发明名称 (HETERO) ARYLACRYLAMIDES FOR THE CONTROL OF ECTOPARASITES
摘要 The present invention relates to new compounds of formula (I) wherein the variables have the meaning as indicated in the claims; in free form and in salt form; and optionally the enantiomers and geometrical isomers thereof. The compounds of formula (I) are useful in the control of parasites, in particular ectoparasites, in and on vertebrates.;
申请公布号 US2015320044(A1) 申请公布日期 2015.11.12
申请号 US201314649268 申请日期 2013.12.20
申请人 DUPONT Emilie;GAUVRY Noëlle;NANCHEN Steve;OGAWA Chikako;TAHTAOUI Chouaib;Novartis Tiergesundheit AG 发明人 Dupont Emilie;Gauvry Noelle;Nanchen Steve;Ogawa Chikako;Tahtaoui Chouaib
分类号 A01N37/34;A01N37/18;C07C255/48;C07D213/40;A01N43/40;C07D307/52;A01N43/08;A01N43/20;C07D305/06;C07D331/04;C07D309/14;A01N43/16;C07D213/75;A01N43/44;A01N43/36;A01N43/80;C07D207/273;C07D205/04;C07D261/04;C07C233/66 主分类号 A01N37/34
代理机构 代理人
主权项 1. A compound of formula including all geometric and stereoisomers, N-oxides, S-oxides, salts and prodrugs thereof, R1 is independently halogen, cyano (—CN), nitro (—NO2), C1-C6-alkyl, C3-C6-cycloalkyl, C2-C6-alkenyl, C2-C6-alkynyl, C1-C6-haloalkyl, C1-C6-alkoxy, C1-C6-haloalkoxy, C1-C6-alkylthio, C1-C6-haloalkylthio, C1-C6-alkylsulfinyl, C1-C6-haloalkylsulfinyl, C1-C6-alkylsulfonyl, C1-C6-haloalkylsulfonyl, N-mono- or N,N-di-C1-C6-alkylamino, C1-C6 alkoxycarbonyl, C1-C6-alkylcarbonyl, aminosulfonyl, C1-C6-alkylaminosulfonyl, C1-C6-alkylsulfonylamino or phenyl which is unsubstituted or substituted by halogen, cyano, nitro, C1-C4-haloalkyl, C1-C4-haloalkoxy or C1-C4-haloalkylthio; or R1 is a C1-C4 carbon chain which optionally contains 1-2 heteroatoms from the group of N, S, O, which is bonded to two adjacent ring positions and which forms an aliphatic, aromatic, heteroaromatic or heterocyclic ring which is optionally mono- or polysubstituted by C1-C6-alkyl or halogen, in which case n is 2; Y is a radical of formula where the second (right-hand) connection site in each case is connected to the C(O)NR7R8 moiety; R7 is H, C1-C6-alkyl which is unsubstituted or substituted by halogen, C1-C4-alkoxy, C1-C2-alkylthio, cyano, nitro, amino or N-mono- or N,N-di-C1-C4alkylamino, or is C2-C4-alkenyl, C2-C4-alkynyl or C3-C6-cycloalkyl; R8 is H; a group —CH═N—OR9; a radical Q; a radical Q1; or is C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, C3-C6-cycloalkyl, C4-C7-alkylcycloalkyl, C4-C7-cycloalkylalkyl, C5-C10-bicyclo-alkylene or C3-C6-cycloalkanone which is each unsubstituted or substituted in the alkyl, cycloalkyl, alkenyl or alkynyl moiety by halogen, hydroxy, carboxy (COOH), C1-C4-alkyl, C1-C6-alkoxy, C1-C6-haloalkoxy, C1-C6-alkylthio, C1-C6-haloalkylthio, C1-C6-alkylsulfinyl, C1-C6-alkylsulfonyl, cyano, nitro, amino, N-mono- or N,N-di-C1-C6-alkylamino, C3-C6-cycloalkylamino, C1-C6-alkoxycarbonyl, C2-C6-alkylcarbonyl, C1-C6-alkylcarbonylamino, aminosulfonyl, N-mono- or N,N, di-C1-C4-alkylaminosulfonyl, a group —C(W′)NR9R10 or a radical Q′; or R7 and R8 together are a group ═C(R11)—NR12R13 or ═C(R11)—C(NH2)—OR12); or R7 and R8 together with the N-atom to which they are attached, form a 3- to 7-membered ring which optionally contains a further heteroatom selected from the group consisting of N, S and O, and which ring is further unsubstituted or mono- or polysubstituted by C1-C2-alkyl, C1-C2-haloalkyl, C1-C2-alkoxy, hydroxy, halogen, cyano, nitro, N,N-di-C1-C2-alkylaminomethyl or N,N-di-C1-C2-alkylaminocarbonylmethyl; Q and Q′ are each independently a C6-C10-aryl, an aliphatic or aromatic 4-, 5- or 6-membered heterocyclic ring, or an aliphatic or aromatic 8-, 9- or 10-membered fused hetero-bicyclic ring, each of them being unsubstituted or mono- or polysubstituted by halogen, hydroxy, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, C3-C6-cycloalkyl, C3-C6-cycloalkyl-C1-C2-alkyl, C1-C6-haloalkyl, C1-C6-alkoxy, C1-C6-haloalkoxy, C1-C6-alkylthio, C1-C6-alkylsulfinyl, C1-C6-alkylsulfonyl, cyano, nitro, amino, N-mono- or N,N-di-C1-C6-alkylamino, C3-C6-cycloalkylamino, COOH, C1-C6-alkoxycarbonyl, C2-C6-alkylcarbonyl, C1-C6-alkylcarbonylamino, aminocarbonyl, N-mono- or N,N-di-C1-C6-alkylaminocarbonyl, aminosulfonyl, N-mono- or N,N, di-C1-C4-alkylaminosulfonyl, unsubstituted or halogen- or nitro-substituted phenyl-C1-C4-alkyl, 5- or 6-membered heterocyclyl-C1-C4-alkyl or a radical Q″; Q″ is a C6-C10-carbocyclic ring or a 4-, 5- or 6-membered heterocyclic ring, each of them being aromatic or not, each of them being unsubstituted or mono- or polysubstituted by halogen, hydroxy, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, C3-C6-cycloalkyl, C1-C6-haloalkyl, C1-C6-alkoxy, C1-C6-haloalkoxy, C1-C6-alkylthio, C1-C6-alkylsulfinyl, C1-C6-alkylsulfonyl, cyano, nitro, amino, N-mono- or N,N-di-C1-C6-alkylamino, C3-C6-cycloalkylamino, COOH, C1-C6-alkoxycarbonyl, C2-C6-alkylcarbonyl, C1-C6-alkylcarbonylamino, aminocarbonyl, N-mono- or N,N-di-C1-C6-alkylaminocarbonyl, aminosulfonyl, or N-mono- or N,N, di-C1-C4-alkylaminosulfonyl; Q1 is a radicalwherein Z is O or CH2 and R14 is H, C1-C4-alkyl, or C1-C4-haloalkyl, R9 is H or C1-C6-alkyl; R10 is H, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, C3-C6-cycloalkyl, C4-C7-alkylcycloalkyl or C4-C7-cycloalkylalkyl, which is each unsubstituted or substituted in the alkyl, alkenyl, alkynyl or cycloalkyl moiety by halogen, cyano, nitro, hydroxy, carboxy (COOH), C1-C6-alkoxy, C1-C6-haloalkoxy, C1-C6-alkylthio, C1-C6-haloalkylthio, C1-C6 alkylsulfinyl, C1-C6-alkylsulfonyl, amino, N-mono- or N,N-di-C1-C6-alkylamino, C3-C6-cycloalkylamino, C1-C6-alkoxycarbonyl, C2-C6-alkylcarbonyl, C1-C6-alkylcarbonylamino, aminocarbonyl, N-mono- or N,N-di-C1-C6-alkylaminocarbonyl, aminosulfonyl, N-mono- or N,N, di-C1-C4-alkylaminosulfonyl or a radical Q″; R11 is H C1-C6-alkyl or C1-C6-alkoxy, and R12 and R13 are each independently of the other C1-C6-alkyl.
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