API and IP Newsletter

 

Contents

• Patent applications by Emcure Pharmaceuticals

• General information

• Daiichi-Singh brothers dispute: Delhi HC orders auctioning of Fortis trademark

• Delhi High Court reinstates Injunction stopping sale of Zydus’ Sigrima

• Intellectual Property

• T 3253/19 (Compositions containing borate-polyol complexes / NOVARTIS) 07-10-2024

Patent applications by Emcure Pharmaceuticals

We follow patent filings by Indian companies. This week, we followed patent applications filed by Emcure Pharmaceutical.

Public domain information shows that about 15 of Emcure’s patent applications have been published in the last five years. This assessment does not evaluate the strength of Emcure's IP or determine its legal status. However, it could provide an idea of the Emcure Development Centre's direction. What types of products are under development at Emcure? 

One must understand that there will be an 18-month lag. Patent applications are generally published 18 months after the priority date. 

Some of our observations are as below.

1. Over the past five years, Emcure has submitted far fewer applications than during the decade from 2009 to 2019. 

2. Some applications are related to complex processes for synthesising eribulin mesylate, iron complexes, etc. 

3. The patent application for synthesising eicosapentaenoic acid suggests Emcure could file a DMF soon for icosapent ethyl. Icosapent ethyl is used to control high blood triglyceride levels. 

4. Interestingly, Emcure is developing a patent portfolio around carmustine, a type of chemotherapy drug, and generic BiCNU. This is an old product and a small one in the US. The BiCNU® brand and generic market had approximately USD 20 million in U.S. sales.

Emcure’s patent portfolio around Carmustine is as follows.

Publication Number	Publication Date	Title	Comments
US20230210793A1	2023-07-06	Preparing administrable solution of carmustine, involves dissolving lyophilized carmustine in sterile propylene glycol, and diluting reconstituted solution with aqueous sodium chloride solution or aqueous dextrose solution	According to the BiCNU® (Carmustine ) prescribing information, the rate of administration should not be more than 1.66 mg/m2/min  BiCNU was approved in 1982. Administration of BiCNU® for less than 2 hours can lead to pain and burning at the site of injection.  According to the BiCNU® prescribing information, the rate of administration should not be more than 1.66 mg/m2/min.  This invention teaches the possibility of rapidly administering carmustine in a concentrated solution comprising propylene glycol and either an aqueous 0.9% sodium chloride solution or an aqueous 5% dextrose solution.
US11865206B2	2024-01-09	Pharmaceutical composition useful for treating e.g. brain tumors glioblastoma, brainstem glioma, medulloblastoma, astrocytoma, ependymoma, and metastatic brain tumors, comprises carmustine dissolved in polysorbate as sole solvent	This invention addresses a need for a stable, liquid, ready-to-use parenteral formulation of carmustine, which can be administered without the hassles of reconstitution.
US20200108010A1	2020-04-09	Use of administrable solution for treating cancer prepared by dissolving lyophilized carmustine in sterile propylene glycol to form reconstituted solution, and diluting solution with aqueous sodium chloride or dextrose solution	This invention addresses the need for improved kits that simplify the preparation and improve the safety of injectable carmustine solutions.
US20210361599A1	2021-11-25	Drug delivery system used for treating patient suffering from brain tumors such as glioblastoma, brainstem glioma, medulloblastoma, astrocytoma, room ependymoma, brain metastases and meningeal leukemia, comprises carmustine and additives	This invention allegedly reduces the undesired side effects of carmustine. It relates to a more efficient drug delivery system, which could increase the therapeutic benefit and pharmaceutical efficacy, reduce toxicity, and decrease side effects. The invention provides a novel drug delivery system for intravenous administration.
US10583101B2	2020-03-10	Lipid suspension composition useful in treatment of brain cancers, e.g. glioblastoma, medulloblastoma, astrocytoma, and ependymoma, multiple myeloma, Hodgkin's disease and non-Hodgkin lymphoma, comprises carmustine and lipid	An object of the present invention is to provide a stable lipid suspension formulation of Carmustine.   This invention provides a process for the preparation of a stable lipid suspension formulation of Carmustine. The process is allegedly simple, cost-effective, and commercially viable.

General information

Daiichi-Singh brothers dispute: Delhi HC orders auctioning of Fortis trademark

The Delhi High Court has ordered the auctioning of the Fortis trademark to execute a Rs 3,500 crore arbitration award in favour of Daiichi Sankyo against ex-Ranbaxy promoters.

