AR039257A1 - Derivados de benzamida - Google Patents

Derivados de benzamida

Info

Publication number
AR039257A1
AR039257A1 ARP030101185A ARP030101185A AR039257A1 AR 039257 A1 AR039257 A1 AR 039257A1 AR P030101185 A ARP030101185 A AR P030101185A AR P030101185 A ARP030101185 A AR P030101185A AR 039257 A1 AR039257 A1 AR 039257A1
Authority
AR
Argentina
Prior art keywords
alkyl
carbamoyl
amino
sulfamoyl
optionally substituted
Prior art date
Application number
ARP030101185A
Other languages
English (en)
Inventor
Elaine Stokes
Roberts Craig
Michael Waring
Original Assignee
Astrazeneca Ab
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
Priority claimed from GB0207863A external-priority patent/GB0207863D0/en
Priority claimed from GB0229930A external-priority patent/GB0229930D0/en
Application filed by Astrazeneca Ab filed Critical Astrazeneca Ab
Publication of AR039257A1 publication Critical patent/AR039257A1/es

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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/26—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/34—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon 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
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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
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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
    • C07D213/60—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
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    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
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    • C07D215/12—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
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    • C07D237/08—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/42—One nitrogen atom
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    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having 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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    • C07D251/12—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D251/14—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hydrogen or carbon atoms directly attached to at least one ring carbon atom
    • C07D251/16—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hydrogen or carbon atoms directly attached to at least one ring carbon atom to only one ring carbon atom
    • C07D251/18—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hydrogen or carbon atoms directly attached to at least one ring carbon atom to only one ring carbon atom with nitrogen atoms directly attached to the two other ring carbon atoms, e.g. guanamines
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    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/22—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/22—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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    • C07D295/04—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/14—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D295/155—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
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    • C07D307/34—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D307/38—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms
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    • C07D401/00—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
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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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    • C07D401/12—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 linked by a chain containing hetero atoms as chain links
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  • Pyridine Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Quinoline Compounds (AREA)
  • Furan Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Thiazole And Isothizaole Compounds (AREA)

