Fluopyram, a pyridyl-ethyl benzamide derivative, is a broad spectrum synthetic fungicide developed by the Bayer group (WO2004/016088). Fluopyram is effective against white mold, gray mold, powdery mildew, apple scab and other fungal diseases. It further exhibits nematicidal properties in various crops. It is a succinate dehydrogenase (SDH) inhibitor that blocks mitochondrial respiration. It acts by binding to the ubiquinone binding site of the enzyme thereby inhibiting succinate to fumarate oxidation of the citric acid cycle. The structure of Fluopyram is shown below:
Bayer IP GmbH, the IP managing and IP holding legal entity of the Bayer Group has got yet another patent on compositions comprising Fluopyram. Bayer Group’s previous patents (US9433214, WO2013110594) disclose compositions with Fluopyram, spore forming bacteria and/or biological control agents having fungicidal, nematicidal and insecticidal properties.
The new US patent 9591856 titled, “Fungicide compositions comprising Fluopyram, at least one succinate dehydrogenase (SDH) inhibitor and optionally at least one triazole fungicide” was granted on March 14, 2017. The patent specifically claims active compounds and compositions comprising Fluopyram, Bixafen, which is another SDH inhibitor and at least one of a triazole fungicide, such as Prothioconazole. Other than the active compound combinations, the composition further comprises auxiliaries, solvents, carriers, surfactants and/or extenders.
This patent document is claimed to be a selection invention specifically over the prior art WO2005/0077901. Selection inventions are specified in EPO guidelines for examination though US laws do not distinguish them from regular inventions. Selection inventions are those that claim individual elements, sub-sets or sub-ranges from existing prior arts and these elements, sub-sets and sub-ranges are not explicitly mentioned in those prior arts.
Among other criteria, the EPO mentions a “two-list principle” in its guidelines for deciding on the novelty of selection inventions. If the elements, sub-sets or sub-ranges are selected from a single list in the prior art, then they are not novel. But if selection is made from two different lists of a certain length to arrive at the combination, then the “two-list principle” is satisfied.
This patent originating from a German conglomerate is more in line with EPO’s guidelines clarifying the basis by which the “two-list principle” is satisfied as a selection invention. It is mentioned that Fluopyram and Bixafen are chosen from a first list of binary combinations in the existing prior art and the triazole fungicide, Prothioconazole is chosen from a second general list of fungicides. Also, Fluopyram and the second SDH inhibitor are chosen from a first list of combinations and the treatment of cereals is chosen from a second list of treatment of crops. The ternary combination of Fluopyram, Bixafen and Prothioconazole are chosen from a first list of active compound combinations and the use “for preventively and/or curatively controlling pathogenic fungi, comprising resistance management, in cereals and/or for selected pathogenic fungi” is chosen from a second list of uses.
The patent further claims methods for improving growth in crops by preventing and/or curing fungal and/or nematodal infections, resistance management and by improving plant physiology effects. The preventive effect is observed up to four weeks after application of the composition. The composition can be applied to seed, any part of the plant or to the soil directly. The invention specifically claims treatment of cereals such as wheat and barley by this ternary composition.
Fluopyram has a different resistance pattern from Bixafen thus broadening the spectrum of activity against the pests. The composition is effective against a range of fungicidal diseases such as powdery mildew, rust diseases, oomycete diseases, plasmopora diseases, blight diseases, leaf blister etc. and also for controlling nematodal infections.
The patent further exemplifies the synergistic effect of the composition by using the formula given below:
X is the efficacy when active compound A is applied at an application rate of m ppm (or g/ha),
Y is the efficacy when active compound B is applied at an application rate of n ppm (or g/ha),
Z is the efficacy when active compound C is applied at an application rate of r ppm (or g/ha),
E is the efficacy when the active compounds A, B and C are applied at application rates of m, n and r ppm (or g/ha), respectively.