IP Library Granted Patent US 10,857,121
Granted Patent B2
US 10,857,121 · App. 15/304,018 · Granted Dec 8, 2020

Use of malononitrile compounds for protecting animals from parasites

Inventors: Charles Meng (Grayson, GA); Christian Miculka (Wiesbaden, DE); Mark Soll (Alpharetta, GA); Ralph Paulini (Bad Durkheim, DE); Matthias Pohlman (Freinsheim, DE); Sebastian Sorgel (Ludwigshafen, DE); Henricus Maria Martinus Bastiaans (Chapel Hill, NC); Sarah Rachel Devereux (Raleigh, NC); Cecille Ebuenga Doyog (Puthotuntungin los Banos, PH); Anna Malveda Umali (Lusacan Tiaong Quezo, PH); Rhoel Suiza Cosare (Calauan Laguna Brgy. Sto. Tomas, PH); Christopher Palmer (San Jose, CA); Takeo Hokama (Mountain View, CA)
Assignees: MERIAL INC.; BASF, SE
A61K31/277A01K11/001A01N37/34A61D7/00A61K9/0046A61K31/357
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Quick Facts
Patent No.
US 10,857,121
App. No.
15/304,018
Granted
Dec 8, 2020
Kind
B2
Abstract

The present invention provides uses of aryl alkyl malononitrile compounds of formula (I), or veterinarily acceptable salts thereof, for controlling and preventing parasite infestations in animals. The invention also provides methods for controlling and preventing parasite infestation in animals comprising administering an effective amount of at least one aryl alkyl malononitrile compound of formulae (I), or a veterinarily acceptable salt thereof, to the animal.

Claims (31)

1. A method for controlling or preventing the parasitic infestation of cattle by Stomoxvs calcitrans or Haematobia irritans comprising administering a pour-on formulation comprising an effective amount of an aryl alkyl malononitrile compound of formula (I), or a salt thereof, to the animal:

wherein

Y is phenyl unsubstituted or substituted with 1, 2, 3, 4 or 5 substituents R 5 ;

Q is phenyl unsubstituted or substituted with 1, 2, 3, 4 or 5 substituents R 6 ;

R 1 is hydrogen or C 1 -C 6 alkyl;

R 2 is hydrogen;

each R 5 is independently halogen;

each R 6 is independently halogen, C 1 -C 6 alkyl, wherein the carbon atoms of the aforementioned C 1 -C 6 alkyl are unsubstituted or substituted with one or more R a , or —OCF 3 ; or R 6 is C 2 -C 6 alkynyl;

each R a is independently halogen;

p is 0; and R 3 and R 4 are not present.

2. The method of claim 1 , wherein:

R 1 is H, methyl, ethyl or isopropyl.

3. The method of claim 1 , wherein R 5 is fluoro.

4. The method of claim 3 , wherein R 6 is fluoro.

5. The method of claim 1 , wherein

Y is phenyl substituted with 1, 2, or 3 substituents R 5 ;

Q is phenyl substituted with 1, 2, or 3 substituents R 6 ;

R 1 is H or methyl;

R 2 is H and

each R 5 is independently halogen.

6. The method of claim 1 , wherein the compound of formula (I), or a salt thereof, is administered via an external device.

7. The method of claim 1 , wherein the volume of the pour-on formulation is about 10 ml to about 100 mL.

8. The method of claim 1 , wherein the concentration of the compound of formula (I) is about 5% (w/v) to about 20% (w/v).

9. The method of claim 1 , wherein the pour-on formulation comprises N-methylpyrrolidone, dimethyl isosorbide or a C 8 to C 12 triglyceride or a C 8 -C 12 esters of propylene glycol, or a combination thereof.

10. The method of claim 1 , wherein the method is at least 70% effective against Haematobia irritans 24 hours after infestation for at least 22 days.

11. The method of claim 1 , wherein the method is at least 90% effective against Haematobia irritans 24 hours after infestation for at least 22 days.

12. The method of claim 1 , wherein the compound of formula (I) has the structure of formula (II):

wherein:

Q is 4-ethynylphenyl;

R 1 , R 51 , R 52 , R 54 and R 55 are each hydrogen; and

R 53 is fluoro.

Assignments (3)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 3, 2020
From: SOERGEL, SEBASTIAN; BASTIAANS, HENRICUS MARIA MARTINUS; POHLMAN, MATTHIAS; PAULINI, RALPH; DEVEREUX, SARAH RACHEL; EBUENGA, CECILLE; SUIZA, RHOEL SUIZA; MALVEDA U., ANNA LOUREN
To: BASF SE
Reel/Frame 054283/0159 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Oct 20, 2020
From: MERIAL, INC.
To: BOEHRINGER INGELHEIM ANIMAL HEALTH USA INC.
Reel/Frame 054140/0297 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 15, 2016
From: MENG, CHARLES; MICULKA, CHRISTIAN; SOLL, MARK
To: MERIAL, INC.
Reel/Frame 040319/0741 →
Continuity (2)
Provisional Application 61980832 · Apr 17, 2014
Related Publication 20170027899A1 · Feb 2, 2017