AR109709A1 - Inhibidores de la fosfatidilinositol 3-quinasa - Google Patents

Inhibidores de la fosfatidilinositol 3-quinasa

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Publication number
AR109709A1
AR109709A1 ARP170102636A ARP170102636A AR109709A1 AR 109709 A1 AR109709 A1 AR 109709A1 AR P170102636 A ARP170102636 A AR P170102636A AR P170102636 A ARP170102636 A AR P170102636A AR 109709 A1 AR109709 A1 AR 109709A1
Authority
AR
Argentina
Prior art keywords
nrarb
alkynyl
alkenyl
alkyl
aryl
Prior art date
Application number
ARP170102636A
Other languages
English (en)
Inventor
William J Watkins
Jennifer Anne Treiberg
Nicholas Alexander Till
Kassandra F Sedillo
Gary Phillips
Stephane Perreault
Leena Patel
Devan Naduthambi
Jayaraman Chandrasekhar
Original Assignee
Gilead Sciences Inc
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
Application filed by Gilead Sciences Inc filed Critical Gilead Sciences Inc
Publication of AR109709A1 publication Critical patent/AR109709A1/es

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C07D235/08—Radicals containing only hydrogen and carbon atoms
    • 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
    • A61K31/41—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
    • A61K31/4164—1,3-Diazoles
    • A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • 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
    • A61K31/535—Heterocyclic 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
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • C07D413/02—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
    • C07D413/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

