Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Reexamination Certificate
2002-05-24
2003-04-15
Levy, Neil S. (Department: 1616)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
C514S341000, C514S407000, C424S084000, C424S405000, C424S409000, C424S410000, C424SDIG001
Reexamination Certificate
active
06548528
ABSTRACT:
An object of the instant invention is to protect a building that has already been built or is going to be built against crawling insects, especially against termites.
The insecticidal compounds of the family of the 1-arylpyrazoles are known to be active against termites.
Conventional termite control operators apply the chemical around or under the building or houses to form a barrier against termites invasion. However loopholes in the treatment may cause failure of protection of the houses.
Another system is to use a bait which contains an attractant for termites so as to force the termites to eat the bait and then to be killed by the active ingredient contained also in that bait.
An object of the invention is to provide an improved process of protection of houses.
Another object of the invention is to provide a treatment against termites which reduce the number of the call-back from house owners of treated houses.
An object of the instant invention is to protect the building with the minimum amount of insecticidally active ingredient.
Another object of the instant invention is to have a good level of protection of buildings against termites while reducing the amount of applied insecticide.
Another object of the instant invention is to reduce the need to treat directly the location where the termites are or are expected to be.
Another object of the instant invention is to provide a curative treatment with reduced need to find out the precise place of termites attacks.
Another object of the instant invention is to provide a curative treatment which is effective even when attacked parts are untreated.
Another object of the instant invention is to provide a curative treatment which is mainly a blind treatment with no checking of the attacked parts.
Another object of the instant invention is to provide a termite treatment functioning like an intangible trap.
Another object of the instant invention is to provide a termite treatment without barrier.
Another object of the instant invention is to provide a termite treatment which is mainly a soil treatment.
It has been found that these goals may be achieved by means of the process of the instant invention.
The present invention relates to a process for the protection of a building that has already been built or is going to be built, whereby an effective amount of an insecticidally active compound is spread around or under the building at discrete locations.
The insecticidally active material which can be used in the invention is an active ingredient which is active by contact (contact with species to be killed) and has no repellent effect on the insects, preferably no repellent effect on the insects to be killed.
A preferred class of active ingredient which can be used in the invention are the compounds without quick knock-down effect, or compounds able to produce a so-called secondary killing effect, that is to say an action of killing insects which have not been directly treated by mean of the said insecticide. Also preferred are the insecticides which are able to kill the termites of the termites nest when brought back by treated termites coming close to the house or building built or to be built.
In a practical point of view, the most preferred compounds are insecticides of the 1-arylpyrazole type, especially those having the formula (I)
in which:
R
1
is CN or methyl or a halogen atom,
R
2
is S(O)
n
R
3
or 4,5-dicyanoimidazol 2-yl or haloalkyl,
R
3
is alkyl or haloalkyl;
R
4
represents a hydrogen or halogen atom or a member of a group consisting of NR
5
R
6
, S(O)
m
R
7
, C(O)R
7
, C(O)O—R
7
, alkyl, haloalkyl, OR
8
and —N═C(R
9
)(R
10
);
R
5
and R
6
independently represent the hydrogen atom or an alkyl, haloalkyl, C(O)alkyl, alkoxycarbonyl or S(O)
r
CF
3
radical; or R
5
and R
6
can together form a divalent alkylene radical which can be interrupted by one or two divalent heteroatoms, such as oxygen or sulfur;
R
7
represents an alkyl or haloalkyl radical;
R
8
represents an alkyl or haloalkyl radical or a hydrogen atom;
R
9
represents an alkyl radical or a hydrogen atom;
R
10
represents a phenyl or heteroaryl group which may optionally be unsubstituted or substituted by one or more halogen atoms or a member of the group consisting of OH, —O-alkyl, —S-alkyl, cyano, and alkyl;
R
11
and R
12
represent, independently of one another, a hydrogen or halogen atom, or CN or NO
2
,
R
13
represents a halogen atom or a haloalkyl, haloalkoxy, S(O)
q
CF
3
or SF
5
group,
X represents a trivalent nitrogen atom or a C—R
12
radical, the other three valences of the carbon atom forming part of the aromatic ring,
m, n, q, and r represent, independently of one another, an integer equal to 0, 1, or 2,
provided that, when R
1
is methyl, then either R
3
is haloalkyl, R
4
is NH
2
, R
11
is Cl, R
13
is CF
3
and X is N; or then R
2
is 4,5-dicyanoimidazol 2-yl, R
4
is Cl, R
11
is Cl, R
13
is CF
3
, and X is ═C—Cl.
Alkyl groups have generally 1 to 6 carbon atoms.
A preferred group of effective 1-arylpyrazoles of the present invention is that wherein:
R
1
is CN; R
3
is a haloalkyl radical; R
4
is NH
2
; X is C—R
12
;
R
11
and R
12
represent, independently of one another, a halogen atom; and
R
13
is a haloalkyl radical.
A most preferred compound is 5-amino 1-(2,6-dichloro 4-trifluoromethyl phenyl) 4-trifluoromethylsulfinyl 3-cyanopyrazole, hereafter designated as compound (A).
Compounds of formula (I) may be prepared according to known processes, for example as described in International Patent Publications n° WO 87/3781, 93/6089, and 94/21606 as well as in European Patent Applications 295117, 403300, 385809 or 679650. German Patent Publication 19511269 and U.S. Pat. Nos. 5,232,940 and 5,236,938 or other process according to the knowledge of a man skilled in the art of chemical synthesis, which is deemed to include the Chemical Abstract and the literature referred to therein. Compositions comprising the compounds of formula (I) may also be prepared according to the teaching of same prior art or similar one.
An advantageous way of practicing the invention is to use the active ingredient in a formulation which does not contain any adjuvant having termite attractant properties. Even though, such attractant may be used optionally, it may be risky, and it may make the residents or owners of the house reluctant against such treatment. Known processes were generally unable to avoid the use of attractant in order to be effective.
The process of the invention may be practiced in a preventive way as well as in a curative way.
The actual treatment by mean of active ingredient may be made inside or outside the outline of the houses or buildings to be built.
It is generally more effective to apply the active ingredient or formulation at a locus where the insects, especially the termites are more frequently crawling or traveling or climbing. These locus are more particularly the corners and/or crossing walls of the buildings or buildings which are going to be built. They are also more particularly the locus which have a greater humidity level than the rest of the perimeter of the house.
The active ingredient is applied advantageously on soil. It might be simple surface treatment or also spraying, mixing, blending or drenching of the soil with a formulation.
The effective amount of compound applied on soil is generally within the range of 0.05 g of active ingredient per m
2
of surface of the soil to 0.0001 g/m
2
. This range is given for the precise locus where the active ingredient is applied.
As already said, the active ingredient is applied on discrete locus. The general rate of application is such that the treated part of the perimeter of the house is 0.5 to 7.5 treated meter per 10 meter of global perimeter, the width of treated locus being in the range of 1 to 50 cm, preferably 5 to 30 cm.
For their application, the compounds of the formula (I), or derivatives thereof, are generally in the form of compositions, which are in various solid or liquid forms.
Solid forms of compositions which can be used are dusting powders (wit
Connolly Bove Lodge and Hutz LLP
Levy Neil S.
Rhone-Poulenc Agro
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