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AR095280A1 - Derivados heterocíclicos de imidazo[1,2-a]piridina - Google Patents

Derivados heterocíclicos de imidazo[1,2-a]piridina

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Publication number
AR095280A1
AR095280A1 ARP140100893A ARP140100893A AR095280A1 AR 095280 A1 AR095280 A1 AR 095280A1 AR P140100893 A ARP140100893 A AR P140100893A AR P140100893 A ARP140100893 A AR P140100893A AR 095280 A1 AR095280 A1 AR 095280A1
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AR
Argentina
Prior art keywords
alkyl
independently selected
halo
optionally substituted
alkoxy
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ARP140100893A
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English (en)
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Galapagos Nv
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Publication of AR095280A1 publication Critical patent/AR095280A1/es

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    • C—CHEMISTRY; METALLURGY
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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
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • 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
    • A61K31/425—Thiazoles
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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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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    • 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
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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
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    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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    • 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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    • A61K31/5375—1,4-Oxazines, e.g. morpholine
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Abstract

Reivindicación 1: Un compuesto de acuerdo con la fórmula (1), donde R¹ᵃ es H, halo o alquilo C₁₋₄; R¹ᵇ es: halo, alquilo C₁₋₄ (alquilo que está opcionalmente sustituido con uno o varios halo independientemente seleccionados), o alcoxi C₁₋₄ (alcoxi que está opcionalmente sustituido con uno o varios halo independientemente seleccionados); X es -S-, -O-, -N=CH-, -CH=N- o -CH=CH-; W es N o CR³, cuando W es N, R² es: H, -CN, halo, alquilo C₁₋₄ (alquilo que está opcionalmente sustituido con uno o varios OH o CN independientemente seleccionados), -C(=O)CH₃, -C(=O)CF₃, -C(=O)OCH₃, -C(=O)NH₂, o -NHC(=O)CH₃, o cuando W es CR³, uno de R² o R³ es: H, -CN, halo, alquilo C₁₋₄ (alquilo que esta opcionalmente sustituido con uno o varios OH o CN independientemente seleccionados), -C(=O)CH₃, C(=O)CF₃, -C(=O)OCH₃, -C(=O)NH₂, -NHC(=O)CH₃, y el otro es H o alquilo C₁₋₄; R⁴ es alquilo C₁₋₄; R⁵ es alquilo C₁₋₄ opcionalmente sustituido con uno o varios CN, OH, halo o -C(=O)NH₂ independientemente seleccionados; uno de R⁶ᵃ o R⁶ᵇ se selecciona de H, -CH₃ y halo, y el otro es H; Cy es: cicloalquilo C₄₋₁₀, heterocicloalquilo mono o bicíclico de 4 - 10 miembros que contiene uno o varios heteroátomos independientemente seleccionados de O, N y S, o heterocicloalquenilo de 4 - 7 miembros que contiene 1 enlace doble, que contiene uno o varios heteroátomos independientemente seleccionados de O, N y S; cada R⁷ se selecciona independientemente de: OH, oxo, halo, y alquilo C₁₋₄ (alquilo que está opcionalmente sustituido con uno o varios OH o alcoxi C₁₋₄ independientemente seleccionados); el índice a es 0, 1 ó 2; R⁸ es -(L¹-W¹)ₘ-L²-G¹, donde L¹ este ausente o bien es -O-, -C(=O)-, -NRⁱ, -NRʰC(=O)- o -SO₂-; W¹ es alquileno C₁₋₄; el índice m es 0 ó 1; L² está ausente o bien es -O-, -C(=O)-, -C(=O)O-, -OC(=O)-, -C(=O)-C(=O)-, -C(=O)-C(=O)NRᵃ-, -NRᵇ-, -C(=O)NRᶜ-, -NRᵈC(=O)-, -NRʲC(=O)O-, -SO₂-, -SO₂NRᵉ- o -NRᶠSO₂-; G¹ es: H, -CN, alquilo C₁₋₄ (alquilo que está opcionalmente sustituido con uno o varios -CN, OH, halo o fenilo independientemente seleccionados), cicloalquilo C₃₋₇ (cicloalquilo que está opcionalmente sustituido con -NH₂), heterocicloalquenilo de 5 - 6 miembros que contiene 1 enlace doble que contiene uno o varios heteroátomos independientemente seleccionados de O, N y S (heterocicloalquenilo que está opcionalmente sustituido con uno o varios grupos R⁹ independientemente seleccionados), heterocicloalquilo mono, bi o espirocíclico de 4 - 10 miembros que contiene uno o varios heteroátomos independientemente seleccionados de O, N y S (heterocicloalquilo que está opcionalmente sustituido con uno o varios grupos R⁹ independientemente seleccionados), o heteroarilo de 5 - 6 miembros que contiene uno o varios heteroátomos independientemente seleccionados de O, N y S (heteroarilo que está opcionalmente sustituido con uno o varios grupos R¹⁰ independientemente seleccionados); cada R⁹ es oxo o R¹⁰; cada R¹⁰ es: -OH, halo, -CN, alquilo C₁₋₄ (alquilo que está opcionalmente sustituido con uno o varios OH, halo o fenilo independientemente seleccionados), alcoxi C₁₋₄, cicloalquilo C₃₋₇, fenilo, -SO₂CH₃, -C(=O)alcoxi C₁₋₄, -C(=O)alquilo C₁₋₄, o -NRᵍC(=O)alquilo C₁₋₄; y cada Rᵃ, Rᵇ, Rᶜ, Rᵈ, Rᵉ, Rᶠ, Rᵍ, Rʰ, Rⁱ y Rʲ se selecciona independientemente de H y alquilo C₁₋₄; o una sal farmacéuticamente aceptable o un solvato o una sal farmacéuticamente aceptable de un solvato de este; o un metabolito biológicamente activo de este.
ARP140100893A 2013-03-14 2014-03-12 Derivados heterocíclicos de imidazo[1,2-a]piridina AR095280A1 (es)

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WO2016040180A1 (en) 2014-09-08 2016-03-17 Samumed, Llc 3-(1h-benzo[d]imidazol-2-yl)-1h-pyrazolo[3,4-c]pyridine and therapeutic uses thereof
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