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AR054621A1 - 1-aril-4-ciclopropilpirazoles sustituidos - Google Patents

1-aril-4-ciclopropilpirazoles sustituidos

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Publication number
AR054621A1
AR054621A1 ARP060102525A ARP060102525A AR054621A1 AR 054621 A1 AR054621 A1 AR 054621A1 AR P060102525 A ARP060102525 A AR P060102525A AR P060102525 A ARP060102525 A AR P060102525A AR 054621 A1 AR054621 A1 AR 054621A1
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AR
Argentina
Prior art keywords
alkyl
cycloalkyl
halogenoalkyl
amino
nrcrd
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ARP060102525A
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English (en)
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Pfizer Ltd
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    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D231/38—Nitrogen atoms
    • A—HUMAN NECESSITIES
    • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01N—PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTS THEREOF; BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES OR AS HERBICIDES; PEST REPELLANTS OR ATTRACTANTS; PLANT GROWTH REGULATORS
    • A01N53/00—Biocides, pest repellants or attractants, or plant growth regulators containing cyclopropane carboxylic acids or derivatives thereof
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
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    • C07D231/16—Halogen atoms or nitro radicals
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    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D231/18—One oxygen or sulfur atom
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    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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Abstract

Composiciones que comprenden dichos compuestos, y a su uso como parasiticidas. Reivindicacion 1:Un compuesto de formula (1):en la que X se selecciona de CR10 o N; R1 se selecciona de halogeno, ciano, hidroxi, alquilo C1-6, alcoxi C1-6, alcanoilo C1- 6, halogenoalquilo C1-6, halogenoalcoxi C1-6, halogenoalcanoilo C1-6, amino, alquil(C1-6)amino, di-alquil(C1-6)amino, het, fenilo, SF5 y S(O)nR11; R2 se selecciona de ciano, hidroxi, C(O)OH, het, fenilo, S(O)nR11, C(O)NRaRb y C(S)NRaRb; o R2 se selecciona de cicloalquilo C3-8, cicloalquil(C3-8)-alquilo(C1-6), alquenilo C2-6, alquinilo C2-6, alcanoilo C1-6, C(O)O-alquilo(C1-6), amino, alquil(C1-6)-amino, y di-alquil(C1-6)-amino, cada uno de los cuales puede estar además opcional e independientemente sustituido con uno o más sustituyentes seleccionados, cuando sea químicamente posible, de ciano, nitro, halogeno, oxo, hidroxi, C(O)OH, C(O)NRcRd, NRcC(O)Rd, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-8, cicloalquil (C3-8)-alquilo(C1-6), cicloalquil (C3-8)-halogenoalquilo(C1-6), alcoxi C1-6, alcanoilo C1-6, -C(O)O-alquilo(C1-6), halogenoalquilo C1-6, halogenocicloalquilo C3-8, halogenoalcoxi C1-6, halogenoalcanoilo C1-6, -C(O)O-halogenoalquilo C1-6, amino, NRcRd, het, fenilo y S(O)nR11; Ra y Rb se seleccionan independientemente de hidrogeno, het, fenilo, y S(O)nR11; o bien uno o ambos de Ra y Rb se seleccionan independientemente de alquilo C1-6, alquenilo C2-6, cicloalquilo C3-6, cicloalquil(C3- 8)-alquilo(C1-6), alcanoilo C1-6, y C(O)O-alquilo(C1-6), y cada uno de Ra o Rb puede estar además opcional e independientemente sustituido con uno o más sustituyentes seleccionados, cuando sea químicamente posible, de ciano, nitro, halogeno, oxo, hidroxi, C(O)OH, C(O)NRcRd, NRcC(O)Rd, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-8, cicloalquil (C3-9)-alquilo(C1-6), cicloalquil(C3-8)-halogenoalquilo(C1-6), alcoxi C1-6, alcanoilo C1-6, -C(O)O-alquilo(C1-6), halogenoalquilo C1- 6, halogenocicloalquilo C3-8, halogenoalcoxi C1-6, halogenoalcanoilo C1-6, -C(O)O-halogenoalquilo(C1-6), amino, NRcRd, het, fenilo y S(O)nR11; o Ra y