Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Reexamination Certificate
2002-05-10
2004-02-10
Pryor, Alton N. (Department: 1616)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
C424S405000
Reexamination Certificate
active
06689796
ABSTRACT:
This Application is a 371 of PCT/GB00/01987 filed Jun. 1, 2000.
The present invention relates to new rodenticidal compositions containing certain halogenated bis-pyridyl amine compounds am rodenticidally-active materials. It also relates to new rodent baits containing said halogenated bis-pyridyl amine compounds.
Infestations of rodents, particularly rats, cause serious problems for people close to the locality of there infestations Rats, for instance, cause damage to food crops in store and in the field and represent a health hazard due to the various diseases which they can carry control and elimination of such infestations is, thus, necessary.
Many poisons for rodents are known. However, to be useful in the control and elimination of infestations of rats, a poison has to meet certain criteria in terms of its properties. For instance, it has to be sufficiently toxic such that the consumption of a relatively small amount of bait containing will be fatal for the rat. It also has to have a smell and a taste which is acceptable to the rat or which can be masked by the smell and taste of the bait in which it is employed. It should also be easy and safe for humans.
According to the present invention there is provided a rodenticidal composition comprising a carrier together with an effective amount of rodenticidally-active compound having the formula I
wherein R
1
, R
2
, R
3
, R
4
, R
5
, R
6
, R
7
and R
8
are the same or different halogen selected from F, Cl and Br atoms. According to a preferred embodiment the amine group in formula I is attached to the two halogenated pyridyl groups at the 4-position. Especially preferred, for use in the present invention, is the compound bis (2,3,5,6-tetrafluoro-4-pyridyl)amine.
Compounds of the formula I above have been discovered by the present inventors to be particularly toxic to rodents, particularly rats, and to have smell and taste that are non-repellent such as to be palatable to rodents.
In the rodenticidal composition the active halogenated bis-pyridyl amine compound is employed in or with a solid carrier which is consumable by the rodents. Such carriers must, like the active compounds, be pallatable to rodents. Typically the carriers will be food items to act as bait for the rodent and these are known generally in the art. Examples of food items that can be used as carriers for the active halogenated bis-pyridyl amine compounds in the present invention include cereal grains, oatmeal, vegetables, biscuits, sugar and molasses.
The compositions of the invention will generally contain up to 200 ppm, and preferably from 20 to 100 ppm of the active halogenated bis-pyridyl amine compound. It is further possible to incorporate into the rodenticidal composition one or more other rodenticidally-active materials, such as anticoagulant-type substances. The incorporation of other active materials into the composition may allow for the use of smaller doses of the halogenated bis-pyridyl amine compounds.
The active halogenated bis-pyridyl amine compounds of Formula I above, especially the compound bis(2,3,5,6-tetrafluoro-4-pyridyl)amine, are particularly useful as the poison component of a rodent bait in particulate form wherein each particle provides a lethal dose of active compound with respect to an adult rodent of the species for which the bait is intended and wherein each particle has a size which allows the rodent species for which the bait is intended to take the particle into its mouth without prior nibbling.
Thus, the present invention further provides a rodent bait comprising food and a poison, said poison being wholly in the form of, or contained in, one or more discrete poison-providing particles of such activity with respect to the rodent species for which the bait is intended that each poison-providing particle provides a lethal dose with respect to an adult rodent of that species, each poison-providing particle being substantially homogeneous and being of a particle size which is such that a rodent of the species for which the bait is intended will take the particle into its mouth without prior nibbling, wherein the poison comprises a compound having the formula I:
wherein R
1
, R
2
, R
3
,R
4
, R
5
, R
6
, R
7
and R
8
are the same or different halogen selected from F, Cl and Br atoms. According to an especially preferred embodiment the active compound used in the rodent bait is bis(2,3,5,6-tetrafluoro-4-pyridyl)amine on account of its high toxicity to rodents. Thus, each particle of the bait is ingested orally as an individual particle; the required particle size can be determined by routine experiment. The term “lethal dose” means a dose which normally is capable of killing an adult rodent of the species concerned when taken orally thereby; to those in the art this means a dose which presents an insignificant chance of survival to the largest rodents of the species concerned which is likely to be encountered.
It will be appreciated, therefore, that this aspect of the present invention is predicated on the concept of concentrating the poison component of the bait in particles each of which is lethal per se, and ensuring that the poison particles are taken as a whole into the mouth of the rodent, i.e., without prior nibbling of the poison particles. As a result the rodent feeds on the bait and consumes the food component thereof, which it can nibble or not depending on its particle size, until sooner or later it comes to a poison particle. When it does so, it consumes that particle whole, and once having it into its mouth and swallowed it, death follows inevitably in view of the lethal dose nature of the particle. In short the rodent either consumes innocuous edible material or a lethal dose of poison. This concept was first proposed in EP-A-0109697. In the present invention, however, use is, made of the compounds of the formula I, especially bis(2,3,5,6-tetrafluoro-4-pyridyl)amine, which have the characteristic that a delay occurs between ingestion of the poison particle and death. It has been observed that a rat will be suspicious of a food source if it sees another which is dead or clearly ill close to that food source. Because a rat which has ingested bait containing a lethal dose of bis(2,3,5.6-tetrafluoro-4-pyridyl)amine can take a few hours, typically 4 to 12 hours, before developing visible symptoms of poisoning other rats will not associate the symptoms of a poisoned rat with the bait and will not, therefore, become bait shy. Thus, whereas as the use of poisons which give no significant delay between ingestion and death becomes less successful as time passes since the bait was first put down, and which typically control only 50% of an infestation of rats, the use of the present invention can give at least 97% control of an infestation of rats in 4 nights;
This approach to the formulation of rodent baits has the advantage that the bait as a whole need only comprise relatively few lethal particles in order to be effective against a number of rodents. Also, the inability to detect the presence of lethal particles results in the rodent feeding normally without bait shyness So that even if it does not happen to consume a poison particle at the first feed, it will not be deterred from feeding again on the same kind of bait.
The present invention makes it possible to use, safely, rodent poisons which are lethal in very small quantities. Hitherto, the poison content of acute baits, in which the poison is homogeneously distributed throughout the food component in accordance with conventional practice has normally been in the concentration range 0.2 to 2.0% (2000 to 20,000 ppm). This is a high concentration from the environmental hazard point of view. In contrast, the maximum concentration of poison envisaged in carrying out the present invention is about 200 ppm, typically 20-80 ppm.
Whilst it is possible for the bait to include only one such poison particle, normally it will contain a number of such particles although a lethal particle taken orally by the rodent will kill it, a larger mammal such as a dog (for which the leth
Hadler Malcolm
Johnson Roger
Lahive & Cockfield LLP
Laurentano, Esq. Anthony A.
Pryor Alton N.
Smith, Esq. DeAnn F.
Sorex Limited
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