Agonists and antagonists of the nicotinic acetylcholine receptor

Details Agonists and antagonists of the nicotinic acetylcholine receptor Agonists and antagonists of the nicotinic acetylcholine receptor

1996-11-21

1998-01-27

Henley, Jr., Raymond

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

514 91, 5142268, 514338, 514339, 514357, 514365, 514385, A61K 3144, A61K 31675, A61K 3154, A61K 31425

Patent

active

057122954

DESCRIPTION:

BRIEF SUMMARY
This is a 371 PCT /EP95/02014 filed May 26, 1995.
The present invention relates to combating endoparasites by means of agonists or antagonism of the nicotinergic acetylcholine receptors of insects.
Agonists or antagonists of the nicotinergic acetylcholine receptors of insects are known. They include the nicotinile insecticides and, very particularly, the chloronicotinile insecticides. It is also known that these compounds have an outstanding action against plant-injurious insects. The systemic action of these compounds in plants against plants-injurious insects is also known.
PCT Application WO 93/24 002 discloses that certain derivatives are suitable for systemic use against fleas in domestic animals. In this type of application, the active compound is administered to the domestic animal by oral or parenteral route, for example by means of an injection, to reach the blood stream of the domestic animal. The fleas then take up the active compound when they suck blood. However, nothing has been disclosed about an action of these compounds against endoparasites.
Surprisingly, it has now been found that agonists or antagonists of the nicotinergic acetylcholine receptors of insects are suitable for combating endoparasites.
Agonists or antagonists of the nicotinogenic acetylcholine receptors of insects are disclosed, for example, in European Published Application Nos. 464 830, 428 941, 425 978, 386 565, 383 091, 375 907, 364 844, 315 826, 259 738, 254 859, 235 725, 212 600, 192 060, 163 855, 154 178, 136 636, 303 570, 302 833, 306 696, 189 972, 455 000, 135 956, 471 372, 302 389; German Offenlegungsschrift Nos. 3 639 877, 3 712 307; Japanese Published Application Nos. 03 220 176, 02 207 083, 63 307 857, 63 287 764, 03 246 283, 04 9371, 03 279 359, 03 255 072; U.S. Pat. Nos. 5,034,524, 4,948,798, 4,918,086, 5,039,686, 5,034,404; PCT Application Nos. WO 91/17 659, 91/4965; French Application No. 2 611 114; Brazilian Application No. 88 03 621.
Reference is thus made expressly to the methods, processes, formulae and definitions described in these publications and to the individual preparations and compounds described therein.
These compounds can preferably be represented by the general formula (I) ##STR1## in which R represents hydrogen, optionally substituted radicals from the group consisting of acyl, alkyl, aryl, aralkyl, heteroaryl or heteroarylalkyl. acyl, alkyl and aryl or represents a bifunctional group linked to the radical Z; radical --CH.dbd. to be linked to the radical Z instead of an H atom; --O--R, --S--R, ##STR2## or represents a bifunctional group linked to the radical A or the radical X.
Particularly preferred compounds of the formula (I) are those in which the radicals have the following meanings: consisting of acyl, alkyl, aryl, aralkyl, heteroaryl, heteroarylalkyl. arylcarbonyl, alkylsulphonyl, arylsulphonyl, (alkyl-)-(aryl-)-phosphoryl, all of which can, in turn, be substituted. C.sub.1-4 -alkyl, specifically methyl, ethyl, i-propyl and sec- or t-butyl, all of which can, in turn, be substituted. phenyl. ring atoms and N, O and S, in particular N, as hetero atoms. Thienyl, furyl, thiazolyl, imidazolyl, pyridyl, benzthiazolyl may be mentioned specifically. heteroarylethyl having up to 6 ring atoms and N, O and S, in particular N, as hetero atoms. preferred are: methyl, ethyl, n- and i-propyl and n-, i- and t-butyl; alkoxy having preferably 1 to 4, in particular 1 or 2, carbon atoms such as methoxy, ethoxy, n- and i-propyloxy and n-, i- and t-butyloxy; alkylthio having preferably 1 to 4, in particular 1 or 2, carbon atoms such as methylthio, ethylthio, n- and i-propylthio and n-, i- and t-butylthio; halogenoalkyl having preferably 1 to in particular I to 2 carbon atoms and preferably 1 to 5, in particular 1 to 3, halogen atoms, the halogen atoms being identical or different and being represented preferably by fluorine, chlorine or bromine, in particular fluorine, such as trifluoromethyl; hydroxyl, halogen, preferably fluorine, chlorine, bromine and iodine, in particular fluorine, chlorine and bromin

REFERENCES:
patent: 4678795 (1987-07-01), Shiokawa et al.
patent: 4812571 (1989-03-01), Shiokawa et al.
patent: 4988712 (1991-01-01), Shiokawa et al.
patent: 5298507 (1994-03-01), Shiokawa et al.
patent: 5504081 (1996-04-01), Lohr et al.
Pinnock, et al., Neuropharmacology, vol. 27, No. 8, pp. 843-848, Aug. 1988.
The Merck Index, 11th ed. p. 1030, cit# 6434, 1989.

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