IP Library Patent Application 15537547
Patent Application
App. No. 15/537,547

USE OF ISOXAZOLINE COMPOUNDS FOR TREATING DEMODICOSIS

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Quick Facts
Patent No.
US None
App. No.
15/537,547
Abstract

The present invention relates to methods of treating demodicosis by administering an isoxazoline compound of formula (I).

Claims (34)

1 . Method of treating generalized demodicosis in mammals comprising administering an effective amount of an isoxazoline compound of formula (I)

wherein

R 1 =halogen, CF 3 , OCF 3 , CN,

n=integer from 0 to 3,

R 2 =C 1 -C 3 -haloalkyl,

T=5- or 6-membered ring, which is optionally substituted by one or more radicals Y,

Y=methyl, halomethyl, halogen, CN, NO 2 , NH 2 —C═S, or two adjacent radicals Y form together a chain;

Q=X—NR 3 R 4 or a 5-membered N-heteroaryl ring, which is optionally substituted by one or more radicals;

X=CH 2 , CH(CH 3 ), CH(CN), CO, CS,

R 3 =hydrogen, methyl, haloethyl, halopropyl, halobutyl, methoxymethyl, methoxyethyl, halomethoxymethyl, ethoxymethyl, haloethoxymethyl, propoxymethyl, ethylaminocarbonylmethyl, ethylaminocarbonylethyl, dimethoxyethyl, propynylaminocarbonylmethyl, N-phenyl-N-methyl-amino, haloethylaminocarbonylmethyl, haloethylaminocarbonylethyl, tetrahydrofuryl, methylaminocarbonylmethyl, (N,N-dimethylamino)-carbonylmethyl, propylaminocarbonylmethyl, cyclopropylaminocarbonylmethyl, propenylaminocarbonylmethyl, haloethylaminocarbonylcyclopropyl,

wherein Z A =hydrogen, halogen, cyano, halomethyl (CF 3 );

R 4 =hydrogen, ethyl, methoxymethyl, halomethoxymethyl, ethoxymethyl, haloethoxymethyl, propoxymethyl, methylcarbonyl, ethylcarbonyl, propylcarbonyl, cyclopropylcarbonyl, methoxycarbonyl, methoxymethylcarbonyl, aminocarbonyl, ethylaminocarbonylmethyl, ethylaminocarbonylethyl, dimethoxyethyl, propynylaminocarbonylmethyl, haloethylaminocarbonylmethyl, cyanomethylaminocarbonylmethyl, or haloethylaminocarbonylethyl;

or R 3 and R 4 together form a substituent selected from the group consisting of:

or a salt or solvate or N oxide thereof.

2 . The method according to claim 1 wherein the isoxazoline compound of formula (I) is fluralaner.

3 . The method according to claim 1 wherein the isoxazoline compound is administered once, twice or three times.

4 . The method according to claim 1 comprising a single administration of the isoxazoline compound to a mammal.

5 . The method according to claim 1 wherein the isoxazoline compound is administered to the mammal orally

6 . The method according to claim 1 wherein the isoxazoline compound is administered to the mammal topically.

7 . The method according to claim 1 wherein the isoxazoline compound is administered to the mammal parenterally by injection.

8 . The method according to claim 1 wherein the mammal is a companion animal.

9 . The method according to claim 1 wherein the companion animal is a dog.

10 . Method of controlling Demodex spp. mites in dogs after a single administration of an isoxazoline compound of formula (I).

11 . The method according to claim 10 wherein the isoxazoline compound of formula (I) is fluralaner.

12 . The method according to claim 10 wherein the Demodex spp. mites are controlled for at least 56 days.

13 . The method according to claim 10 wherein the isoxazoline compound is administered to the mammal orally.

14 . The method according to claim 10 wherein the isoxazoline compound is administered to the mammal topically.

15 . The method according to claim 10 wherein the isoxazoline compound is administered to the mammal parenterally by injection.

16 . The method according to claim 1 wherein the isoxazoline compound is afoxalaner.

17 . The method according to claim 1 wherein the isoxazoline compound is sarolaner.

18 . The method according to claim 1 comprising a single administration of 10-40 mg/kg bodyweight fluralaner to dogs that have been diagnosed with generalized demodicosis.

19 . The method of claim 1 , where n is 1, 2 or 3.

20 . The method of claim 1 , wherein R 2 is CF 3 or CF 2 Cl.

21 . The method of claim 1 , wherein two adjacent radicals Y form together a three or four membered chain.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 19, 2017
From: WILLIAMS, HEIKE; HECKEROTH, ANJA REGINA; TANZLER, JANINA; FRENAIS, REGIS JOEL ALAIN
To: INTERVET INC.
Reel/Frame 042745/0826 →