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Pesticides

A technology for C1-C6, compounds, applied in the field of new insecticides, which can solve the problems of treatment aversion, inability to achieve, premature stop, etc.

Inactive Publication Date: 2004-12-01
NOVARTIS AG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Such an intensive treatment procedure however requires a high level of training and experience has shown that after only a short period of time a stress response occurs on the part of the animal and on the part of the animal caretaker, which often leads to aversion to the handling and to its premature stop
[0014] Prolongation of the action of this class of inherently extremely potent substances is thus a long-desired, but apparently unattainable goal

Method used

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Examples

Experimental program
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Effect test

preparation example Construction

[0270] Preparation of primary products

[0271] Carbonic acid (chloromethyl ester) (4-nitrophenyl ester) preparation:

[0272]

[0273] A solution of 69.6 g of 4-nitrophenol and 39.6 g of pyridine in 500 ml of dichloromethane was added dropwise to a solution of 71 g of chloromethyl chloroformate in 1000 ml of dichloromethane at 0° C. over a period of 30 minutes. The reaction mixture was stirred at 0 °C for another 2 h, then 1000 ml of H 2 O. The organic phase was washed with 250 ml each of 1N NaOH and aqueous sodium chloride and dried over magnesium sulfate.

[0274] After concentrating off the solvent, 111 g of a white solid with a melting point of 61-62°C were obtained.

[0275] Preparation of Carbonic Acid (Iodomethyl Ester) (4-Nitrophenyl Ester)

[0276]

[0277] 34.8g carbonic acid (chloromethyl ester) (4-nitrophenyl ester), 45.0g NaI and 2.52g NaHCO 3 Suspended in 350 ml of acetone, the obtained suspension was stirred at a temperature of 40° C. for 16 ho...

Embodiment 1

[1095] Example 1: A tablet comprising 25 mg of a compound of general formula (I) is prepared as follows:

[1096] Element (for 1000 pieces)

[1097] The compound of general formula (I) 25.0g

[1098] Lactose 100.7g

[1099] Wheat starch 7.5g

[1100] Polyethylene glycol 6000 5.0g

[1101] Talc 5.0g

[1102] Magnesium stearate 1.8g

[1103] Demineralized water q.s.

[1104] preparation : All solid components are first sieved through a 0.6 mm mesh size sieve. Then the active ingredient, lactose, talc and half of the starch are mixed together. The other half of the starch was then suspended in 40 ml of water and the suspension was added to a boiling solution of polyethylene glycol in 100 ml of water. The obtained starch paste is added to the main batch, the mixture is granulated and water is added if necessary. The granules are dried overnight at 35°C, sieved through a 1.2 mm mesh size sieve, blended with magnesium stearate and compressed to form tablets having a m...

Embodiment 2

[1105] Example 2: Solution for Injection

[1106] Compound of general formula (I) 0.1-10%, preferably 0.5-5%

[1107] Nonionic surfactant 0.1-30%, preferably 0.5-10%

[1108] Mixture of ethanol and propylene glycol 60-99%, preferably 85-90%

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Abstract

Novel pesticides of formula (I), wherein the substituents R, R1, R2, R2', T, U, X and Y are as defined in claim 1, are described. Also described are compositions suitable for use as parasiticides comprising those compounds as active ingredient and to methods of controlling parasites that are based on the administration of those compounds or compositions, and to the use of the said compounds and compositions in a method of controlling parasites and in the manufacture of pesticides for use against parasites. Also described are intermediates of formula (XX) wherein R1, R2, R2', T, U, X and Y are as defined in claim 1 and Hal is halogen. The latter also exhibit parasiticidal activity and are suitable for the preparation of the compounds of formula (I).

Description

technical field [0001] The present invention relates to novel insecticides of the following general formula (I) which have improved resistance to parasites; to compositions suitable for use as parasiticides comprising these compounds as active ingredients and to compositions containing these compounds or compositions Application-based methods of controlling parasites, and to the use of said compounds and compositions in methods of controlling parasites and in the manufacture of insecticides to combat parasites. Also described are intermediates of general formula (XX), which themselves have parasiticidal activity and are well suited for the preparation of compounds of general formula (I). Background technique [0002] A number of insecticides are known to be useful in controlling parasites in warm-blooded animals. This control is mainly carried out by two different methods; either by exposure of the host animal to local and thus external treatments, or...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D277/20A01N47/12A01N47/16A01N47/18A01N47/44A61D7/00A61P7/04A61P33/00C07D213/61C07D277/32C07D417/06
CPCC07D277/32C07D417/06A01N47/44C07D213/61A01N47/12A01N47/16A61P33/00A61P33/14A61P7/04
Inventor T·戈贝尔E·亨博特-德罗兹M·施瓦曾伯克
Owner NOVARTIS AG
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