NON-SYSTEMIC CONTROL OF PARASITES
Use of agonists and antagonists of the nicotinergic acetylcholine receptors of insects for the non-systemic control of parasitic insects, such as fleas, lice and flies, on humans and on animals.
1 - 6 . (canceled)
7 . A method for non-systemically controlling a parasitic insect on a human or animal, said method comprising contacting said parasitic insect with an effective amount therefor of an agonist or antagonist of the nicotinergic acetylcholine receptor of an insect in such a way that said agonist or antagonist of the nicotinergic acetylcholine receptor of an insect does not become systemically distributed within said human or animal.
8 . The method according to claim 7 , wherein the agonist or antagonist of the nicotinergic acetylcholine receptor of an insect is a compound of the formula I:
in which
R represents hydrogen or optionally substituted acyl, alkyl, aryl, aralkyl, heteroaryl or heteroarylalkyl;
A represents a monofunctional group selected from hydrogen, acyl, alkyl and aryl or represents a bifunctional group which is linked to the radical Z;
E represents an electron-attracting radical;
X represents the radicals —CH═ or —N═, it being possible for the radical —CH═ to be linked to the radical Z instead of a hydrogen atom;
Z represents a monofunctional group selected from alkyl, —O—R, —S—R and
or represents a bifunctional group which is linked to the radical A or the radical X.
9 . The method according to claim 8 , wherein:
R represents optionally substituted heteroarylmethyl or heteroarylethyl having up to 6 carbon atoms and N, O and/or S as heteroatoms;
A represents hydrogen or optionally substituted alkyl or alkylene having 1 to 4 carbon atoms, wherein alkylene is optionally interrupted by N, O and/or S;
A and Z optionally together form a saturated or unsaturated heterocyclic ring together with the atoms to which they are bonded, wherein said heterocyclic ring optionally has an additional 1 or 2 identical or different heteroatoms and/or hetero groups;
E represents NO 2 , CN or halogenoalkylcarbonyl;
X represents —CH═ or —N═;
Z represents optionally substituted alkyl, —OR, —SR or —NRR; or
Z optionally together with the atom to which it is bonded and the radical:
instead of X, form a saturated or unsaturated heterocyclic ring.
10 . The method according to claim 7 , wherein the agonist or antagonist of the nicotinergic acetylcholine receptor of an insect is a compound of the formula II or III:
in which
n represents 1 or 2;
Subst. represents hydrogen; and
A represents a monofunctional group selected from hydrogen, acyl, alkyl and aryl or represents a bifunctional group which is linked to the radical Z;
E represents an electron-attracting radical;
X represents the radicals —CH═ or —N═, it being possible for the radical —CH═ to be linked to the radical Z instead of a hydrogen atom;
Z represents a monofunctional group selected from alkyl, —O—R, —S—R and
or represents a bifunctional group which is linked to the radical A or the radical X.
11 . The method according to claim 7 , wherein the parasitic insects are fleas.
12 . The method according to claim 7 , wherein the parasitic insects are lice.
13 . The method according to claim 7 , wherein said contacting of parasitic insect with said agonist or antagonist of the nicotinergic acetylcholine receptor of an insect is effected by:
a) topically applying said agonist or antagonist to the dermis of said human or animal; or
b) contacting the dermis of said human or animal with an article containing said agonist or antagonist.
14 . The method according to claim 7 , which is carried out on an animal, wherein said animal is a dog or cat infested with fleas.
15 . The method according to claim 7 , which is carried out on a human, wherein the human is infected with lice.