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Isoxazoline Patent Landscape Results

In sections A to C below, we share selected preliminary results for our isoxazoline case study. Section A illustrates a general overview of isoxazoline patent publications (section A1). We further segment the isoxazoline patent landscape by time: results from the last 20 years since 1999 (section A2) and those before from 1955 until 1999 (section A3). Analysis of the isoxazoline patent landscape by timeframe allows one to evaluate how the field has evolved. Interestingly, we find that many of the key players are different between these two timeframes, and most of the isoxazoline patent publications are published in the last 20 years.

In section B, we segment the isoxazoline patent dataset by industry and focus on patent publications relevant to the animal health industry.


A1. Isoxazoline Patent Publications Overview

>3500 isoxazoline patent families were retrieved using PatentInspiration by AULIVE.

 
Isoxazoline Patent Publications Overview   •Among these patent families, ± 500  patent families are  directly relevant  to isoxazolines (the “ core” isoxazoline patent dataset, shown on figure 1),  where  isoxazoline(s)  is  the  or  one of the main topics  of the patent publications.  •A large proportion  (±70%)  of these core patent families was published within the last 20 years, indicating an increase in  innovation  activities on isoxazolines during this time period.  •Interestingly, the core isoxazoline patent publications began as early as in the  1950s  and  1960s , demonstrating active isoxazoline  innovation  activities for at least the last  60  years.  • Isoxazoline innovation  activities occur in  diverse scientific fields  beyond  veterinary sciences (red, fig 1) , as a substantial portion of isoxazoline patent publications is related to  agriculture-crop protection (green, fig 1)  or  human medicine (also red, fig 1).

Isoxazoline Patent Publications Overview

•Among these patent families, ±500 patent families are directly relevant to isoxazolines (the “core” isoxazoline patent dataset, shown on figure 1), where isoxazoline(s) is the or one of the main topics of the patent publications.

•A large proportion (±70%) of these core patent families was published within the last 20 years, indicating an increase in innovation activities on isoxazolines during this time period.

•Interestingly, the core isoxazoline patent publications began as early as in the 1950s and 1960s, demonstrating active isoxazoline innovation activities for at least the last 60 years.

Isoxazoline innovation activities occur in diverse scientific fields beyond veterinary sciences (red, fig 1), as a substantial portion of isoxazoline patent publications is related to agriculture-crop protection (green, fig 1) or human medicine (also red, fig 1).

 

A2. Key Isoxazoline Patent Players

The last 20 years  (1999 to present)  Though the current main commercial application of isoxazolines is focused on animal health, the  key isoxazoline patent players  are from  diverse  industries including  chemical  (eg  Nissan Chemical  and  Du Pont ),  agriculture  (eg S yngenta  and  Bayer Cropscience ) and  pharmaceutical  (eg  Novartis  and  Janssen ) companies, with the chemical companies having the largest isoxazoline patent portfolios. The Isoxazoline-relevant  veterinary sciences  companies (eg  Zoetis ,  Merial and Intervet ) are also on the key player list, but with smaller isoxazoline patent portfolios.

The last 20 years (1999 to present)

Though the current main commercial application of isoxazolines is focused on animal health, the key isoxazoline patent players are from diverse industries including chemical (eg Nissan Chemical and Du Pont), agriculture (eg Syngenta and Bayer Cropscience) and pharmaceutical (eg Novartis and Janssen) companies, with the chemical companies having the largest isoxazoline patent portfolios. The Isoxazoline-relevant veterinary sciences companies (eg Zoetis, Merial and Intervet) are also on the key player list, but with smaller isoxazoline patent portfolios.

Before 1999  (Year 1955 to 1998)   Key Isoxazoline Patent Players before 1999  are also from  diverse industries , but interestingly, they  differ  from those of the last 20 years. Here, the key players include  agrochemical  (eg  Sankyo  and  BASF ) and  pharmaceutical  (eg  Du Pont Merck Pharma  and  Pfizer ) companies. Even though these patent publications have expired validities, for technology landscape purposes, they are valuable resources with potentials for further isoxazoline innovation opportunities and insights.

