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AR084280A1 - Compuestos heterociclicos nitrogenados sustituidos fusionados en posicion 6,6 y usos de los mismos - Google Patents

Compuestos heterociclicos nitrogenados sustituidos fusionados en posicion 6,6 y usos de los mismos

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Publication number
AR084280A1
AR084280A1 ARP110104673A ARP110104673A AR084280A1 AR 084280 A1 AR084280 A1 AR 084280A1 AR P110104673 A ARP110104673 A AR P110104673A AR P110104673 A ARP110104673 A AR P110104673A AR 084280 A1 AR084280 A1 AR 084280A1
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Argentina
Prior art keywords
alkyl
link
group
alkenylene
haloalkyl
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ARP110104673A
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English (en)
Inventor
Lewis J Gazzard
Emily Hanan
Samuel Kintz
Joseph P Lyssikatos
Hans Edward Purkey
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Hoffmann La Roche
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Publication of AR084280A1 publication Critical patent/AR084280A1/es

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    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
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    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/22—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems 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 carbon atoms of the nitrogen-containing ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D401/02—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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D401/02—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
    • 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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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D401/14—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 three or more hetero rings
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    • C07—ORGANIC CHEMISTRY
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    • C07D405/02—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
    • 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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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—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
    • C07D405/14—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 three or more hetero rings
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
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    • C07D413/02—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
    • C07D413/12—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 chain containing hetero atoms as chain links
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    • C07—ORGANIC CHEMISTRY
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    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond

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  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

