Analysis on the distribution of domestic patents of sunitinib applied for listing and accepted by Kelun pharmaceutical

According to the monitoring results of pharmaceutical intelligence database, on August 1, 2019, the listing application of sunitinib malate API and capsule applied by Hunan Kelun Pharmaceutical Co., Ltd was accepted by CDE Sunitinib malate is a protein tyrosine kinase inhibitor anti-tumor drug developed and sold by Pfizer, which was approved by FDA as early as January 2006 At present, the indications approved by FDA include gastrointestinal stromal tumor (GIST), renal cell carcinoma (RCC) and pancreatic neuroendocrine tumor (PNET), and these three indications have been approved by China A number of domestic enterprises have set up imitations of sunitinib malate This paper analyzes the domestic patent distribution of sunitinib Background (1) according to the pharmaceutical intelligence database, at present, in addition to Hunan Kelun Pharmaceutical Co., Ltd., sunitinib listing application has been started (the acceptance number at the beginning of CYHS), including Qilu pharmaceutical, Zhengda Tianqing and hausen pharmaceutical, etc （2） Market situation 1 According to IMS database, global sales of sunitinib are shown in Figure 1 Figure 1 global sales of sunitinib over the years 2 According to the PDB database information in the domestic market, the change trend of the sum of sunitinib used in the domestic sample hospitals is shown in Figure 2 Figure 2 domestic patent layout of sunitinib in domestic sample hospitals (I) patent layout of sunitinib in the original research is shown in Table 1 Table 1 the original Chinese patent layout of sunitinib can be seen from table 1 that the patent layout of the original research party mainly involves compounds and crystal forms It should be noted that although the American patent of cn02815892 X is not included in the orange peel book, and the patent does not limit the Z / E configuration of the compound, in the examination opinion of cn201410730965.6 patent application, the patent is used as the reference document (sunitinib malate I) to determine the creativity of the preparation method of sunitinib malate L （2） Analysis of patent layout of non original research party 1 Material patent (1) derivative patent Table 2 Chinese patent of non original research Party's sunitinib derivative (2) crystal form patent Table 3 Chinese patent layout of non original research Party's sunitinib crystal form (3) intermediate patent Table 4 Chinese patent of sunitinib intermediate 2 Product patent Table 5 distribution of Chinese patents for non original research fangsunitinib products 3 Method patents (1) patent for preparation method of API 6 Patent for preparation method of API 2 Patent for preparation method of pharmaceutical products 7 Patent for preparation method of pharmaceutical products of sunitinib 3 Patent for quality research method Table 8 Chinese patent layout of sunitinib quality research method (4) new drug use patent Table 9 conclusion of Chinese patent layout of sunitinib pharmaceutical use as an IPR working in generic drug R & D and production enterprises, the author is often confused by questions such as "what patent protection does our products have" It is true that how to innovate in the background of imitation, especially in the context of meeting the requirements of consistency evaluation, may be one of the common problems faced by many peers It can be seen from the analysis of this paper that the patent layout of sunitinib in China focuses on derivatives, crystal forms, intermediates, preparation products, composition products, preparation methods, quality research methods and pharmaceutical applications Among them, those closely related to the products to be listed may be crystal type patent, preparation product, preparation method patent and quality research method patent The patent for the preparation method of API (including crystal form and intermediate) may be one of the main ways for many generic pharmaceutical manufacturers to seek substantive patent protection However, the authorization of the patent for the preparation method of API of sunitinib is not ideal, and many patent applications have creative defects that are difficult to overcome In the practical operation, in addition to doing a good job in pre application search and patentability of the method, the author thinks that another way can be found to start with impurities For example, the new method may not be creative for the preparation of the target compound, but it may generate new impurities The protection of the method is indirectly realized through the protection of impurities The quality research method patent is also a kind of patent closely related to the product For example, Zhongshan wanhan Pharmaceutical Co., Ltd where the author works has realized the protection of its main product orlistat capsule through the patent "a method for determining the degradation of impurities in orlistat capsule" (Patent No.: zl201610077367.2), not only through the identification of high-tech products and enterprises by virtue of the patent, Based on the method disclosed in the patent, the quality and popularity of the product are improved, and the gratifying commercial income is obtained In contrast, the author only detected one patent of sunitinib quality research method Although it is authorized, it is invalid because of not paying the annual fee.