Fluindapyr: A new fungicide molecule from Isagro, effective against Asian soybean rust (ASR)
Fluindapyr is a new, patent-protected proprietary active ingredient that has been shown to be highly effective in controlling Asian soybean rust (ASR) when used in certain premix formulations.
Isagro already submitted Fluindapyr for registration in India. Recently, 54th CIB meeting, Fluindapyr has been submitted to be in Schedule, Insecticide Act, 1968. As per details available, apart from India, Fluindapyr is not yet registered in any other territory.
Fluindapyr a novel fungicide discovered by ISAGRO S.P.A belongs to succinate dehydrogenase inhibitors (SDHI) class of compounds that have a mode of action which inhibits the energy production process in pathogenic fungi. Evaluations conducted have ascertained that Fluindapyr exhibits high efficacy against a broad range of plant diseases on various crops, especially on Asian soybean rust (ASR) when used in certain premix formulations. It is also effective on maize, cereals, OSR, rice. Fluindapyr is expected to offer new solutions that are capable of controlling such major diseases on important crops.
As per mammalian as well as Ecotoxicological data submitted by Isagro, Fluindapyr was found to be safe.
Mammalian toxicity:
- Acute Oral LD50 : >2000mg/kg b.w.
- Acute dermal (rat) : LD50>2000 mg/kg b.w.
- Acute inhalation (rat) : LC50 > 5.19 mg/L
- Skin irritation : Non irritant
- Skin sensitization : Sensitizer
- Mutagenicity : Non- Mutagenic
Eco-toxicity:
- Avian acute oral LD50 (Bob-white quail) : >2250mg/kg
- Acute toxicity LC50 (fish) : 121 ug/1
- Acute oral LD50 (bees) : >32.8ug/bee
- Acute contact LD50 (bee) : >300ug/bee
- Chronic toxicity LC50 (earth worms) : >1000 mg/kg
Fluindapyr is a new active ingredient that has been shown to be highly effective in controlling Asian soybean rust (ASR) when used in certain premix formulations.
IP Scenario:
SDHI fungicides were discovered more than 40 years ago. Due to the limited disease and application spectrum of the “first generation” carboxamides, resistance under commercial conditions remained limited to a few crop/pathogens. Inpyrfluxam was discovered by Sumitomo. Sumitomo filed a Patent US4742074 filed in 1985, where the Applicant claims the basic moiety, however does not claim difluoromethyl substituent as one of the possible alternatives (Inpyrfluxam has difluoromethyl substituent on the pyrazole ring).
Subsequently, Monsanto filed their Patent US5093347 in 1991, where they specifically claim the compound with difluoromethyl substituent on the pyrazole ring. Patent Specifically claims the compound under discussion (3-difluoromethyl-1-methyl-N-(1,1,3-trimethylindane-4-yl)pyrazole-4-carboxamide), however, Monsanto failed to identify specific isomer that is responsible for activity.
Later, in 2011, Sumitomo identified a predominantly R enantiomeric mixture (R form/S form ratio in the range of 90/10 to 10,000/1) at which Monsanto’s pyrazole carboxamide fungicide exhibited excellent fungicidal activity and filed a patent application (WO2011162397) globally. Sumitomo’s product was named Inpyrfluxam,
Isagro filed a patent application WO2012084812 in 2011, covering Fluindapyr, which was a fluoro derivative of Inpyrfluxam. Isagro’s Patent is granted in Australia, Brazil, Canada, China, Europe, Italy, Japan, Korea, Mexico, US, South Africa, Peru, New Zealand, US, South Africa; while patent applications are pending in other countries like Argentina, Colombia, Chile, Bolivia, Paraguay, Eurasia, Costa Rica, Ecuador, Egypt, Philippines, Guatemala, Honduras, India, Indonesia, Israel, Kenya, Malaysia, Morocco, Dominican Republic, Sri Lanka, Thailand, Tunisia, Ukraine, Vietnam.
Recently, Arysta reached an agreement with Isagro regarding the distribution of Fluindapyr based mixtures for use in soybeans and other row crops in Brazil. Isagro will submit the regulatory dossier for the first mixture based on Fluindapyr to Brazilian authorities in the first half of 2018.
Fluindapyr-based mixtures products soon to be registered in Brazil as Isagro already submitted an application for registration in Brazil. These new mixtures will target soybeans and other row crops.
One mixture – containing the proprietary molecule tetraconazole – will be directly commercialized by Isagro on a nonexclusive basis, while the other one – containing the active ingredient prothioconazole – will be distributed on an exclusive basis by Arysta LifeScience within the frame of the commercial agreement which was announced of the beginning of this year.
For More details: Subscribe AgroPat*(http://chemrobotics.com/#/)
- AgroPat provides techno-legal solutions to Agrochemical Discovery and Generic industry.
- AgroPat platforms covers more than 4500 Active Ingredients (Al’s) with all information including synthesis (ROS), formulation, combination, innovator, patents including product patent, developer, utmost important biology data containing spectrum, MoA, DFU, toxicity, which can play a major role in decision making for any individual /company/ university/ industry.
- Provide aboriginal information, which enables product developer to know about state of the art in relevant subject matter, which includes innovator Patent / Non-Patent literature, which is critical for the generic industry.