Abstract

Composición farmacéutica.Reivindicación 1: Compuestos de la fórmula (1) o sales farmacéuticamente aceptables de los mismos; en la que: Y está ausente o se elige entre el grupo formado por -C(=O)-, -N(H)C(=O)-, -N(Ra)C(=O)-, -O-C(=O)-, -N(H)S(O)1-2-, -N(Ra)S(O)1-2- y -S(O)2-, en los que Ra se elige entre el grupo formado por alquilo C1-6, haloalquilo C1-6, alcoxi C1-6, heteroalquilo C1-6, alquenilo C2-6 y alquinilo C2-6; R2 es -(Xb)0-1-Rb, dicho Xb se elige entre el grupo formado por alquileno C1-6, alquenileno C2-6, alquinileno C2-6, heteroalquileno C1-6, ciclcloalquileno de 3 - 6 eslabones y heterocicloalquileno de 3 - 6 eslabones; Rb se elige entre el grupo formado por hidrógeno, alquilo C1-6, haloalquilo C1-6, heteroalquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo de 3 - 6 eslabones, heterocicloalquilo de 3 - 6 eslabones, arilo de 6 - 10 eslabones y heteroarilo de 5 - 10 eslabones, en los que las porciones alifáticas y aromáticas de Xb y Rb están opcionalmente sustituidas con independencia entre sí por 1 - 5 sustituyentes Rb1 elegidos entre el grupo formado por alquilo C1-6, haloalquilo C1-6, heteroalquilo C1-6, F, Cl, Br, I, -OH, -NH2, -SH, -CN, -NO2, -N3, -C(=O)OH, alcoxi C1-6, alquilamino C1-6, di(alquil C1-6)amino, heterocicloalquilo de 3 - 6 eslabones, -(alquenileno C1-4)0-1-C(=O)-(alquilo C1-4), -(alquenileno C1-4)0-1-C(=O)O-(alquilo C1-4), -(alquenileno C1-4)0-1-C(=O)N(H)-(alquilo C1-4), -(alquenileno C1-4)0-1-C(=O)N-(alquilo C1-4)2, -(alquenileno C1-4)0-1-S(O)2(alquilo C1-4), -(alquenileno C1-4)0-1-C(=O)-(heteroalquilo C1-4) y -(alquenileno C1-4)0-1-C(=O)-(heterocicloalquilo C3-6), y en la que si Rb es un arilo de 6 eslabones o un heteroarilo de 5 - 6 eslabones, entonces cualesquiera dos sustituyentes unidos a átomos adyacentes de dichos arilo o heteroarilo se combinan opcionalmente para formar un anillo carbocíclico de 3 - 6 eslabones o un anillo heterocíclico de 3 - 6 eslabones que contiene 1 - 3 heteroátomos elegidos entre N, O y S y están opcionalmente sustituidos por 1 - 3 sustituyentes Rb1; X1 es N o N+-O-; X2, X3 y X4 son en cada caso C, o uno de X2, X3 y X4 es N o N+-O- y los demás de X2, X3 y X4 son en cada caso C; R3 se elige entre el grupo formado por hidrógeno, alquilo C1-6, haloalquilo C1-6, alcoxi C1-6, alquilamino C1-6, di(alquil C1-6)amino, F, Cl, Br, I, -CN, -CF3, -OCF3, -SF5 y -N3; R4 se elige entre el grupo formado por hidrógeno, alquilo C1-6, haloalquilo C1-6, F, Cl, Br, I, -CN, -NO2, -N3, -SH, -OH, alcoxi C1-6, -CF3, -OCF3, -SF5, alquilamino C1-6 y di(alquil C1-6)amino, o está ausente si X4 es N+-O-; R5 es (Xc)0-1-Rc, dicho Xc se elige entre el grupo formado por alquileno C1-6, alquenileno C2-6, heteroalquileno C2-6, alquinileno C2-6, -N(H)-, -N(Rxc)-, -O-, -S(O)2-, -C(=O)-, -C(=O)O-, -C(=O)N(H)-, -N(H)C(=O)- y -OC(=O)-, en los que Rxc se elige entre el grupo formado por alquilo C1-6, haloalquilo C1-6, heteroalquilo C1-6, alquenilo C2-6, alquinilo C2-6, y en los que Rc se elige entre el grupo formado por hidrógeno, F, Cl, Br, I, -CN, -NO2, -NH2, -OH, -CF3, -OCF3, -SF5, alcoxi C1-6, alquilamino C1-6, di(alquil C1-6)amino, alquilo C1-6, haloalquilo C1-6, heteroalquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo de 3 - 6 eslabones, heterocicloalquilo de 3 - 6 eslabones, arilo de 6 eslabones y heteroarilo de 5 - 6 eslabones, en los que las porciones alifáticas y aromáticas de Xc y Rc están opcionalmente sustituidas por 1 - 5 sustituyentes Rc1 elegidos entre el grupo formado por alquilo C1-6, heteroalquilo C1-6, F, Cl, Br, I, -OH, -NH2, -SH, -CN, -NO2, -N3, -C(=O)OH, -N(alquilo C1-6)2, -NH(alquilo C1-6), -O(alquilo C1-6), -(alquenileno C1-4)0-1-C(=O)-(alquilo C1-4), -(alquenileno C1-4)0-1-C(=O)O-(alquilo C1-4), -(alquenileno C1-4)0-1-C(=O)N(H)-(alquilo C1-4), -(alquenileno C1-4)0-1-C(=O)N(alquilo C1-4)2, -(alquenileno C1-4)0-1-S(O)2(alquilo C1-4), -(alquenileno C1-4)0-1-C(=O)-(heteroalquilo C1-4) y -(alquenileno C1-4)0-1-C(=O)-(heterocicloalquilo C3-6), o R5 está ausente si X3 es N o N+-O-; R6 se elige entre el grupo formado por hidrógeno, alquilo C1-6, haloalquilo C1-6, heteroalquilo C1-6, alcoxi C1-6, alquilamino C1-6, di(alquil C1-6)amino, alquenilo C2-6, alquinilo C2-6, F, Cl, Br, I, -OH, -NH2, -SH, -CN, -NO2, -CF3, -OCF3, -SF5 y -N3, o R6 está ausente si X2 es N o N+-O-; A está ausente o se elige entre el grupo formado por -O-, -N(H)-, -N(Rd)-, -S(O)2, -S(O)-, -S-, -(Xd)0-1-N(H)C(=O)-, -(Xd)0-1-N(Rd)C(=O)-, -Xd-, -(Xd)0-1-C(=O)-N(H)-, -(Xd)0-1-C(=O)N(Rd)-, -(Xd)0-1-C(=O)-, -C(=O)-(Xd)0-1-, -(Xd)0-1-OC(=O)- y (Xd)0-1-C(=O)O, en los que Xd se elige entre el grupo formado por