Rb junto con el átomo de N al que están unidos pueden formar un anillo heterocíclico saturado, parcialmente saturado, insaturado o aromático, de tres a siete miembros, que puede contener opcionalmente uno o más átomos adicionales N, O o S y que puede estar además opcionalmente sustituido con uno o más sustituyentes seleccionados, cuando sea químicamente posible de ciano, nitro, halogeno, oxo, hidroxi, C(O)OH, C(O)NRcRd, NRcC(O)Rd, alquilo C2-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-8, cicloalquil(C3-8)-alquilo(C1-6), cicloalquil(C3-8)-halogenoalquilo(C1-6), alcoxi C1-6, alcanoilo C1-6, -C(O)O-alquilo(C1-6), halogenoalquilo C1-6, halogenocicloalquilo C3-8, halogenoalcoxi C1-6, halogenoalcanoilo C1-6, -C(O)O-halogenoalquilo(C1-6), amino, NRcRd, het, fenilo y S(O)nR11; o R2 y Re junto con el átomo de N al que está unido Re pueden formar un anillo heterocíclico saturado, parcialmente saturado o insaturado, de seis a siete miembros, que puede contener opcionalmente uno o más átomos adicionales N, O o S, y que puede estar además opcionalmente sustituido con uno o más sustituyentes seleccionados, cuando sea químicamente posible, de ciano, nitro, halogeno, oxo, hidroxi, C(O)OH, C(O)NRcRd, NRcC(O)Rd, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-8, cicloalquil(C3-8)-alquilo(C1-6), cicloalquil(C3-8)-halogenoalquilo(C1-6), alcoxi C1-6, alcanoilo C1-6, -C(O)O-alquilo(C1-6), halogenoalquilo C1-6, halogenocicloalquilo C3-8, halogenoalcoxi C1-6, halogenoalcanoilo C1-6, -C(O)O-halogenoalquilo(C1-6), amino, NRcRd, het, fenilo y S(O)nR11; R3, R4, R5 y R6 se seleccionan independientemente de hidrogeno, halogeno, ciano, hidroxi, C(O)OH, nitro, fenilo, y S(O)nR11; o bien uno o más de R3, R4, R5 y R6 se seleccionan independientemente de alquilo C1-4, C(O)NRcRd, C(S)NRcRd, alcoxi C1-4, alcanoilo C1-4, C(O)O-alquilo(C1-4), amino, R3, R4, R5 y R6 que pueden estar además opcional e independientemente sustituidos con uno o más sustituyentes seleccionados, cuando sea químicamente posible, de ciano, nitro, halogeno, hidroxi, alquilo C1-4 y amino; y donde no más de dos de R3, R4, R5 y R6 se seleccionan de ciano, hidroxi, C(O)OH, nitro, fenilo, S(O)nR11, C(O)NRcRd, C(S)NRcRd, alcoxi C1-4, alcanoilo C1-4, C(O)O-alquilo(C1-4) y amino; R7 se selecciona de halogeno, alquilo C1-6 y alcoxi C1-6, en el que cuando R7 es alquilo C1-6 o alcoxi C1-6, R7 puede estar opcionalmente sustituido con uno o más sustituyentes halogeno; R8 se selecciona de hidrogeno, ciano, hidroxi, C(O)OH, nitro, halogeno, het, fenilo y S(O)nR11; o R8 se selecciona de alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-8, cicloalquil (C3-8)-alquilo(C1-6), alcoxi C1-6, alcanoilo C1-6, y C(O)O-alquilo(C1-6), R8 que puede estar además opcional e independientemente sustituido con uno o más sustituyentes seleccionados, cuando sea químicamente posible, de ciano, nitro, halogeno, oxo, hidroxi, C(O)OH, C(O)NRcRd, NRcC(O)Rd, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-8, cicloalquil (C3-8)-alquilo(C1-6), cicloalquil(C3-8)-halogenoalquilo(C1-6), alcoxi C1-6, alcanoilo C1-6, -C(O)O-alquilo(C1-6), halogenoalquilo C1-6, halogenocicloalquilo C3-8, halogenoalcoxi C1-6, halogenoalcanoilo C1-6, -C(O)O-halogenoalquilo(C1-6), amino, NRcRd, het, fenilo y S(O)nR11; o R8 es amino, R8 que puede estar además opcional e independientemente sustituido con uno o más sustituyentes seleccionados, cuando sea químicamente posible de C(O)OH, C(O)NRcRd, NRcC(O)Rd, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-8, cicloalquil(C3-8)-alquilo(C1-6), cicloalquil(C3-8)-halogenoalquilo(C1-6), alcoxi C1-6, alcanoilo C1-6, -C(O)O-alquilo(C1-6), halogenoalquilo C1-6, halogenocicloalquilo C3-8, halogenoalcoxi C1-6, halogenoalcanoilo C1-6, -C(O)O- halogenoalquilo(C1-6), het, fenilo y S(O)nR11; R9 se selecciona de hidrogeno, halogeno, ciano, hidroxi, C(O)OH, nitro, het, fenilo, S(O)nR11 y NReRf; o R9 se selecciona de alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-8, cicloalquil(C3-8)-alquilo(C1-6), alcoxi C1-6, cicloalquil(C3-8)-alcoxi(C1-6), alcanoilo C1-6, C(O)O-alquilo(C1-6), R9 que puede estar además opcional e independientemente sustituido con uno o más sustituyentes seleccionados, cuando sea químicamente posible, de ciano, nitro, halogeno, oxo, hidroxi, C(O)OH, C(O)NRcRd, NRcC(O)Rd, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-8, cicloalquil (C3-8)-alquilo(C1-6), cicloalquil (C3-8)-halogenoalquilo(C1-6), alcoxi C1-6, alcanoilo C1-6, -C(O)O-alquilo(C1-6), halogenoalquilo C1-6, halogenocicloalquilo C3-8, halogenoalcoxi C1-6, halogenoalcanoilo C1-6, -C(O)O-halogenoalquilo(C1-6), amino, NRcRd, het, fenilo y S(O)nR11; Re y Rf se seleccionan independientemente de hidrogeno, het, fenilo y S(O)nR11; o bien uno o ambos de Re y Rf se seleccionan independientemente de alquilo C1-6, alquenilo C2-6, cicloalquilo C3-8, cicloalquil(C3-8)-alquilo(C1-6), alcanoilo C1-6, C(O)O-alquilo(C1-6), -C(O)O-alquil(C1-6)-cicloalquilo(C3-8), - C(O)O-cicloalquilo(C3-6), y cada uno de Re o Rf puede estar además opcional e independientemente sustituido con uno o más sustituyentes seleccionados, cuando sea químicamente posible, de ciano, nitro, halogeno, oxo, hidroxi, C(O)OH, C(O)NRcRd, NRcC(O)Rd, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-8, cicloalquil (C3-8)-alquilo(C1-6), cicloalquil(C3-8)-halogenoalquilo(C1-6), alcoxi C1-6, alcanoilo C1-6, -C(O)O-alquilo(C1-6), halogenoalquilo C1-6, halogenocicloalquilo C3- 8, halogenoalcoxi C1-6, halogenoalcanoilo C1-6, -C(O)O-halogenoalquilo(C1-6), amino, NRcRd, het, fenilo y S(O)nR11; o Re y Rf junto con el átomo de N al que están unidos pueden formar un anillo heterocíclico saturado, parcialmente saturado, insaturado o aromático, de tres a siete miembros, que puede contener opcionalmente uno o más átomos adicionales N, O o S y que puede estar además opcionalmente sustituido con uno o más sustituyentes seleccionados, cuando sea químicamente posible de ciano, nitro, halogeno, oxo, hidroxi, C(O)OH, C(O)NRcRd, NRcC(O)Rd, alquilo C2-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-8, cicloalquil (C3-8)-alquilo(C1-6), cicloalquil(C3-8)-halogenoalquilo(C1-6), alcoxi C1-6, alcanoilo C1-6, -C(O)O- alquilo(C1-6), halogenoalquilo C1-6, halogenocicloalquilo C3-8, halogenoalcoxi C1-6, halogenoalcanoilo C1-6, -C(O)O-halogenoalquilo(C1-6), amino, NRcRd, het, fenilo y S(O)nR11; o Re y R2 junto con los átomos a los que están unidos pueden formar un anillo heterocíclico de seis a siete miembros como se ha descrito previamente; R10 se selecciona de halogeno, alquilo C1-6 y alcoxi C1-6 y en el que cuando R10 es alquilo C1-6 o alcoxi C1-6 puede estar opcionalmente sustituido con uno o más sustituyentes halogeno; cada uno de Rc y Rd se selecciona independientemente de hidrogeno, alquilo C1-6, alquenilo C2-6, cicloalquilo C3-8, cicloalquil(C3-8)-alquilo(C1-6), halogenoalquilo C1-6, cicloalquil (C3-8)-halogenoalquilo(C1-6), alcanoilo C1- 6, halogenoalcanoilo C1-6, C(O)O-alquilo(C1-6), het, fenilo y S(O)nR11; o Rc y Rd junto con el átomo de N al que está unido al menos uno de ellos, pueden formar un anillo heterocíclico saturado, parcialmente saturado, insaturado o aromático, de tres a siete miembros, que puede contener opcionalmente uno o más átomos N, O o S; cada n es independientemente 0, 1 o 2; cada R11 se selecciona independientemente de hidrogeno, hidroxi, alquilo C1-6, halogenoalquilo C1-6, amino, alquil (C1-6)-amino y di- alquil(C1-6)-amino; cada fenilo puede estar opcionalmente sustituido con uno o más sustituyentes adicionales seleccionados del grupo que consiste en halogeno, ciano, nitro, hidroxi, alquilo C1-6, halogenoalquilo C1-6, alcoxi C1-6, halogenoalcoxi C1- 6, amino, alquil(C1-6)-amino, di-alquil(C1-6)-amino, -NHS(O)nR11, y S(O)nR11; y cada het representa de forma independiente un anillo heterocíclico de cuatr
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