AR088872A1 - Derivados de uracilo como inhibidores de la quinasa axl y c-met - Google Patents

Derivados de uracilo como inhibidores de la quinasa axl y c-met

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Publication number
AR088872A1
AR088872A1 ARP120104293A ARP120104293A AR088872A1 AR 088872 A1 AR088872 A1 AR 088872A1 AR P120104293 A ARP120104293 A AR P120104293A AR P120104293 A ARP120104293 A AR P120104293A AR 088872 A1 AR088872 A1 AR 088872A1
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Argentina
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optionally substituted
alkyl
heterocyclyl
independently selected
aryl
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ARP120104293A
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Dandu Reddeppareddy
I Hudkins Robert
A Josef Kurt
P Prouty Catherine
Tripathy Rabindranath
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Cephalon Inc
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Publication of AR088872A1 publication Critical patent/AR088872A1/es

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    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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
    • C07D239/28—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
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/52—Two oxygen atoms
    • C07D239/54—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
    • 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
    • C07D401/14—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—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
    • C07D417/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/056—Ortho-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring

Abstract

Reivindicación 1: Un compuesto de la fórmula (1) o una sal del mismo; caracterizado porque: E y G se seleccionan independientemente entre H, alquilo C₁₋₆ opcionalmente sustituido 1 - 6 R¹⁹, alquenilo C₂₋₆ opcionalmente sustituido 1 - 6 R¹⁹, alquinilo C₂₋₆ opcionalmente sustituido 1 - 6 R¹⁹, arilo C₆₋₁₁ opcionalmente sustituido 1 - 6 R¹⁹, cicloalquilo C₃₋₁₁ opcionalmente sustituido 1 - 6 R¹⁹, heterociclilo de 3 - 15 miembros opcionalmente sustituido 1 - 6 R¹⁹, heteroarilo de 5 - 15 miembros opcionalmente sustituido 1 - 6 R¹⁹, -C(=O)R²⁰, -C(=O)OR²⁰, -C(=O)NR²²R²³, -S(=O)₂R²⁰, y -S(=O)₂NR²²R²³; X es N o C-R⁴; Y es N o C-R¹ᵈ; R³ es H o alquilo C₁₋₆; D es -O-, -S-, -SO-, -SO₂-, -C(=O)-, -CHOH-, -CH₂-, -NH- o -N-alquilo C₁₋₆-; W es CH o N; Rᵃ, Rᵇ, Rᶜ, Rᵈ, R¹ᵃ, R¹ᵇ, R¹ᶜ, R¹ᵈ, y R⁴ se seleccionan independientemente entre H, alquilo C₁₋₆ opcionalmente sustituido 1 - 6 R¹¹⁹, alquenilo C₂₋₆ opcionalmente sustituido 1 - 6 R¹¹⁹, alquinilo C₂₋₆ opcionalmente sustituido 1 - 6 R¹¹⁹, arilo C₆₋₁₁ opcionalmente sustituido 1 - 6 R¹¹⁹, cicloalquilo C₃₋₁₁ opcionalmente sustituido 1 - 6 R¹¹⁹, heterociclilo de 3 - 15 miembros opcionalmente