Details for Patent: 8,513,202

Which drugs does patent 8,513,202 protect, and when does it expire?

Patent 8,513,202 protects INVOKAMET XR, INVOKAMET, and INVOKANA, and is included in three NDAs.

This patent has forty-nine patent family members in thirty-eight countries.

Summary for Patent: 8,513,202

Title:	Crystalline form of 1-(.beta.-D-glucopyranosyl)-4-methyl-3-[5-(4-fluorophenyl)-2-thienylmethy- l]benzene hemihydrate
Abstract:	A novel crystal form of 1-(.beta.-D-glucopyranosyl)-4-methyl-3-[5-(4-fluorophenyl)-2-thienylmethy- l]benzene hemihydrate, and having favorable characteristics, is characterized by its x-ray powder diffraction pattern and/or by its infra-red spectrum.
Inventor(s):	Nomura; Sumihiro (Osaka, JP), Kawanishi; Eiji (Osaka, JP)
Assignee:	Mitsubishi Tanabe Pharma Corporation (Osaka-Shi, JP)
Application Number:	13/103,557
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 8,513,202
Patent Claim Types: see list of patent claims	Compound; Process; Composition; Use;

United States Patent 8,513,202: A Comprehensive Analysis

Introduction

Crystalline Form of 1-(β-D-glucopyranosyl)-4-methyl-3-[5-(4-fluorophenyl)-2-thienylmethyl]benzene Hemihydrate

United States Patent 8,513,202, issued on August 20, 2013, pertains to a crystalline form of 1-(β-D-glucopyranosyl)-4-methyl-3-[5-(4-fluorophenyl)-2-thienylmethyl]benzene hemihydrate. This compound is significant as an inhibitor of sodium-dependent glucose transporters (SGLT) and has therapeutic applications in treating diabetes and related complications[1][2].

Scope of the Patent

Claims and Scope

The patent claims cover the crystalline compound itself, methods for its preparation and isolation, and pharmaceutical compositions that include the compound along with a pharmaceutically acceptable carrier[1]. The crystalline form of the compound is described as being in a hemihydrate form, which is crucial for its stability and efficacy[1].

Therapeutic Applications

Therapeutic Uses

The crystalline compound of Patent 8,513,202 is designed to inhibit sodium-dependent glucose transporters, thereby reducing blood glucose levels. This makes it useful in treating various conditions related to diabetes, including type 1 and type 2 diabetes mellitus, diabetic complications such as retinopathy, neuropathy, and nephropathy, postprandial hyperglycemia, delayed wound healing, insulin resistance, hyperglycemia, hyperinsulinemia, elevated blood levels of fatty acids and glycerol, hyperlipidemia, obesity, hypertriglyceridemia, Syndrome X, atherosclerosis, and hypertension[1].

Preparation and Isolation Methods

Methods of Preparation

The patent provides detailed methods for preparing and isolating the crystalline form of the compound. These methods involve forming a solution of the compound and precipitating it from solution using appropriate solvents. Impurities can act as crystallization inhibitors and need to be removed using conventional techniques such as silica gel column chromatography[1].

Pharmaceutical Compositions

Pharmaceutical Compositions

The patent also covers pharmaceutical compositions that include the crystalline form of the compound along with a pharmaceutically acceptable carrier. These compositions are designed to enhance the therapeutic efficacy of the compound when administered to patients[1].

Legal Status and Infringement Cases

Legal Status and Infringement Cases

There have been legal actions related to this patent. For instance, Mitsubishi Tanabe Pharma Corporation and Janssen Pharmaceuticals have filed lawsuits against companies like Sandoz Inc. and Zydus Pharmaceuticals for infringement of this patent. These lawsuits aim to protect the exclusive rights granted by the patent and prevent unauthorized use or manufacture of the compound[2][5].

Patent Landscape

Patent Landscape Overview

The patent landscape for this compound is significant within the context of diabetes treatment. The IPC classification for this patent falls under C07D, which pertains to heterocyclic compounds. This classification indicates that a substantial portion of patent applications related to this compound involve heterocyclic structures[3].

