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AR054631A1 - DERIVADOS DE L-ALFA-GLUTAMINA COMO INHIBIDORES DE GLUTAMATO AGRECANASA, INTERMEDIARIOS Y MÉTODOS DE SíNTESIS DE LOS MISMOS Y COMPOSICIONES FARMACÉUTICAS QUE LOS CONTIENEN. - Google Patents

DERIVADOS DE L-ALFA-GLUTAMINA COMO INHIBIDORES DE GLUTAMATO AGRECANASA, INTERMEDIARIOS Y MÉTODOS DE SíNTESIS DE LOS MISMOS Y COMPOSICIONES FARMACÉUTICAS QUE LOS CONTIENEN.

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Publication number
AR054631A1
AR054631A1 ARP060102979A ARP060102979A AR054631A1 AR 054631 A1 AR054631 A1 AR 054631A1 AR P060102979 A ARP060102979 A AR P060102979A AR P060102979 A ARP060102979 A AR P060102979A AR 054631 A1 AR054631 A1 AR 054631A1
Authority
AR
Argentina
Prior art keywords
aryl
heteroaryl
alkyl
cycloalkyl
alkenyl
Prior art date
Application number
ARP060102979A
Other languages
English (en)
Original Assignee
Wyeth Corp
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Wyeth Corp filed Critical Wyeth Corp
Publication of AR054631A1 publication Critical patent/AR054631A1/es

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    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
    • C07D213/82—Amides; Imides in position 3
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    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/54—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/56—Amides
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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
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Abstract

Estos compuestos son inhibidores de metaloproteinasa. Reivindicacion 1: Un compuesto de la Formula (1), o una sal del mismo, farmacéuticamente aceptable, caracterizado porque W es -C(O)-, -OC(O)-, -NHC(O)-, -C(O)O-, o -C(O)NH-; R1 es fenilo, heteroarilo, bifenilo, arilo bicíclico, arilo tricíclico, heteroarilo bicíclico, o heteroarilo tricíclico, cada uno opcionalmente sustituido con uno o más de R5 o R6, y cuando R1 es sustituido con uno más de R5 o R6, los sustituyentes pueden ser idénticos o diferentes; R2 es hidrogeno, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, -(CH2)nR11, -OH, o alquilo -O-C1-6; R3 es CO2H, -CONH2, -CONHOH, -CONHSO2R7, tetrazol, -SO2NHR7, -SO3H, -PO(OH)NH2, -PO(OH)OR7, -CONHR7, -COOR7, un grupo mimético de ácido, o un heteroarilo o heterocicloalquilo de 5 o 6 elementos, que contiene 1 a 4 heteroátomos seleccionados de O, N, S; R4 es-CO2H, -CONH2, - (CH2)nOR7, o -CONR9R10; R5 es arilo, heteroarilo, -(CH2)n-arilo, -(CH2)n-heteroarilo, -O-arilo, -O- heteroarilo, -S-arilo, -S-heteroarilo, -NH-arilo, -NH-heteroarilo, -CO-alquilo C1-6, -CO-arilo, -CO-heteroarilo, -SO2-alquilo C1-6, -SO2-arilo, -SO2-heteroarilo, -SO2NH-arilo, -SO2NH-heteroarilo, -NHSO2-alquilo C1-6, -NHSO2-arilo, -NHSO2- heteroarilo, -NHCO-arilo, -NHCO-heteroarilo, -CONH-arilo, -CONH-heteroarilo, alquilo C1-6, -O-alquilo