API and IP Newsletter
Contents
FDA approvals in April 2021.
General information.
Chinese patent reforms to bolster pharma innovation.
Private investment in the healthcare industry: The road ahead.
Intellectual Property.
APIXABAN formulation patent decision by EPO..
FDA approvals in April 2021
Every month we follow approvals by USFDA and comment about processes followed to manufactured small molecule APIs.
In one of the earlier weeks, we covered process chemistry details of Infigratinib. This week, let us understand chemistry of Sotorasib.
WO2018217651A1, relates to the compound, where example 41 and claim 4 relate to Sotorasib.
Example 41
6-Fluoro-7-(2-fluoro-6-hydroxyphenyl)-l-(4-methyl-2-(2-propanyl)-3-pyridinyl)-4-((2.S)- 2-methyl-4-(2-propenoyl)-l-piperazinyl)pyrido[2,3-i/]pyrimidin-2(lH)-one
GVK is importing 2,6-dichloro-5-fluoronicotinic acid and there is a high likelihood that GVK must be developing Sotorasib. It is a seven step synthesis from 2,6-dichloro-5-fluoronicotinic acid.
General information
Chinese patent reforms to bolster pharma innovation
GlobalData explained that this is the latest in a series of regulatory landscape changes in the Chinese market, including the introduction of renewed and expanded Marketing Authorization Holder (MAH) System in December 2019; the new and revised Drug Regulation Registration (DRR) in March 2020; and the introduction of break-through therapy designation in July 2020.
Private investment in the healthcare industry: The road ahead
It is one of the largest sectors of the Indian economy in terms of revenue and employment, both. Forecasts by the think tank suggest that the industry may reach $372 billion by 2022 while generating over 500,000 new jobs per year. (Read more)
Intellectual Property
APIXABAN formulation patent decision by EPO
EP 2538925 was granted based on 12 claims. Eleven oppositions were filed against the grant of the patent. This patent was revoked at the first instance.
Patentee BMS appealed. This post is about Article 123 (2) of EPC and this is the appeal board decision at EPO. In my understanding, Article 123 (2) is the most ruthless article in the entire EPC. According to Article 123 (2) of EPC, European patent application or the European patent may not be amended in such a way that it contains subject-matter which extends beyond the content of the application as filed.
The Appeal Board revoked the patent for not complying to Article 123 (2).
Without going into details, the amended claim 1 of the main request was as follows:
"A tablet comprising a pharmaceutical composition, wherein the pharmaceutical composition comprises up to 5 mg apixaban and a pharmaceutically acceptable diluent or carrier, wherein the apixaban is in particulate and crystalline form and the individual apixaban particles, whether the particles exist singly or are agglomerated, have a D90 less than 89 micron as measured by laser light scattering, wherein the composition consists of the following components:-------
To counter Article 123 (2) arguments, the patentee referred Paragraph 006 in the patent. It is as follows:
[0006] The present invention relates to a tablet or capsule comprising a pharmaceutical composition, wherein the pharmaceutical composition comprises apixaban and a pharmaceutically acceptable diluent or carrier, wherein the apixaban is in particulate and crystalline form and the individual apixaban particles, whether the particles exist singly or are agglomerated, have a D90 equal to or less than 89 μm as measured by laser light scattering.
And to support Paragraph 006, patentee also referred to Table 3 in the patent as filed, to defend Article 123 (2). Table 3 is as below:
The appeal board said, according to Article 123, the tablet compositions comprising up to 5 mg apixaban mentioned in paragraph [0006] were not exemplified in Table 3 of the application as filed, which only referred to a tablet containing 20 mg apixaban. The middle column related according to its heading explicitly to a "5% w/w Drug Loaded Granulation", not to a tablet. The tablet compositions of paragraph [0006] could therefore not be further characterized by features from Table 3.
The appeal was dismissed. Decision is here.
Disclaimer
Sidvim LifeSciences Private Ltd has taken due care and caution in developing this document. Since the data used for analysis in this document is based on the information available in the public domain, its adequacy or accuracy or completeness cannot be guaranteed. This document is for information only and Sidvim is not responsible for losses that may or may not arise due to any decisions made based on the same. No part of the document shall constitute or be represented as a legal opinion of any kind or nature. No warranties or guarantees, expressed or implied, are included in or intended by the document, except that it has been prepared in accordance with the current generally accepted practices and standards consistent with the level of care and skill exercised under similar circumstances by professional consultants or firms that perform the same or similar services.
