API and IP Newsletter
Contents
Novo Nordisk, Eli Lilly Face 55 Lawsuits Over Life Threatening Weight Loss Drug Side Effects
Indian pharma industry relies heavily on ingredients made in China: Report
New molecule approval by FDA-Capivasertib
We follow FDA approvals in small molecules. We do cover chemistry, IP, we analyse import export data to guess who are the companies who would be working on this product, who could file DMF soon etc.
In this write-up generally we do not cover too much about mechanism of action of the drug.
In December 2023, FDA approved Capivasertib.
Capivasertib sold under the brand name Truqap, is an anti-cancer medication used for the treatment of breast cancer.
Truqap is the first AKT inhibitor. But the biomarker restriction along the PI3K-AKT pathway disappointed the analyst a bit and they lowered its peak sales estimate for to $1.28 billion, from their previous projection of $2.36 billion.( Here)
Capivasertib ‘AZD5363’ is alternatively known as: (S)-4-amino-N-(1-(4-chlorophenyl)-3-hydroxypropyl)-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamide, and its chemical structure is shown below:
WO2009/047563 discloses Capivasertib as Example 9 and introduces several processes for its preparation on pages 39-42.
The published methods for preparing Capivasertib were satisfactory for the preparation of relatively small quantities.
WO2015181532: Relates to intermediates and improved yields of Capivasertib
Metrochem and few other companies are importing 4-Chloropyrrolo[2,3-d]-pyrimidine, which is RM for Capivasertib and which is about USD 400-500 per KG. So one can expect this would be very costly API.
These companies perhaps working in developing Capivasertib.
TRUQAP film-coated tablets are supplied for oral administration with 160 mg or 200 mg capivasertib.
The tablets contain croscarmellose sodium, dibasic calcium phosphate, magnesium stearate, and microcrystalline cellulose.
The film coat contains the following inactive ingredients:
Copovidone, hypromellose, iron oxide black, iron oxide red, iron oxide yellow, medium chain triglycerides, polydextrose, polyethylene glycol 3350, and titanium dioxide.
General information
Novo Nordisk, Eli Lilly Face 55 Lawsuits Over Life Threatening Weight Loss Drug Side Effects
A U.S. judicial panel has consolidated lawsuits against pharma giants Novo Nordisk and Eli Lilly over alleged gastrointestinal side effects from weight loss drugs.
News here.
Indian pharma industry relies heavily on ingredients made in China: Report
The Biden administration embraced a plan from India’s government last year to edge China out of its position as a leader in making ingredients for generic pharmaceuticals sold in the US. But a new report shows that much of those ingredients are likely still coming from China anyway.
News here
Intellectual Property
L `OREAL Vs Noxell Corporation
The appellant (patent proprietor, Noxell Corporation) lodged an appeal against the decision of the opposition division revoking European patent EP-2926802 for lack of inventive step
Patent was initially challenged by L `OREAL.
Claim 1 of the patent as granted reads as follows:
A hair colouring composition comprising, in a cosmetically acceptable carrier:
- one or more oxidizing agent(s);
- one or more alkalizing agent(s);
- one or more oxidative dye precursor(s) selected from the group consisting of 2-methoxymethyl-p-phenylenediamine, cosmetically acceptable salts thereof and mixtures thereof;
- one or more oil(s),
wherein the composition comprises a total amount of oil(s) of more than 20%, preferably at least 30%, more preferably at least 50 % by total weight of the composition."
The opposition was based on lack of inventive step and insufficiency disclosure based inter alia on documents
D1: WO-A-2012/095398 and
D3: CA-A-2 576 189.
According to the opposition division, D3 represented the closest state of the art to the invention. It related to a hair dyeing compositions comprising 1,4-diamino-2-methoxymethylbenzene (MBB).
The objective technical problem was the provision of a colouring composition comprising MBB that achieved improved colouring intensity.