Abstract

Reivindicación 1: Un compuesto que tiene la estructura de la fórmula (1), en donde, R¹ se selecciona de: los compuestos del grupo de fórmulas (2); n es 1, 2, 3 ó 4; s es 1, 2 ó 3; t es 1 ó 2; cada X¹, X², X³, X⁴, X⁵, X⁶ y X⁷ se selecciona, de modo independiente, de C y N; R² se selecciona de hidrógeno, halo, ciano, hidroxi, amino, -C(O)Rᵃ, -C(O)ORᵇ, -C(O)NRᵃRᵇ, -N(Rᵃ)C(O)Rᵇ, -S(O)NRᵃRᵇ, -S(O)₂NRᵃRᵇ, -S(O)Rᵍ, -S(O)₂Rᵍ, -NRᵃRᵇ, -ORᵃ, -SRᵇ, alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, cicloalquilo C₃₋₈, arilo C₆₋₁₀, heteroarilo de 5 - 10 miembros que contiene 1 a 4 heteroátomos seleccionados del grupo que consiste en N, O y S y heterociclilo de 4 - 10 miembros que contiene 1 a 4 heteroátomos seleccionados del grupo que consiste en N, O y S; en donde cada alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, cicloalquilo C₃₋₈, arilo C₆₋₁₀, heteroarilo de 5 - 10 miembros y heterociclilo de 4 - 10 miembros está opcionalmente sustituido con uno a cuatro R¹⁰¹; R³ se selecciona de hidrógeno, halo, ciano, hidroxi, amino, -C(O)Rᵃ, -C(O)ORᵇ, -C(O)NRᵃRᵇ, -N(Rᵃ)C(O)Rᵇ, -N(Rᵃ)C(O)NRᵃRᵇ, -OC(O)NRᵃRᵇ, -NRᵃS(O)₂NRᵃRᵇ, -NRᵃS(O)₂Rᵃ, -N(Rᵃ)C(O)NRᵃRᵇ, -OC(O)NRᵃRᵇ, -NRᵃS(O)₂NRᵃRᵇ, -NRᵃS(O)₂Rᵃ, -S(O)NRᵃRᵇ, -S(O)₂NRᵃRᵇ, -S(O)Rᵍ, -S(O)₂Rᵍ-NRᵃRᵇ, -ORᵃ, -SRᵇ, alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, cicloalquilo C₃₋₈, arilo C₆₋₁₀, heteroarilo de 5 - 10 miembros que contiene 1 a 4 heteroátomos seleccionados del grupo que consiste en N, O y S y heterociclilo de 4 - 10 miembros que contiene 1 a 4 heteroátomos seleccionados del grupo que consiste en N, O y S; en donde cada alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, cicloalquilo C₃₋₈, arilo C₆₋₁₀, heteroarilo de 5 - 10 miembros y heterociclilo de 4 - 10 miembros está opcionalmente sustituido con uno a cuatro R¹⁰²; R⁴ se selecciona de heteroarilo de 5 - 10 miembros que contiene 1 a 4 heteroátomos seleccionados del grupo que consiste en N, O y S y heterociclilo de 4 - 10 miembros que contiene 1 a 4 heteroátomos seleccionados del grupo que consiste en N, O y S; en donde cada heteroarilo de 5 - 10 miembros y heterociclilo de 4 - 10 miembros está opcionalmente sustituido con uno a cuatro R¹⁰³; cada R⁵ se selecciona, de modo independiente, de hidrógeno, halo, ciano, hidroxi, amino, -C(O)Rᵃ, -C(O)ORᵇ, -C(O)NRᵃRᵇ, -N(Rᵃ)C(O)Rᵇ, -N(Rᵃ)C(O)NRᵃRᵇ, -N(Rᵃ)C(O)NRᵃRᵇ, -OC(O)NRᵃRᵇ, -NRᵃS(O)₂NRᵃRᵇ, -NRᵃS(O)₂Rᵃ, -OC(O)NRᵃRᵇ, -NRᵃS(O)₂NRᵃRᵇ, -NRᵃS(O)₂Rᵃ, -S(O)NRᵃRᵇ, -S(O)₂NRᵃRᵇ, -S(O)Rᵍ, -S(O)₂Rᵍ, -NRᵃRᵇ, -ORᵃ, -SRᵇ, alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, cicloalquilo C₃₋₈, arilo C₆₋₁₀, heteroarilo de 5 - 10 miembros que contiene 1 a 4 heteroátomos seleccionados del grupo que consiste en N, O y S y heterociclilo de 4 - 10 miembros que contiene 1 a 4 heteroátomos seleccionados del grupo que consiste en N, O y S; en donde cada alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, cicloalquilo C₃₋₈, arilo C₆₋₁₀, heteroarilo de 5 - 10 miembros y heterociclilo de 4 - 10 miembros está opcionalmente sustituido con uno a cuatro R¹⁰⁴; cada R⁶ se selecciona, de modo independiente, de hidrógeno, halo, ciano, hidroxi, amino, -C(O)Rᵃ, -C(O)ORᵇ, -C(O)NRᵃRᵇ, -N(Rᵃ)C(O)Rᵇ, -S(O)NRᵃRᵇ, -S(O)₂NRᵃRᵇ, -S(O)Rᵍ, -S(O)₂Rᵍ,-NRᵃRᵇ, -ORᵃ, -SRᵇ, alquilo C₁₋₆, alquenilo C₂₋₆ o alquinilo