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Azivudin, who is in the hands of Roche, talks about the need to circumvent patents in drug development

  • Last Update: 2021-08-28
  • Source: Internet
  • Author: User
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Author: andrewmed

Freedom to Operate (FTO) means that enterprises can freely use and develop technology without infringing on the patent rights of others, and put the products or services produced by the technology into the market

Innovative drugs are often a race against time.

However, when the candidate compound is sufficiently active and meets the requirements of patentability, FTO (free implementation) is sometimes not necessary

Patent for Azivudine Compounds of Real Biology

Patent for Azivudine Compounds of Real Biology

The compound patent application of Azivudine was filed on August 7, 2007.

The compound 15 in claim 2 is azvudine

Roche's patent layout

Roche's patent layout

In fact, as early as 2002, the multinational pharmaceutical giant Roche has applied for a patent for a compound containing Azivudine for the treatment of hepatitis C (HCV).

When R1 is an azido group, R2 is a hydroxyl group, R3 is hydrogen, R4 is F, and R11 is hydrogen, Ia is azvudine

In addition, Roche also gave an example compound 24, which is different from azvudine with only one F atom.

On November 13, 2007 (at this time, the patent of azvudine compound at Zhengzhou University has not yet been published, and the publication time is May 14, 2008), Roche researchers published the following article in the Journal of Biological Chemistry,

This article published the structure and activity data of Azivudine (RO-0622), which is quite amazing.

RO-0622 activity data

Previously, Roche also published the chemical structure, preparation method and HCV inhibitory activity data of azivudine analog R1479 on Bioorganic & Medicinal Chemistry Letters on February 4, 2007.

Although Azivudine falls into the scope of Roche's patent protection, it does not affect its own patent authorization

Free implementation of patents (FTO)

Free implementation of patents (FTO)

Under normal circumstances, the free implementation of patentable drugs (FTO) is very important, and nucleoside antiviral drugs are taken as an example

Nowadays, the king of antiviral drugs-Pharmasset (Pharmasset) was also interested in nucleosides when developing anti-HCV drugs, but the patents of Roche compounds were first, allowing Gilead to consider free implementation of drugs (FTO) Under the premise of choosing another way, in 2008, he applied for a patent for anti-hepatitis B virus drugs (CN101932590)

Gilead chose an alkyl group substituted with a fluorine atom at the 2'position substituent

If the story continues in this way, it is inevitable that there will be a patent war or patent cross-licensing between Roche and the real creatures of the Azfudine patentee

Azivudine's new mechanism of action

Azivudine's new mechanism of action

Whether it is Me-too or FIC, with the continuous advancement of scientific research and the continuous discovery and elucidation of new diseases and mechanisms, the boundaries will become increasingly blurred

In October 2020, Professor Chang Junbiao and others published a research article on the mechanism of Azvudine inhibiting COVID-19, which, like Remdesivir, inhibits COVID-19 virus RNA replication

In April 2021, Azvudine launched a phase III clinical trial for the treatment of COVID-19 in Brazil and other countries.
It can be seen that it has good effects on anti-HIV-1 and COVID-19.
Azivudine is highly expected

On July 21, 2021, the National Medical Products Administration (NMPA) announced that it has conditionally approved Class 1 new drugs, the first new nucleoside reverse transcriptase and auxiliary protein Vif dual target inhibitor-Azivudine tablets ( Azvudine) was launched in combination with nucleoside reverse transcriptase inhibitors and non-nucleoside reverse transcriptase inhibitors to treat adult HIV-1 infected patients with high viral loads.
The real organism is the marketing license holder of Azvudine tablets.


The patent problem of Azivudine has been settled, but the patent story of innovative drugs has never stopped unfolding
For drug development, especially the development of popular target drugs, the corresponding research around patents is a topic that can never be avoided, just as the emerging technologies PROTAC, monoclonal antibodies, double antibodies, RNA, ADC, PDC, etc.
, are outside the traditional medicine.
A new battlefield has been opened up and the scope of patentable drugs has been continuously expanded

Candidates can be freely implemented (FTO) is extremely important, and it is of course the best situation to be able to implement freely
However, due to fierce competition, it is more difficult to completely avoid prior patents or free implementation (FTO).
When high-active compounds are patented, they should abandon FTO and obtain patent rights first, carry out subsequent development, and determine the final pre-clinical After the data results, it can also be used as an option for drug development in deciding whether to proceed with subsequent clinical development
However, unless luck is as good as a real creature, it is necessary to cooperate with the prior patent owner or initiate an invalidation lawsuit

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