Before 1999 (Year 1955 to 1998)

Key Isoxazoline Patent Players before 1999 are also from diverse industries, but interestingly, they differ from those of the last 20 years. Here, the key players include agrochemical (eg Sankyo and BASF) and pharmaceutical (eg Du Pont Merck Pharma and Pfizer) companies. Even though these patent publications have expired validities, for technology landscape purposes, they are valuable resources with potentials for further isoxazoline innovation opportunities and insights.


B1. Isoxazolines Patent Landscape in Animal Health

Who are the key players and their collaborators?

•What are the main applications and hosts?

Who are the key academic organizations? Who do they collaborate with?

•What are the main themes and trends (segmented by geography, year or patent topics)?

•What are the target parasites?

•What are the administration modes?

•Is a specific isoxazoline long or short acting?


B2. Selected results in Animal Health

A. Number of Patent Publications

> 220 patent families were retrieved, including those relevant to current isoxazoline commercial products.

B. Scientific Topics

The scientific competences of the animal health isoxazoline patent publications are rather diverse. These include new isoxazoline molecules, synthesis methods, applications, compositions and route of administrations. The patent in section D describes a new method of isoxazoline synthesis.

C. Key Animal Health Industrial Players

These include the four veterinary companies commercializing isoxazolines, their R&D partners and others. For example, Fluralaner (brand name Bravecto) is sold by Merck Animal Health in the US and by MSD Animal Health in Europe. This is a collaboration between MSD Animal Health and Nissan Chemical Corporation, who first invented fluralaner. We also retrieved isoxazoline animal health patents from Nissan Chemical Corporation.

D. Academic Players

There are academic laboratories working on diverse aspects of isoxazolines. Patent number WO2018191871A1 is an example for patents in the academic players category.

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Patent WO2018191871A1

Method For Use In Preparing Isoxazoline Derivative

2018 By Zhangjiagang Institute of Industrial Technologies

This patent is one of the most recent isoxazoline patent applications, and it describes a method to synthesize isoxazolines. Though most of the isoxazoline patent applicants are from commercial organizations, the applicant of this patent is from an academic research organization.

E. New Host and Applications of Isoxazolines

There are several host or application patent publications. Patent number WO2015091900A1 is an example patent with new host and application for isoxazolines.

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Patent WO2015091900A1

Use Of Isoxazoline Derivatives For The Treatment Or Prevention Of Arthropod Infestations In Poultry

2015 Intervet

This patent describes a new isoxazoline application beyond cats and dogs; here, the main host animal is poultry. This patent is about method of treating or preventing arthropod infestations of poultry animals by using a composition containing an isoxazoline compound, for example in medicated drinking water.


C. Summary

•Isoxazolines have long innovation history (>60 years) in diverse scientific fields, including in agriculture-crop protection, chemical, agrochemical, animal health and pharmaceutical industries.

•Isoxazolines have high innovation potentials for additional applications in and beyond the animal health industry. 

•A recent study by scientists at Calibr and TropiQ Health Sciences (Miglianico et al, PNAS, 2018, 115(29):E6920) demonstrated the potential of isoxazolines as insecticides to prevent outbreaks of malaria, zika virus and other insect borne diseases.

•By segmenting the isoxazoline patent dataset by industry and additional variables, we were able to extract insights that are distinct for each variable which further provide opportunities for cross-industry learnings and benchmarking analyses.

Important (September 2018): The U.S Food and Drug Administration (FDA) issued an alert to pet owners and veterinarians about the potential for neurologic adverse events in dogs and cats when treated with the isoxazoline class of drugs. FDA noted that some animals receiving Bravecto, Nexgard or Simparica have experienced adverse events such as muscle tremors, ataxia, and seizures. These products have been approved by FDA for treatment and management of flea and tick infestations. Another product in this class, Credelio, has recently been approved by FDA. These products continue to be safe and effective for the majority of animals. FDA is working with manufacturers of isoxazoline products to include new label information to highlight neurologic events, because these events were seen consistently across the isoxazoline class of products.


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