the invention.
• Patent Landscape: The patent must be considered within the broader landscape of protein kinase inhibitors, including prior art and competing patents.
• Administrative and Judicial Challenges: The patent is subject to challenges through PTAB and federal court litigation.
• Patent Analytics: Tools like Claim Coverage Matrix and Claim Charts are essential for managing and analyzing the patent portfolio.

FAQs

Q: What is the primary therapeutic application of the pyrrolopyrimidine compounds described in US 9,416,136?

A: The primary therapeutic application is the treatment of protein kinase-associated disorders, including cancer and inflammatory diseases.

Q: How do administrative challenges like IPR affect the validity of patents like US 9,416,136?

A: IPR proceedings before PTAB can challenge the validity of patents by requiring a lower burden of proof compared to federal court litigation, potentially leading to the cancellation of patent claims if they are found to be unpatentable.

Q: What role do Claim Coverage Matrix and Claim Charts play in managing patent portfolios?

A: These tools help in categorizing patents by claims and scope concepts, identifying gaps in coverage, and highlighting future design opportunities, making it easier to manage and analyze large numbers of patent claims.

Q: How can regulatory approval processes impact the patent term of pharmaceutical patents?

A: Regulatory approval processes can extend the patent term through mechanisms like patent term extension (PTE) due to regulatory review periods.

Q: What are some potential commercial implications of holding a patent like US 9,416,136 in the pharmaceutical industry?

A: Holding such a patent can provide market exclusivity, deter competitors from infringing on the protected claims, and ensure a competitive edge in the market.

Sources

1. US9416136B2 - Pyrrolopyrimidine compounds and their uses - Google Patents
2. The Patent Trial and Appeal Board and Inter Partes Review - Congressional Research Service
3. Patent Analytics - Schwegman, Lundberg & Woessner, P.A.
4. In re Cellect - United States Court of Appeals for the Federal Circuit
5. FEB 0 6 2018 - Regulations.gov - FDA Review of KISQALI

Drugs Protected by US Patent 9,416,136

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Novartis	KISQALI	ribociclib succinate	TABLET;ORAL	209092-001	Mar 13, 2017		RX	Yes	Yes	9,416,136					IN COMBINATION WITH AN AROMATASE INHIBITOR FOR THE TREATMENT OF PRE/PERIMENOPAUSAL OR POSTMENOPAUSAL WOMEN WITH HR-POSITIVE, HER2-NEGATIVE ADVANCED OR METASTATIC BREAST CANCER, AS INITIAL ENDOCRINE-BASED THERAPY
Novartis	KISQALI	ribociclib succinate	TABLET;ORAL	209092-001	Mar 13, 2017		RX	Yes	Yes	9,416,136					IN COMBINATION WITH FULVESTRANT FOR THE TREATMENT OF POSTMENOPAUSAL WOMEN WITH HR-POSITIVE, HER2-NEGATIVE ADVANCED OR METASTATIC BREAST CANCER, AS INITIAL ENDOCRINE BASED THERAPY OR FOLLOWING DISEASE PROGRESSION ON ENDOCRINE THERAPY
Novartis	KISQALI	ribociclib succinate	TABLET;ORAL	209092-001	Mar 13, 2017		RX	Yes	Yes	9,416,136					IN COMBINATION WITH AN AROMATASE INHIBITOR AS INITIAL ENDOCRINE-BASED THERAPY FOR TREATMENT OF POSTMENOPAUSAL WOMEN WITH HORMONE RECEPTOR (HR)-POSITIVE, HUMAN EPIDERMAL GROWTH FACTOR RECEPTOR 2 (HER-2)-NEGATIVE ADVANCED OR METASTATIC BREAST CANCER
Novartis	KISQALI	ribociclib succinate	TABLET;ORAL	209092-001	Mar 13, 2017		RX	Yes	Yes	9,416,136					IN COMBINATION WITH AN AROMATASE INHIBITOR FOR THE ADJUVANT TREATMENT OF ADULTS WITH HORMONE RECEPTOR (HR)-POSITIVE, HUMAN EPIDERMAL GROWTH FACTOR RECEPTOR 2 (HER2)-NEGATIVE STAGE II AND III EARLY BREAST CANCER AT HIGH RISK OF RECURRENCE
Novartis	KISQALI	ribociclib succinate	TABLET;ORAL	209092-001	Mar 13, 2017		RX	Yes	Yes	9,416,136					IN COMBINATION WITH FULVESTRANT AS INITIAL ENDOCRINE-BASED THERAPY OR FOLLOWING DISEASE PROGRESSION ON ENDOCRINE THERAPY IN POSTMENOPAUSAL WOMEN OR IN MEN, FOR THE TREATMENT OF HR-POSITIVE, HER2-NEGATIVE ADVANCED OR METASTATIC BREAST CANCER
Novartis	KISQALI	ribociclib succinate	TABLET;ORAL	209092-001	Mar 13, 2017		RX	Yes	Yes	9,416,136					IN COMBINATION WITH AN AROMATASE INHIBITOR AS INITIAL ENDOCRINE-BASED THERAPY FOR THE TREATMENT OF ADULT PATIENTS WITH HORMONE RECEPTOR (HR)-POSITIVE, HUMAN EPIDERMAL GROWTH FACTOR RECEPTOR 2 (HER2)-NEGATIVE ADVANCED OR METASTATIC BREAST CANCER
Novartis	KISQALI	ribociclib succinate	TABLET;ORAL	209092-001	Mar 13, 2017		RX	Yes	Yes	9,416,136					IN COMBINATION WITH FULVESTRANT AS INITIAL ENDOCRINE-BASED THERAPY OR FOLLOWING DISEASE PROGRESSION ON ENDOCRINE THERAPY, FOR THE TREATMENT OF ADULT PATIENTS WITH HR-POSITIVE, HER2-NEGATIVE ADVANCED OR METASTATIC BREAST CANCER

International Family Members for US Patent 9,416,136

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	2331547		300909	Netherlands
European Patent Office	2331547		PA2017039	Lithuania
European Patent Office	2331547		CR 2017 00060	Denmark
European Patent Office	2331547		122017000102	Germany
European Patent Office	2331547		LUC00048	Luxembourg
European Patent Office	2331547		2017C/052	Belgium
European Patent Office	2331547		1790067-1	Sweden