C1-6, -S-alquilo C1-6, -NR-alquilo C1-6, -NHCO-alquilo C1-6, -CONH alquilo C1-6, -O-cicloalquilo C3-6, -S-cicloalquilo C3-6, -NH-cicloalquilo C3-6, -NHCO-cicloalquilo C3-6 o -CONH-cicloalquilo C3-6; cada alquilo, arilo, cicloalquilo o heteroarilo, opcionalmente sustituido con uno o más de R6, y cuando R5 es sustituido con más de un R6, los sustituyentes pueden ser idénticos o diferentes; R6 y R12 son cada uno independientemente, hidrogeno, halogeno, -CN, -OCF3, -CF3, -NO2, -OH, -SH, -NR7R8, -CONR7R8, NR8COR7, NR8CO2R7, -CO2R7, -COR7-, -SO2-alquilo C1-6, -SO2-arilo, -SO2-heteroarilo, SO2R7, NR7SO2R8, SO2NR7R8; alquilo C1-6, -O-alquilo C1- 6, -S-alquilo C1-6, -NH-alquilo C1-6, -NHCO-alquilo C1-6, -CONH-alquilo C1-6, -O-cicloalquilo C3-6, -S-cicloalquilo C3-6, -NH-cicloalquilo C3-6, -NHCO-cicloalquilo C3-6. -CONH-cicloalquilo C3-6, heterocicloalquilo, -alquilo C1-6-OR7, alquinilo C2-6, alquenilo C2-6, -O-alquil-cicloalquilo C3-6, -O-alquenilo, -O-alquilo C1-6 sustituido con arilo, arilo, heteroarilo, -(CH2)n-arilo, -(CH2)n-heteroarilo, -O-arilo, -O-heteroarilo, -S-arilo, o - S-heteroarilo; cada alquilo, arilo, cicloalquilo, heterocicloalquilo, heteroarilo, alquenilo o alquinilo, opcionalmente sustituido con uno o más de R13; R7 y R8 son cada uno independientemente hidrogeno, alquilo C1-6, arilo, heteroarilo, alquenilo C2-6, alquinilo C2-6, cicloalquilo, -(CH2)n-arilo, o -(CH2)n-heteroarilo; o R7 y R8 junto con el átomo al cual están unidos, pueden formar un grupo cíclico de cinco a siete elementos que contiene hasta 3 heteroátomos seleccionados entre N, O, o S; R9 y R10 son cada uno independientemente hidrogeno, alquilo C1-6, alquilo C1-6-OH, alquilo C1-6-O-alquilo C1-6, arilo, cicloalquilo, heteroarilo, alquenilo C2-6, alquinilo C2-6, arilo bicíclico, arilo tricíclico, heteroarilo bicíclico o heteroarilo tricíclico, cada alquilo, arilo, cicloalquilo o heteroarilo, opcionalmente sustituido con uno o más de R12; o R9 y R10 juntos pueden formar un grupo cíclico de cinco a siete elementos que contienen hasta 3 heteroátomos seleccionados de N, O o S; R11 es arilo, heteroarilo o cicloalquilo; R13 es halogeno, -O-alquilo C1-6, -CO2H, -OH, -CF3. hidrogeno, alquilo C1-6, arilo, heteroarilo, alquenilo C2-6, alquinilo C1-6, cicloalquilo, cicloalquilo sustituido con -OH, arilo sustituido con -NH2, arilo sustituido con -O-alquilo C1-6, -(CH2)n-arilo, o -(CH2)n-heteroarilo; m es 0 - 4; n es 0 - 4; y p es 0 - 2. Reivindicacion 20: Un compuesto de formula (2); o una sal del mismo farmacéuticamente aceptable, caracterizado porque R1 es fenilo, heteroarilo, bifenilo, arilo bicíclico, arilo tricíclico, heteroarilo bicíclico, o heteroarilo tricíclico, cada uno opcionalmente sustituido con uno o más de R5 o R6, y cuando R1 es sustituido con uno más de R5 o R6, los sustituyentes pueden ser idénticos o diferentes. R2 es hidrogeno, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, -(CH2)n-R11, -OH, o