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AR061883A1 - Isoxazolinas sustituidas, composiciones farmaceuticas que las contienen, metodo de preparacion y usos en enfermedades causadas por aumento de la proliferacion celular. - Google Patents

Isoxazolinas sustituidas, composiciones farmaceuticas que las contienen, metodo de preparacion y usos en enfermedades causadas por aumento de la proliferacion celular.

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Publication number
AR061883A1
AR061883A1 ARP070103078A ARP070103078A AR061883A1 AR 061883 A1 AR061883 A1 AR 061883A1 AR P070103078 A ARP070103078 A AR P070103078A AR P070103078 A ARP070103078 A AR P070103078A AR 061883 A1 AR061883 A1 AR 061883A1
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Argentina
Prior art keywords
alkyl
nrac
ora
aryl
hydroxy
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ARP070103078A
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English (en)
Inventor
Dominic Brittain
Benjamin Bader
Philip Llenau
Gerhard Siemeister
Takayuki Tatamiya
Hilmar Weinmann
Christoph Huwe
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Bayer Schering Pharma Ag
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Publication of AR061883A1 publication Critical patent/AR061883A1/es

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Abstract

Reivindicacion 1: Un compuesto caracterizado porque responde a la formula general (1) en donde R1 representa un sustituyente seleccionado entre el grupo que comprende, y consiste preferentemente en un hidrogeno, sulfenilo, sulfinilo, sulfonilo, alquilo C1-6, alquilsulfenilo C1-6, alquilsulfinilo C1-6, alquilsulfonilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-10, heterocicloalquilo C3-10, haloalquilo C1-6, hidroxi C1-6-alquilo, arilo, heteroarilo, nitro, -C(=O)Ra, -C(=O)ORa, - C(=O)N(Ra)2, -C(=S)N(Ra)2, -S(=O)2Ra, -S(=O)2N(Ra)2, -P(=O)(ORa)2, en donde dicho sustituyente sulfenilo, sulfinilo, sulfonilo, alquilo C1-6, alquilsulfenilo C1-6, alquilsulfinilo C1-6, alquilsulfonilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-10, heterocicloalquilo C3-10, haloalquilo C1-6, hidroxi C1-6-alquilo, arilo, heteroarilo, nitro, -C(=O)Ra, -C(=O)ORa, -C(=O)N(Ra)2, -C(=S)N(Ra)2, -S(=O)2Ra, -S(=O)2N(Ra)2, -P(=O)(ORa)2, está a su vez opcionalmente sustituido, una o más veces, en la misma forma o en forma diferente, con R5; R2 y R3, en forma independiente entre sí, representan un sustituyente seleccionado entre el grupo que comprende, y consiste preferentemente en un átomo de hidrogeno o halogeno, ciano, hidroxi, mercapto, sulfenilo, sulfinilo, sulfonilo, amino, alquilo C1-6, alcoxi C1-6, alquiltio C1-6, alquilsulfenilo C1-6, alquilsulfinilo C1-6, alquilsulfonilo C1-6, alquilamino C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-10, heterocicloalquilo C3-10, haloalquilo