Compound patents of class 1 NDA chemicals in China and their progress abroad
-
Last Update: 2017-10-11
-
Source: Internet
-
Author: User
Search more information of high quality chemicals, good prices and reliable suppliers, visit
www.echemi.com
The patent layout and globalization strategy in new drug research and development is an indispensable decision for pharmaceutical companies At the same time, with the joining of CFDA in ICH, the reform of various pharmaceutical policies and the upsurge of pharmaceutical entrepreneurship in various regions, the pace of domestic new drug research and development may gradually be in line with the international standards In this paper, the compound patents and foreign development progress of class 1 NDA chemicals (including marketed and under review chemicals) from 2007 to now in China are sorted out, which is helpful to understand the research and development status of domestic representative drugs in the past decade The drugs listed in Table 1 of class 1 marketed drugs in China are all sold in the pharmaceutical market, and there is no NDA chemicals without progress, rejection or delisting, such as kazufloxacin, Semillon, dicyclopentadine, flumatenib, etc Table 1 Compound patents of class 1 marketed drugs in China and foreign progress note 1: the original research patent wo1990009176 of pirfenidone has not entered China, and domestic enterprises directly develop and market it without authorization introduction agreement, which belongs to a special situation Note 2: the CN number in the above table is the application number The author has not found out the CN patent of the above table's elamud and heimpofen which are not listed in the above table It can be seen from the list of patent and obligee of class 1 marketed pharmaceutical compound in China that the exetane of Beida Pharmaceutical Co., Ltd and sidabamide of microchip biology are both independently researched, developed, manufactured and sold, as well as anti-tumor drugs Among them, sidabamide has entered the second phase of clinical practice in the United States, but it is not the micro organism itself that has been put into research and development Instead, Huya Bioscience is responsible for overseas development As early as more than ten years ago, the micro organism transferred the international patent of sidabamide exclusively to the U.S Shanghai sub organism As for the development rights of sidaban in other Asian countries such as Japan and South Korea, Shanghai Asia bio transferred to Eisai Four non-tumor drugs (arixib, Antofloxacin, alisartan ester, moroxynidazole) independently developed by domestic institutions / pharmaceutical enterprises have not entered the foreign clinical and patient market As a separate paragraph, the reason is that there is a transfer of rights in the compound patent or production and sales and only between domestic institutions / pharmaceutical enterprises In 2012, xinlitai and Shanghai Ellis signed a strategic cooperation agreement to purchase the preparation production technology of alisartan ester, a Shanghai Ellis class 1 hypotensive patent product, for about 340 million yuan, and obtained the exclusive sales right of the product The patent right of apatinib is quite special Recently, the Patent Reexamination Board of the State Intellectual Property Office decided that the patent right of zl201510398190.1 (methanesulphonate a crystal form of nicotinamide derivatives and its preparation method and application) of xuanchuang biology was all invalid, which also made many people in the circle shocked However, the original compound patent of apatinib should belong to cn02138671 applied by Nanjing Kaiheng (now Hangzhou Rongli medicine) in 2002 Later, advanchen lab's PCT application wo2005000232 didn't enter China, while Hengrui only applied for apatinib mesylate salt patent cn200810149651 a few years later, and the patent cited cn02138671 Whether the dispute over apatinib's compound patent right will be studied, let's see if it changes In Table 1 above, not all class 1 new drugs are independently developed by domestic pharmaceutical enterprises and scientific research institutions Among them, iprazole, alamod and nanofloxacin are all imported by foreign enterprises with authorization, and iprazole and nanofloxacin are listed and sold in South Korea and Japan respectively, and there is no drug enterprise research and development in foreign countries to enter clinical practice This kind of model introduced from foreign authorization also has a more skilled model in domestic pharmaceutical enterprises, such as zaiding Pharmaceutical (just listed on NASDAQ), but its products have not yet been listed Table 2 Compound patents in class 1 production review in China and foreign progress note 1: p-toluenesulfonamide of HongRi pharmaceutical and noraconitine hydrochloride of Rundu pharmaceutical are in withdrawal status, and the four chemicals not listed in Table 2 above are in NDA review in CDE, and there is no withdrawal of clinical self-examination The crystal type patent of VEGF receptor antagonist of Hutchison Whampoa is cn200910199259, which was jointly developed with Lilly after 2013 There is no foreign development progress at present The piratinib (VEGF / EGFR / erbB2 receptor antagonist) of Hengrui medicine just entered the NDA review in August 2017, and it had a clinical phase I in the United States two years ago, and it is unknown whether to continue clinical trials in the United States Zhengda Tianqing's androtinib (VEGF / FGF / PDGF receptor antagonists) was jointly developed with adecheng (the priority application of the compound patent was submitted to USPTO in the United States in early 2007) Currently, androtinib is also in the third phase of clinical practice in the United States It can be seen from the structural formula (Unofficial source) of the compound in Figure 1 that the skeleton similarity of androtinib and pyrrolotinib is still very high Three of the four chemicals are Tinian antitumor drugs, while danorevir (HCV NS3 inhibition) belongs to the field of anti hepatitis C, from intermune and array Biopharma is authorized to introduce, and the lack of research and development progress abroad may be impacted by Gilead's hepatitis C treatment, but at present, sofosbuvir of Gilead is also about to be imported into China, bringing a lot of competition for danorevir of Geli pharmaceutical industry Figure 1 In summary of the four structural formulas of class 1 chemical drugs in the production review, patent sources of class 1 new drugs in China mainly include independent research and development, introduction from domestic scientific research institutions, and authorized introduction from foreign pharmaceutical companies / institutions However, most of the class 1 Chemicals researched and developed in China have not carried out clinical practice or sought to be listed in foreign countries, either because of product quality and competitive pressure, or because of their own strategic positioning, the difficulties brought by going to sea make them backward The content and time of patent layout (core patent + peripheral patent) of class 1 chemical drugs (preclinical, clinical or listed) independently developed by domestic enterprises / institutions must be considered in many aspects A feasible way to make progress in foreign countries is to transfer the rights and interests to foreign pharmaceutical enterprises, such as the agreement between microchip biology and Shanghai Asian biology, the development of anti hepatitis B chemical drugs by Zhengda Tianqing and Johnson & Johnson Agreement (Note: at present, the transfer of international rights and interests of domestic biological drugs is hot, such as Baiji Shenzhou and Xinda biological, etc.) Of course, it is still hoped that domestic powerful enterprises can synchronize their high-quality class 1 Chemicals developed in China with overseas development and sales through joint ventures / wholly-owned subsidiaries or direct exports, so as to benefit foreign patients as well If there are any inappropriate points mentioned above, please criticize and correct them Thank you!
This article is an English version of an article which is originally in the Chinese language on echemi.com and is provided for information purposes only.
This website makes no representation or warranty of any kind, either expressed or implied, as to the accuracy, completeness ownership or reliability of
the article or any translations thereof. If you have any concerns or complaints relating to the article, please send an email, providing a detailed
description of the concern or complaint, to
service@echemi.com. A staff member will contact you within 5 working days. Once verified, infringing content
will be removed immediately.