sustituido 1 - 6 R¹¹⁹, heteroarilo de 5 - 15 miembros opcionalmente sustituido 1 - 6 R¹¹⁹, halógeno, -CN, -C(=O)R¹¹⁰, -C(=O)OR¹¹⁰, -C(=O)NR¹¹²R¹¹³, -NC, -NO₂, -NR¹¹²R¹¹³, -NR¹¹⁴C(=O)R¹¹⁰, -NR¹¹⁴C(=O)OR¹¹¹, -NR¹¹⁴C(=O)NR¹¹²R¹¹³, -NR¹¹⁴S(=O)₂R¹¹¹, -NR¹¹⁴S(=O)₂NR¹¹²R¹¹³, -OR¹¹⁰, -OCN, -OC(=O)R¹¹⁰, -OC(=O)NR¹¹²R¹¹³, -OC(=O)OR¹¹⁰, -S(=O)ₙR¹¹⁰, y -S(=O)₂NR¹¹²R¹¹³; o cualquiera de Rᵃ y Rᵇ, Rᵃ y Rᵈ, y Rᵇ y Rᶜ pueden, junto con los átomos que los ligan, forman un arilo C₆₋₁₁ opcionalmente sustituido 1 - 6 R¹¹⁹, cicloalquilo C₃₋₁₁ opcionalmente sustituido 1 - 6 R¹¹⁹, heterociclilo de 3 - 15 miembros opcionalmente sustituido 1 - 6 R¹¹⁹ o un heteroarilo de 5 - 15 miembros opcionalmente sustituido 1 - 6 R¹¹⁹; R¹⁹ cada vez que ocurre, se selecciona independientemente entre alquilo C₁₋₆ opcionalmente sustituido 1 - 6 R³⁹, alquenilo C₂₋₆ opcionalmente sustituido 1 - 6 R³⁹, alquinilo C₂₋₆ opcionalmente sustituido 1 - 6 R³⁹, arilo C₆₋₁₁ opcionalmente sustituido 1 - 6 R³⁹, cicloalquilo C₃₋₁₁ opcionalmente sustituido 1 - 6 R³⁹, heterociclilo de 3 - 15 miembros opcionalmente sustituido 1 - 6 R³⁹, heteroarilo de 5 - 15 miembros opcionalmente sustituido 1 - 6 R³⁹, halógeno, -CN, -C(=O)R³⁰, -C(=O)OR³⁰, -C(=O)NR³²R³³, -NO₂, -NR³²R³³, -NR³⁴C(=O)R³⁰, -NR³⁴C(=O)OR³¹, -NR³⁴C(=O)NR³²R³³, -NR³⁴S(=O)₂R³¹, -NR³⁴S(=O)₂NR³²R³³, -OR³⁰, =O, -OC(=O)R³⁰, -OC(=O)NR³²R³³, -OC(=O)OR³⁰, -S(=O)ₙR³⁰, y -S(=O)₂NR³²R³³; R²⁰, R²¹, R²⁴, R³⁰, R³¹, y R³⁴ cada vez que ocurre, se selecciona independientemente entre H, alquilo C₁₋₆ opcionalmente sustituido 1 - 6 R⁴⁹, alquenilo C₂₋₆ opcionalmente sustituido 1 - 6 R⁴⁹, alquinilo C₂₋₆ opcionalmente sustituido 1 - 6 R⁴⁹, arilo C₆₋₁₁ opcionalmente sustituido 1 - 6 R⁴⁹, cicloalquilo C₃₋₁₁ opcionalmente sustituido 1 - 6 R⁴⁹, heterociclilo de 3 - 15 miembros opcionalmente sustituido 1 - 6 R⁴⁹, y heteroarilo de 5 - 15 miembros opcionalmente sustituido 1 - 6 R⁴⁹; R²², R²³, R³² y R³³ cada vez que ocurre, se selecciona independientemente entre H, alquilo C₁₋₆ opcionalmente sustituido 1 - 6 R⁵⁹, alquenilo C₂₋₆ opcionalmente sustituido 1 - 6 R⁵⁹, alquinilo C₂₋₆ opcionalmente sustituido 1 - 6 R⁵⁹, arilo C₆₋₁₁ opcionalmente sustituido 1 - 6 R⁵⁹, cicloalquilo C₃₋₁₁ opcionalmente sustituido 1 - 6 R⁵⁹, heterociclilo de 3 - 15 miembros opcionalmente sustituido 1 - 6 R⁵⁹, y heteroarilo de 5 - 15 miembros opcionalmente sustituido 1 - 6 R⁵⁹; o cualquiera de R²² y R²³ y/o R³² y R³³ pueden formar, junto con el átomo de nitrógeno al que están ligados, un heterociclilo de 3 - 15 miembros opcionalmente sustituido 1 - 6 R⁶⁹ o un heteroarilo de 5 - 15 miembros opcionalmente sustituido 1 - 6 R⁶⁹; R³⁹, R⁴⁹, R⁵⁹ y R⁶⁹ cada vez que ocurre, se selecciona independientemente entre alquilo C₁₋₆ opcionalmente sustituido 1 - 6 R⁷⁹, alquenilo C₂₋₆ opcionalmente sustituido 1 - 6 R⁷⁹, alquinilo C₂₋₆ opcionalmente sustituido 1 - 6 R⁷⁹, arilo C₆₋₁₁ opcionalmente sustituido 1 - 6 R⁷⁹, cicloalquilo