Abstract

Derivados de benzamida, procesos para su preparación, composiciones farmacéuticas que los contienen y su uso en el tratamiento de enfermedades y trastornos clínicos mediados por la histona deacetilasa. Reivindicación 1: Un compuesto caracterizado porque responde a la fórmula (1) donde el anillo A es un heterociclilo, donde si dicho heterociclilo contiene una porción -NH- dicho N puede ser opcionalmente sustituido por un grupo seleccionado entre K; R1 es un sustituyente sobre C y se selecciona entre halo, nitro, ciano, hidroxi, trifluorometilo, trifluorometoxi, amino, carboxi, carbamoilo, mercapto, sulfamoilo, (C1-6) alquilo, (C2-6) alquenilo, (C2-6) alquinilo, (C1-6) alcoxi, (C1-6) alcanoilo, (C1-6) alcanoiloxi, N-(C1-6 alquil) amino, N,N-(C1-6 alquil)2amino, C1-6 alcanoilamino, N-(C1-6alquil)carbamoilo, N,N-(C1-6alquil)2carbamoilo, (C1-6) alquilS(O)a donde a es entre 0 y 2, C1-6 alcoxicarbonilo, N-(C1-6 alquil)sulfamoilo, N,N-(C1-6 alquil)2sulfamoilo, arilo, ariloxi, aril(C1-6)alquilo, grupo heterocíclico, (grupo heterocíclico) C1-6 alquilo, o un grupo (B-E); donde R1, incluyendo el grupo (B-E), puede ser opcionalmente sustituido sobre C por uno o más W; y donde si dicho grupo heterocíclico contiene una porción -NH- dicho N puede ser opcionalmente sustituido por J; W es halo, nitro, ciano, hidroxi, trifluorometilo, trifluorometoxi, amino, carboxi, carbamoilo, mercapto, sulfamoilo, C1-6 alquilo, C2-6 alquenilo, C2-6 alquinilo, C1-6 alcoxi, C1-6 alcanoilo, C1-6 alcanoiloxi, N-(C1-6 alquil)amino, N,N-(C1-6alquil)2amino, C1-6 alcanoilamino, N-(C1-6alquil)carbamoilo, N,N-(C1-6alquil)2carbamoilo, C1-6 alquilS(O)a donde a es entre 0 y 2, C1-6 alcoxicarbonilo, N-(C1-6alquil)sulfamoilo, N,N-(C1-6alquil)2sulfamoilo, o un grupo (B'-E'-); donde W, incluyendo el grupo (B'-E'-), puede ser opcionalmente sustituido sobre C por uno o más Y; Y y Z se seleccionan en forma independiente entre halo, nitro, ciano, hidroxi, trifluorometilo, trifluorometoxi, amino, carboxi, carbamoilo, mercapto, sulfamoilo, C1-6 alquilo, C2-6 alquenilo, C2-6 alquinilo, C1-6 alcoxi, C1-6 alcanoilo, C1-6 alcanoiloxi, N-(C1-6 alquil) amino, N,N-(C1-6 alquil)2amino, C1-6 alcanoilamino, N-(C1-6 alquil)carbamoilo, N,N-(C1-6 alquil)2carbamoilo, C1-6 alquilS(O)a, donde a es entre 0 y 2, C1-6 alcoxicarbonilo, N-(C1-6alquil)sulfamoilo o N,N-(C1-6 alquil)2 sulfamoilo; G, J, y K se seleccionan en forma independiente entre C1-8 alquilo, C2-8 alquenilo, C1-8 alcanoilo, C1-8 alquilsulfonilo, C1-8 alcoxicarbonilo, carbamoilo, N-(C1-8 alquil) carbamoilo, N,N-(C1-8 alquil)carbamoilo, benciloxicarbonilo, benzoilo, fenilsulfonilo, arilo, aril(C1-6)alquilo o (grupo heterocíclico)C1-6 alquilo; donde G, J y K pueden ser opcionalmente sustituidos sobre C por uno o más Q; y donde si dicho grupo heterocíclico contiene una porción -NH- dicho N puede ser opcionalmente sustituido por H o C1-6 alquilo; Q es halo, nitro, ciano, hidroxi, trifluorometilo, trifluorometoxi, amino, carboxi, carbamoilo, mercapto, sulfamoilo, C1-6 alquilo, C2-6 alquenilo, C2-6 alquinilo, C1-6 alcoxi, C1-6 alcanoilo, C1-6 alcanoiloxi, N-(C1-6 alquil)amino, N,N-(C1-6 alquil)2amino, C1-6 alcanoilamino, N-(C1-6 alquil)carbamoilo, N,N-(C1-6 alquil)2carbamoilo, C1-6 alquil S(O)a donde a es entre 0 y 2, C1-6 alcoxicarbonilo, C1-6 alcoxicarbonilamino, N-(C1-6 alquil)sulfamoilo, N,N-(C1-6 alquil)2sulfamoilo, arilo, ariloxi, arilo C1-6 alquilo, aril C1-6alcoxi, grupo heterocíclico, (grupo heterocíclico)C1-6 alquilo, (grupo heterocíclico)C1-6 alcoxi o un grupo (B"-E"-); donde Q, incluyendo el grupo (B"-E"-), puede ser opcionalmente sustituido sobre C por uno o más Z; B, B' y B" se seleccionan en forma independiente entre C1-6 alquilo, C2-6 alquenilo, C2-6 alquinilo, C3-8 cicloalquilo, C3-8cicloalquil(C1-6)alquilo, arilo, aril C1-6 alquilo, grupo heterocíclico, (grupo heterocíclico)C1-6 alquilo, fenilo o fenil C1-6 alquilo; donde B, B', y B" pueden ser opcionalmente sustituidos sobre C por uno o más D; y donde si dicho grupo heterocíclico contiene una porción -NH- dicho N puede ser opcionalmente sustituido por un grupo seleccionado entre G; E, E', y E" se seleccionan en forma independiente entre -N(Ra)-, -O-, -C(O)O-, -OC(O)-, -C(O)-, -N(Ra)C(O)-, -N(Ra)C(O)N(Rb)-, -N(Ra)C(O)O-,-OC(O)N(Ra)-, -C(O)N(Ra), -S(O)r-, SO2N(Ra)-, -N(Ra)SO2-, donde Ra y Rb se seleccionan en forma independiente entre H o alquilo C1-6 opcionalmente sustituido por uno o más F y r es 0-2; D y F se seleccionan en forma independiente entre halo, nitro, ciano, hidroxi, trifluorometilo, trifluorometoxi, amino, carboxi, carbamoilo, mercapto, sulfamoilo, C1-6 alquilo, C2-6 alquenilo, C2-6 alquinilo, C1-6 alcoxi, C1-6 alcanoilo, C1-6 alcanoiloxi, N-(C1-6 alquil)amino, N,N-(C1-6 alquil)2amino, C1-6 alcanoilamino, N-(C1-6 alquil)carbamoilo, N,N-(C1-6 alquil)2 carbamoilo, C1-6 alquil S(O)a donde a es entre 0 y 2, C1-6 alcoxicarbonilo, N-(C1-6 alquil)sulfamoilo o N,N-(C1-6alquil)2sulfamoilo; m es 0, 1, 2, 3 o 4; donde los valores de R1 pueden ser iguales o diferentes; R2 es halo; n es 0, 1 o 2; donde los valores de R2 pueden ser iguales o diferentes; R3 es amino o hidroxi; R4 es halo, nitro, ciano, hidroxi, trifluorometilo, trifluorometoxi, amino, carboxi, carbamoilo, mercapto, sulfamoilo, C1-3 alquilo, C2-3 alquenilo, C2-3 alquinilo, C1-3alcoxi, C1-3alcanoilo, C1-3 alcanoiloxi, N-(C1-3 alquil)amino, N,N-(C1-3 alquil)2 amino, C1-3 alcanoilamino, N-(C1-3 alquil)carbamoilo, N,N-(C1-3 alquil)2carbamoilo, C1-3 alquil S(O)a donde a es entre 0 y 2, C1-3 alcoxicarbonilo, N-(C1-3 alquil)sulfamoilo, N,N-(C1-3 alquil)2sulfamoilo; p es 0, 1 o 2; donde los valores de R4 pueden ser iguales o diferentes; o una sal aceptable para uso farmacéutico o éster hidrolizable in vivo o amida del mismo; con la salvedad de que dicho compuesto no es N-(2-amino-6-hidroxifenil)-4-(1-metilhomopiperazin-4-il)benzamida; N-(2-amino-6-metilfenil)-4-(1-metilhomopiperazin-4-il)benzamida; N-(2-aminofenil)-4-(1-t-butoxicarbonilhomopiperazin-4-il)benzamida, o N-(2-aminofenil)-4-(1-metilhomopiperazin-4-il)benzamida.
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