API and IP Newsletter
Contents
FDA approvals in December: Part II
The synthesis of 2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)-JV- benzylacetamide (KX2-391/ Tirbanibulin ) dihydro chloride is shown below and reported in WO2010135429A2.
General information.
Tenability of Passing Off Action against ‘Covishield’ Vaccine of Serum Institute of India.
Sci-Hub Case: The Court Should Protect Science From Greedy Academic Publishers.
Intellectual Property.
Naproxen and Esomeprazole Mg DR CAFC decision.
FDA approvals in December: Part II
The objective of this write-up is to deep dive in synthetically manufactured API. Last week, we covered two APIs, this week in API Newsletter we would cover other two APIs
1.) Tirbanibulin
2.) Berotralstat
Tirbanibulin:
The compound KX2-391 (Tirbanibulin) is a biaryl compound for modulating a kinase cascade and is disclosed in U.S. Pat. No. 7,300,931
The synthesis of 2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)-JV- benzylacetamide (KX2-391/ Tirbanibulin ) dihydro chloride is shown below and reported in WO2010135429A2.
GVK, Teva, TCG Lifesciences, GLR innovation are importing KSM 4-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)phenol from the UK, US and China. Very soon, one could expect DMFs filed by these companies.
Berotralstat:
Basic composition of matter patent could be WO2015134998A1. Preparation of 1 -(3-(aminomethyl)phenyl)-N-(5-((3-cyanophenyl)(cyclopropyl- methylamino)methyl)-2-fliiorophenyl)-3-(triiluoromethyl)- l H-pyrazole-5-carboxaniide (54e). Berotralstat reported as compound 54e.
Crystalline form reported in WO 2020/092898.
Avra and Sai are importing 3-Cyanobenzaldehyde which is RM of Berotralstat. Interestingly, lot of 3-Cyanobenzaldehyde is being imported by Sigma Aldrich and it is clear that many Gx API developers are buying development quantities from Sigma Aldrich.
General information:
Tenability of Passing Off Action against ‘Covishield’ Vaccine of Serum Institute of India
The trademark applications, which were filed by the Cutis Biotech and the Serum Institute of India, are pending before the Registry. ( News here)
Sci-Hub Case: The Court Should Protect Science From Greedy Academic Publishers
A copyright infringement suit filed by three publishing giants against Sci-Hub and Libgen before the Delhi High Court on December 21, 2020. News here.
Intellectual Property
Naproxen and Esomeprazole Mg DR CAFC decision
Naproxen and Esomeprazole Magnesium Delayed-Release Tablets (RLD: Vimovo®) had an annual sale of approximately USD 400 million in the U.S. (IQVIA MAT January 2020).
Lupin Launches Authorized Generic version of Vimovo in. March 2020. (Here)
Horizon and Nuvo sued Dr. Reddy’s Laboratories Inc., Dr. Reddy’s Laboratories, Ltd., and several others for patent infringement in multiple lawsuits
OB listed patents are as below.
This case was related to US `698 and US `208 patents listed in OB and expiration in 2031 and 2029 respectively. The suit was about word “target” in claim and whether it has an indefinite meaning.
Claim 1 reads:
A method for treating osteoarthritis, rheumatoid arthritis, or ankylosing spondylitis comprising orally administering to a patient in need thereof an AM unit dose form and, 10 hours (±20%) later, a PM unit dose form, wherein: the AM and PM unit dose forms each comprises: naproxen, or a pharmaceutically acceptable salt thereof, in an amount to provide 500 mg of naproxen, and esomeprazole or a pharmaceutically acceptable salt thereof in an amount to provide 20 mg of esomeprazole; said esomeprazole, or pharmaceutically acceptable salt thereof, is released from said AM and PM unit dose forms at a pH of 0 or greater, the AM and PM unit dose forms target: i) a pharmacokinetic (pk) profile for naproxen where: --------
Appellate Court (CAFC) confirmed the claim term “target” to mean “set as a goal,” and affirmed the district court’s grant of summary judgment holding the claims of the ’698 patent and the ’208 patent invalid for indefiniteness. Case details 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.
