AstraZeneca loses another round-intermediate patents are also invalidated by Xinlitai.

AstraZeneca's ticagrelor is the first triazolo [4,5-D] pyrimidine anti-platelet aggregation drug. It was approved by the US FDA in July 2011 and obtained my country's Food and Drug Administration in November 2012. The import drug license issued by the bureau officially entered the Chinese market. Compared to its main competitor, clopidogrel, ticagrelor does not require hepatic metabolic activation and is characterized by more rapid and potent platelet inhibition. Since its launch, ticagrelor has been recommend as the first-line or preferred antiplatelet drug for ACS patients by many European and American guidelines, and its sales are also rising. In 2016, global sales have reached $0.839 billion, which is expected to enter the "blockbuster" club. Ticagrelor was included in the Medicare drug list in 2017, and there is huge room for growth in the future.

Shenzhen Xinlitai Pharmaceutical Co., Ltd. took the lead.

After taking the lead in completing the bioequivalence experiment, Xinlitai was the first to submit a listing application on March 9, 2017. In the list published by CDE on November 22, 2017, Xinlitai's ticagrelor tablets were included in the priority review procedure. It can be seen that Xinlitai has basically cleared the obstacles on the road to drug registration, waiting to become the first imitation manufacturer of ticagrelor.

However, whether Xinlitai's ticagrelor generic drug can be sold smoothly depends not only on whether it has obtained the drug marketing license, but also on other limiting factors, the most important of which includes whether there are "patent barriers". If you go on sale at the risk of patent infringement in order to take the lead in seizing the market, you may face large compensation or even a ban in the future.

In AstraZeneca's patent application in China, only four patents are authorized, namely, one compound structural formula, two crystal form patents and one intermediate patent. Now the compound structural formula and crystal form II patents are all declared invalid. The other patent granted is the intermediate patent CN1200940C, that is, the method for preparing intermediate pyrimidine compounds and the intermediate used in this method are protected in the claim of patent number 01810564.5, as well as the use of intermediates to prepare ticagrelor, has recently been declared invalid.

If Xinlitai's generic drug listing application can be approved by priority review in 2018, it will take about 3 years to wait until the relevant patents expire without the risk of infringement. By that time, the friends in the back line will all catch up and start from the same starting line. This is certainly what Xinlitai does not want to see, so it is only through patent challenges to remove obstacles early.

Therefore, Xinlitai first put forward the invalidation request for the compound patent on April 27, 2017, and then put forward the invalidation request for the crystal form II patent on June 22, 2017, and then on August 2, 2017, that is, the claim of patent number 01810564.5 protects the method for preparing the intermediate pyrimidine compound, the intermediate used in the method, and the method for preparing ticagrelor using the intermediate. All three cases are currently concluded with the declaration of invalidity of all the patents involved.

On October 10, 2017, the Patent Reexamination Board of the State Intellectual Property Office announced the decision on the invalidation of Patent No. 33591, declaring the invention patent No. 99815926.3 "New Triazolo (4,5-D) Pyrimidine Compound" invalid.

On November 22, 2017, the Patent Reexamination Board of the State Intellectual Property Office made decision No. 33975 invalidation, declaring AstraZeneca's Chinese patent No. 200610002509.5 invalid.

On January 30, 2018, the Patent Reexamination Board of the State Intellectual Property Office announced the invalidation decision No. 34725, declaring AstraZeneca's No. 01810564.5 invention patent right to be completely invalid. This is AstraZeneca's battle for the crystal patent of ticagrelor. The last moat intermediate patent was also invalidated by Xinlitai.