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Title:
DICYCLANIL SALT WITH DODECYLBENZENESULFONATE AND USE OF SUCH A SALT IN COMBATING AND CONTROLLING OF PARASITES
Document Type and Number:
WIPO Patent Application WO/2020/060429
Kind Code:
A4
Abstract:
The present invention relates to 6-diamino-2- cyclopropylaminopyrimidine-5-carbonitrile (dicyclanil) dodecylbenzenesulfonate, a method of preparing dicyclanil dodecylbenzenesulfonate, antiparasitic, preferably larvicide compositions comprising dicyclanil dodecylbenzenesulfonate, and a use of dicyclanil dodecylbenzenesulfonate in combating and controlling of parasites, in particular diptera larvae, in particular larvae of blow flies of the Calliphoridae family, in particular larvae of Lucilia cuprina and Lucilia sericata, in humans and animals.

Inventors:
ŚWIĘTOSŁAWSKI JANUSZ (PL)
WIECZOREK WOJCIECH (PL)
GŁÓWKA JÓZEF (PL)
Application Number:
PL2019/050052
Publication Date:
July 23, 2020
Filing Date:
September 19, 2019
Export Citation:
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Assignee:
ICB PHARMA TOMASZ SWIETOSLAWSKI PAWEL SWIETOSLAWSKI SPOLKA JAWNA (PL)
International Classes:
A61P33/00; A61K31/505; C07C309/31; C07D239/50
Attorney, Agent or Firm:
ŁUKASZYK, Szymon (PL)
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Claims:
AMENDED CLAIMS

received by the International Bureau on 04 June 2020 (04.07.2020)

1. 4,6-diamino-2-cyclopropylaminopyrimidine-5-carbonitrile

dodecylbenzenesulfonate, which is substantially less water-soluble than 4,6- diamino-2-cyclopropylaminopyrimidine-5-carbonitrile.

2. A method of preparing 4,6-diamino-2-cyclopropylaminopyrimidine-5-carbonitrile dodecylbenzenesulfonate, characterized in that 4,6-diamino-2- cyclopropylaminopyrimidine-5-carbonitrile is reacted with dodecylbenzenesulfonic acid.

3. The method according to claim 2, characterized in that said reaction is carried out in a glycol ether/water solvent system, wherein the preferred glycol ether is selected from the group comprising dipropylene glycol monomethyl ether, diethylene glycol monoethyl ether and mixtures thereof in all ratios.

4. The method according to claim 2 or 3, characterized in that said reaction is carried out in situ and the molar ratio of dodecylbenzenesulfonic acid to 4,6- diamino-2-cyclopropylaminopyrimidine-5-carbonitrile in said reaction is preferably from 0.50 to 1.10, and more preferably from 0.70 to 0.98.

5. An antiparasitic, preferably larvicide, composition comprising 4,6-diamino-2- cyclopropylaminopyrimidine-5-carbonitrile dodecylbenzenesulfonate.

6. The composition according to claim 5, characterized in that the content of 4,6- diamino-2-cyclopropylaminopyrimidine-5-carbonitrile dodecylbenzenesulfonate is from 1 to 25% by weight, preferably from 10 to 15% by weight, of the composition.

7. The composition according to claim 5 or 6, characterized in that it comprises castor oil in an amount of from 1 to 10% by weight of the composition.

8. The composition according to claim 5 or 6 or 7, characterized in that it further comprises a glycol ether selected from the group comprising dipropylene glycol monomethyl ether and diethylene glycol monoethyl ether and/or mixtures thereof in any ratio, in an amount of from 50 to 90% by weight of the composition and water in an amount of up to 10% by weight of the composition.

AMENDED SHEET (ARTICLE 19)

14

9. 4,6-diamino-2-cyclopropylaminopyrimidine-5-carbonitrile

dodecylbenzenesulfonate for use in combating and controlling of parasites, in particular diptera larvae, in particular larvae of blow flies of the Calliphoridae family, in particular larvae of Lucilia cuprina and Lucilia sericata, in humans and animals.

10. 4,6-diamino-2-cyclopropylaminopyrimidine-5-carbonitrile

dodecylbenzenesulfonate for use according to claim 9, wherein said 4,6- diamino-2-cyclopropylaminopyrimidine-5-carbonitrile dodecyl benzene sulfonate is applied topically to a human or animal body.

AMENDED SHEET (ARTICLE 19)

15