C1-6, hidroxiC1-6-alquilo, arilo, ariloxi, heteroarilo, heteroariloxi, nitro, -C(=O)Ra, -C(=O)ORa, -C(=O)N(Ra)2, -C(=S)N(Ra)2, -NRaC(=O)ORa, -NRaC(=O)N(Ra)2, -NRaC(=O)Ra, -NRaC(=S)Ra, OC(=O)N(Ra)2, -NRaS(=O)2Ra, -S(=O)2Ra, -S(=O)2N(Ra)2, -P(=O)(ORa)2, -alquil C1-6-N(Ra)2, -alquil C1-6-C(=O)Ra, -alquil C1-6-C(=O)ORa, -alquil C1-6-C(=O)N(Ra)2, -alquil C1-6-C(=S)N(Ra)2, alquil C1-6-NRaC(=O)ORa, -alquil C1-6-NRaC(=O)N(Ra)2, -alquil C1-6-NRaC(=S)N(Ra)2, -alquil C1-6-NRaC(=O)Ra, -alquil C1-6-NRaC(=S)Ra, -alquil C1-6-OC(=O)N(Ra)2, -alquil-NRaS(=O)2Ra, -alquil C1-6-S(=O)2Ra, -alquil C1-6-S(=O)2N(Ra)2, -alquil C1-6-P(=O)(ORa)2, en donde dicho sustituyente hidroxi, mercapto, sulfenilo, sulfinilo, sulfonilo, amino, alquilo C1-6, alcoxi C1-6, alquiltio C1-6, alquilsulfenilo C1-6, alquilsulfinilo C1-6, alquilsulfonilo C1-6, alquilamino C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-10, heterocicloalquilo C3-10, haloalquilo C1-6, hidroxiC1-6- alquilo, arilo, ariloxi, heteroarilo, heteroariloxi, nitro, -C(=O)Ra, -C(=O)ORa, -C(=O)N(Ra)2, -C(=S)N(Ra)2, -NRaC(=O)ORa, -NRaC(=O)N(Ra)2, -NRaC(=O)Ra, -NRaC(=S)Ra, OC(=O)N(Ra)2, -NRaS(=O)2Ra, -S(=O)2Ra, -S(=O)2N(Ra)2, -P(=O)(ORa)2, -alquil C1-6- N(Ra)2, -alquil C1-6-C(=O)Ra, -alquil C1-6-C(=O)ORa, -alquil C1-6-C(=O)N(Ra)2, -alquil C1-6-C(=S)N(Ra)2, alquil C1-6-NRaC(=O)ORa, -alquil C1-6-NRaC(=O)N(Ra)2, -alquil C1-6-NRaC(=S)N(Ra)2, -alquil C1-6-NRaC(=O)Ra, -alquil C1-6-NRaC(=S)Ra, -alquil C1- 6-OC(=O)N(Ra)2, -alquil-NRaS(=O)2Ra, -alquil C1-6-S(=O)2Ra, -alquil C1-6-S(=O)2N(Ra)2, -alquil C1-6-P(=O)(ORa)2, está a su vez opcionalmente sustituido, una o más veces, en la misma forma o en forma diferente, con R5; o juntos forman un cicloalquilo C3-10 o heterocicloalquilo C3-10; A representa un grupo arilo o heteroarilo; X representa, en forma independiente en cada caso, un sustituyente seleccionado entre el grupo que comprende, y consiste preferentemente en un átomo de hidrogeno, fluor, cloro, bromo, y yodo, en donde al menos un sustituyente X es un átomo de fluor; en donde: dicho grupo -(CX2)nCX3 está a su vez opcionalmente sustituido, una o más veces, en la misma forma o en forma diferente, con R5; Z representa un grupo alquenilo C2-6, que está a su vez opcionalmente sustituido, una o más veces, en la misma forma o en forma diferente, con R5; R4 representa un sustituyente seleccionado entre el grupo que comprende, y consiste preferentemente en un átomo de hidrogeno o halogeno, ciano, hidroxi, mercapto, sulfenilo, sulfinilo, sulfonilo, amino, alquilo C1-6, alcoxi C1-6, alquiltio C1-6, alquilsulfenilo C1-6, alquilsulfinilo C1-6, alquilsulfonilo C1-6, alquilamino C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-10, heterocicloalquilo C3-10, haloalquilo C1-6, hidroxiC1-6-alquilo, arilo, ariloxi, heteroarilo, heteroariloxi, nitro, -C(=O)Ra, -C(=O)ORa, -C(=O)N(Ra)2, -C(=S)N(Ra)2, -NRaC(=O)ORa, -NRaC(=O)N(Ra)2, -NRaC(=O)Ra, -NRaC(=S)Ra, OC(=O)N(Ra)2, - NRaS(=O)2Ra, -S(=O)2Ra, -S(=O)2N(Ra)2, -P(=O)(ORa)2, -alquil C1-6-N(Ra)2, -alquil