alquilo -O-C1-6; R5 es arilo, heteroarilo, -(CH2)n-arilo, -(CH2)n-heteroarilo, -O-arilo, -O--heteroarilo, -S-arilo, -S- heteroarilo, -NH-arilo, -NH-heteroarilo, -CO-alquilo C1-6, -CO-arilo, - CO-heteroarilo, -SO2-alquilo C1-6, -SO2- arilo, -SO2-heteroarilo, -SO2NH-arilo, -SO2NH-heteroarilo, -NHSO2-alquilo C1-6, -NHSO2-arilo, -NHSO2-heteroarilo, -NHCO-arilo, -NHCO--heteroarilo, -CONH-arilo, -CONH-heteroarilo, alquilo C1-6, -O-alquilo C1- 6, -S-alquilo C1-6, -NH-alquilo C1-6 , -NHCO-alquilo C1-6, CONH-alquilo C1-6, -O-cicloalquilo C3-6, -S-cicloalquilo C3-6 , -NH-cicloalquilo C3-6, -NHCO-cicloalquilo C3-6, o -CONH-cicloalquilo cada alquilo, arilo, cicloalquilo o heteroarilo, opcionalmente sustituido con uno o más de R6, y cuando R5 es sustituido con más de un R6, los sustituyentes pueden ser idénticos o diferentes; R6 y R12 son cada uno independientemente, hidrogeno, halogeno, -CN, -OCF3, -CF3, -NO2, -OH, -SH, -NR7R8, - CONR7R8, NR8COR7, NR8CO2R7, -CO2R7, -COR7, -SO2-alquilo C1-6, -SO2- arilo, -SO2-heteroarilo, SO2R7, NR7SO2R8, SO2NR7R8 alquilo C1-6 , -O-alquilo C1-6, -S-alquilo C1-6, -NH-alquilo C1-6, -NHCO-alquilo C1-6, -CONH-alquilo C1-6, -O-cicloalquilo C3-6, - S-cicloalquilo C3-6, -NH-cicloalquilo C3-6, -NHCO- cicloalquilo C3-6, -CONH-cicloalquilo C3-6, heterocicloalquilo, -alquilo C1-6-OR7, alquinilo C2-6, alquenilo C2-6, -O-alquil-cicloalquilo C3-6, -O-alquenilo, -O-alquilo C1-6 sustituido con arilo, arilo, heteroarilo, -(CH2)n-arilo, -(CH2)n-heteroarilo, -O-arilo, -O-heteroarilo, -S-arilo, o -S-heteroarilo; cada alquilo, arilo, cicloalquilo, heterocicloalquilo, heteroarilo, alquenilo o alquinilo, opcionalmente sustituido con uno o más de R13; R7 y R8 son cada uno independientemente hidrogeno, alquilo C1-6, arilo, heteroarilo, alquenilo C2-6, alquinilo C2-6, cicloalquilo, -(CH2)n-arilo, o -(CH2)n-heteroarilo; o R7 y R8 junto con el átomo al cual están unidos, pueden formar un grupo cíclico de cinco a siete elementos que contiene hasta 3 heteroátomos seleccionados entre N, O, o S; R11 es arilo, heteroarilo o cicloalquilo; R13 es halogeno, -O-alquilo C1-6, -CO2H, -OH, - CF3, hidrogeno, alquilo C1-6, arilo, heteroarilo, alquenilo C2-6, alquinilo C2-6, cicloalquilo, cicloalquilo sustituido con -OH, arilo sustituido con -NH2, arilo sustituido con -O-alquilo C1-6, -(CH2)n-arilo, o -(CH2)n-heteroarilo; R14 y R15 son cada uno independientemente hidrogeno, alquilo C1-6, arilo, heteroarilo, alquenilo C2-6, alquinilo C2-6, cicloalquilo, heterocicloalquilo, -(CH2)n-arilo, arilo bicíclico, arilo tricíclico, heteroarilo bicíclico o heteroarilo tricíclico, cada alquilo, arilo, cicloalquilo o heteroarilo, opcionalmente sustituido con uno o más de R12; o R14 y R15 juntos pueden formar un grupo cíclico de cinco a siete elementos que contienen hasta 3 heteroátomos seleccionados de N, O o S; n es 0 - 4; y p es 0 - 2.
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