D1 aimed to improve the intensity and/or evenness of hair coloration. It suggested dyeing compositions comprising at least 20wt.% of oils. The skilled person starting from D3 and faced with the problem of improving colour intensity would have considered a higher oil content in the hair dye composition according to the teaching of D1. The subject-matter of claim 1 of the patent as granted was therefore obvious over D3 in combination with D1.
According to Patentee, D3 was the closest prior art to the invention. However, the technical problem to be solved was to provide a low to moderate skin-sensitizing hair colouring composition that achieved an increased colour intensity without compromising the evenness of the hair colour.
In support of their arguments the appellant patentee filed, an experimental report aiming at showing the effect of the addition of oil on the evenness of the colour, starting from mineral oil-free compositions exhibiting the same colour intensity.
D1 neither disclosed nor suggested that the hair colouring compositions provided specific performances in term of colour intensity and evenness of the hair colour. The claimed subject-matter involved therefore an inventive step over the combination of D3 with D1.
The parties agreed that D3 represents the closest prior art to the invention. The Board also agreed.
This document relates to compositions for dyeing keratin fibres. It discloses an aqueous or aqueous-alcoholic oxidation dye composition comprising 1,4-diamino-2-methoxymethylbenzene (MBB), as the oxidation base. It revealed that this 1,4-diaminobenzene has improved physiological compatibility, especially it is non-sensitizing. The oxidation dye precursor composition is mixed with an oxidizing agent prior to application to form a ready-to-apply hair dye composition. The colouring composition preferably comprises at least a source of alkalising agent
Technical problem: The appellant patentee defined the technical problem to be solved as providing a low to moderate skin-sensitizing hair colouring composition that achieves an increased colour intensity without compromising the evenness of the final hair colour.
Solution: The proposed solution is the hair colouring composition of claim 1 of the patent as granted characterized by the presence in the composition of at least of 20 % by weight of oil(s).
Success: In the present case, it is not necessary to assess whether the test reports filed by the appellant patentee demonstrate convincingly that the claimed compositions solve the above mentioned technical problem.
Obviousness: It remains to be decided whether the proposed solution of adding at least 20% by weight of fatty substances into the dye composition of D3 in order to improve the colour intensity without compromising the evenness of the final hair colour is obvious in the light of the prior art.
D1 relates to a process for the oxidation dyeing of keratin fibres. This document aims to improve the colour obtained by an oxidative dyeing process, in particular to improve the power/intensity and/or uniformity of the hair colour. This is achieved by mixing extemporaneously at the time of use the oxidation dye composition and the oxidizing composition in such a way that the ready-to-use dyeing composition obtained comprises at least 25% by weight of fatty substance.
D1 discloses that the fatty substance may be an oil. The oil is a fatty substance that is liquid at room temperature and is insoluble in water at ordinary temperature (25°C) and at atmospheric pressure (760 mmHg). The oils may be liquid fatty alcohols, liquid fatty esters or linear of branched hydrocarbons such as liquid paraffins, petroleum jelly or polydecenes or mixtures thereof.
In the example, composition A comprises 60% by weight of liquid petroleum jelly and composition B 20% by weight. After mixing composition A with composition B at a ratio 1:1, the ready-to-use colouring composition comprises 40% by weight of petroleum jelly.
Thus, D1 gives the skilled person a concrete hint as to how to solve the technical problem of providing a dyeing composition having improved colour, in particular improved intensity and homogeneity, namely by adding into the hair colouring compositions known from the closest prior art D3 fatty substances in concentrations within the claimed range, for instance liquid petroleum jelly, thereby arriving at the composition of claim 1 having a total amount of oil of more than 20% by total weight of the composition.
A skilled person would therefore arrive at the compositions of claim 1, since it is obvious to follow the hint given in D1 for the colour improvement, with a reasonable expectation of success, especially as the compositions of D3 are already low to moderate skin-sensitizing.
Hence the Appeal Board opined, the proposed solution of adding at least 20% by weight of fatty substances into the dye composition of D3 in order to improve intensity and homogeneity of the coloration is therefore obvious in the light of D1.
The patent was revoked.
Decision here
