Details for Patent: 11,236,091

Which drugs does patent 11,236,091 protect, and when does it expire?

Patent 11,236,091 protects LUMAKRAS and is included in one NDA.

This patent has twenty-three patent family members in nineteen countries.

Summary for Patent: 11,236,091

Title:	Solid state forms
Abstract:	The present disclosure provides crystalline and amorphous forms of 6-fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-(4-methyl-2-(2-propanyl)-3-pyridi- nyl)-4-((2S)-2-methyl-4-(2-propenoyl)-1-piperazinyl)pyrido[2,3-d]pyrimidin- -2(1H)-one, including several anhydrous, hydrate and solvate forms, and solid state forms thereof, pharmaceutical compositions, and methods of treating a disease mediated by KRAS G12C inhibition.
Inventor(s):	Chaves; Mary (Arlington, MA), Lopez; Patricia (Woodland Hills, CA), Agarwal; Prashant (Chelsea, MA), Amegadzie; Albert (Moorpark, CA), Azali; Stephanie (Woodland Hills, CA), Shimanovich; Roman (Brighton, MA), Kelly; Ron C. (Westlake Village, CA), Reid; Darren Leonard (Belmont, MA)
Assignee:	Amgen Inc. (Thousand Oaks, CA)
Application Number:	16/878,824
Patent Claim Types: see list of patent claims	Use; Composition; Compound; Dosage form;

Detailed Analysis of the Scope and Claims of United States Patent 11,236,091

Introduction

The United States Patent 11,236,091, assigned to Amgen Inc., is a significant patent in the field of cancer treatment, particularly focusing on KRAS G12C inhibitors. Here, we will delve into the scope, claims, and the broader patent landscape surrounding this invention.

Patent Overview

Title and Inventors

The patent titled "Solid state forms" was issued on February 1, 2022, to inventors Mary Chaves, Patricia Lopez, Prashant Agarwal, Albert Amegadzie, Stephanie Azali, Roman Shimanovich, Ron C. Kelly, and Darren Leonard Reid[2].

Assignee

The patent is assigned to Amgen Inc., a leading biotechnology company known for its innovative treatments in various medical fields[2].

Scope of the Patent

Subject Matter

The patent covers the solid state forms of a specific compound, identified as 6-fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-(4-methyl-2-(2-propanyl)-3-pyridinyl)-4-((2S)-2-methyl-4-(2-propenoyl)-1-piperazinyl)pyrido[2,3-d]pyrimidin-2(1H)-one. This compound is a selective inhibitor of the KRAS G12C mutant protein, which is implicated in various cancers, including non-small cell lung cancer (NSCLC) and colorectal cancer (CRC)[2][4].

Solid State Forms

The patent describes various solid state forms of the compound, including crystalline and amorphous forms, as well as different anhydrous, hydrate, and solvate forms. These forms are crucial for the stability, efficacy, and manufacturing process of the drug. For instance, differences in stability can arise from changes in chemical reactivity or mechanical characteristics, such as susceptibility to breakdown at high humidity[4].

Claims of the Patent

Independent Claims

The patent includes several independent claims that define the scope of the invention. These claims cover:

• The specific chemical structure of the compound.
• Various solid state forms, including crystalline and amorphous forms.
• Pharmaceutical compositions containing these solid state forms.
• Methods of treating diseases mediated by KRAS G12C inhibition using these compositions[2][4].

Dependent Claims

Dependent claims further specify the independent claims by detailing:

• Specific polymorphs and their characteristics.
• Methods of preparing these solid state forms.
• Dosage forms and their stability under different conditions[4].

Patent Landscape

Related Patents

The patent landscape surrounding KRAS G12C inhibitors is robust, with several related patents issued to Amgen Inc.:

• Patent 10,519,146: Covers KRAS G12C inhibitors, their compositions, and methods of use for treating various cancers. This patent expires on May 21, 2038[2].
• Patent 11,426,404: Focuses on methods of administering a KRAS G12C inhibitor and expires on September 15, 2040[2].

Patent Expiration Dates

The patent in question, US 11,236,091, expires on May 20, 2040. This timeline is crucial for understanding the exclusive rights period and potential generic competition[2].

Drug Exclusivity

In addition to patent protection, the FDA may grant exclusivity periods that can run concurrently with or independently of patent protection. This exclusivity can range from 180 days to seven years, depending on the circumstances[2].

Impact on Cancer Treatment

KRAS G12C Inhibition

KRAS G12C is a mutant form of the KRAS protein that is commonly found in certain types of cancer. Inhibitors targeting this mutation, like the one described in the patent, represent a significant advancement in cancer therapy. These inhibitors have shown promise in clinical trials for treating NSCLC and CRC, among other cancers[2][4].

Clinical Significance

The solid state forms described in the patent are critical for the development of stable and effective pharmaceutical formulations. This ensures that the drug maintains its efficacy and safety profile over its shelf life, which is vital for patient treatment outcomes.