alquileno C1-6, alquenileno C2-6, alquinileno C2-6, heteroalquieno C1-6, arileno de 6 - 10 eslabones, heteroarileno de 5 - 10 eslabones, cicloalquileno de 3 - 10 eslabones, heterocicloalquileno de 3 - 10 eslabones, y Rd en cada aparición se elige con independencia entre el grupo formado por alquilo C1-6, alquenilo C2-6, heteroalquilo C1-6 y haloalquilo C1-6, en los que las porciones alifáticas o aromáticas de Xd y Rd están opcionalmente sustituidas con independencia entre sí por 1 - 5 sustituyentes Rd1 elegidos entre el grupo formado por alquilo C1-6, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, alquilamino C1-6, di(alquil C1-6)amino, F, Cl, Br, I, -OH, -NH2, -SH, -CN, -NO2, -CF3, -OCF3, -SF5 y N3; B se elige entre el grupo formado por alquilo C1-6, haloalquilo C1-6, heteroalquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo de 3 - 6 eslabones, heterocicloalquilo de 4 - 9 eslabones, arilo de 6 - 10 eslabones y heteroarilo de 5 - 6 eslabones, en los que las porciones alifáticas o aromáticas de B están opcionalmente sustituidas con independencia por 1 - 5 sustituyentes RB1 elegidos entre el grupo formado por alquilo C1-6, haloalquilo C1-6, heteroalquilo C1-6, alcoxi C1-6, alquilamino C1-6, di(alquil C1-6)-amino, heterocicloalquilo C3-6, F, Cl, Br, I, -OH, -NH2, -SH, -CF3, -OCF3, -SF5, -(Xe)0-1-CN, -(Xe)0-1-NO2, -(Xe)0-1-N3, -(Xe)0-1-OH, -(Xe)0-1-H, -(Xe)0-1-N(H)Re, -(Xe)0-1-N(Re)2, -(Xe)0-1-SRe, -(Xe)0-1-C(O)Re, (Xe)0-1-S(O)2Re, -(Xe)0-1-S(O)Re, -N(H)S(O)2Re, -N(Re)S(O)2Re, -(Xe)0-1-C(=O)ORe, -(Xe)0-1-C(=O)OH, -(Xe)0-1-C(=O)N(H)Re, -(Xe)0-1-C(=O)-N(Re)Re, -(Xe)0-1-N(H)C(=O)Re, -(Xe)0-1N(Re)C(=O)Re, en los que si B es un arilo de 6 eslabones o un heteroarilo de 5 - 6 eslabones, entonces cualesquiera dos sustituyentes unidos a átomos adyacentes de dichos arilo o heteroarilo se combinan opcionalmente para formar un anillo carbocíclico de 3 - 6 eslabones o un anillo heterocíclico de 3 - 6 eslabones que contienen opcionalmente 1 - 3 heteroátomos elegidos entre N, O y S, y están opcionalmente sustituidos por 1 - 3 sustituyentes RB1; en los que Xe se elige entre el grupo formado por alquileno C1-6, alquenileno C2-6, alquinileno C2-6, heteroalquileno C1-6, cicloalquileno C3-6 y heterocicloalquileno C3-6, y Re en cada aparición se elige con independencia entre el grupo formado por alquilo C1-6, haloalquilo C1-6, heteroalquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo de 3 - 7 eslabones, heterocicloalquilo de 3 - 7 eslabones, fenilo y heteroarilo de 5 - 6 eslabones, en los que las porciones alifáticas o aromáticas de Xe y Re están opcionalmente sustituidas con independencia entre sí por 1 - 5 sustituyentes Re1 elegidos entre el grupo formado por alquilo C1-6, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, alquilamino C1-6, di(alquil C1-6)amino, F, Cl, Br, I, -OH, -NH2, -SH, -CN, -NO2, -CF3, -OCF3, -SF5 y -N3, en los que cada dos grupos Re unidos al mismo átomo de nitrógeno se combinan opcionalmente para formar un anillo heterocíclico de 3 - 7 eslabones o heteroarilo de 5 - 10 eslabones que contiene 1 - 3 heteroátomos elegidos entre N, O y S; y en la que si X3 es N, R3 es H, R4 es H o NH2, R6 es -OH e -Y-R2 es diferente de H, entonces -A-B no es tiazol-4-ilo sustituido por 2-tiofenil-S(O)2CH2-, fenil-S(O)2-CH2-, 4-piridilo ni piridil-S(O)2CH2-, si X3 es N, R3 es H o Cl, R4 es H, R6 es -OH, -NH2 o -NHCH3 e -Y-R2 es hidrógeno, 4-tetrahidropiranilo, 4-((CH3CH2)2N(CH2)3-4-O)-fenilo, (CH3CH2)2N-(CH2)4-, 3-(4-metilpiperazinil)-propilo o trifluoroacetilo, entonces -A-B no es 2-clorofenilo, 2-metilfenilo, 2,6-di-clorofenilo, 3,5-dimetoxifenilo, 3,4-dimetoxifenilo, fenilo, 2-cloro-6-(2-etoxietoxi)-fenilo, si X3 es N, R3, R4 y R6 son en cada caso H, e -Y-R2 es hidrógeno, ciclohexilo, (CH3CH2)2NCH2CH2-, CH3N(H)-CH2CH2-, (CH3)2NCH2CH2-, (CH3)3CC(=O)- ó 2-(4-morfolinil)-etilo, entonces -A-B no es 3,4-dimetoxifenilo ni piridin-2-on-3-ilo opcionalmente sustituido, si X4 es N, R3 es H, R5 es isopropilo, R6 es metoxi, -A-B es propilo o isopropilo, entonces -Y-R2 es diferente de piridilo opcionalmente sustituido, si X4 es N, R3, R5, R6 son en cada caso H, -A-B es metilos entonces -Y-R2 es diferente de hidrógeno, si R3, R4, R5 y R6 son en cada caso H, e -Y-R2 es hidrógeno, ciclohexilo, (CH3CH2)2NCH2CH2-, CH3N(H)CH2-CH2-, (CH3)2NCH2CH2-, (CH3)3CC(=O)- ó 2-(4-morfolinil)-etilo, entonces -A-B no es 3,4- dimetoxifenilo ni piridin-2-on-3-ilo opcionalmente sustituido, si R3, R4 y R5 son en cada caso hidrógeno, -Y-R2 es distinto de hidrógeno, entonces uno de R6 y -A-B es diferente de etoxi.
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