News here

Delhi High Court reinstates Injunction stopping sale of Zydus’ Sigrima

The Division Bench of Delhi High Court, on October 16, 2024, reinstated the injunction preventing Zydus Lifesciences from manufacturing, selling, or marketing its breast cancer drug Sigrima, a biosimilar of Roche’s Pertuzumab (Perjeta). The decision, made in response to Roche’s appeal on October 16, 2024, reversed an earlier order from October 9, 2024.

News here

Intellectual Property 

T 3253/19 (Compositions containing borate-polyol complexes / NOVARTIS) 07-10-2024

Travoprost Formulation

This is regarding EP 2420223 patent issued to Novartis, titled Aqueous pharmaceutical compositions of Travoprost containing borate-polyol complexes.

The patent proprietor, Novartis AG, and both opponents (Generics [UK] Limited and  Alfred E. Tiefenbacher  ) filed appeals against the opposition division's interlocutory decision, which found that, based on auxiliary request 1 and the amended claim 1, the patent met the requirements of the EPC.

Claim 1 as granted, read as follows:

"A multi-dose ophthalmic composition configured for topical application as drops directly to the eye, comprising:

first polyol, the first polyol being mannitol, wherein the first polyol is at least 0.25 but less than 1.5 w/v % of the composition;

second polyol, the second polyol being selected from propylene glycol, glycerine or a combination thereof, wherein the second polyol is at least 0.1 but less than 5 w/v % of the composition;

borate, wherein the borate is at least 0.25 w/v % of the composition but less than 0.5 w/v % of the composition;

antimicrobial preservative wherein the preservative is at least 0.0003 but less than 0.003 w/v % of the composition and wherein the preservative is a polymeric quaternary ammonium compound;

travoprost;

polyoxyethylene (40) hydrogenated castor oil wherein the polyoxyethylene (40) hydrogenated castor oil is at least 0.03 but less than 0.5 w/v % of the composition; and

water,

wherein the pH of the composition is from 6.4 to 7.2; and

wherein the composition is substantially free of any benzalkonium chloride."

In claim 1 of auxiliary request 1, the range for the amount of borate was amended to "at least 0.25 w/v % of the composition but less than 0.35 w/v % of the composition".

In this write-up, we will understand Article 123 (2) of EPC. 

Article 123(2) of the European Patent Convention reads as follows: “The European patent application or patent may not be amended in such a way that it contains subject matter which extends beyond the content of the application as filed”

Let us understand how The Appeal Board opined on Article 123 (2) in this instance. 

Claim 1 of the sole pending request (i.e. auxiliary request 1) specifies the following ranges:

(a) the first polyol mannitol is at least 0.25 but less than 1.5 w/v % of the composition and

(b) the borate is at least 0.25 but less than 0.35 w/v % of the composition.

The relevant question is whether the amendments remain within the limits of what a skilled person would derive directly and unambiguously, using common general knowledge, from the whole application as filed.

The application, as filed, does not disclose the above ranges. Instead, these ranges combine endpoints disclosed in the following passages of the application as filed:

The range 0.25-1.5 w/v% for the amount of the first polyol being mannitol combines:

- the narrowest lower limit recited, for the first polyol in general, on page 7, lines 8-12:

"The first polyol is typically at least about 0.01 w/v %, more typically at least about 0.15 w/v % and more typically at 0.25 w/v % of the ophthalmic composition. The first polyol is also typically less than about 5.0 w/v %, more typically less than about 1.6 w/v % and even more typically less than about 0.5 w/v % of the ophthalmic composition.";

with

- the upper limit mentioned on page 18, lines 32-34 (or similarly on page 19, lines 16-17) as part of a discussion of the examples:

"Thus, for the present invention, it is generally preferred to keep mannitol concentration below about 1.5%".

As to the amount of borate, the range 0.25-0.35 w/v% combines the narrowest lower and upper limits recited in the paragraph bridging pages 7 and 8:

"Typically, for the present invention, the borate is at least about 0.05 w/v %, more typically at least about 0.1 w/v % and still more typically at least about 0.25 w/v % of the ophthalmic composition. Furthermore, the borate can advantageously be less than about 0.75 w/v %, more typically less than about 0.5 w/v % and still more typically less than about 0.4 w/v %, and even possibly less than about 0.35 w/v % of the ophthalmic composition."

However, in the Board's opinion, the application as filed does not disclose these ranges in combination. The above passages provide lists of lower and upper limits, from which a host of ranges may potentially be created, respectively, for the amounts of mannitol and borate. Yet the application as filed contains no pointer to the combination of ranges selected in claim 1, such that this combination does not emerge directly and unambiguously from the application as filed.

Accordingly, the Board said auxiliary request 1 does not comply with Article 123(2) EPC requirements. The European patent EP 2420223 is amended in such a way that it contains subject matter which extends beyond the content of the application as filed

Hence the patent was revoked.

Decision here