Conclusion

The United States Patent 11,236,091 is a pivotal patent in the field of cancer treatment, particularly for KRAS G12C inhibitors. It covers a range of solid state forms of a key compound, ensuring the stability and efficacy of the drug. Understanding the scope, claims, and patent landscape is essential for both the development of new treatments and the strategic planning of pharmaceutical companies.

Key Takeaways

• The patent covers various solid state forms of a KRAS G12C inhibitor.
• It includes crystalline, amorphous, anhydrous, hydrate, and solvate forms.
• The patent expires on May 20, 2040.
• Related patents cover the composition and administration of KRAS G12C inhibitors.
• The invention is crucial for the treatment of cancers such as NSCLC and CRC.

FAQs

What is the main subject of United States Patent 11,236,091?

The main subject is the solid state forms of a compound that acts as a selective inhibitor of the KRAS G12C mutant protein.

Who are the inventors of this patent?

The inventors include Mary Chaves, Patricia Lopez, Prashant Agarwal, Albert Amegadzie, Stephanie Azali, Roman Shimanovich, Ron C. Kelly, and Darren Leonard Reid.

What types of cancers can be treated with the compound described in this patent?

The compound is useful for treating cancers such as non-small cell lung cancer (NSCLC) and colorectal cancer (CRC).

What is the significance of solid state forms in this patent?

The solid state forms are crucial for ensuring the stability, efficacy, and manufacturing process of the drug, affecting its chemical reactivity and mechanical characteristics.

When does the patent expire?

The patent expires on May 20, 2040.

Sources

1. United States Patent and Trademark Office - US11426404.pdf
2. Drugs.com - Generic Lumakras Availability
3. SSRN - Patent Claims and Patent Scope
4. Google Patents - US11236091B2 - Solid state forms
5. Unified Patents - WO-2017058915-A1 - Inhibitors of Kras G12c Mutant Proteins

Recent additions to Drugs Protected by US Patent 11,236,091

These patents are from the daily update and have not yet been integrated into the regular database

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	Type	RLD	Patent No.	Product	Substance	Delist Req.	Patent Expiration	Usecode	Patented / Exclusive Use
Amgen Inc	LUMAKRAS	sotorasib	TABLET	214665	May 28, 2021	RX	Yes	11,236,091	Y	Y			U-3306	TREATMENT OF ADULT PATIENTS WITH KRAS G12C-MUTATED LOCALLY ADVANCED OR METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC), AS DETERMINED BY AN FDA-APPROVED TEST, WHO HAVE RECEIVED AT LEAST ONE PRIOR SYSTEMIC THERAPY
Amgen Inc	LUMAKRAS	sotorasib	TABLET	214665	Jun 26, 2024	RX	Yes	11,236,091	Y	Y			U-3306	TREATMENT OF ADULT PATIENTS WITH KRAS G12C-MUTATED LOCALLY ADVANCED OR METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC), AS DETERMINED BY AN FDA-APPROVED TEST, WHO HAVE RECEIVED AT LEAST ONE PRIOR SYSTEMIC THERAPY
Amgen Inc	LUMAKRAS	sotorasib	TABLET	214665	Jan 20, 2023	RX	Yes	11,236,091	Y	Y			U-3306	TREATMENT OF ADULT PATIENTS WITH KRAS G12C-MUTATED LOCALLY ADVANCED OR METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC), AS DETERMINED BY AN FDA-APPROVED TEST, WHO HAVE RECEIVED AT LEAST ONE PRIOR SYSTEMIC THERAPY

Drugs Protected by US Patent 11,236,091

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Amgen Inc	LUMAKRAS	sotorasib	TABLET;ORAL	214665-001	May 28, 2021		RX	Yes	No	11,236,091		Y	Y		TREATMENT OF ADULT PATIENTS WITH KRAS G12C-MUTATED LOCALLY ADVANCED OR METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC), AS DETERMINED BY AN FDA-APPROVED TEST, WHO HAVE RECEIVED AT LEAST ONE PRIOR SYSTEMIC THERAPY
Amgen Inc	LUMAKRAS	sotorasib	TABLET;ORAL	214665-003	Jun 26, 2024		RX	Yes	No	11,236,091		Y	Y		TREATMENT OF ADULT PATIENTS WITH KRAS G12C-MUTATED LOCALLY ADVANCED OR METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC), AS DETERMINED BY AN FDA-APPROVED TEST, WHO HAVE RECEIVED AT LEAST ONE PRIOR SYSTEMIC THERAPY
Amgen Inc	LUMAKRAS	sotorasib	TABLET;ORAL	214665-002	Jan 20, 2023		RX	Yes	Yes	11,236,091		Y	Y		TREATMENT OF ADULT PATIENTS WITH KRAS G12C-MUTATED LOCALLY ADVANCED OR METASTATIC NON-SMALL CELL LUNG CANCER (NSCLC), AS DETERMINED BY AN FDA-APPROVED TEST, WHO HAVE RECEIVED AT LEAST ONE PRIOR SYSTEMIC THERAPY

International Family Members for US Patent 11,236,091

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Argentina	118978
Australia	2020280024
Brazil	112021023277
Canada	3140392
Canada	3225293