C1-6-C(=O)Ra, -alquil C1-6-C(=O)ORa, -alquil C1-6-C(=O)N(Ra)2, -alquil C1-6-C(=S)N(Ra)2, alquil C1-6-NRaC(=O)ORa, -alquil C1-6-NRaC(=O)N(Ra)2, -alquil C1-6- NRaC(=S)N(Ra)2, -alquil C1-6-NRaC(=O)Ra, -alquil C1-6-NRaC(=S)Ra, -alquil C1-6-OC(=O)N(Ra)2, -alquil-NRaS(=O)2Ra, -alquil C1-6-S(=O)2Ra, -alquil C1-6-S(=O)2N(Ra)2, -alquil C1-6-P(=O)(ORa)2, en donde dicho sustituyente hidroxi, mercapto, sulfenilo, sulfinilo, sulfonilo, amino, alquilo C1-6, alcoxi C1-6, alquiltio C1-6, alquilsulfenilo C1-6, alquilsulfinilo C1-6, alquilsulfonilo C1-6, alquilamino C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-10, heterocicloalquilo C3-10, haloalquilo C1- 6, hidroxiC1-6-alquilo, arilo, ariloxi, heteroarilo, heteroariloxi, nitro, -C(=O)Ra, -C(=O)ORa, -C(=O)N(Ra)2, -C(=S)N(Ra)2, -NRaC(=O)ORa, -NRaC(=O)N(Ra)2, -NRaC(=O)Ra, -NRaC(=S)Ra, OC(=O)N(Ra)2, -NRaS(=O)2Ra, -S(=O)2Ra, -S(=O)2N(Ra)2, -P(=O)(ORa)2, - alquil C1-6-N(Ra)2, -alquil C1-6-C(=O)Ra, -alquil C1-6-C(=O)ORa, -alquil C1-6-C(=O)N(Ra)2, -alquil C1-6-C(=S)N(Ra)2, alquil C1-6-NRaC(=O)ORa, -alquil C1-6-NRaC(=O)N(Ra)2, -alquil C1-6-NRaC(=S)N(Ra)2, -alquil C1-6-NRaC(=O)Ra, -alquil C1-6-NRaC(=S)Ra, -alquil C1-6-OC(=O)N(Ra)2, -alquil-NRaS(=O)2Ra, -alquil C1-6-S(=O)2Ra, -alquil C1-6-S(=O)2N(Ra)2, -alquil C1-6-P(=O)(ORa)2, está a su vez opcionalmente sustituido, una o más veces, en la misma forma o en forma diferente, con R5; R5 representa un sustituyente seleccionado entre el grupo que comprende, y consiste preferentemente en un átomo de hidrogeno o halogeno, ciano, hidroxi, mercapto, sulfenilo, sulfinilo, sulfonilo, amino, alquilo C1-6, alcoxi C1-6, alquiltio C1-6, alquilsulfenilo C1- 6, alquilsulfinilo C1-6, alquilsulfonilo C1-6, alquilamino C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-10, heterocicloalquilo C3-10, haloalquilo C1-6, hidroxiC1-6-alquilo, arilo, ariloxi, heteroarilo, heteroariloxi, nitro, -C(=O)Ra, - C(=O)ORa, -C(=O)N(Ra)2, -C(=S)N(Ra)2, -NRaC(=O)ORa, -NRaC(=O)N(Ra)2, -NRaC(=O)Ra, -NRaC(=S)Ra, OC(=O)N(Ra)2, -NRaS(=O)2Ra, -S(=O)2Ra, -S(=O)2N(Ra)2, -P(=O)(ORa)2, en donde dicho sustituyente hidroxi, mercapto, sulfenilo, sulfinilo, sulfonilo, amino, alquilo C1-6, alcoxi C1-6, alquiltio C1-6, alquilsulfenilo C1-6, alquilsulfinilo C1-6, alquilsulfonilo C1-6, alquilamino C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-10, heterocicloalquilo C3-10, haloalquilo C1-6, hidroxiC1-6-alquilo, arilo, ariloxi, heteroarilo, heteroariloxi, nitro, -C(=O)Ra, -C(=O)ORa, -C(=O)N(Ra)2, -C(=S)N(Ra)2, -NRaC(=O)ORa, -NRaC(=O)N(Ra)2, -NRaC(=O)Ra, -NRaC(=S)Ra, OC(=O)N(Ra)2, -NRaS(=O)2Ra, -S(=O)2Ra, -S(=O)2N(Ra)2, -P(=O)(ORa)2 está a su vez opcionalmente sustituido, una o más veces, en la misma forma o en forma diferente con Rb; Ra representa, en forma independiente en cada caso, un sustituyente, que es idéntico o diferente, seleccionado entre el grupo que comprende, y consiste preferentemente en un átomo de hidrogeno o