AR098048A1 - Inhibidores de fgfr4 - Google Patents

Inhibidores de fgfr4

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Publication number
AR098048A1
AR098048A1 ARP140103845A ARP140103845A AR098048A1 AR 098048 A1 AR098048 A1 AR 098048A1 AR P140103845 A ARP140103845 A AR P140103845A AR P140103845 A ARP140103845 A AR P140103845A AR 098048 A1 AR098048 A1 AR 098048A1
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AR
Argentina
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alkyl
group
alkoxy
hydrogen
nr5r6
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ARP140103845A
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English (en)
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Eisai R&D Man Co Ltd
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Publication of AR098048A1 publication Critical patent/AR098048A1/es

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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K9/0021Intradermal administration, e.g. through microneedle arrays, needleless injectors
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    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • C07ORGANIC CHEMISTRY
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    • C07C53/15Saturated compounds having only one carboxyl group bound to an acyclic carbon atom or hydrogen containing halogen
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    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic 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
    • C07D239/28Heterocyclic 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
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    • C07D401/02Heterocyclic 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
    • C07D401/04Heterocyclic 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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    • C07D413/12Heterocyclic 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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Abstract

En el presente documento se proporcionan compuestos útiles como inhibidores de FGFR4, así como sus métodos de uso. FGFR4 definido como Receptor del Factor de Crecimiento de Fibroblastos 4. Reivindicación 1: Un compuesto de fórmula (1), en donde: R³ se selecciona del grupo que consta de: alquilo C₁₋₆, alcoxi C₁₋₆-alquilo C₁₋₆, NR¹⁰R¹¹-alquilo C₁₋₆, heterociclilo-R¹⁰-alquilo C₁₋₆, arilo-R¹⁰-alquilo C₁₋₆, y heteroarilo-R¹⁰-alquilo C₁₋₆, en donde R¹⁰ y R¹¹ cada uno se selecciona de modo independiente del grupo que consta de: hidrógeno y alquilo C₁₋₆; E se selecciona del grupo que consta de: -NR¹³C(O)CR¹⁴=CHR¹⁵, y -NR¹³C(O)CºCR¹⁴, en donde R¹³ se selecciona del grupo que consta de: hidrógeno y metilo, y R¹⁴ y R¹⁵ cada uno se selecciona de modo independiente del grupo que consta de: hidrógeno, metilo, flúor y cloro; R¹² se selecciona del grupo que consta de: hidrógeno, halo, alquilo C₁₋₆, alcoxi C₁₋₆, hidroxialquilo C₁₋₆, hidroxialcoxi C₁₋₆, alcoxi C₁₋₆-alcoxi C₁₋₆, alcoxi C₁₋₆-alquilo C₁₋₆, heterociclilo-R⁵R⁶, -C(O)heterociclilo-R⁵R⁶, R⁵R⁶-heterociclilo-alquilo C₁₋₆, NR⁵R⁶, NR⁵R⁶-alquilo C₁₋₆, -C(O)NR⁵R⁶, y NR⁵R⁶-alquiloxi C₁₋₆, en donde R⁵ y R⁶ cada uno se selecciona de modo independiente del grupo que consta de hidrógeno, alquilo C₁₋₆, hidroxialquilo C₁₋₆, aminoalquilo C₁₋₆, -C(O)alquilo C₁₋₆ y alquilo C₁₋₆sulfonilo; y R¹ es fenilo, en donde dicho fenilo está sustituido 2, 3, ó 4 veces con halo o alcoxi C₁₋₆ independientemente seleccionados; o una sal farmacéuticamente aceptable del mismo.
ARP140103845A 2013-10-18 2014-10-16 Inhibidores de fgfr4 AR098048A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201361892881P 2013-10-18 2013-10-18

Publications (1)

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AR098048A1 true AR098048A1 (es) 2016-04-27

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US (4) US9434697B2 (es)
EP (2) EP3421457B1 (es)
JP (2) JP6139788B2 (es)
KR (1) KR101826015B1 (es)
CN (2) CN110354128A (es)
AR (1) AR098048A1 (es)
AU (2) AU2014337291B9 (es)
BR (1) BR112016008110B1 (es)
CA (1) CA2924206C (es)
CL (1) CL2016000918A1 (es)
CY (1) CY1121129T1 (es)
DK (1) DK3057943T3 (es)
ES (1) ES2679521T3 (es)
HK (1) HK1223091A1 (es)
HR (1) HRP20181129T1 (es)
HU (1) HUE039268T2 (es)
IL (1) IL244373B (es)
JO (1) JO3515B1 (es)
LT (1) LT3057943T (es)
MX (1) MX2016004933A (es)
MY (1) MY184733A (es)
NZ (1) NZ717559A (es)
PE (1) PE20160679A1 (es)
PH (1) PH12016500676A1 (es)
PL (1) PL3057943T3 (es)
PT (1) PT3057943T (es)
RS (1) RS57444B1 (es)
RU (1) RU2715708C2 (es)
SG (1) SG11201602069WA (es)
SI (1) SI3057943T1 (es)
TW (1) TWI597268B (es)
UA (1) UA116920C2 (es)
WO (2) WO2015057963A1 (es)

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