API and IP Newsletter
Contents
New Drug Approvals in June 2021.
General information.
Should You Apply for Glenmark Life Sciences IPO?.
New technology can pave the way for development of long-acting drugs.
Intellectual Property.
DAPAGLIFLOZIN Appeal order by Delhi HC.
New Drug Approvals in June 2021
In SIDVIM, we analyse FDA approvals every month and try to understand chemistry of the approved small molecules.
Ibrexafungerp
Today, let us discuss the chemistry of Ibrexafungerp. It is disclosed in WO2010019203A1 in example 173.
1S,4aR,6aS,7R,8R,10aR,10bR,12aR,14R,15R)-15-[[(2R)-2-amino-2,3,3-trimethylbutyl]oxy]-8-[(1R)-1,2-dimethylpropyl]-14-[5-(4-pyridinyl)-1H-1,2,4-triazol-1-yl]-1,6,6a,7,8,9,10,10a,10b,11,12,12a-dodecahydro-1,6a,8,10a-tetramethyl-4H-1,4a-propano-2H-phenanthro[1,2-c]pyran-7-carboxylic acid
A suspension of Intermediate 33 (2.83 g, 0.046 mol) and N-[(1E)-(dimethylamino) methylidene] pyridine-4-carboxamide (0.93 g, 0.052 mol) in acetic acid (44.4 mL) was blanketed with nitrogen and heated in a 90°C oil bath for 1 hour. The mixture was cooled to room temperature, evaporated and purified by reverse phase HPLC using a 19 x 150 mm Sunfire Preparative C18 OBD column eluting with acetonitrile/water + 0.1% TFA. The product fractions were combined, concentrated under vacuum and freeze-dried to give the title compound (2.21 g) as a white solid (trifluoroacetic acid salt).
Citrate salt is not specifically covered but generically disclosed.
As per I/E database, Lupin is importing very small quantity of dimethylamino) methylidene] pyridine derivative and might be at advance stage of API development.
General information
Should You Apply for Glenmark Life Sciences IPO?
We need to look at the parent first before turning to Glenmark Life Sciences. The complex API business, which forms a substantial chunk of GLS, enjoys high margins and decent market share. Although the company's top-line and bottom-line growth rates have declined substantially in FY2021, the current pandemic environment supports revenue and net profit growth to remain double-digit for the foreseeable future. As a sector, we are bullish on the Indian pharmaceutical industry. (Read more)
New technology can pave the way for development of long-acting drugs
The research group has developed a unique biomedical technology that can be used to create coagulation factors with a significantly longer duration of action than what is the case today. The starting point is in-depth studies of a biological mechanism. This insight has enabled us to design super albumin, which is a designed protein variant that can be coupled to protein-based drugs and allow them to remain in the bloodstream for a considerably longer time. (Read more)
Intellectual Property
DAPAGLIFLOZIN Appeal order by Delhi HC
The crux of the Case was based on Obvious Type Double patenting doctrine in USA. To seek a grant of patent invention must be “patentably distinct”. This doctrine prevents small variations of earlier patents prevents grant of not “patentably distinct” applications. If both patents are owned by the same entity/owners, the Obvious Type Double patenting objections can be overcome by filing “Terminal Disclaimer”, which disclaims the portion of the 20-year term of the second patent that extends beyond the earlier patent’s term.
In this case there are two patents issued to AstraZeneca.
First, IN 205147 [genus patent] and second IN 235625 [species patent] covers DAPAGLIFLOZIN".
Patentee pleaded, "DAPAGLIFLOZIN “(DAPA) falls within the scope of Indian Patent Numbers IN 205147. Patentee further pleaded DAPA is covered in IN 205147 (Markush claim) but disclosed in IN 235625.
The Generics challenged IN ‘625’s validity on grounds that it was anticipated by IN ‘147. One of the issues was “Obviousness-type double patenting” objection. In US, terminal disclaimer was filed for equivalent of IN `625 to counter anticipation arguments. In short, in US both equivalents of IN `147 and IN `625 would expire on same day. (In US, there is Patent Term extensions due to regulatory delay. There could be possibility of adaption of different patent prosecution strategies by the innovator in different countries such as India and in US. But this is not a point or the topic of this write-up)
In short, AstraZeneca pleaded DAPA is disclosed generally in IN `147 and specifically in IN `625.
1. During the hearing, Hon. Judge enquired, if DAPA was not disclosed in IN `147 and was in fact not known to the patentee (AstraZeneca) also, what would have happened, if someone other than AstraZeneca would have discovered DAPA, even if by using teachings of IN `147?
2. The counsel of AstraZeneca contended that AstraZeneca was an owner of IN `147 (genus patent), even prior to the discovery of DAPA. AstraZeneca could have sued “other” who discovered DAPA before AstraZeneca. However, such “other” could also sue anyone including AstraZeneca based on its DAPA patent and AstraZeneca also could not have manufactured DAPA without such others' permission.
3. It was further explained that if 'A' has a patent for a basic invention and 'B' later obtains a patent for an improvement to this invention, then 'B' is not free to use his invention without permission of 'A' and 'A' cannot use the improved version without permission of 'B'.
4. Based on this the Court came to conclusion, IN `147 claims a discovery/invention of a group of formulations, which was capable, with further research, of acting as a drug/medicine for inhibiting reabsorption of sugar in kidneys.
5. If AstraZeneca could not have manufactured DAPA, then the Court inferred, prima facie it appears, AstraZeneca could not have restrained any other person who discovered DAPA, even if the other person would have acquired knowledge from IN `147.
6. This inference created the doubt in the minds of Hon. Judge. Why AstraZeneca pleaded and claimed infringement of both (IN `147 and IN `625) patents?
7. The Hon. Judge expected AstraZeneca to confine their claim for infringement to IN `625 only, but AstraZeneca stuck to their stand of infringement of IN `147 too by the Generics.
8. Therefore, the Court concluded it is obvious that AstraZeneca have no legs to stand on, by claiming infringement of only IN `625, without also claiming infringement of IN `147.
9. So finally, the Court concluded, if DAPA was disclosed in IN `147, even if better disclosed in IN `625, it cannot enjoy two rounds of 20 years of protection, when the legislative policy is to grant protection for a period of one term of 20 years.
Decision here.
Disclaimer
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used for analysis in this document is based on the information available in the
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This document is for information only and Sidvim is not responsible for losses
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