Conclusion

Key Takeaways

1. Crystalline Compound: The patent covers a specific crystalline form of 1-(β-D-glucopyranosyl)-4-methyl-3-[5-(4-fluorophenyl)-2-thienylmethyl]benzene hemihydrate.
2. Therapeutic Applications: The compound is an inhibitor of sodium-dependent glucose transporters and is useful in treating various diabetes-related conditions.
3. Preparation Methods: Detailed methods for preparing and isolating the crystalline form are provided.
4. Pharmaceutical Compositions: The patent includes pharmaceutical compositions that enhance the therapeutic efficacy of the compound.
5. Legal Status: There have been legal actions to protect the exclusive rights granted by this patent.

FAQs

1. What is the specific crystalline compound covered by Patent 8,513,202?

   • The crystalline compound is 1-(β-D-glucopyranosyl)-4-methyl-3-[5-(4-fluorophenyl)-2-thienylmethyl]benzene hemihydrate[1].

2. What are the therapeutic applications of this compound?

   • It is used to inhibit sodium-dependent glucose transporters, thereby reducing blood glucose levels and treating conditions like type 1 and type 2 diabetes mellitus, diabetic complications, postprandial hyperglycemia, and others[1].

3. How is the crystalline form prepared and isolated?

   • The preparation involves forming a solution of the compound and precipitating it from solution using appropriate solvents. Impurities are removed using conventional techniques like silica gel column chromatography[1].

4. Are there any legal actions related to this patent?

   • Yes, there have been lawsuits filed against companies like Sandoz Inc. and Zydus Pharmaceuticals for infringement of this patent[2][5].

5. What is the significance of the IPC classification for this patent?

   • The IPC classification falls under C07D, indicating that a substantial portion of patent applications related to this compound involve heterocyclic structures[3].

Sources Cited

1. US Patent 8,513,202 - Crystalline form of 1-(β-D-glucopyranosyl)-4-methyl-3-[5-(4-fluorophenyl)-2-thienylmethyl]benzene hemihydrate[1].
2. PharmaCompass - Mitsubishi Tanabe Pharma Corp. v. Sandoz Inc. for patent infringement[2].
3. BioRxiv - A novel approach to understanding patents from drug discovery[3].
4. GreyB - Diabetes drug patents expiring from 2024 till 2028[4].
5. FDA Document - Canagliflozin and Metformin Hydrochloride[5].

Drugs Protected by US Patent 8,513,202

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Janssen Pharms	INVOKAMET XR	canagliflozin; metformin hydrochloride	TABLET, EXTENDED RELEASE;ORAL	205879-002	Sep 20, 2016		RX	Yes	No	8,513,202		Y	Y		REDUCTION OF RISK OF MAJOR ADVERSE CARDIOVASCULAR EVENTS IN THE TREATMENT OF TYPE 2 DIABETES MELLITUS PATIENTS
Janssen Pharms	INVOKAMET XR	canagliflozin; metformin hydrochloride	TABLET, EXTENDED RELEASE;ORAL	205879-002	Sep 20, 2016		RX	Yes	No	8,513,202		Y	Y		REDUCTION OF RISK OF END STAGE KIDNEY DISEASE, DOUBLING OF SERUM CREATININE, CARDIOVASCULAR DEATH, AND HOSPITALIZATION FOR HEART FAILURE IN THE TREATMENT OF TYPE 2 DIABETES MELLITUS PATIENTS
Janssen Pharms	INVOKAMET XR	canagliflozin; metformin hydrochloride	TABLET, EXTENDED RELEASE;ORAL	205879-002	Sep 20, 2016		RX	Yes	No	8,513,202		Y	Y		TREATMENT OF TYPE 2 DIABETES MELLITUS

Foreign Priority and PCT Information for Patent: 8,513,202

Foriegn Application Priority Data
Foreign Country	Foreign Patent Number	Foreign Patent Date
Japan	2006-327019	Dec 04, 2006

International Family Members for US Patent 8,513,202

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Argentina	064099
Argentina	107510
Argentina	118450