C₂₋₆; cada R⁷ se selecciona, de modo independiente, de hidrógeno, halo, ciano, hidroxi, amino, -C(O)Rᵃ, -C(O)ORᵇ, -C(O)NRᵃRᵇ, -N(Rᵃ)C(O)Rᵇ, -S(O)NRᵃRᵇ, -S(O)₂NRᵃRᵇ, -S(O)Rᵍ, -S(O)₂Rᵍ, -NRᵃRᵇ, -ORᵃ, -SRᵇ, alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, cicloalquilo C₃₋₈, arilo C₆₋₁₀, heteroarilo de 5 - 10 miembros que contiene 1 a 4 heteroátomos seleccionados del grupo que consiste en N, O y S y heterociclilo de 4 - 10 miembros que contiene 1 a 4 heteroátomos seleccionados del grupo que consiste en N, O y S; en donde cada alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, cicloalquilo C₃₋₈, arilo C₆₋₁₀, heteroarilo de 5 - 10 miembros y heterociclilo de 4 - 10 miembros está opcionalmente sustituido con uno a cuatro R¹⁰⁰; cada Rᵃ y Rᵇ se selecciona, de modo independiente, de hidrógeno arilo C₆₋₁₀, alquilo C₁₋₆, alquenilo C₂₋₆ y alquinilo C₂₋₆; en donde cada alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, está opcionalmente sustituido con uno a cuatro R²⁰⁰; cada R¹⁰⁰, R¹⁰¹, R¹⁰², R¹⁰³ y R¹⁰⁴ se selecciona, de modo independiente, de hidrógeno, halo, ciano, hidroxi, amino, oxo, tioxo, vinilo, -C(O)Rᶜ, -C(O)ORᶜ, -C(O)NRᶜRᵈ, -N(Rᶜ)C(O)Rᵈ, -N(Rᶜ)C(O)NRᶜRᵈ, -N(Rᶜ)C(O)NRᶜRᵈ, -OC(O)NRᶜRᵈ, -NRᶜS(O)₂NRᶜRᵈ, -NRᶜS(O)₂Rᶜ, -OC(O)NRᶜRᵈ, -NRᶜS(O)₂NRᶜRᵈ, -NRᶜS(O)₂Rᶜ, -S(O)NRᶜRᵈ, -S(O)₂NRᶜRᵈ, -S(O)Rᶜ, -S(O)₂Rᵍ, -NRᶜRᵈ, -ORᶜ, -SRᵈ, alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, cicloalquilo C₃₋₈, arilo C₆₋₁₀, heteroarilo de 5 - 10 miembros y heterociclilo de 4 - 10 miembros; en donde cada alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, cicloalquilo C₃₋₈, arilo C₆₋₁₀, heteroarilo de 5 - 10 miembros y heterociclilo de 4 - 10 miembros está opcionalmente sustituido con uno a cuatro R²⁰¹; cada Rᶜ y Rᵈ se selecciona, de modo independiente, de hidrógeno arilo C₆₋₁₀, alquilo C₁₋₆, alquenilo C₂₋₆ y alquinilo C₂₋₆; cada R²⁰⁰ y R²⁰¹ se selecciona, de modo independiente, de hidrógeno, halo, ciano, hidroxi, amino, oxo, tioxo, vinilo, -C(O)Rᵉ, -C(O)ORᵉ, -C(O)NRᵉRᶠ, -N(Rᵉ)C(O)Rᶠ, -S(O)NRᵉRᶠ, -S(O)₂NRᵉRᶠ, -S(O)Rᵍ, -S(O)₂Rᵍ, -NRᵉRᶠ, -ORᵉ, -SRᵉ, alquilo C₁₋₆, alquenilo C₂₋₆ y alquinilo C₂₋₆; cada Rᵉ y Rᶠ se selecciona, de modo independiente, de hidrógeno alquilo C₁₋₆, alquenilo C₂₋₆ y alquinilo C₂₋₆; cada Rᵍ se selecciona, de modo independiente, de alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, cicloalquilo C₃₋₈, arilo C₆₋₁₀, heteroarilo de 5 - 10 miembros que contiene 1 a 4 heteroátomos seleccionados del grupo que consiste en N, O y S y heterociclilo de 4 - 10 miembros que contiene 1 a 4 heteroátomos seleccionados del grupo que consiste en N, O y S; en donde cada alquilo C₁₋₆, alquenilo C₂₋₆, alquinilo C₂₋₆, cicloalquilo C₃₋₈, arilo C₆₋₁₀, heteroarilo de 5 - 10 miembros y heterociclilo de 4 - 10 miembros está opcionalmente sustituido con uno a cuatro R²⁰⁰; o una de sus sales, isómeros farmacéuticamente aceptables o una mezcla de ellos.
ARP170102636A 2016-09-23 2017-09-25 Inhibidores de la fosfatidilinositol 3-quinasa AR109709A1 (es)

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US201662398802P 2016-09-23 2016-09-23

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US (1) US10479770B2 (es)
AR (1) AR109709A1 (es)
TW (1) TW201825465A (es)
WO (1) WO2018057805A1 (es)

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