halogeno, ciano, hidroxi, mercapto, sulfenilo, sulfinilo, sulfonilo, amino, alquilo C1-6, alcoxi C1-6, alquiltio C1-6, alquilsulfenilo C1-6, alquilsulfinilo C1-6, alquilsulfonilo C1-6, alquilamino C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-10, heterocicloalquilo C3-10, haloalquilo C1-6, hidroxiC1-6-alquilo, arilo, ariloxi, heteroarilo, heteroariloxi, nitro, -C(=O)Rb, -C(=O)ORb, -C(=O)N(Rb)2, -C(=S)N(Rb)2, -NRbC(=O)ORb, -NRbC(=O)N(Rb)2, - NRbC(=O)Rb, -NRbC(=S)Rb, OC(=O)N(Rb)2, -NRbS(=O)2Rb, -S(=O)2Rb, -S(=O)2N(Rb)2, -P(=O)(ORb)2, en donde dicho sustituyente hidroxi, mercapto, sulfenilo, sulfinilo, sulfonilo, amino, alquilo C1-6, alcoxi C1-6, alquiltio C1-6, alquilsulfenilo C1-6, alquilsulfinilo C1-6, alquilsulfonilo C1-6, alquilamino C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-10, heterocicloalquilo C3-10, haloalquilo C1-6, hidroxiC1-6-alquilo, arilo, ariloxi, heteroarilo, heteroariloxi, está a su vez opcionalmente sustituido, una o más veces, en la misma forma o en forma diferente con Rb; Rb representa, en forma independiente en cada caso, un sustituyente, que es idéntico o diferente, seleccionado entre el grupo que comprende, y consiste preferentemente en un átomo de hidrogeno o halogeno, ciano, -Orc, -N(Rc)2, -SRc, -S(=O)Rc, S(=PO)ORc, S(=O)2Rc, -S(=O)2ORc, alquilo C1-6, alcoxi C1-6, alquiltio C1-6, alquilsulfenilo C1-6, alquilsulfinilo C1-6, alquilsulfonilo C1-6, alquilamino C1- 6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-10, heterocicloalquilo C3-10, haloalquilo C1-6, hidroxiC1-6-alquilo, arilo, ariloxi, heteroarilo, heteroariloxi, nitro, -C(=O)Rc, -C(=O)ORc, -C(=O)N(Rc)2, -C(=S)N(Rc)2, -NRcC(=O)ORc, - NRcC(=O)N(Rc)2, -NRcC(=O)Rc, -NRcC(=S)Rc, OC(=O)N(Rc)2, -NRcS(=O)2Rc, -S(=O)2N(Rc)2, -P(=O)(ORc)2, Rc representa, en forma independiente en cada caso, un sustituyente, que es idéntico o diferente, seleccionado entre el grupo que comprende, y consiste preferentemente en un H, arilo y alquilo C1-6, n representa un entero entre 0, 1, 2, 3, 4, 5, o 6; m representa un entero entre 0, 1, 2, 3, 4, o 5; y p representa un entero entre 0, 1, 2, 3, 4, o 5; con la salvedad de que en dicho compuesto de formula general (1) , cuando R1 es un átomo de hidrogeno; R2 es un átomo de hidrogeno; R3 es un átomo de cloro; X es un átomo de fluor; n = 0; p = 0; A es un grupo fenilo sustituido con R4; m = 3; uno de dichos sustituyentes R4 es un átomo de cloro, o un grupo nitrilo en la posicion para- respecto del átomo de carbono que lleva la isoxazolina; entonces otro de dichos sustituyentes R4 no es un átomo de fluor en la p
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JP2005539001A (ja) * 2002-08-02 2005-12-22 アージェンタ・ディスカバリー・リミテッド ヒストンデアセチラーゼインヒビターとしての置換チエニルヒドロキサム酸
CN100409748C (zh) * 2002-09-28 2008-08-13 王正权 取代苯基异噁唑类除草剂

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JP2009542752A (ja) 2009-12-03
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