Nova Patents
EP3078664A1

Antiparasitic dihydroazole compositions

Abstract

The present invention relates to composition comprising dihydroazole of formula (I) and salts thereof: Wherein R1, A1, A2, G, X and Y are as defined in the description, compositions thereof, processes for their preparation and their uses to prevent or treat parasitic infections or infestations in animals and as pesticides.

EP3078664A1, drawing sheet 1
Sheet 1 of 41

Term

4.2 yearsto projected expiry

Projected expiry 16 December 2030, counted from filing; an application has no term until it is granted.

  1. Priority and filed
  2. Published
  3. Today
  4. Projected expiry

26 claims: 3 independent, 23 dependent

  1. 1
    A composition for the treatment or prevention of a parasitic infection or infestation in an animal comprising:a) dihydroazole compound of formula (I), or a pharmaceutically acceptable salt thereof: wherein: R 1 is hydrogen, halogen, -CN, or alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, haloalkynyl, cycloalkyl, halocycloalkyl, alkylcycloalkyl or cycloalkylalkyl, each which is unsubstituted or substituted with one or more of halogen, hydroxy, amino, alkyl- or di(alkyl)amino, alkyl, cycloalkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, haloalkynyl, alkoxy, haloalkoxy, alkylthio, haloalkylthio, R 7 S(O)-, R 7 S(O) 2 -, R 7 C(O)-, R 7 R 8 NC(O)-, R 7 OC(O)-, R 7 C(O)O-, R 7 C(O)NR 8 -, -CN or -NO 2 ;X is aryl or heteroaryl, which may be unsubstituted or substituted by one or more of halogen, hydroxy, amino, alkyl- or di(alkyl)amino, alkyl, cycloalkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, haloalkynyl, alkoxy, haloalkoxy, alkylthio, haloalkylthio, R 7 S(O)-, R 7 S(O) 2 -, R 7 C(O)-, R 7 R 8 NC(O)-, R 7 OC(O)-, R 7 C(O)O-, R 7 C(O)NR 8 -, -CN or -NO 2 ;A 1 and A 2 are independently oxygen, NR 2 or CR 7 R 8 ;G is G-1 or G-2;B 1 , B 2 , B 3 , B 4 and B 5 are independently N or C-R 9 ;Y is hydrogen, halogen, -CN;or Y is alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, haloalkynyl, cycloalkyl, alkylcycloalkyl, cycloalkylalkyl, aryl, or heterocyclyl or heteroaryl each of which is unsubstituted or substituted with one or more of halogen, hydroxy, amino, alkyl- or di(alkyl)amino, alkyl, cycloalkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, haloalkynyl, alkoxy, haloalkoxy, alkylthio, haloalkylthio, R 7 S(O)-, R 7 S(O) 2 -, R 7 C(O)-, R 7 R 8 NC(O)-, R 7 OC(O)-, R 7 C(O)O-, R 7 C(O)NR 8 -, -CN or -NO 2 ;or Y is Y-1, Y-2, Y-3, Y-4, Y-5, Y-6, Y-7, Y-8, Y-9, Y-10, Y-11, Y-12 or Y-13;R 2 , R 3 are independently hydrogen, alkyl, haloalkyl, thioalkyl, alkylthioalkyl, hydroxyalkyl, alkoxylakyl, alkenyl, haloalkenyl, alkynyl, haloalkynyl, cycloalkyl, R 10 S(O)-, R 10 S(O) 2 -, R 10 C(O)-, R 10 C(S)-, R 10 R 11 NC(O)-, R 10 R 11 NC(S)- R 10 OC(O)-;R 4 , R 5 and R 6 are independently hydrogen, alkyl, haloalkyl, thioalkyl, alkylthioalkyl, hydroxyalkyl, alkoxylakyl, alkenyl, haloalkenyl, alkynyl, haloalkynyl, cycloalkyl, aryl or heteroaryl;R 7 and R 8 are independently hydrogen, alkyl, haloalkyl, thioalkyl, alkylthioalkyl, hydroxyalkyl, alkoxylakyl, alkenyl, haloalkenyl, alkynyl or haloalkynyl;R 9 is hydrogen, halogen, -CN, or alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, haloalkynyl, cycloalkyl, halocycloalkyl, alkylcycloalkyl or cycloalkylalkyl, each which is unsubstituted or substituted with one or more of halogen, hydroxy, amino, alkyl- or di(alkyl)amino, alkyl, cycloalkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, haloalkynyl, alkoxy, haloalkoxy, alkylthio, haloalkylthio, R 7 S(O)-, R 7 S(O) 2 -, R 7 C(O)-, R 7 R 8 NC(O)-, R 7 OC(O) -, R 7 C(O)O-, R 7 C(O)NR 8 -, -CN or -NO 2 ;R 10 , R 11 , R 12 and R 13 are each independently hydrogen, alkyl, haloalkyl, thioalkyl, alkylthioalkyl, hydroxyalkyl, alkoxylakyl, alkenyl, haloalkenyl, alkynyl or haloalkynyl;or R 10 together with R 11 form =O, =S or =NR 2 ;or R 12 together with R 13 form =O, =S or =NR 2 ;W is O, S or NR 2 ;n is 1-4;and m is 0, 1 or 2;b) one or more additional parasiticidal active agent;and a pharmaceutically acceptable carrier.
  2. 18
    The composition according to any of the preceding claims, wherein the one or more additional active agent is selected from the group consisting of an arylpyrazole, a neonicotinoid, a pyrethroid, an amino acetonitrile compound, a paraherquamide, a spinosyn active, a cyclic depsipeptide, a benzimidazole active, an imidazothiazole active, a tetrahydropyrimidine active, praziquantel, an avermectin, a milbemycin and an insect growth regulator.
  3. 24
    The composition of any preceding claim, wherein the composition is an oral formulation, a topical formulation or an injectable formulation.
Independent claims3