US 2003/0166688 A1Published application

Spot-on formulations for combating parasites

AssigneeMerial Limited

InventorsMark D. Soll, Albert Boeckh

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Abstract

In particular this invention provides for spot-on compositions for the treatment or prophylaxis of parasite infestations in mammals or birds which comprise: (1) a composition comprising (A) an effective amount of a 1-phenylpyrazole derivative; and (B) an effective amount of emamectin; (2) an acceptable liquid carrier vehicle; and (3) optionally, a crystallization inhibitor. The invention also provides for a method of treating parasitic infestations or for the prophylaxis of parasite infestations in mammals or birds which comprises topically applying to said mammal treating parasitic infestations or for the prophylaxis of parasite infestations in mammals or birds which comprises topically applying to said mammal or bird an effective amount of a composition according to the present invention.

Claims52

Dependent claims

A spot-on formulation for the treatment or prophylaxis of parasite infestation in mammals or birds which comprises

(1) a composition comprising
(A) an effective amount of at least one compound of the formula
7
in which:
R1 is a halogen, CN or methyl;
R2 is —S(O)nR3, 4,5-dicyanoimidazol-2-yl, haloalkyl;
R3 is alkyl or haloalkyl;
R4 represents hydrogen halogen atom, NR5R6, —S(O)mR7, —C(O)R7—C(O)OR7, alkyl, haloalkyl, OR8 or —N═C(R9) (R10);
R5 and R6 independently represent hydrogen, alkyl, haloalkyl, —C(O)alkyl, —S(O)rCF3 or alkoxycarbonyl or R5 and R6 together form a divalent alkylene radical which is optionally interrupted by one or two divalent heteroatoms;
R7 represents alkyl or haloalkyl;
R8 represents hydrogen alkyl or haloalkyl;
R9 represents hydrogen or alkyl;
R10 represents an optionally substituted aryl or an optionally substituted heteroaryl group;
R11 and R12 represent, independently of one another, hydrogen, halogen CN or NO2;
R13 represents halogen haloalkyl, haloalkoxy, S(O)qCF3 or SF5 group;
m, n, q and r represent, independently of one another, an integer equal to 0, 1 or 2;
X represents a trivalent nitrogen atom or a C—R12 radical, the three other
valencies of the carbon atom forming part of the aromatic ring;
with the proviso that, when R1 is methyl, then either R3 is haloalkyl, R4 is NH2, R11 is Cl, R13 is CF3 and X is N or else R2 is 4,5-dicyanoimidazol-2-yl, R4 is Cl, R11 is C1, R13 is CF3 and X is C—Cl;
and
(B) an effective amount of emamectin or a salt thereof;
(2) a pharmaceutically or veterinary acceptable liquid carrier vehicle;
and
(3) optionally, a crystallization inhibitor.

21 more elements

A method for combating parasites of a cat or dog comprising localized cutaneous application to the cat or dog, between the shoulders, at a frequency not greater than monthly, of a spot-on composition, which comprises, in a veterinarily acceptable vehicle, an amount parasitically effective of at least one compound (A), and an amount parasitically effective of at least one compound (B), wherein:

compound (A) is an ectoparasiticide of the formula (I)
8
in which:
R1 is CN;
R2 is S(O)nR3;
R3 is haloalkyl;
R4 represents NH2;
R11 represents halogen atom;
R13 represents haloalkyl;
n represents an integer equal to 0, 1 or 2;
X represents a radical C—R12;
R12 represents a halogen atom;
and
compound (B) is an endectocidal parasiticide which is emamectin or a salt thereof and,
the vehicle is for a localized cutaneous application to the animal between the shoulders and contains an organic solvent, an organic cosolvent and/or a crystallization inhibitor wherein:
the crystallization inhibitor selected from the group consisting of polyvinylpyrrolidone, copolymers of vinyl acetate and vinylpyrrolidone, polyoxyethylenated sorbitan esters and mixtures thereof;
the organic solvent comprises acetone, ethyl acetate, methanol, ethanol, isopropanol, dimethylformamide, dichloromethane or diethyl glycol monoethyl ether;
said solvent optionally supplemented by C8-C10 caprylic/capric triglyceride, oleic acid or propylene glycol;
and
the organic cosolvent selected from the group consisting of ethanol, isopropanol, and methanol;
whereby there is a prolonged release of compound (A) in or on the body of the cat or dog and there is a measurable plasma level of compound (B) in the cat or dog.

18 more elements

Dependencies are inferred from the claim text.

Facts

Application: 10/279,356Filed 24 Oct 2002
Priority: FR 96/1144619 Sep 1996
Published: 4 Sep 2003
Term ends: Not estimatedThe source records don’t support an estimate.

Classification5 codes

A01N 43/56
Having rings with two nitrogen atoms as the only ring hetero atoms: 1,2-Diazoles; Hydrogenated 1,2-diazoles
A01N 47/02
Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom not being member of a…:…
A61K 31/70
Medicinal preparations containing organic active ingredients: carbohydrates; Sugars; Derivatives thereof
A01N
Preservation of bodies of humans or animals or plants or parts thereof

Family

Application09/271,470Continuation in part · filed 17 Mar 1999
Application09/376,736Division · filed 17 Aug 1999
Application09/376,736Continuation in part · filed 17 Aug 1999
Application10/155,397Continuation in part · filed 24 May 2002
Application10/155,397Division · filed 24 May 2002
Application10/279,356Continuation in part · filed 24 Oct 2002
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From the US filing history. Foreign family members aren’t listed.