C₃₋₁₁ opcionalmente sustituido 1 - 6 R⁷⁹, heterociclilo de 3 - 15 miembros opcionalmente sustituido 1 - 6 R⁷⁹, heteroarilo de 5 - 15 miembros opcionalmente sustituido 1 - 6 R⁷⁹, halógeno, -CN, -C(=O)R⁷⁰, -C(=O)OR⁷⁰, -C(=O)NR⁷²R⁷³, -NO₂, -NR⁷²R⁷³, -NR⁷⁴C(=O)R⁷⁰, -NR⁷⁴C(=O)OR⁷¹, -NR⁷⁴C(=O)NR⁷²R⁷³, -NR⁷⁴S(=O)₂R⁷¹, -NR⁷⁴S(=O)₂NR⁷²R⁷³, -OR⁷⁰, =O, -OC(=O)R⁷⁰, -OC(=O)NR⁷²R⁷³, -S(=O)ₙR⁷⁰, y -S(=O)₂NR⁷²R⁷³; R⁷⁰, R⁷¹, R⁷², R⁷³, y R⁷⁴ cada vez que ocurre, se selecciona independientemente entre H, alquilo C₁₋₆ y haloalquilo C₁₋₆; R⁷⁹ cada vez que ocurre, se selecciona independientemente entre alquilo C₁₋₆, haloalquilo C₁₋₆, bencilo, halógeno, -CN, -C(=O)(alquilo C₁₋₆), -C(=O)O(alquilo C₁₋₆), -C(=O)N(alquilo C₁₋₆)₂, -C(=O)OH, -C(=O)NH₂, -C(=O)NH-alquilo C₁₋₆, -NO₂, -NH₂, -NH-alquilo C₁₋₆, -N(alquilo C₁₋₆)₂, -NHC(=O)alquilo C₁₋₆, -NHS(=O)₂alquilo C₁₋₆, -OH, -O-alquilo C₁₋₆, =O, -OC(=O)alquilo C₁₋₆, -OS(=O)₂alquilo C₁₋₆, -S(=O)₂alquilo C₁₋₆, y -S(=O)₂N(alquilo C₁₋₆)₂; R¹¹⁰, R¹¹¹, y R¹¹⁴ cada vez que ocurre, se selecciona independientemente entre H, alquilo C₁₋₆ opcionalmente sustituido 1 - 6 R¹²⁹, alquenilo C₂₋₆ opcionalmente sustituido 1 - 6 R¹²⁹, alquinilo C₂₋₆ opcionalmente sustituido 1 - 6 R¹²⁹, arilo C₆₋₁₁ opcionalmente sustituido 1 - 6 R¹²⁹, cicloalquilo C₃₋₁₁ opcionalmente sustituido 1 - 6 R¹²⁹, heterociclilo de 3 - 15 miembros opcionalmente sustituido 1 - 6 R¹²⁹, y heteroarilo de 5 - 15 miembros opcionalmente sustituido 1 - 6 R¹²⁹; R¹¹² y R¹¹³ cada vez que ocurre, se selecciona independientemente entre H, alquilo C₁₋₆ opcionalmente sustituido 1 - 6 R¹³⁹, alquenilo C₂₋₆ opcionalmente sustituido 1 - 6 R¹³⁹, alquinilo C₂₋₆ opcionalmente sustituido 1 - 6 R¹³⁹, arilo C₆₋₁₁ opcionalmente sustituido 1 - 6 R¹³⁹, cicloalquilo C₃₋₁₁ opcionalmente sustituido 1 - 6 R¹³⁹, heterociclilo de 3 - 15 miembros opcionalmente sustituido 1 - 6 R¹³⁹, y heteroarilo de 5 - 15 miembros opcionalmente sustituido 1 - 6 R¹³⁹; o cualquiera de R¹¹² y R¹¹³ pueden formar, junto con el átomo de nitrógeno al que están ligados, un heterociclilo de 3 - 15 miembros opcionalmente sustituido 1 - 6 R¹⁴⁹ o un heteroarilo de 5 - 15 miembros opcionalmente sustituido 1 - 6 R¹⁴⁹; R¹¹⁹ cada vez que ocurre, se selecciona independientemente entre alquilo C₁₋₆ opcionalmente sustituido 1 - 6 R¹⁵⁹, alquenilo C₂₋₆ opcionalmente sustituido 1 - 6 R¹⁵⁹, alquinilo C₂₋₆ opcionalmente sustituido 1 - 6 R¹⁵⁹, arilo C₆₋₁₁ opcionalmente sustituido 1 - 6 R¹⁵⁹, cicloalquilo C₃₋₁₁ opcionalmente sustituido 1 - 6 R¹⁵⁹, heterociclilo de 3 - 15 miembros opcionalmente sustituido 1 - 6 R¹⁵⁹, heteroarilo de 5 - 15 miembros opcionalmente sustituido 1 - 6 R¹⁵⁹, halógeno, -CN, -C(=O)R¹⁵⁰, -C(=O)OR¹⁵⁰, -C(=O)NR¹⁵²R¹⁵³, -NC, -NO₂, -NR¹⁵²R¹⁵³, -NR¹⁵&#x2
ARP120104293A 2011-11-14 2012-11-14 Derivados de uracilo como inhibidores de la quinasa axl y c-met AR088872A1 (es)

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