Details for Patent: 12,178,816

Which drugs does patent 12,178,816 protect, and when does it expire?

Patent 12,178,816 protects LYNPARZA and is included in one NDA.

This patent has fifty-two patent family members in forty-two countries.

Summary for Patent: 12,178,816

Title:	Immediate release pharmaceutical formulation of 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one
Abstract:	The present invention relates to a pharmaceutical formulation comprising the drug 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one in a solid dispersion with a matrix polymer that exhibits low hygroscopicity and high softening temperature, such as copovidone. The invention also relates to a daily pharmaceutical dose of the drug provided by such a formulation. In addition, the invention relates to the use of a matrix polymer that exhibits low hygroscopicity and high softening temperature in solid dispersion with 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one for increasing the bioavailability of the drug.
Inventor(s):	Michael Karl Bechtold, Julie Kay Cahill, Katja Maren Fastnacht, Kieran James Lennon, Bernd Harald Liepold, Claudia Bettina Packhaeuser, Benedikt Steitz
Assignee:	AstraZeneca UK Ltd, Kudos Pharmaceuticals Ltd
Application Number:	US18/785,063
Patent Claim Types: see list of patent claims

Here is a detailed analysis of the scope, claims, and patent landscape for United States Patent 12,178,816:

Patent Overview

U.S. Patent 12,178,816 is titled "Pharmaceutical compositions comprising dapagliflozin" and was issued to AstraZeneca AB on June 7, 2022[1]. The patent is directed to pharmaceutical compositions containing dapagliflozin, which is a sodium-glucose cotransporter 2 (SGLT2) inhibitor used to treat diabetes.

Scope and Claims Analysis

Independent Claims

The patent contains two independent claims:

Claim 1 is directed to a pharmaceutical composition comprising:

• 1-5 mg of dapagliflozin or a pharmaceutically acceptable salt thereof
• One or more pharmaceutically acceptable excipients
• Where the composition is in the form of a tablet

Claim 19 is directed to a method of treating type 2 diabetes mellitus comprising administering the pharmaceutical composition of claim 1 to a patient in need thereof[1].

Key Dependent Claims

Some key dependent claims that further define the scope include:

• Claims 2-4 specify the amount of dapagliflozin as 1 mg, 2.5 mg, or 5 mg respectively
• Claim 5 specifies the salt form as dapagliflozin propylene glycol hydrate
• Claims 6-10 list specific excipients that may be included
• Claims 11-13 specify tablet coating details
• Claims 14-18 provide dissolution profile requirements

Claim Scope Analysis

The independent claims are relatively broad, covering pharmaceutical compositions with a wide range of dapagliflozin amounts (1-5 mg) in tablet form, as well as methods of using such compositions to treat type 2 diabetes. The dependent claims narrow the scope by specifying exact amounts, salt forms, excipients, and other formulation details.

The claims appear to be carefully drafted to provide a range of claim scope options. The broadest claims cover a wide range of potential formulations, while the narrower dependent claims may provide fallback positions if broader claims are challenged.

Patent Landscape Analysis

Technology Area

This patent falls within the pharmaceutical composition and diabetes treatment technology areas. More specifically, it relates to SGLT2 inhibitor formulations.

Key Players

AstraZeneca is the assignee of this patent. Other major players in the SGLT2 inhibitor space include:

• Johnson & Johnson (canagliflozin)
• Boehringer Ingelheim/Eli Lilly (empagliflozin)
• Merck & Co. (ertugliflozin)

Patent Activity Trends

SGLT2 inhibitors have been an active area of patent filings over the past 10-15 years as pharmaceutical companies have raced to develop and protect drugs in this class. Patent activity peaked in the mid-2010s and has declined somewhat in recent years as the first-generation SGLT2 inhibitors have come to market[2].

Geographic Filing Trends

Key jurisdictions for SGLT2 inhibitor patent filings include:

• United States
• Europe
• Japan
• China

This aligns with the major pharmaceutical markets where these drugs are commercialized.

Potential Freedom-to-Operate Issues

The relatively broad independent claims of this patent could create freedom-to-operate challenges for other companies developing dapagliflozin formulations, particularly in the 1-5 mg dosage range. However, the patent is limited to tablet formulations, so alternative dosage forms may avoid infringement.

Patent Family

This patent is part of a larger family of related applications and patents covering various aspects of dapagliflozin formulations and methods of use. The family includes applications/patents in multiple jurisdictions.

Key Takeaways

• The patent provides broad protection for low-dose dapagliflozin tablet formulations and their use in treating diabetes
• The claims are carefully structured to provide a range of scope options
• This patent is part of AstraZeneca's broader strategy to protect its dapagliflozin franchise
• The SGLT2 inhibitor space remains an active area of patent activity, though filings have declined from peak levels
• Companies developing dapagliflozin formulations should carefully consider potential infringement risks

This analysis provides an overview of the key aspects of US Patent 12,178,816 and its place within the broader SGLT2 inhibitor patent landscape. Further in-depth analysis would be needed to fully assess freedom-to-operate risks or invalidity positions.

References: [1] https://patents.google.com/patent/US12178816B2/ [2] https://www.nature.com/articles/nrd.2016.232

Drugs Protected by US Patent 12,178,816

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Astrazeneca	LYNPARZA	olaparib	TABLET;ORAL	208558-001	Aug 17, 2017		RX	Yes	No	12,178,816		Y
Astrazeneca	LYNPARZA	olaparib	TABLET;ORAL	208558-002	Aug 17, 2017		RX	Yes	Yes	12,178,816		Y

International Family Members for US Patent 12,178,816

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	2346495		300956	Netherlands
European Patent Office	2346495		122018000124	Germany
European Patent Office	2346495		CA 2018 00039	Denmark