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AR109711A1 - Inhibidores de fosfatidilinositol 3-quinasa - Google Patents

Inhibidores de fosfatidilinositol 3-quinasa

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Publication number
AR109711A1
AR109711A1 ARP170102638A ARP170102638A AR109711A1 AR 109711 A1 AR109711 A1 AR 109711A1 AR P170102638 A ARP170102638 A AR P170102638A AR P170102638 A ARP170102638 A AR P170102638A AR 109711 A1 AR109711 A1 AR 109711A1
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AR
Argentina
Prior art keywords
nrarb
alkynyl
alkenyl
alkyl
aryl
Prior art date
Application number
ARP170102638A
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English (en)
Inventor
Jennifer Anne Treiberg
Nicholas Alexander Till
Gary Phillips
Stephane Perreault
Leena Patel
Jayaraman Chandrasekhar
Original Assignee
Gilead Sciences Inc
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Publication date
Application filed by Gilead Sciences Inc filed Critical Gilead Sciences Inc
Publication of AR109711A1 publication Critical patent/AR109711A1/es

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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • 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
    • A61K31/41—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
    • A61K31/4196—1,2,4-Triazoles
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4409—Non condensed pyridines; Hydrogenated derivatives thereof only substituted in position 4, e.g. isoniazid, iproniazid
    • 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
    • A61K31/4709—Non-condensed quinolines and 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
    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • 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
    • C07D403/14—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
    • 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
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings

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  • Chemical & Material Sciences (AREA)
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  • Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Immunology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Urology & Nephrology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Reivindicación 1: Un compuesto que tiene la estructura de la fórmula (1), donde n es 1, 2, 3 ó 4; s es 1 ó 2; t es 1 ó 2; cada R¹ se selecciona independientemente entre 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 a 10 miembros que contiene 1 a 4 heteroátomos seleccionados del grupo que consiste en N, O, y S, y heterociclilo de 4 a 10 miembros que contiene 1 a 4 heteroátomos seleccionados del grupo que consiste en N, O, y S; donde cada alquilo-C₁₋₆, alquenilo-C₂₋₆, alquinilo-C₂₋₆, cicloalquilo-C₃₋₈, arilo-C₆₋₁₀, heteroarilo de 5 a 10 miembros y heterociclilo de 4 a 10 miembros está opcionalmente sustituido con uno a cuatro R¹⁰⁰; R² se selecciona entre 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 a 10 miembros que contiene 1 a 4 heteroátomos seleccionados del grupo que consiste en N, O, y S, y heterociclilo de 4 a 10 miembros que contiene 1 a 4 heteroátomos seleccionados del grupo que consiste en N, O, y S; donde cada alquilo-C₁₋₆, alquenilo-C₂₋₆, alquinilo-C₂₋₆, cicloalquilo-C₃₋₈, arilo-C₆₋₁₀, heteroarilo de 5 a 10 miembros y heterociclilo de 4 a 10 miembros está opcionalmente sustituido con uno a cuatro R¹⁰¹; R³ se selecciona entre 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, -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 a 10 miembros que contiene 1 a 4 heteroátomos seleccionados del grupo que consiste en N, O, y S, y heterociclilo de 4 a 10 miembros que contiene 1 a 4 heteroátomos seleccionados del grupo que consiste en N, O, y S; donde cada alquilo-C₁₋₆, alquenilo-C₂₋₆, alquinilo-C₂₋₆, cicloalquilo-C₃₋₈, arilo-C₆₋₁₀, heteroarilo de 5 a 10 miembros y heterociclilo de 4 a 10 miembros está opcionalmente sustituido con uno a cuatro R¹⁰²; R⁴ es un heteroarilo de 5 a 10 miembros; donde dicho heteroarilo de 5 a 10 miembros está opcionalmente sustituido con uno a cuatro R¹⁰³; cada R⁵ es independientemente seleccionado entre 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, -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 a 10 miembros que contiene 1 a 4 heteroátomos seleccionados del grupo que consiste en N, O, y S, y heterociclilo de 4 a 10 miembros que contiene 1 a 4 heteroátomos seleccionados del grupo que consiste en N, O, y S; donde cada alquilo-C₁₋₆, alquenilo-C₂₋₆, alquinilo-C₂₋₆, cicloalquilo-C₃₋₈, arilo-C₆₋₁₀, heteroarilo de 5 a 10 miembros y heterociclilo de 4 a 10 miembros está opcionalmente sustituido con uno a cuatro R¹⁰⁴; cada R⁶ se selecciona independientemente entre 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 Rᵃ y Rᵇ se selecciona independientemente entre hidrógeno, alquilo-C₁₋₆, alquenilo-C₂₋₆ y alquinilo-C₂₋₆; 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 independientemente entre hidrógeno, halo, ciano, hidroxi, amino, oxo, tioxo, vinilo, -C(O)Rᶜ, -C(O)ORᶜ, -C(O)NRᶜRᵈ, -N(Rᶜ)C(O)Rᵈ, -N(Rᵃ)C(O)NRᵃRᵇ, -OC(O)NRᵃRᵇ, -NRᵃS(O)₂NRᵃRᵇ, -NRᵃS(O)₂Rᵃ, -S(O)NRᶜRᵈ, -S(O)₂NRᶜRᵈ, -S(O)Rᵍ, -S(O)₂Rᵍ, -NRᶜRᵈ, -ORᶜ, -SRᵈ, alquilo-C₁₋₆, alquenilo-C₂₋₆, alquinilo-C₂₋₆, cicloalquilo-C₃₋₈, arilo-C₆₋₁₀, heteroarilo de 5 a 10 miembros y heterociclilo de 4 a 10 miembros; donde cada alquilo-C₁₋₆, alquenilo-C₂₋₆, alquinilo-C₂₋₆, cicloalquilo-C₃₋₈, arilo-C₆₋₁₀, heteroarilo de 5 a 10 miembros y heterociclilo de 4 a 10 miembros está opcionalmente sustituido con uno a cuatro R²⁰¹; cada Rᶜ y Rᵈ se selecciona independientemente entre hidrógeno, arilo-C₆₋₁₀, alquilo-C₁₋₆, alquenilo-C₂₋₆ y alquinilo-C₂₋₆; cada R²⁰⁰ y R²⁰¹ se selecciona independientemente entre 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 o alquinilo-C₂₋₆; cada Rᵉ y Rᶠ se selecciona independientemente entre hidrógeno, alquilo-C₁₋₆, alquenilo-C₂₋₆ y alquinilo-C₂₋₆; cada Rᵍ se selecciona independientemente entre alquilo-C₁₋₆, alquenilo-C₂₋₆, alquinilo-C₂₋₆, cicloalquilo-C₃₋₈, arilo-C₆₋₁₀, heteroarilo de 5 a 10 miembros que contiene 1 a 4 heteroátomos seleccionados del grupo que consiste en N, O y S y heterociclilo de 4 a 10 miembros que contiene 1 a 4 heteroátomos seleccionados del grupo que consiste en N, O, y S; donde cada alquilo-C₁₋₆, alquenilo-C₂₋₆, alquinilo-C₂₋₆, cicloalquilo-C₃₋₈, arilo-C₆₋₁₀, heteroarilo de 5 a 10 miembros y heterociclilo de 4 a 10 miembros está opcionalmente sustituido con uno a cuatro R²⁰⁰; o una sal farmacéuticamente aceptable, un isómero o una mezcla de los mismos.
ARP170102638A 2016-09-23 2017-09-25 Inhibidores de fosfatidilinositol 3-quinasa AR109711A1 (es)

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